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Cannabidiol as potential anticancer drug大麻二酚是潜在的抗癌药物

  1. Top of page
  2. Cannabidiol as potential anticancer drug大麻二酚是潜在的抗癌药物
  3. Is the cardiovascular system a therapeutic target for cannabidiol?心血管系统是大麻二酚的治疗靶点吗?
  4. Cannabidiol for neurodegenerative disorders: important new clinical applications for this phytocannabinoid?以大麻二酚治疗神经退行性疾病:这是这种植物源性大麻素类重要的新临床作用吗?
  5. Pharmacogenomics of warfarin in populations of African descent非洲裔人群中的华法令药物基因组学
  6. Drug-induced QT interval prolongation: does ethnicity of the thorough QT study population matter?药物诱导性QT间期延长:全面QT研究人群的种族有影响吗?
  7. Online learning applied to a course on rational therapeutics: an international comparison between final year students of two medical schools对合理治疗学课程实施的在线学习:两所医科大学最后一年学生之间的国际比较
  8. Double-blind, randomized, placebo-controlled study of safety, tolerability, pharmacokinetics and pharmacodynamics of TAK-683, an investigational metastin analogue in healthy men在健康人中针对研究性metastin类似物——TAK-683——的安全性、耐药性、药代动力学和药效学进行的一项双盲、随机、安慰剂对照研究
  9. Insulin at normal physiological levels does not prolong QTc interval in thorough QT studies performed in healthy volunteers正常生理水平的胰岛素在健康志愿者中进行的全面QT研究中不延长QTc间期
  10. An oral TRPV1 antagonist attenuates laser radiant-heat-evoked potentials and pain ratings from UVB-inflamed and normal skin一种能降低UVB致炎皮肤和正常皮肤激光辐射热诱发电位和疼痛评分的口服TRPV1拮抗剂
  11. Relationship between the receptor occupancy profile and pleiotropic effects of angiotensin II receptor blockers血管紧张素II受体阻断剂受体占有特征与多效作用之间的关系
  12. Low doses of fludrocortisone and hydrocortisone, alone or in combination, on vascular responsiveness to phenylephrine in healthy volunteers健康志愿者单独或联合应用低剂量氟氢可的松和氢化可的松对苯福林血管反应性的作用
  13. The effect of CYP3A inhibitors and inducers on the pharmacokinetics of telaprevir in healthy volunteersCYP3A抑制剂和诱导剂对特拉匹韦在健康志愿者中的药代动力学所起的作用
  14. The pharmacokinetics of darexaban are not affected to a clinically relevant degree by rifampicin, a strong inducer of P-glycoprotein and CYP3A4利福平(P-糖蛋白和CYP3A4的强效诱导剂)对darexaban的药代动力学影响无临床意义
  15. Effect of a herbal extract containing curcumin and piperine on midazolam, flurbiprofen and paracetamol (acetaminophen) pharmacokinetics in healthy volunteers一种含姜黄素和胡椒碱的草药提取物对咪达唑仑、氟比洛芬和扑热息痛(醋氨酚)在健康志愿者中的药代动力学影响
  16. Population pharmacokinetics of unbound mycophenolic acid in adult allogeneic haematopoietic cell transplantation: effect of pharmacogenetic factors未结合麦考酚酸在成人异基因造血干细胞移植中的人群药代动力学:遗传药理学因素的作用
  17. Apixaban, an oral, direct factor Xa inhibitor: single dose safety, pharmacokinetics, pharmacodynamics and food effect in healthy subjects口服Xa因子直接抑制剂——阿哌沙班:健康志愿者单次给药的安全性、药代动力学、药效学和食物作用
  18. Assessment of potential drug interactions by characterization of human drug metabolism pathways using non-invasive bile sampling利用非侵入式胆汁取样鉴定人体药物代谢通路评估潜在的药物相互作用
  19. Effect of peginterferon alfa-2a (40KD) on cytochrome P450 isoenzyme activity聚乙二醇干扰素alfa-2b(40KD)对细胞色素P450同工酶活性的作用
  20. Pharmacokinetics of eribulin mesylate in patients with solid tumours receiving repeated oral rifampicin甲磺酸艾日布林在接受重复剂量口服利福平的实体肿瘤患者中的药代动力学
  21. Association between eIF3a polymorphism and severe toxicity caused by platinum-based chemotherapy in non-small cell lung cancer patients非小细胞肺癌患者中的eIF3a基因多态性与铂类药物化疗导致严重毒性之间的相关性
  22. First-in-man safety and pharmacokinetics of synthetic ozonide OZ439 demonstrates an improved exposure profile relative to other peroxide antimalarials合成性臭氧化物OZ439的首次人类安全性和药代动力学分析表明其暴露特性优于其他过氧化物抗疟药
  23. Effects of atomoxetine on the QT interval in healthy CYP2D6 poor metabolizers阿托莫西汀对健康CYP2D6弱代谢者QT间期的作用

Paola Massi, Marta Solinas, Valentina Cinquina & Daniela Parolaro

过年几年来,有多方面的证据支持大麻素类有抗肿瘤生成作用,包括Δ9-四氢大麻酚(Δ9-THC),合成性激动剂,内源性大麻素类和内源性大麻素转运和降解抑制剂等。大麻素类确定有抗增殖和抗凋亡作用,众所周知它们可扰乱肿瘤血管新生、癌症细胞迁移、粘附、侵袭和转移。然而,Δ9-THC和另外一些大麻素激动剂的临床应用常常因其不受欢迎的精神活性副作用而受到局限,正是由于这个原因,近年来人们对于那些对Δ9-THC有结构性亲和性的非精神活性大麻素类化合物的兴趣大大提高了,本综述将重点分析CBD在几种类型的癌症中调节肿瘤发生不同环节的效果,突显将CBD/CBD类似物开发为替代性治疗药的重要性。

Is the cardiovascular system a therapeutic target for cannabidiol?心血管系统是大麻二酚的治疗靶点吗?

  1. Top of page
  2. Cannabidiol as potential anticancer drug大麻二酚是潜在的抗癌药物
  3. Is the cardiovascular system a therapeutic target for cannabidiol?心血管系统是大麻二酚的治疗靶点吗?
  4. Cannabidiol for neurodegenerative disorders: important new clinical applications for this phytocannabinoid?以大麻二酚治疗神经退行性疾病:这是这种植物源性大麻素类重要的新临床作用吗?
  5. Pharmacogenomics of warfarin in populations of African descent非洲裔人群中的华法令药物基因组学
  6. Drug-induced QT interval prolongation: does ethnicity of the thorough QT study population matter?药物诱导性QT间期延长:全面QT研究人群的种族有影响吗?
  7. Online learning applied to a course on rational therapeutics: an international comparison between final year students of two medical schools对合理治疗学课程实施的在线学习:两所医科大学最后一年学生之间的国际比较
  8. Double-blind, randomized, placebo-controlled study of safety, tolerability, pharmacokinetics and pharmacodynamics of TAK-683, an investigational metastin analogue in healthy men在健康人中针对研究性metastin类似物——TAK-683——的安全性、耐药性、药代动力学和药效学进行的一项双盲、随机、安慰剂对照研究
  9. Insulin at normal physiological levels does not prolong QTc interval in thorough QT studies performed in healthy volunteers正常生理水平的胰岛素在健康志愿者中进行的全面QT研究中不延长QTc间期
  10. An oral TRPV1 antagonist attenuates laser radiant-heat-evoked potentials and pain ratings from UVB-inflamed and normal skin一种能降低UVB致炎皮肤和正常皮肤激光辐射热诱发电位和疼痛评分的口服TRPV1拮抗剂
  11. Relationship between the receptor occupancy profile and pleiotropic effects of angiotensin II receptor blockers血管紧张素II受体阻断剂受体占有特征与多效作用之间的关系
  12. Low doses of fludrocortisone and hydrocortisone, alone or in combination, on vascular responsiveness to phenylephrine in healthy volunteers健康志愿者单独或联合应用低剂量氟氢可的松和氢化可的松对苯福林血管反应性的作用
  13. The effect of CYP3A inhibitors and inducers on the pharmacokinetics of telaprevir in healthy volunteersCYP3A抑制剂和诱导剂对特拉匹韦在健康志愿者中的药代动力学所起的作用
  14. The pharmacokinetics of darexaban are not affected to a clinically relevant degree by rifampicin, a strong inducer of P-glycoprotein and CYP3A4利福平(P-糖蛋白和CYP3A4的强效诱导剂)对darexaban的药代动力学影响无临床意义
  15. Effect of a herbal extract containing curcumin and piperine on midazolam, flurbiprofen and paracetamol (acetaminophen) pharmacokinetics in healthy volunteers一种含姜黄素和胡椒碱的草药提取物对咪达唑仑、氟比洛芬和扑热息痛(醋氨酚)在健康志愿者中的药代动力学影响
  16. Population pharmacokinetics of unbound mycophenolic acid in adult allogeneic haematopoietic cell transplantation: effect of pharmacogenetic factors未结合麦考酚酸在成人异基因造血干细胞移植中的人群药代动力学:遗传药理学因素的作用
  17. Apixaban, an oral, direct factor Xa inhibitor: single dose safety, pharmacokinetics, pharmacodynamics and food effect in healthy subjects口服Xa因子直接抑制剂——阿哌沙班:健康志愿者单次给药的安全性、药代动力学、药效学和食物作用
  18. Assessment of potential drug interactions by characterization of human drug metabolism pathways using non-invasive bile sampling利用非侵入式胆汁取样鉴定人体药物代谢通路评估潜在的药物相互作用
  19. Effect of peginterferon alfa-2a (40KD) on cytochrome P450 isoenzyme activity聚乙二醇干扰素alfa-2b(40KD)对细胞色素P450同工酶活性的作用
  20. Pharmacokinetics of eribulin mesylate in patients with solid tumours receiving repeated oral rifampicin甲磺酸艾日布林在接受重复剂量口服利福平的实体肿瘤患者中的药代动力学
  21. Association between eIF3a polymorphism and severe toxicity caused by platinum-based chemotherapy in non-small cell lung cancer patients非小细胞肺癌患者中的eIF3a基因多态性与铂类药物化疗导致严重毒性之间的相关性
  22. First-in-man safety and pharmacokinetics of synthetic ozonide OZ439 demonstrates an improved exposure profile relative to other peroxide antimalarials合成性臭氧化物OZ439的首次人类安全性和药代动力学分析表明其暴露特性优于其他过氧化物抗疟药
  23. Effects of atomoxetine on the QT interval in healthy CYP2D6 poor metabolizers阿托莫西汀对健康CYP2D6弱代谢者QT间期的作用

Christopher P. Stanley, William H. Hind & Saoirse E. O’Sullivan

大麻二酚(CBD)对糖尿病、亨廷顿病、癌症和结肠炎等多种疾病有良好的治疗作用。现在越来越多的证据还表明CBD有益于心血管系统。CBD对离体动脉有直接作用,能引起急性、时间依赖性血管舒张。CBD体外培养能增强内皮依赖性血管舒张受损动物模型中的血管舒张反应。CBD对高糖环境、炎症或动物模型中诱导的2型糖尿病等导致的血管损伤有保护作用,并能降低此类环境相关的血管渗透性过高。所有这些研究中的一个共同主题是CBD的抗炎和抗氧化作用。体内CBD处理能保护心脏的缺血-再灌注损伤和糖尿病相关的心肌病。同样,在一个不同的缺血-再灌注模型中,CBD均显示能减少动物卒中模型中的梗死面积和提高血流量,其对5HT1A受体拮抗有敏感性。虽然急性或慢性CBD处理似乎对血液动力学的作用甚微,但不论是CBD全身应用还是颅内应用都能减少对应激模型的心血管反应,该作用可被5HT1A受体拮抗剂抑制。在血液中,CBD可影响白细胞的存活和死亡率、白细胞迁移和血小板聚集。总的来说,这些临床前资料似乎表明CBD处理对心脏及对外周和脑血管有积极的作用。但是要使这个假说变得更可靠、要确定作用机制及确定人体是否会观察到相似的CBD反应,还必须进行更多的工作才行。

Cannabidiol for neurodegenerative disorders: important new clinical applications for this phytocannabinoid?以大麻二酚治疗神经退行性疾病:这是这种植物源性大麻素类重要的新临床作用吗?

  1. Top of page
  2. Cannabidiol as potential anticancer drug大麻二酚是潜在的抗癌药物
  3. Is the cardiovascular system a therapeutic target for cannabidiol?心血管系统是大麻二酚的治疗靶点吗?
  4. Cannabidiol for neurodegenerative disorders: important new clinical applications for this phytocannabinoid?以大麻二酚治疗神经退行性疾病:这是这种植物源性大麻素类重要的新临床作用吗?
  5. Pharmacogenomics of warfarin in populations of African descent非洲裔人群中的华法令药物基因组学
  6. Drug-induced QT interval prolongation: does ethnicity of the thorough QT study population matter?药物诱导性QT间期延长:全面QT研究人群的种族有影响吗?
  7. Online learning applied to a course on rational therapeutics: an international comparison between final year students of two medical schools对合理治疗学课程实施的在线学习:两所医科大学最后一年学生之间的国际比较
  8. Double-blind, randomized, placebo-controlled study of safety, tolerability, pharmacokinetics and pharmacodynamics of TAK-683, an investigational metastin analogue in healthy men在健康人中针对研究性metastin类似物——TAK-683——的安全性、耐药性、药代动力学和药效学进行的一项双盲、随机、安慰剂对照研究
  9. Insulin at normal physiological levels does not prolong QTc interval in thorough QT studies performed in healthy volunteers正常生理水平的胰岛素在健康志愿者中进行的全面QT研究中不延长QTc间期
  10. An oral TRPV1 antagonist attenuates laser radiant-heat-evoked potentials and pain ratings from UVB-inflamed and normal skin一种能降低UVB致炎皮肤和正常皮肤激光辐射热诱发电位和疼痛评分的口服TRPV1拮抗剂
  11. Relationship between the receptor occupancy profile and pleiotropic effects of angiotensin II receptor blockers血管紧张素II受体阻断剂受体占有特征与多效作用之间的关系
  12. Low doses of fludrocortisone and hydrocortisone, alone or in combination, on vascular responsiveness to phenylephrine in healthy volunteers健康志愿者单独或联合应用低剂量氟氢可的松和氢化可的松对苯福林血管反应性的作用
  13. The effect of CYP3A inhibitors and inducers on the pharmacokinetics of telaprevir in healthy volunteersCYP3A抑制剂和诱导剂对特拉匹韦在健康志愿者中的药代动力学所起的作用
  14. The pharmacokinetics of darexaban are not affected to a clinically relevant degree by rifampicin, a strong inducer of P-glycoprotein and CYP3A4利福平(P-糖蛋白和CYP3A4的强效诱导剂)对darexaban的药代动力学影响无临床意义
  15. Effect of a herbal extract containing curcumin and piperine on midazolam, flurbiprofen and paracetamol (acetaminophen) pharmacokinetics in healthy volunteers一种含姜黄素和胡椒碱的草药提取物对咪达唑仑、氟比洛芬和扑热息痛(醋氨酚)在健康志愿者中的药代动力学影响
  16. Population pharmacokinetics of unbound mycophenolic acid in adult allogeneic haematopoietic cell transplantation: effect of pharmacogenetic factors未结合麦考酚酸在成人异基因造血干细胞移植中的人群药代动力学:遗传药理学因素的作用
  17. Apixaban, an oral, direct factor Xa inhibitor: single dose safety, pharmacokinetics, pharmacodynamics and food effect in healthy subjects口服Xa因子直接抑制剂——阿哌沙班:健康志愿者单次给药的安全性、药代动力学、药效学和食物作用
  18. Assessment of potential drug interactions by characterization of human drug metabolism pathways using non-invasive bile sampling利用非侵入式胆汁取样鉴定人体药物代谢通路评估潜在的药物相互作用
  19. Effect of peginterferon alfa-2a (40KD) on cytochrome P450 isoenzyme activity聚乙二醇干扰素alfa-2b(40KD)对细胞色素P450同工酶活性的作用
  20. Pharmacokinetics of eribulin mesylate in patients with solid tumours receiving repeated oral rifampicin甲磺酸艾日布林在接受重复剂量口服利福平的实体肿瘤患者中的药代动力学
  21. Association between eIF3a polymorphism and severe toxicity caused by platinum-based chemotherapy in non-small cell lung cancer patients非小细胞肺癌患者中的eIF3a基因多态性与铂类药物化疗导致严重毒性之间的相关性
  22. First-in-man safety and pharmacokinetics of synthetic ozonide OZ439 demonstrates an improved exposure profile relative to other peroxide antimalarials合成性臭氧化物OZ439的首次人类安全性和药代动力学分析表明其暴露特性优于其他过氧化物抗疟药
  23. Effects of atomoxetine on the QT interval in healthy CYP2D6 poor metabolizers阿托莫西汀对健康CYP2D6弱代谢者QT间期的作用

Javier Fernández-Ruiz, Onintza Sagredo, M. Ruth Pazos, Concepción García, Roger Pertwee, Raphael Mechoulam & José Martínez-Orgado

大麻二酚(CBD)是一种对许多疾病有治疗作用的植物源性大麻素类,其作用的分子机制仍未被充分了解。CBD在一些实验模型中可以作为抗炎、抗惊厥、抗氧化、止吐、抗焦虑和抗精神病药物,因此分别是治疗神经炎症、 癫痫、氧化损伤、呕吐恶心、焦虑和精神分裂症的潜在药物。在结合抗炎和抗氧化特性的基础上,CBD的神经保护作用潜力备受关注,目前已经进入针对各种神经退行性疾病进行的临床前研究之中。事实上,与Δ9-四氢大麻酚相结合的CBD已经在亨廷顿病患者中接受临床评估,以确定其作为改变病情进展疗法的潜力。CBD似乎不是通过激活内源性大麻素系统中植物源性大麻素类(如Δ9-四氢大麻酚)的关键靶点——即CB1和CB2受体——而发挥其神经保护作用的,因为虽然有文献表明在特定的病理条件(如未成熟脑损伤)下CBD对CB2受体有活性,但是其在这些大麻素类受体上的活性微乎其微。在内源性大麻素系统内,CBD对内源性大麻素类的灭活(即FAAH酶抑制)有抑制作用,从而能增强这些内源性分子对大麻素受体的作用,在某些特定病理条件下也显示了这一点。CBD不仅能通过内源性大麻素系统发挥其作用,也能导致5-羟色胺或腺苷酸代谢型受体的直接或间接激活,还能靶向PPAR家族的核受体及离子 通道。

Pharmacogenomics of warfarin in populations of African descent非洲裔人群中的华法令药物基因组学

  1. Top of page
  2. Cannabidiol as potential anticancer drug大麻二酚是潜在的抗癌药物
  3. Is the cardiovascular system a therapeutic target for cannabidiol?心血管系统是大麻二酚的治疗靶点吗?
  4. Cannabidiol for neurodegenerative disorders: important new clinical applications for this phytocannabinoid?以大麻二酚治疗神经退行性疾病:这是这种植物源性大麻素类重要的新临床作用吗?
  5. Pharmacogenomics of warfarin in populations of African descent非洲裔人群中的华法令药物基因组学
  6. Drug-induced QT interval prolongation: does ethnicity of the thorough QT study population matter?药物诱导性QT间期延长:全面QT研究人群的种族有影响吗?
  7. Online learning applied to a course on rational therapeutics: an international comparison between final year students of two medical schools对合理治疗学课程实施的在线学习:两所医科大学最后一年学生之间的国际比较
  8. Double-blind, randomized, placebo-controlled study of safety, tolerability, pharmacokinetics and pharmacodynamics of TAK-683, an investigational metastin analogue in healthy men在健康人中针对研究性metastin类似物——TAK-683——的安全性、耐药性、药代动力学和药效学进行的一项双盲、随机、安慰剂对照研究
  9. Insulin at normal physiological levels does not prolong QTc interval in thorough QT studies performed in healthy volunteers正常生理水平的胰岛素在健康志愿者中进行的全面QT研究中不延长QTc间期
  10. An oral TRPV1 antagonist attenuates laser radiant-heat-evoked potentials and pain ratings from UVB-inflamed and normal skin一种能降低UVB致炎皮肤和正常皮肤激光辐射热诱发电位和疼痛评分的口服TRPV1拮抗剂
  11. Relationship between the receptor occupancy profile and pleiotropic effects of angiotensin II receptor blockers血管紧张素II受体阻断剂受体占有特征与多效作用之间的关系
  12. Low doses of fludrocortisone and hydrocortisone, alone or in combination, on vascular responsiveness to phenylephrine in healthy volunteers健康志愿者单独或联合应用低剂量氟氢可的松和氢化可的松对苯福林血管反应性的作用
  13. The effect of CYP3A inhibitors and inducers on the pharmacokinetics of telaprevir in healthy volunteersCYP3A抑制剂和诱导剂对特拉匹韦在健康志愿者中的药代动力学所起的作用
  14. The pharmacokinetics of darexaban are not affected to a clinically relevant degree by rifampicin, a strong inducer of P-glycoprotein and CYP3A4利福平(P-糖蛋白和CYP3A4的强效诱导剂)对darexaban的药代动力学影响无临床意义
  15. Effect of a herbal extract containing curcumin and piperine on midazolam, flurbiprofen and paracetamol (acetaminophen) pharmacokinetics in healthy volunteers一种含姜黄素和胡椒碱的草药提取物对咪达唑仑、氟比洛芬和扑热息痛(醋氨酚)在健康志愿者中的药代动力学影响
  16. Population pharmacokinetics of unbound mycophenolic acid in adult allogeneic haematopoietic cell transplantation: effect of pharmacogenetic factors未结合麦考酚酸在成人异基因造血干细胞移植中的人群药代动力学:遗传药理学因素的作用
  17. Apixaban, an oral, direct factor Xa inhibitor: single dose safety, pharmacokinetics, pharmacodynamics and food effect in healthy subjects口服Xa因子直接抑制剂——阿哌沙班:健康志愿者单次给药的安全性、药代动力学、药效学和食物作用
  18. Assessment of potential drug interactions by characterization of human drug metabolism pathways using non-invasive bile sampling利用非侵入式胆汁取样鉴定人体药物代谢通路评估潜在的药物相互作用
  19. Effect of peginterferon alfa-2a (40KD) on cytochrome P450 isoenzyme activity聚乙二醇干扰素alfa-2b(40KD)对细胞色素P450同工酶活性的作用
  20. Pharmacokinetics of eribulin mesylate in patients with solid tumours receiving repeated oral rifampicin甲磺酸艾日布林在接受重复剂量口服利福平的实体肿瘤患者中的药代动力学
  21. Association between eIF3a polymorphism and severe toxicity caused by platinum-based chemotherapy in non-small cell lung cancer patients非小细胞肺癌患者中的eIF3a基因多态性与铂类药物化疗导致严重毒性之间的相关性
  22. First-in-man safety and pharmacokinetics of synthetic ozonide OZ439 demonstrates an improved exposure profile relative to other peroxide antimalarials合成性臭氧化物OZ439的首次人类安全性和药代动力学分析表明其暴露特性优于其他过氧化物抗疟药
  23. Effects of atomoxetine on the QT interval in healthy CYP2D6 poor metabolizers阿托莫西汀对健康CYP2D6弱代谢者QT间期的作用

Guilherme Suarez-Kurtz & Mariana R. Botton

尽管华法令的治疗指数很窄,而达到其临床目标作用的所需剂量也有众所周知的个体间和个体内差异,但它仍然是全球最常被处方的口服抗凝药。药物基因多态性是华法令药代动力学和药效学的主要决定因子,被纳入在多个华法令剂量算法中。本综述重点关注华法令在次撒哈拉人、非裔美国人和混血的巴西人中的药物遗传学。这些人口虽说都是 “黑人”,但是在多个方面互不相同,最值得注意的是近来他们与欧洲人整合的程度——这个因素会影响与华法令达到临床目标作用的剂量要求相关的药物基因多态性的频率分布。虽然VKORC1(3673G > A,rs9923231)、CYP2C9(分别为等位基因*2和*3、rs1799853和rs1057910)和有争议的CYP4F2(rs2108622)的这一小部分多态性涵盖了绝大部分的白人华法令剂量变量的药物基因组学影响,但是它们及其他一些基因(如CALU rs339097)的另外一些多态性也能提高被测黑人人口中药物遗传学华法令剂量算法的预测能力。以个体化策略启动华法令疗法以提高非洲裔人群的安全性和成本效益必须考虑他们的药物遗传多样性和社会经济、文化和医疗因素。要在全世界华法令处方者都很方便采用的算法中说明这种多样性就必须从不同人群水平的试验中收集信息,但也必须严格评价临床药理学文献中常用但是不能准确反映遗传先祖和人口多样性的种族标签。

Drug-induced QT interval prolongation: does ethnicity of the thorough QT study population matter?药物诱导性QT间期延长:全面QT研究人群的种族有影响吗?

  1. Top of page
  2. Cannabidiol as potential anticancer drug大麻二酚是潜在的抗癌药物
  3. Is the cardiovascular system a therapeutic target for cannabidiol?心血管系统是大麻二酚的治疗靶点吗?
  4. Cannabidiol for neurodegenerative disorders: important new clinical applications for this phytocannabinoid?以大麻二酚治疗神经退行性疾病:这是这种植物源性大麻素类重要的新临床作用吗?
  5. Pharmacogenomics of warfarin in populations of African descent非洲裔人群中的华法令药物基因组学
  6. Drug-induced QT interval prolongation: does ethnicity of the thorough QT study population matter?药物诱导性QT间期延长:全面QT研究人群的种族有影响吗?
  7. Online learning applied to a course on rational therapeutics: an international comparison between final year students of two medical schools对合理治疗学课程实施的在线学习:两所医科大学最后一年学生之间的国际比较
  8. Double-blind, randomized, placebo-controlled study of safety, tolerability, pharmacokinetics and pharmacodynamics of TAK-683, an investigational metastin analogue in healthy men在健康人中针对研究性metastin类似物——TAK-683——的安全性、耐药性、药代动力学和药效学进行的一项双盲、随机、安慰剂对照研究
  9. Insulin at normal physiological levels does not prolong QTc interval in thorough QT studies performed in healthy volunteers正常生理水平的胰岛素在健康志愿者中进行的全面QT研究中不延长QTc间期
  10. An oral TRPV1 antagonist attenuates laser radiant-heat-evoked potentials and pain ratings from UVB-inflamed and normal skin一种能降低UVB致炎皮肤和正常皮肤激光辐射热诱发电位和疼痛评分的口服TRPV1拮抗剂
  11. Relationship between the receptor occupancy profile and pleiotropic effects of angiotensin II receptor blockers血管紧张素II受体阻断剂受体占有特征与多效作用之间的关系
  12. Low doses of fludrocortisone and hydrocortisone, alone or in combination, on vascular responsiveness to phenylephrine in healthy volunteers健康志愿者单独或联合应用低剂量氟氢可的松和氢化可的松对苯福林血管反应性的作用
  13. The effect of CYP3A inhibitors and inducers on the pharmacokinetics of telaprevir in healthy volunteersCYP3A抑制剂和诱导剂对特拉匹韦在健康志愿者中的药代动力学所起的作用
  14. The pharmacokinetics of darexaban are not affected to a clinically relevant degree by rifampicin, a strong inducer of P-glycoprotein and CYP3A4利福平(P-糖蛋白和CYP3A4的强效诱导剂)对darexaban的药代动力学影响无临床意义
  15. Effect of a herbal extract containing curcumin and piperine on midazolam, flurbiprofen and paracetamol (acetaminophen) pharmacokinetics in healthy volunteers一种含姜黄素和胡椒碱的草药提取物对咪达唑仑、氟比洛芬和扑热息痛(醋氨酚)在健康志愿者中的药代动力学影响
  16. Population pharmacokinetics of unbound mycophenolic acid in adult allogeneic haematopoietic cell transplantation: effect of pharmacogenetic factors未结合麦考酚酸在成人异基因造血干细胞移植中的人群药代动力学:遗传药理学因素的作用
  17. Apixaban, an oral, direct factor Xa inhibitor: single dose safety, pharmacokinetics, pharmacodynamics and food effect in healthy subjects口服Xa因子直接抑制剂——阿哌沙班:健康志愿者单次给药的安全性、药代动力学、药效学和食物作用
  18. Assessment of potential drug interactions by characterization of human drug metabolism pathways using non-invasive bile sampling利用非侵入式胆汁取样鉴定人体药物代谢通路评估潜在的药物相互作用
  19. Effect of peginterferon alfa-2a (40KD) on cytochrome P450 isoenzyme activity聚乙二醇干扰素alfa-2b(40KD)对细胞色素P450同工酶活性的作用
  20. Pharmacokinetics of eribulin mesylate in patients with solid tumours receiving repeated oral rifampicin甲磺酸艾日布林在接受重复剂量口服利福平的实体肿瘤患者中的药代动力学
  21. Association between eIF3a polymorphism and severe toxicity caused by platinum-based chemotherapy in non-small cell lung cancer patients非小细胞肺癌患者中的eIF3a基因多态性与铂类药物化疗导致严重毒性之间的相关性
  22. First-in-man safety and pharmacokinetics of synthetic ozonide OZ439 demonstrates an improved exposure profile relative to other peroxide antimalarials合成性臭氧化物OZ439的首次人类安全性和药代动力学分析表明其暴露特性优于其他过氧化物抗疟药
  23. Effects of atomoxetine on the QT interval in healthy CYP2D6 poor metabolizers阿托莫西汀对健康CYP2D6弱代谢者QT间期的作用

Rashmi R. Shah

药物反应的种族差异已有详尽记录。药物诱导的QT间期延长是一个重大的安全问题,因此管理部门建议以临床全面QT研究(TQT)来了解新药的QT间期延长潜力。突破预设的管理限制实证研究由于要求必须有严谨的心电图监测而对后期临床试验有显著影响。现阶段进行的一些研究,虽然当前在统计学方面还站不住脚,但它们对研究人群的种族不影响TQT研究的假设提出了质疑。对现有药物遗传学和临床信息综合考虑的结果表明,药物的QT间期延长作用可能有种族间差异,白人可能比其他人种更加敏感。这些信息表明 (a) 这些差异可能依赖于药物的QT延长效果,(b) 要揭示这种差异,暴露–反应分析可能比QTc间期的简单变化更敏感。如果白人中的QT反应通常被发现比非白人更强烈,那么这对国内认可在外国人口中进行的TQT研究资料可能有显著的管理意义。然而,在将一个种族人群中的TQT研究结果外推至另一个种族人群和推测任何差异的最终临床相关性时,有必要对每一种药物都进行个体考量。必须在白人、东方/亚洲人口和非洲人口之间进一步进行设计充分、影响力更强的研究,方可得出坚实的 结论。

Online learning applied to a course on rational therapeutics: an international comparison between final year students of two medical schools对合理治疗学课程实施的在线学习:两所医科大学最后一年学生之间的国际比较

  1. Top of page
  2. Cannabidiol as potential anticancer drug大麻二酚是潜在的抗癌药物
  3. Is the cardiovascular system a therapeutic target for cannabidiol?心血管系统是大麻二酚的治疗靶点吗?
  4. Cannabidiol for neurodegenerative disorders: important new clinical applications for this phytocannabinoid?以大麻二酚治疗神经退行性疾病:这是这种植物源性大麻素类重要的新临床作用吗?
  5. Pharmacogenomics of warfarin in populations of African descent非洲裔人群中的华法令药物基因组学
  6. Drug-induced QT interval prolongation: does ethnicity of the thorough QT study population matter?药物诱导性QT间期延长:全面QT研究人群的种族有影响吗?
  7. Online learning applied to a course on rational therapeutics: an international comparison between final year students of two medical schools对合理治疗学课程实施的在线学习:两所医科大学最后一年学生之间的国际比较
  8. Double-blind, randomized, placebo-controlled study of safety, tolerability, pharmacokinetics and pharmacodynamics of TAK-683, an investigational metastin analogue in healthy men在健康人中针对研究性metastin类似物——TAK-683——的安全性、耐药性、药代动力学和药效学进行的一项双盲、随机、安慰剂对照研究
  9. Insulin at normal physiological levels does not prolong QTc interval in thorough QT studies performed in healthy volunteers正常生理水平的胰岛素在健康志愿者中进行的全面QT研究中不延长QTc间期
  10. An oral TRPV1 antagonist attenuates laser radiant-heat-evoked potentials and pain ratings from UVB-inflamed and normal skin一种能降低UVB致炎皮肤和正常皮肤激光辐射热诱发电位和疼痛评分的口服TRPV1拮抗剂
  11. Relationship between the receptor occupancy profile and pleiotropic effects of angiotensin II receptor blockers血管紧张素II受体阻断剂受体占有特征与多效作用之间的关系
  12. Low doses of fludrocortisone and hydrocortisone, alone or in combination, on vascular responsiveness to phenylephrine in healthy volunteers健康志愿者单独或联合应用低剂量氟氢可的松和氢化可的松对苯福林血管反应性的作用
  13. The effect of CYP3A inhibitors and inducers on the pharmacokinetics of telaprevir in healthy volunteersCYP3A抑制剂和诱导剂对特拉匹韦在健康志愿者中的药代动力学所起的作用
  14. The pharmacokinetics of darexaban are not affected to a clinically relevant degree by rifampicin, a strong inducer of P-glycoprotein and CYP3A4利福平(P-糖蛋白和CYP3A4的强效诱导剂)对darexaban的药代动力学影响无临床意义
  15. Effect of a herbal extract containing curcumin and piperine on midazolam, flurbiprofen and paracetamol (acetaminophen) pharmacokinetics in healthy volunteers一种含姜黄素和胡椒碱的草药提取物对咪达唑仑、氟比洛芬和扑热息痛(醋氨酚)在健康志愿者中的药代动力学影响
  16. Population pharmacokinetics of unbound mycophenolic acid in adult allogeneic haematopoietic cell transplantation: effect of pharmacogenetic factors未结合麦考酚酸在成人异基因造血干细胞移植中的人群药代动力学:遗传药理学因素的作用
  17. Apixaban, an oral, direct factor Xa inhibitor: single dose safety, pharmacokinetics, pharmacodynamics and food effect in healthy subjects口服Xa因子直接抑制剂——阿哌沙班:健康志愿者单次给药的安全性、药代动力学、药效学和食物作用
  18. Assessment of potential drug interactions by characterization of human drug metabolism pathways using non-invasive bile sampling利用非侵入式胆汁取样鉴定人体药物代谢通路评估潜在的药物相互作用
  19. Effect of peginterferon alfa-2a (40KD) on cytochrome P450 isoenzyme activity聚乙二醇干扰素alfa-2b(40KD)对细胞色素P450同工酶活性的作用
  20. Pharmacokinetics of eribulin mesylate in patients with solid tumours receiving repeated oral rifampicin甲磺酸艾日布林在接受重复剂量口服利福平的实体肿瘤患者中的药代动力学
  21. Association between eIF3a polymorphism and severe toxicity caused by platinum-based chemotherapy in non-small cell lung cancer patients非小细胞肺癌患者中的eIF3a基因多态性与铂类药物化疗导致严重毒性之间的相关性
  22. First-in-man safety and pharmacokinetics of synthetic ozonide OZ439 demonstrates an improved exposure profile relative to other peroxide antimalarials合成性臭氧化物OZ439的首次人类安全性和药代动力学分析表明其暴露特性优于其他过氧化物抗疟药
  23. Effects of atomoxetine on the QT interval in healthy CYP2D6 poor metabolizers阿托莫西汀对健康CYP2D6弱代谢者QT间期的作用

Robert Likic, Casey White, Sandro Cinti, Joel Purkiss, Joseph Fantone, Chris Chapman, Luka Bielen, Igor Francetic & Cary Engleberg

关于该课题的已知结论
  • 基于网络的学习不受教学场地、师资力量、学生数量或印刷资源的限制。
  • 投入开发成本之后,网络学习的展开非常有成本效益,并能长期进行。
  • 本研究的目的是对改编和全球性应用有关合理处方的电子学习资源的可行性和作用进行评估。
本研究的新发现
  • 共享、与治疗相关、基于网络的教育资源,能提供符合成本效益的方法和安全的环境,使学生的治疗技巧有所 改善。
  • 共享的在线学习资源对预算紧张、良好师资力量不足和教学场地有限的教学机构来说非常具有吸引力。
  • 在不久的将来,处方在线教学资源共享或共同发展中的学术伙伴关系将更常见。

Double-blind, randomized, placebo-controlled study of safety, tolerability, pharmacokinetics and pharmacodynamics of TAK-683, an investigational metastin analogue in healthy men在健康人中针对研究性metastin类似物——TAK-683——的安全性、耐药性、药代动力学和药效学进行的一项双盲、随机、安慰剂对照研究

  1. Top of page
  2. Cannabidiol as potential anticancer drug大麻二酚是潜在的抗癌药物
  3. Is the cardiovascular system a therapeutic target for cannabidiol?心血管系统是大麻二酚的治疗靶点吗?
  4. Cannabidiol for neurodegenerative disorders: important new clinical applications for this phytocannabinoid?以大麻二酚治疗神经退行性疾病:这是这种植物源性大麻素类重要的新临床作用吗?
  5. Pharmacogenomics of warfarin in populations of African descent非洲裔人群中的华法令药物基因组学
  6. Drug-induced QT interval prolongation: does ethnicity of the thorough QT study population matter?药物诱导性QT间期延长:全面QT研究人群的种族有影响吗?
  7. Online learning applied to a course on rational therapeutics: an international comparison between final year students of two medical schools对合理治疗学课程实施的在线学习:两所医科大学最后一年学生之间的国际比较
  8. Double-blind, randomized, placebo-controlled study of safety, tolerability, pharmacokinetics and pharmacodynamics of TAK-683, an investigational metastin analogue in healthy men在健康人中针对研究性metastin类似物——TAK-683——的安全性、耐药性、药代动力学和药效学进行的一项双盲、随机、安慰剂对照研究
  9. Insulin at normal physiological levels does not prolong QTc interval in thorough QT studies performed in healthy volunteers正常生理水平的胰岛素在健康志愿者中进行的全面QT研究中不延长QTc间期
  10. An oral TRPV1 antagonist attenuates laser radiant-heat-evoked potentials and pain ratings from UVB-inflamed and normal skin一种能降低UVB致炎皮肤和正常皮肤激光辐射热诱发电位和疼痛评分的口服TRPV1拮抗剂
  11. Relationship between the receptor occupancy profile and pleiotropic effects of angiotensin II receptor blockers血管紧张素II受体阻断剂受体占有特征与多效作用之间的关系
  12. Low doses of fludrocortisone and hydrocortisone, alone or in combination, on vascular responsiveness to phenylephrine in healthy volunteers健康志愿者单独或联合应用低剂量氟氢可的松和氢化可的松对苯福林血管反应性的作用
  13. The effect of CYP3A inhibitors and inducers on the pharmacokinetics of telaprevir in healthy volunteersCYP3A抑制剂和诱导剂对特拉匹韦在健康志愿者中的药代动力学所起的作用
  14. The pharmacokinetics of darexaban are not affected to a clinically relevant degree by rifampicin, a strong inducer of P-glycoprotein and CYP3A4利福平(P-糖蛋白和CYP3A4的强效诱导剂)对darexaban的药代动力学影响无临床意义
  15. Effect of a herbal extract containing curcumin and piperine on midazolam, flurbiprofen and paracetamol (acetaminophen) pharmacokinetics in healthy volunteers一种含姜黄素和胡椒碱的草药提取物对咪达唑仑、氟比洛芬和扑热息痛(醋氨酚)在健康志愿者中的药代动力学影响
  16. Population pharmacokinetics of unbound mycophenolic acid in adult allogeneic haematopoietic cell transplantation: effect of pharmacogenetic factors未结合麦考酚酸在成人异基因造血干细胞移植中的人群药代动力学:遗传药理学因素的作用
  17. Apixaban, an oral, direct factor Xa inhibitor: single dose safety, pharmacokinetics, pharmacodynamics and food effect in healthy subjects口服Xa因子直接抑制剂——阿哌沙班:健康志愿者单次给药的安全性、药代动力学、药效学和食物作用
  18. Assessment of potential drug interactions by characterization of human drug metabolism pathways using non-invasive bile sampling利用非侵入式胆汁取样鉴定人体药物代谢通路评估潜在的药物相互作用
  19. Effect of peginterferon alfa-2a (40KD) on cytochrome P450 isoenzyme activity聚乙二醇干扰素alfa-2b(40KD)对细胞色素P450同工酶活性的作用
  20. Pharmacokinetics of eribulin mesylate in patients with solid tumours receiving repeated oral rifampicin甲磺酸艾日布林在接受重复剂量口服利福平的实体肿瘤患者中的药代动力学
  21. Association between eIF3a polymorphism and severe toxicity caused by platinum-based chemotherapy in non-small cell lung cancer patients非小细胞肺癌患者中的eIF3a基因多态性与铂类药物化疗导致严重毒性之间的相关性
  22. First-in-man safety and pharmacokinetics of synthetic ozonide OZ439 demonstrates an improved exposure profile relative to other peroxide antimalarials合成性臭氧化物OZ439的首次人类安全性和药代动力学分析表明其暴露特性优于其他过氧化物抗疟药
  23. Effects of atomoxetine on the QT interval in healthy CYP2D6 poor metabolizers阿托莫西汀对健康CYP2D6弱代谢者QT间期的作用

Graham Scott, Irfan Ahmad, Katy Howard, David MacLean, Cristina Oliva, Steve Warrington, Darren Wilbraham & Paul Worthington

关于该课题的已知结论
  1. Metastin是KiSS1基因表达的一种肽类,是促性腺激素释放激素系统的调节剂。
  2. TAK-683是metastin类似物,研究表明其对雄性大鼠有睾酮抑制作用。
  3. Metastin类似物,如TAK-683,正作为去势难治性前列腺癌的治疗药被研究。
本研究的新发现
  • 本文报告了两项1期研究中关于健康人应用TAK-683的首次人体试验资料。
  • TAK-683单次皮下给药和持续皮下给药时耐药性良好。
  • TAK-683持续给药能将睾酮浓度抑制至去势水平以下。这是Metastin类似物的该作用在人体的首次体现。促黄体生成激素和卵泡刺激素浓度也被抑制,但是该作用没有一致的剂量依赖性。

Insulin at normal physiological levels does not prolong QTc interval in thorough QT studies performed in healthy volunteers正常生理水平的胰岛素在健康志愿者中进行的全面QT研究中不延长QTc间期

  1. Top of page
  2. Cannabidiol as potential anticancer drug大麻二酚是潜在的抗癌药物
  3. Is the cardiovascular system a therapeutic target for cannabidiol?心血管系统是大麻二酚的治疗靶点吗?
  4. Cannabidiol for neurodegenerative disorders: important new clinical applications for this phytocannabinoid?以大麻二酚治疗神经退行性疾病:这是这种植物源性大麻素类重要的新临床作用吗?
  5. Pharmacogenomics of warfarin in populations of African descent非洲裔人群中的华法令药物基因组学
  6. Drug-induced QT interval prolongation: does ethnicity of the thorough QT study population matter?药物诱导性QT间期延长:全面QT研究人群的种族有影响吗?
  7. Online learning applied to a course on rational therapeutics: an international comparison between final year students of two medical schools对合理治疗学课程实施的在线学习:两所医科大学最后一年学生之间的国际比较
  8. Double-blind, randomized, placebo-controlled study of safety, tolerability, pharmacokinetics and pharmacodynamics of TAK-683, an investigational metastin analogue in healthy men在健康人中针对研究性metastin类似物——TAK-683——的安全性、耐药性、药代动力学和药效学进行的一项双盲、随机、安慰剂对照研究
  9. Insulin at normal physiological levels does not prolong QTc interval in thorough QT studies performed in healthy volunteers正常生理水平的胰岛素在健康志愿者中进行的全面QT研究中不延长QTc间期
  10. An oral TRPV1 antagonist attenuates laser radiant-heat-evoked potentials and pain ratings from UVB-inflamed and normal skin一种能降低UVB致炎皮肤和正常皮肤激光辐射热诱发电位和疼痛评分的口服TRPV1拮抗剂
  11. Relationship between the receptor occupancy profile and pleiotropic effects of angiotensin II receptor blockers血管紧张素II受体阻断剂受体占有特征与多效作用之间的关系
  12. Low doses of fludrocortisone and hydrocortisone, alone or in combination, on vascular responsiveness to phenylephrine in healthy volunteers健康志愿者单独或联合应用低剂量氟氢可的松和氢化可的松对苯福林血管反应性的作用
  13. The effect of CYP3A inhibitors and inducers on the pharmacokinetics of telaprevir in healthy volunteersCYP3A抑制剂和诱导剂对特拉匹韦在健康志愿者中的药代动力学所起的作用
  14. The pharmacokinetics of darexaban are not affected to a clinically relevant degree by rifampicin, a strong inducer of P-glycoprotein and CYP3A4利福平(P-糖蛋白和CYP3A4的强效诱导剂)对darexaban的药代动力学影响无临床意义
  15. Effect of a herbal extract containing curcumin and piperine on midazolam, flurbiprofen and paracetamol (acetaminophen) pharmacokinetics in healthy volunteers一种含姜黄素和胡椒碱的草药提取物对咪达唑仑、氟比洛芬和扑热息痛(醋氨酚)在健康志愿者中的药代动力学影响
  16. Population pharmacokinetics of unbound mycophenolic acid in adult allogeneic haematopoietic cell transplantation: effect of pharmacogenetic factors未结合麦考酚酸在成人异基因造血干细胞移植中的人群药代动力学:遗传药理学因素的作用
  17. Apixaban, an oral, direct factor Xa inhibitor: single dose safety, pharmacokinetics, pharmacodynamics and food effect in healthy subjects口服Xa因子直接抑制剂——阿哌沙班:健康志愿者单次给药的安全性、药代动力学、药效学和食物作用
  18. Assessment of potential drug interactions by characterization of human drug metabolism pathways using non-invasive bile sampling利用非侵入式胆汁取样鉴定人体药物代谢通路评估潜在的药物相互作用
  19. Effect of peginterferon alfa-2a (40KD) on cytochrome P450 isoenzyme activity聚乙二醇干扰素alfa-2b(40KD)对细胞色素P450同工酶活性的作用
  20. Pharmacokinetics of eribulin mesylate in patients with solid tumours receiving repeated oral rifampicin甲磺酸艾日布林在接受重复剂量口服利福平的实体肿瘤患者中的药代动力学
  21. Association between eIF3a polymorphism and severe toxicity caused by platinum-based chemotherapy in non-small cell lung cancer patients非小细胞肺癌患者中的eIF3a基因多态性与铂类药物化疗导致严重毒性之间的相关性
  22. First-in-man safety and pharmacokinetics of synthetic ozonide OZ439 demonstrates an improved exposure profile relative to other peroxide antimalarials合成性臭氧化物OZ439的首次人类安全性和药代动力学分析表明其暴露特性优于其他过氧化物抗疟药
  23. Effects of atomoxetine on the QT interval in healthy CYP2D6 poor metabolizers阿托莫西汀对健康CYP2D6弱代谢者QT间期的作用

Jorg Taubel, Ulrike Lorch, Georg Ferber, Jatinder Singh, Velislav N. Batchvarov, Irina Savelieva & A. John Camm

关于该课题的已知结论
  • 用餐,尤其是当饮食中富含碳水化合物时,会使QT/RR关系发生改变。这是一个令人感兴趣的问题,因为这表明正常的生理变化能显著改变QTc
  • 目前我们对用餐后QTc缩短的潜在作用还不清楚。饮食可引起等摩尔量的C肽(C-peptide)和胰岛素释放。
  • 已经有其他作者描述过C肽应用后的QTc缩短,并有一项研究报告了胰岛素对QTc的延长作用。
本研究的新发现
  • 本研究以400 mg的莫西沙星(moxifloxacin)单次给药为阳性对照,考查了胰岛素在全面QT(TQT)研究的严格条件下对QT间期的作用。
  • 正常血糖钳夹期间的胰岛素浓度被升高至45μlU/ml的恒定浓度,在此期间内源性C肽释放被成功抑制。
  • 在正常血糖钳夹期间未发现QTcF的显著变化。观察到的最大作用是给药1.5小时后QTcF缩短2.6 ms(95% CI −5.3,0.2)。胰岛素对QTcF无影响,这一发现可通过浓度—反应分析得以证实——浓度—反应分析表明,QTc缩短与C肽有关,葡萄糖对此有反作用,从而能部分抵消C肽的作用,导致QTcF净值降低。

An oral TRPV1 antagonist attenuates laser radiant-heat-evoked potentials and pain ratings from UVB-inflamed and normal skin一种能降低UVB致炎皮肤和正常皮肤激光辐射热诱发电位和疼痛评分的口服TRPV1拮抗剂

  1. Top of page
  2. Cannabidiol as potential anticancer drug大麻二酚是潜在的抗癌药物
  3. Is the cardiovascular system a therapeutic target for cannabidiol?心血管系统是大麻二酚的治疗靶点吗?
  4. Cannabidiol for neurodegenerative disorders: important new clinical applications for this phytocannabinoid?以大麻二酚治疗神经退行性疾病:这是这种植物源性大麻素类重要的新临床作用吗?
  5. Pharmacogenomics of warfarin in populations of African descent非洲裔人群中的华法令药物基因组学
  6. Drug-induced QT interval prolongation: does ethnicity of the thorough QT study population matter?药物诱导性QT间期延长:全面QT研究人群的种族有影响吗?
  7. Online learning applied to a course on rational therapeutics: an international comparison between final year students of two medical schools对合理治疗学课程实施的在线学习:两所医科大学最后一年学生之间的国际比较
  8. Double-blind, randomized, placebo-controlled study of safety, tolerability, pharmacokinetics and pharmacodynamics of TAK-683, an investigational metastin analogue in healthy men在健康人中针对研究性metastin类似物——TAK-683——的安全性、耐药性、药代动力学和药效学进行的一项双盲、随机、安慰剂对照研究
  9. Insulin at normal physiological levels does not prolong QTc interval in thorough QT studies performed in healthy volunteers正常生理水平的胰岛素在健康志愿者中进行的全面QT研究中不延长QTc间期
  10. An oral TRPV1 antagonist attenuates laser radiant-heat-evoked potentials and pain ratings from UVB-inflamed and normal skin一种能降低UVB致炎皮肤和正常皮肤激光辐射热诱发电位和疼痛评分的口服TRPV1拮抗剂
  11. Relationship between the receptor occupancy profile and pleiotropic effects of angiotensin II receptor blockers血管紧张素II受体阻断剂受体占有特征与多效作用之间的关系
  12. Low doses of fludrocortisone and hydrocortisone, alone or in combination, on vascular responsiveness to phenylephrine in healthy volunteers健康志愿者单独或联合应用低剂量氟氢可的松和氢化可的松对苯福林血管反应性的作用
  13. The effect of CYP3A inhibitors and inducers on the pharmacokinetics of telaprevir in healthy volunteersCYP3A抑制剂和诱导剂对特拉匹韦在健康志愿者中的药代动力学所起的作用
  14. The pharmacokinetics of darexaban are not affected to a clinically relevant degree by rifampicin, a strong inducer of P-glycoprotein and CYP3A4利福平(P-糖蛋白和CYP3A4的强效诱导剂)对darexaban的药代动力学影响无临床意义
  15. Effect of a herbal extract containing curcumin and piperine on midazolam, flurbiprofen and paracetamol (acetaminophen) pharmacokinetics in healthy volunteers一种含姜黄素和胡椒碱的草药提取物对咪达唑仑、氟比洛芬和扑热息痛(醋氨酚)在健康志愿者中的药代动力学影响
  16. Population pharmacokinetics of unbound mycophenolic acid in adult allogeneic haematopoietic cell transplantation: effect of pharmacogenetic factors未结合麦考酚酸在成人异基因造血干细胞移植中的人群药代动力学:遗传药理学因素的作用
  17. Apixaban, an oral, direct factor Xa inhibitor: single dose safety, pharmacokinetics, pharmacodynamics and food effect in healthy subjects口服Xa因子直接抑制剂——阿哌沙班:健康志愿者单次给药的安全性、药代动力学、药效学和食物作用
  18. Assessment of potential drug interactions by characterization of human drug metabolism pathways using non-invasive bile sampling利用非侵入式胆汁取样鉴定人体药物代谢通路评估潜在的药物相互作用
  19. Effect of peginterferon alfa-2a (40KD) on cytochrome P450 isoenzyme activity聚乙二醇干扰素alfa-2b(40KD)对细胞色素P450同工酶活性的作用
  20. Pharmacokinetics of eribulin mesylate in patients with solid tumours receiving repeated oral rifampicin甲磺酸艾日布林在接受重复剂量口服利福平的实体肿瘤患者中的药代动力学
  21. Association between eIF3a polymorphism and severe toxicity caused by platinum-based chemotherapy in non-small cell lung cancer patients非小细胞肺癌患者中的eIF3a基因多态性与铂类药物化疗导致严重毒性之间的相关性
  22. First-in-man safety and pharmacokinetics of synthetic ozonide OZ439 demonstrates an improved exposure profile relative to other peroxide antimalarials合成性臭氧化物OZ439的首次人类安全性和药代动力学分析表明其暴露特性优于其他过氧化物抗疟药
  23. Effects of atomoxetine on the QT interval in healthy CYP2D6 poor metabolizers阿托莫西汀对健康CYP2D6弱代谢者QT间期的作用

Klaus Schaffler, Peter Reeh, W. Rachel Duan, Andrea E. Best, Ahmed A. Othman, Connie R. Faltynek, Charles Locke & Wolfram Nothaft

关于该课题的已知结论
  • 研究显示,新型TRPV1拮抗剂——ABT-102——在多个临床前疼痛模型中有疗效。过去许多疼痛计量研究(algesimetric studies)中批准的激光(辐射热)诱发电位幅度和直观模拟疼痛程度标尺法,被用来评估ABT-102在正常皮肤和UVB发炎皮肤中与安慰剂和两种活性对照相比较时的镇痛和抗痛觉过敏作用。
本研究的新发现
  • 利用该模型获得的结果表明,ABT-102有良好的耐受性,并能以剂量依赖方式有效减轻热痛敏和非热痛敏性疼痛。疼痛计量模型显示有可重复性,并证实其在一小部分正常健康志愿者中的适用性。

Relationship between the receptor occupancy profile and pleiotropic effects of angiotensin II receptor blockers血管紧张素II受体阻断剂受体占有特征与多效作用之间的关系

  1. Top of page
  2. Cannabidiol as potential anticancer drug大麻二酚是潜在的抗癌药物
  3. Is the cardiovascular system a therapeutic target for cannabidiol?心血管系统是大麻二酚的治疗靶点吗?
  4. Cannabidiol for neurodegenerative disorders: important new clinical applications for this phytocannabinoid?以大麻二酚治疗神经退行性疾病:这是这种植物源性大麻素类重要的新临床作用吗?
  5. Pharmacogenomics of warfarin in populations of African descent非洲裔人群中的华法令药物基因组学
  6. Drug-induced QT interval prolongation: does ethnicity of the thorough QT study population matter?药物诱导性QT间期延长:全面QT研究人群的种族有影响吗?
  7. Online learning applied to a course on rational therapeutics: an international comparison between final year students of two medical schools对合理治疗学课程实施的在线学习:两所医科大学最后一年学生之间的国际比较
  8. Double-blind, randomized, placebo-controlled study of safety, tolerability, pharmacokinetics and pharmacodynamics of TAK-683, an investigational metastin analogue in healthy men在健康人中针对研究性metastin类似物——TAK-683——的安全性、耐药性、药代动力学和药效学进行的一项双盲、随机、安慰剂对照研究
  9. Insulin at normal physiological levels does not prolong QTc interval in thorough QT studies performed in healthy volunteers正常生理水平的胰岛素在健康志愿者中进行的全面QT研究中不延长QTc间期
  10. An oral TRPV1 antagonist attenuates laser radiant-heat-evoked potentials and pain ratings from UVB-inflamed and normal skin一种能降低UVB致炎皮肤和正常皮肤激光辐射热诱发电位和疼痛评分的口服TRPV1拮抗剂
  11. Relationship between the receptor occupancy profile and pleiotropic effects of angiotensin II receptor blockers血管紧张素II受体阻断剂受体占有特征与多效作用之间的关系
  12. Low doses of fludrocortisone and hydrocortisone, alone or in combination, on vascular responsiveness to phenylephrine in healthy volunteers健康志愿者单独或联合应用低剂量氟氢可的松和氢化可的松对苯福林血管反应性的作用
  13. The effect of CYP3A inhibitors and inducers on the pharmacokinetics of telaprevir in healthy volunteersCYP3A抑制剂和诱导剂对特拉匹韦在健康志愿者中的药代动力学所起的作用
  14. The pharmacokinetics of darexaban are not affected to a clinically relevant degree by rifampicin, a strong inducer of P-glycoprotein and CYP3A4利福平(P-糖蛋白和CYP3A4的强效诱导剂)对darexaban的药代动力学影响无临床意义
  15. Effect of a herbal extract containing curcumin and piperine on midazolam, flurbiprofen and paracetamol (acetaminophen) pharmacokinetics in healthy volunteers一种含姜黄素和胡椒碱的草药提取物对咪达唑仑、氟比洛芬和扑热息痛(醋氨酚)在健康志愿者中的药代动力学影响
  16. Population pharmacokinetics of unbound mycophenolic acid in adult allogeneic haematopoietic cell transplantation: effect of pharmacogenetic factors未结合麦考酚酸在成人异基因造血干细胞移植中的人群药代动力学:遗传药理学因素的作用
  17. Apixaban, an oral, direct factor Xa inhibitor: single dose safety, pharmacokinetics, pharmacodynamics and food effect in healthy subjects口服Xa因子直接抑制剂——阿哌沙班:健康志愿者单次给药的安全性、药代动力学、药效学和食物作用
  18. Assessment of potential drug interactions by characterization of human drug metabolism pathways using non-invasive bile sampling利用非侵入式胆汁取样鉴定人体药物代谢通路评估潜在的药物相互作用
  19. Effect of peginterferon alfa-2a (40KD) on cytochrome P450 isoenzyme activity聚乙二醇干扰素alfa-2b(40KD)对细胞色素P450同工酶活性的作用
  20. Pharmacokinetics of eribulin mesylate in patients with solid tumours receiving repeated oral rifampicin甲磺酸艾日布林在接受重复剂量口服利福平的实体肿瘤患者中的药代动力学
  21. Association between eIF3a polymorphism and severe toxicity caused by platinum-based chemotherapy in non-small cell lung cancer patients非小细胞肺癌患者中的eIF3a基因多态性与铂类药物化疗导致严重毒性之间的相关性
  22. First-in-man safety and pharmacokinetics of synthetic ozonide OZ439 demonstrates an improved exposure profile relative to other peroxide antimalarials合成性臭氧化物OZ439的首次人类安全性和药代动力学分析表明其暴露特性优于其他过氧化物抗疟药
  23. Effects of atomoxetine on the QT interval in healthy CYP2D6 poor metabolizers阿托莫西汀对健康CYP2D6弱代谢者QT间期的作用

Hitoshi Ando, Kentarou Ushijima, Keiko Hosohata, Tetsuo Saito & Akio Fujimura

关于该课题的已知结论
  1. 血管紧张素II受体阻断剂(ARBs)对高血压患者的治疗临床有效。
  2. ARBs除能控制血压外还有多种作用,包括抗氧化和抗糖尿病特性。
本研究的新发现
  1. ARBs的受体占有存在差异。
  2. ARBs的受体占有特性与它们对氧化应激标记物的作用减小相关,但与其对胰岛素耐药性标记物的作用减小无关。
  3. ARBs可能既有受体占有依赖性又有受体占有非依赖性多效作用。

Low doses of fludrocortisone and hydrocortisone, alone or in combination, on vascular responsiveness to phenylephrine in healthy volunteers健康志愿者单独或联合应用低剂量氟氢可的松和氢化可的松对苯福林血管反应性的作用

  1. Top of page
  2. Cannabidiol as potential anticancer drug大麻二酚是潜在的抗癌药物
  3. Is the cardiovascular system a therapeutic target for cannabidiol?心血管系统是大麻二酚的治疗靶点吗?
  4. Cannabidiol for neurodegenerative disorders: important new clinical applications for this phytocannabinoid?以大麻二酚治疗神经退行性疾病:这是这种植物源性大麻素类重要的新临床作用吗?
  5. Pharmacogenomics of warfarin in populations of African descent非洲裔人群中的华法令药物基因组学
  6. Drug-induced QT interval prolongation: does ethnicity of the thorough QT study population matter?药物诱导性QT间期延长:全面QT研究人群的种族有影响吗?
  7. Online learning applied to a course on rational therapeutics: an international comparison between final year students of two medical schools对合理治疗学课程实施的在线学习:两所医科大学最后一年学生之间的国际比较
  8. Double-blind, randomized, placebo-controlled study of safety, tolerability, pharmacokinetics and pharmacodynamics of TAK-683, an investigational metastin analogue in healthy men在健康人中针对研究性metastin类似物——TAK-683——的安全性、耐药性、药代动力学和药效学进行的一项双盲、随机、安慰剂对照研究
  9. Insulin at normal physiological levels does not prolong QTc interval in thorough QT studies performed in healthy volunteers正常生理水平的胰岛素在健康志愿者中进行的全面QT研究中不延长QTc间期
  10. An oral TRPV1 antagonist attenuates laser radiant-heat-evoked potentials and pain ratings from UVB-inflamed and normal skin一种能降低UVB致炎皮肤和正常皮肤激光辐射热诱发电位和疼痛评分的口服TRPV1拮抗剂
  11. Relationship between the receptor occupancy profile and pleiotropic effects of angiotensin II receptor blockers血管紧张素II受体阻断剂受体占有特征与多效作用之间的关系
  12. Low doses of fludrocortisone and hydrocortisone, alone or in combination, on vascular responsiveness to phenylephrine in healthy volunteers健康志愿者单独或联合应用低剂量氟氢可的松和氢化可的松对苯福林血管反应性的作用
  13. The effect of CYP3A inhibitors and inducers on the pharmacokinetics of telaprevir in healthy volunteersCYP3A抑制剂和诱导剂对特拉匹韦在健康志愿者中的药代动力学所起的作用
  14. The pharmacokinetics of darexaban are not affected to a clinically relevant degree by rifampicin, a strong inducer of P-glycoprotein and CYP3A4利福平(P-糖蛋白和CYP3A4的强效诱导剂)对darexaban的药代动力学影响无临床意义
  15. Effect of a herbal extract containing curcumin and piperine on midazolam, flurbiprofen and paracetamol (acetaminophen) pharmacokinetics in healthy volunteers一种含姜黄素和胡椒碱的草药提取物对咪达唑仑、氟比洛芬和扑热息痛(醋氨酚)在健康志愿者中的药代动力学影响
  16. Population pharmacokinetics of unbound mycophenolic acid in adult allogeneic haematopoietic cell transplantation: effect of pharmacogenetic factors未结合麦考酚酸在成人异基因造血干细胞移植中的人群药代动力学:遗传药理学因素的作用
  17. Apixaban, an oral, direct factor Xa inhibitor: single dose safety, pharmacokinetics, pharmacodynamics and food effect in healthy subjects口服Xa因子直接抑制剂——阿哌沙班:健康志愿者单次给药的安全性、药代动力学、药效学和食物作用
  18. Assessment of potential drug interactions by characterization of human drug metabolism pathways using non-invasive bile sampling利用非侵入式胆汁取样鉴定人体药物代谢通路评估潜在的药物相互作用
  19. Effect of peginterferon alfa-2a (40KD) on cytochrome P450 isoenzyme activity聚乙二醇干扰素alfa-2b(40KD)对细胞色素P450同工酶活性的作用
  20. Pharmacokinetics of eribulin mesylate in patients with solid tumours receiving repeated oral rifampicin甲磺酸艾日布林在接受重复剂量口服利福平的实体肿瘤患者中的药代动力学
  21. Association between eIF3a polymorphism and severe toxicity caused by platinum-based chemotherapy in non-small cell lung cancer patients非小细胞肺癌患者中的eIF3a基因多态性与铂类药物化疗导致严重毒性之间的相关性
  22. First-in-man safety and pharmacokinetics of synthetic ozonide OZ439 demonstrates an improved exposure profile relative to other peroxide antimalarials合成性臭氧化物OZ439的首次人类安全性和药代动力学分析表明其暴露特性优于其他过氧化物抗疟药
  23. Effects of atomoxetine on the QT interval in healthy CYP2D6 poor metabolizers阿托莫西汀对健康CYP2D6弱代谢者QT间期的作用

Bruno Laviolle, Erwan Donal, Pascale Le Maguet, Fabrice Lainé & Eric Bellissant

关于该课题的已知结论
  • 研究表明以生理学剂量联合应用氢化可的松和氟氢可的松能改善对血管加压素无反应的感染性休克患者——尤其是相对肾上腺功能不足患者的预后。
  • 单药应用氢化可的松显示能增强健康志愿者的苯福林(phenylephrine)升压反应和感染性休克患者的去甲肾上腺素升压反应。氟氢可的松无相似资料。
  • 当前对感染性休克中双重补充糖皮质激素(氢化可的松)和盐皮质激素(氟氢可的松)的必要性存在争议。
本研究的新发现
  • 单药应用氟氢可的松和氢化可的松能减轻低醛固酮血症健康志愿者中的苯福林加压反应。
  • 氢化可的松和氟氢可的松的这些相似作用很可能表达了这两种类固醇在急性容积负荷背景下的快速非基因组血管扩张作用。

The effect of CYP3A inhibitors and inducers on the pharmacokinetics of telaprevir in healthy volunteersCYP3A抑制剂和诱导剂对特拉匹韦在健康志愿者中的药代动力学所起的作用

  1. Top of page
  2. Cannabidiol as potential anticancer drug大麻二酚是潜在的抗癌药物
  3. Is the cardiovascular system a therapeutic target for cannabidiol?心血管系统是大麻二酚的治疗靶点吗?
  4. Cannabidiol for neurodegenerative disorders: important new clinical applications for this phytocannabinoid?以大麻二酚治疗神经退行性疾病:这是这种植物源性大麻素类重要的新临床作用吗?
  5. Pharmacogenomics of warfarin in populations of African descent非洲裔人群中的华法令药物基因组学
  6. Drug-induced QT interval prolongation: does ethnicity of the thorough QT study population matter?药物诱导性QT间期延长:全面QT研究人群的种族有影响吗?
  7. Online learning applied to a course on rational therapeutics: an international comparison between final year students of two medical schools对合理治疗学课程实施的在线学习:两所医科大学最后一年学生之间的国际比较
  8. Double-blind, randomized, placebo-controlled study of safety, tolerability, pharmacokinetics and pharmacodynamics of TAK-683, an investigational metastin analogue in healthy men在健康人中针对研究性metastin类似物——TAK-683——的安全性、耐药性、药代动力学和药效学进行的一项双盲、随机、安慰剂对照研究
  9. Insulin at normal physiological levels does not prolong QTc interval in thorough QT studies performed in healthy volunteers正常生理水平的胰岛素在健康志愿者中进行的全面QT研究中不延长QTc间期
  10. An oral TRPV1 antagonist attenuates laser radiant-heat-evoked potentials and pain ratings from UVB-inflamed and normal skin一种能降低UVB致炎皮肤和正常皮肤激光辐射热诱发电位和疼痛评分的口服TRPV1拮抗剂
  11. Relationship between the receptor occupancy profile and pleiotropic effects of angiotensin II receptor blockers血管紧张素II受体阻断剂受体占有特征与多效作用之间的关系
  12. Low doses of fludrocortisone and hydrocortisone, alone or in combination, on vascular responsiveness to phenylephrine in healthy volunteers健康志愿者单独或联合应用低剂量氟氢可的松和氢化可的松对苯福林血管反应性的作用
  13. The effect of CYP3A inhibitors and inducers on the pharmacokinetics of telaprevir in healthy volunteersCYP3A抑制剂和诱导剂对特拉匹韦在健康志愿者中的药代动力学所起的作用
  14. The pharmacokinetics of darexaban are not affected to a clinically relevant degree by rifampicin, a strong inducer of P-glycoprotein and CYP3A4利福平(P-糖蛋白和CYP3A4的强效诱导剂)对darexaban的药代动力学影响无临床意义
  15. Effect of a herbal extract containing curcumin and piperine on midazolam, flurbiprofen and paracetamol (acetaminophen) pharmacokinetics in healthy volunteers一种含姜黄素和胡椒碱的草药提取物对咪达唑仑、氟比洛芬和扑热息痛(醋氨酚)在健康志愿者中的药代动力学影响
  16. Population pharmacokinetics of unbound mycophenolic acid in adult allogeneic haematopoietic cell transplantation: effect of pharmacogenetic factors未结合麦考酚酸在成人异基因造血干细胞移植中的人群药代动力学:遗传药理学因素的作用
  17. Apixaban, an oral, direct factor Xa inhibitor: single dose safety, pharmacokinetics, pharmacodynamics and food effect in healthy subjects口服Xa因子直接抑制剂——阿哌沙班:健康志愿者单次给药的安全性、药代动力学、药效学和食物作用
  18. Assessment of potential drug interactions by characterization of human drug metabolism pathways using non-invasive bile sampling利用非侵入式胆汁取样鉴定人体药物代谢通路评估潜在的药物相互作用
  19. Effect of peginterferon alfa-2a (40KD) on cytochrome P450 isoenzyme activity聚乙二醇干扰素alfa-2b(40KD)对细胞色素P450同工酶活性的作用
  20. Pharmacokinetics of eribulin mesylate in patients with solid tumours receiving repeated oral rifampicin甲磺酸艾日布林在接受重复剂量口服利福平的实体肿瘤患者中的药代动力学
  21. Association between eIF3a polymorphism and severe toxicity caused by platinum-based chemotherapy in non-small cell lung cancer patients非小细胞肺癌患者中的eIF3a基因多态性与铂类药物化疗导致严重毒性之间的相关性
  22. First-in-man safety and pharmacokinetics of synthetic ozonide OZ439 demonstrates an improved exposure profile relative to other peroxide antimalarials合成性臭氧化物OZ439的首次人类安全性和药代动力学分析表明其暴露特性优于其他过氧化物抗疟药
  23. Effects of atomoxetine on the QT interval in healthy CYP2D6 poor metabolizers阿托莫西汀对健康CYP2D6弱代谢者QT间期的作用

Varun Garg, Gurudatt Chandorkar, Yijun Yang, Nathalie Adda, Lindsay McNair, Katia Alves, Frances Smith & Rolf P. G. van Heeswijk

关于该课题的已知结论
  1. 特拉匹韦(Telaprevir)是一种治疗患有代偿性肝病的基因1型慢性丙型肝炎成年患者的丙型肝炎病毒蛋白酶抑制剂。体外研究表明CYP3A是参与特拉匹韦代谢的主要细胞色素P-450(CYP)同工酶。理解特拉匹韦与CYP3A抑制剂或诱导剂联合应用时的潜在药物间相互作用非常重要。
本研究的新发现
  1. CYP3A诱导剂利福平和依法韦仑能降低特拉匹韦的暴露水平,降低程度因其强度不同而有差异。特拉匹韦单次给药后联合应用CYP3A强抑制剂酮康唑可提高其暴露水平。然而,在稳定状态下,特拉匹韦暴露相对不易受CYP3A抑制剂影响。

The pharmacokinetics of darexaban are not affected to a clinically relevant degree by rifampicin, a strong inducer of P-glycoprotein and CYP3A4利福平(P-糖蛋白和CYP3A4的强效诱导剂)对darexaban的药代动力学影响无临床意义

  1. Top of page
  2. Cannabidiol as potential anticancer drug大麻二酚是潜在的抗癌药物
  3. Is the cardiovascular system a therapeutic target for cannabidiol?心血管系统是大麻二酚的治疗靶点吗?
  4. Cannabidiol for neurodegenerative disorders: important new clinical applications for this phytocannabinoid?以大麻二酚治疗神经退行性疾病:这是这种植物源性大麻素类重要的新临床作用吗?
  5. Pharmacogenomics of warfarin in populations of African descent非洲裔人群中的华法令药物基因组学
  6. Drug-induced QT interval prolongation: does ethnicity of the thorough QT study population matter?药物诱导性QT间期延长:全面QT研究人群的种族有影响吗?
  7. Online learning applied to a course on rational therapeutics: an international comparison between final year students of two medical schools对合理治疗学课程实施的在线学习:两所医科大学最后一年学生之间的国际比较
  8. Double-blind, randomized, placebo-controlled study of safety, tolerability, pharmacokinetics and pharmacodynamics of TAK-683, an investigational metastin analogue in healthy men在健康人中针对研究性metastin类似物——TAK-683——的安全性、耐药性、药代动力学和药效学进行的一项双盲、随机、安慰剂对照研究
  9. Insulin at normal physiological levels does not prolong QTc interval in thorough QT studies performed in healthy volunteers正常生理水平的胰岛素在健康志愿者中进行的全面QT研究中不延长QTc间期
  10. An oral TRPV1 antagonist attenuates laser radiant-heat-evoked potentials and pain ratings from UVB-inflamed and normal skin一种能降低UVB致炎皮肤和正常皮肤激光辐射热诱发电位和疼痛评分的口服TRPV1拮抗剂
  11. Relationship between the receptor occupancy profile and pleiotropic effects of angiotensin II receptor blockers血管紧张素II受体阻断剂受体占有特征与多效作用之间的关系
  12. Low doses of fludrocortisone and hydrocortisone, alone or in combination, on vascular responsiveness to phenylephrine in healthy volunteers健康志愿者单独或联合应用低剂量氟氢可的松和氢化可的松对苯福林血管反应性的作用
  13. The effect of CYP3A inhibitors and inducers on the pharmacokinetics of telaprevir in healthy volunteersCYP3A抑制剂和诱导剂对特拉匹韦在健康志愿者中的药代动力学所起的作用
  14. The pharmacokinetics of darexaban are not affected to a clinically relevant degree by rifampicin, a strong inducer of P-glycoprotein and CYP3A4利福平(P-糖蛋白和CYP3A4的强效诱导剂)对darexaban的药代动力学影响无临床意义
  15. Effect of a herbal extract containing curcumin and piperine on midazolam, flurbiprofen and paracetamol (acetaminophen) pharmacokinetics in healthy volunteers一种含姜黄素和胡椒碱的草药提取物对咪达唑仑、氟比洛芬和扑热息痛(醋氨酚)在健康志愿者中的药代动力学影响
  16. Population pharmacokinetics of unbound mycophenolic acid in adult allogeneic haematopoietic cell transplantation: effect of pharmacogenetic factors未结合麦考酚酸在成人异基因造血干细胞移植中的人群药代动力学:遗传药理学因素的作用
  17. Apixaban, an oral, direct factor Xa inhibitor: single dose safety, pharmacokinetics, pharmacodynamics and food effect in healthy subjects口服Xa因子直接抑制剂——阿哌沙班:健康志愿者单次给药的安全性、药代动力学、药效学和食物作用
  18. Assessment of potential drug interactions by characterization of human drug metabolism pathways using non-invasive bile sampling利用非侵入式胆汁取样鉴定人体药物代谢通路评估潜在的药物相互作用
  19. Effect of peginterferon alfa-2a (40KD) on cytochrome P450 isoenzyme activity聚乙二醇干扰素alfa-2b(40KD)对细胞色素P450同工酶活性的作用
  20. Pharmacokinetics of eribulin mesylate in patients with solid tumours receiving repeated oral rifampicin甲磺酸艾日布林在接受重复剂量口服利福平的实体肿瘤患者中的药代动力学
  21. Association between eIF3a polymorphism and severe toxicity caused by platinum-based chemotherapy in non-small cell lung cancer patients非小细胞肺癌患者中的eIF3a基因多态性与铂类药物化疗导致严重毒性之间的相关性
  22. First-in-man safety and pharmacokinetics of synthetic ozonide OZ439 demonstrates an improved exposure profile relative to other peroxide antimalarials合成性臭氧化物OZ439的首次人类安全性和药代动力学分析表明其暴露特性优于其他过氧化物抗疟药
  23. Effects of atomoxetine on the QT interval in healthy CYP2D6 poor metabolizers阿托莫西汀对健康CYP2D6弱代谢者QT间期的作用

Dorien Groenendaal, Gregory Strabach, Alberto Garcia-Hernandez, Takeshi Kadokura, Marten Heeringa, Roelof Mol, Charlotte Eltink & Hartmut Onkels

关于该课题的已知结论
  • Darexaban是一种为多种适用症开发为抗血栓形成药的口服凝血因子Xa的直接抑制剂。其他几种新型口服抗凝剂经CYP3A4酶代谢和P-糖蛋白转运,它们与利福平和酮康唑之间存在有临床意义的药物相互作用。
  • Darexaban几乎可以完全被代谢为其主要的活性成分——darexaban葡糖苷酸。在体外,CYP3A4代谢不参与darexaban葡糖苷酸的形成和代谢;darexaban(但不是darexaban葡糖苷酸)是一种体外P-糖蛋白底物。
本研究的新发现
  • 本研究显示,利福平对darexaban葡糖苷酸和darexaban药代动力学特征的影响无临床意义,这表明darexaban与CYP3A4或P-糖蛋白诱导剂之间的药物相互作用潜势很小。
  • 本研究旨在确定darexaban/darexaban葡糖苷酸对人体CYP3A4和P-糖蛋白体内诱导的敏感性。

Effect of a herbal extract containing curcumin and piperine on midazolam, flurbiprofen and paracetamol (acetaminophen) pharmacokinetics in healthy volunteers一种含姜黄素和胡椒碱的草药提取物对咪达唑仑、氟比洛芬和扑热息痛(醋氨酚)在健康志愿者中的药代动力学影响

  1. Top of page
  2. Cannabidiol as potential anticancer drug大麻二酚是潜在的抗癌药物
  3. Is the cardiovascular system a therapeutic target for cannabidiol?心血管系统是大麻二酚的治疗靶点吗?
  4. Cannabidiol for neurodegenerative disorders: important new clinical applications for this phytocannabinoid?以大麻二酚治疗神经退行性疾病:这是这种植物源性大麻素类重要的新临床作用吗?
  5. Pharmacogenomics of warfarin in populations of African descent非洲裔人群中的华法令药物基因组学
  6. Drug-induced QT interval prolongation: does ethnicity of the thorough QT study population matter?药物诱导性QT间期延长:全面QT研究人群的种族有影响吗?
  7. Online learning applied to a course on rational therapeutics: an international comparison between final year students of two medical schools对合理治疗学课程实施的在线学习:两所医科大学最后一年学生之间的国际比较
  8. Double-blind, randomized, placebo-controlled study of safety, tolerability, pharmacokinetics and pharmacodynamics of TAK-683, an investigational metastin analogue in healthy men在健康人中针对研究性metastin类似物——TAK-683——的安全性、耐药性、药代动力学和药效学进行的一项双盲、随机、安慰剂对照研究
  9. Insulin at normal physiological levels does not prolong QTc interval in thorough QT studies performed in healthy volunteers正常生理水平的胰岛素在健康志愿者中进行的全面QT研究中不延长QTc间期
  10. An oral TRPV1 antagonist attenuates laser radiant-heat-evoked potentials and pain ratings from UVB-inflamed and normal skin一种能降低UVB致炎皮肤和正常皮肤激光辐射热诱发电位和疼痛评分的口服TRPV1拮抗剂
  11. Relationship between the receptor occupancy profile and pleiotropic effects of angiotensin II receptor blockers血管紧张素II受体阻断剂受体占有特征与多效作用之间的关系
  12. Low doses of fludrocortisone and hydrocortisone, alone or in combination, on vascular responsiveness to phenylephrine in healthy volunteers健康志愿者单独或联合应用低剂量氟氢可的松和氢化可的松对苯福林血管反应性的作用
  13. The effect of CYP3A inhibitors and inducers on the pharmacokinetics of telaprevir in healthy volunteersCYP3A抑制剂和诱导剂对特拉匹韦在健康志愿者中的药代动力学所起的作用
  14. The pharmacokinetics of darexaban are not affected to a clinically relevant degree by rifampicin, a strong inducer of P-glycoprotein and CYP3A4利福平(P-糖蛋白和CYP3A4的强效诱导剂)对darexaban的药代动力学影响无临床意义
  15. Effect of a herbal extract containing curcumin and piperine on midazolam, flurbiprofen and paracetamol (acetaminophen) pharmacokinetics in healthy volunteers一种含姜黄素和胡椒碱的草药提取物对咪达唑仑、氟比洛芬和扑热息痛(醋氨酚)在健康志愿者中的药代动力学影响
  16. Population pharmacokinetics of unbound mycophenolic acid in adult allogeneic haematopoietic cell transplantation: effect of pharmacogenetic factors未结合麦考酚酸在成人异基因造血干细胞移植中的人群药代动力学:遗传药理学因素的作用
  17. Apixaban, an oral, direct factor Xa inhibitor: single dose safety, pharmacokinetics, pharmacodynamics and food effect in healthy subjects口服Xa因子直接抑制剂——阿哌沙班:健康志愿者单次给药的安全性、药代动力学、药效学和食物作用
  18. Assessment of potential drug interactions by characterization of human drug metabolism pathways using non-invasive bile sampling利用非侵入式胆汁取样鉴定人体药物代谢通路评估潜在的药物相互作用
  19. Effect of peginterferon alfa-2a (40KD) on cytochrome P450 isoenzyme activity聚乙二醇干扰素alfa-2b(40KD)对细胞色素P450同工酶活性的作用
  20. Pharmacokinetics of eribulin mesylate in patients with solid tumours receiving repeated oral rifampicin甲磺酸艾日布林在接受重复剂量口服利福平的实体肿瘤患者中的药代动力学
  21. Association between eIF3a polymorphism and severe toxicity caused by platinum-based chemotherapy in non-small cell lung cancer patients非小细胞肺癌患者中的eIF3a基因多态性与铂类药物化疗导致严重毒性之间的相关性
  22. First-in-man safety and pharmacokinetics of synthetic ozonide OZ439 demonstrates an improved exposure profile relative to other peroxide antimalarials合成性臭氧化物OZ439的首次人类安全性和药代动力学分析表明其暴露特性优于其他过氧化物抗疟药
  23. Effects of atomoxetine on the QT interval in healthy CYP2D6 poor metabolizers阿托莫西汀对健康CYP2D6弱代谢者QT间期的作用

Laurie P. Volak, Michael J. Hanley, Gina Masse, Suwagmani Hazarika, Jerold S. Harmatz, Vladimir Badmaev, Muhammed Majeed, David J. Greenblatt & Michael H. Court

关于该课题的已知结论
  1. 姜黄(Curcumina longa)提取物姜黄素和其他姜黄素类化合物正被作为癌症和阿尔茨海默病的潜在治疗药进行开发。
  2. 姜黄素类化合物的口服生物利用度较低,这在一定程度上与其广泛代谢有关。
  3. 利用结合黑胡椒的提取物——胡椒碱,能提高姜黄素类的口服利用度。
  4. 体外研究表明,姜黄素类和胡椒碱都有可能干扰CYP3A、CYP2C9、UGT和/或SULT的体内药物代谢作用。
本研究的新发现
  1. 本研究的结果表明,短期应用以胡椒碱增强药效的姜黄素类制备,不大可能产生与CYP3A、CYP2C9或扑热息痛(醋氨酚)结合酶代谢的药物有关的相互作用。
  2. 受测对象尽管使用了标准化胡椒素强化姜黄素制备,但仍然观察到较低的(非结合)姜黄素类和胡椒碱血药浓度,而相互作用的缺乏可能与短期疗程(2天)和/或这种低血药浓度相关。

Population pharmacokinetics of unbound mycophenolic acid in adult allogeneic haematopoietic cell transplantation: effect of pharmacogenetic factors未结合麦考酚酸在成人异基因造血干细胞移植中的人群药代动力学:遗传药理学因素的作用

  1. Top of page
  2. Cannabidiol as potential anticancer drug大麻二酚是潜在的抗癌药物
  3. Is the cardiovascular system a therapeutic target for cannabidiol?心血管系统是大麻二酚的治疗靶点吗?
  4. Cannabidiol for neurodegenerative disorders: important new clinical applications for this phytocannabinoid?以大麻二酚治疗神经退行性疾病:这是这种植物源性大麻素类重要的新临床作用吗?
  5. Pharmacogenomics of warfarin in populations of African descent非洲裔人群中的华法令药物基因组学
  6. Drug-induced QT interval prolongation: does ethnicity of the thorough QT study population matter?药物诱导性QT间期延长:全面QT研究人群的种族有影响吗?
  7. Online learning applied to a course on rational therapeutics: an international comparison between final year students of two medical schools对合理治疗学课程实施的在线学习:两所医科大学最后一年学生之间的国际比较
  8. Double-blind, randomized, placebo-controlled study of safety, tolerability, pharmacokinetics and pharmacodynamics of TAK-683, an investigational metastin analogue in healthy men在健康人中针对研究性metastin类似物——TAK-683——的安全性、耐药性、药代动力学和药效学进行的一项双盲、随机、安慰剂对照研究
  9. Insulin at normal physiological levels does not prolong QTc interval in thorough QT studies performed in healthy volunteers正常生理水平的胰岛素在健康志愿者中进行的全面QT研究中不延长QTc间期
  10. An oral TRPV1 antagonist attenuates laser radiant-heat-evoked potentials and pain ratings from UVB-inflamed and normal skin一种能降低UVB致炎皮肤和正常皮肤激光辐射热诱发电位和疼痛评分的口服TRPV1拮抗剂
  11. Relationship between the receptor occupancy profile and pleiotropic effects of angiotensin II receptor blockers血管紧张素II受体阻断剂受体占有特征与多效作用之间的关系
  12. Low doses of fludrocortisone and hydrocortisone, alone or in combination, on vascular responsiveness to phenylephrine in healthy volunteers健康志愿者单独或联合应用低剂量氟氢可的松和氢化可的松对苯福林血管反应性的作用
  13. The effect of CYP3A inhibitors and inducers on the pharmacokinetics of telaprevir in healthy volunteersCYP3A抑制剂和诱导剂对特拉匹韦在健康志愿者中的药代动力学所起的作用
  14. The pharmacokinetics of darexaban are not affected to a clinically relevant degree by rifampicin, a strong inducer of P-glycoprotein and CYP3A4利福平(P-糖蛋白和CYP3A4的强效诱导剂)对darexaban的药代动力学影响无临床意义
  15. Effect of a herbal extract containing curcumin and piperine on midazolam, flurbiprofen and paracetamol (acetaminophen) pharmacokinetics in healthy volunteers一种含姜黄素和胡椒碱的草药提取物对咪达唑仑、氟比洛芬和扑热息痛(醋氨酚)在健康志愿者中的药代动力学影响
  16. Population pharmacokinetics of unbound mycophenolic acid in adult allogeneic haematopoietic cell transplantation: effect of pharmacogenetic factors未结合麦考酚酸在成人异基因造血干细胞移植中的人群药代动力学:遗传药理学因素的作用
  17. Apixaban, an oral, direct factor Xa inhibitor: single dose safety, pharmacokinetics, pharmacodynamics and food effect in healthy subjects口服Xa因子直接抑制剂——阿哌沙班:健康志愿者单次给药的安全性、药代动力学、药效学和食物作用
  18. Assessment of potential drug interactions by characterization of human drug metabolism pathways using non-invasive bile sampling利用非侵入式胆汁取样鉴定人体药物代谢通路评估潜在的药物相互作用
  19. Effect of peginterferon alfa-2a (40KD) on cytochrome P450 isoenzyme activity聚乙二醇干扰素alfa-2b(40KD)对细胞色素P450同工酶活性的作用
  20. Pharmacokinetics of eribulin mesylate in patients with solid tumours receiving repeated oral rifampicin甲磺酸艾日布林在接受重复剂量口服利福平的实体肿瘤患者中的药代动力学
  21. Association between eIF3a polymorphism and severe toxicity caused by platinum-based chemotherapy in non-small cell lung cancer patients非小细胞肺癌患者中的eIF3a基因多态性与铂类药物化疗导致严重毒性之间的相关性
  22. First-in-man safety and pharmacokinetics of synthetic ozonide OZ439 demonstrates an improved exposure profile relative to other peroxide antimalarials合成性臭氧化物OZ439的首次人类安全性和药代动力学分析表明其暴露特性优于其他过氧化物抗疟药
  23. Effects of atomoxetine on the QT interval in healthy CYP2D6 poor metabolizers阿托莫西汀对健康CYP2D6弱代谢者QT间期的作用

Adam Frymoyer, Davide Verotta, Pamala Jacobson & Janel Long-Boyle

关于该课题的已知结论
  • 未结合麦考酚酸(MPA)在成年异基因造血干细胞移植(alloHCT)接受者中有很大的药代动力学差异,较低的暴露与较高的急性移植物抗宿主病(aGVHD)相关。
  • 患者特异性临床因素可能无法解释患者间差异。
本研究的新发现
  • 本研究首次探讨了遗传药理学因素对成年alloHCT接受者中未结合MPA的药代动力学影响。
  • 此外,加深了对未结合MPA暴露与aGVHD之间关系的理解。

Apixaban, an oral, direct factor Xa inhibitor: single dose safety, pharmacokinetics, pharmacodynamics and food effect in healthy subjects口服Xa因子直接抑制剂——阿哌沙班:健康志愿者单次给药的安全性、药代动力学、药效学和食物作用

  1. Top of page
  2. Cannabidiol as potential anticancer drug大麻二酚是潜在的抗癌药物
  3. Is the cardiovascular system a therapeutic target for cannabidiol?心血管系统是大麻二酚的治疗靶点吗?
  4. Cannabidiol for neurodegenerative disorders: important new clinical applications for this phytocannabinoid?以大麻二酚治疗神经退行性疾病:这是这种植物源性大麻素类重要的新临床作用吗?
  5. Pharmacogenomics of warfarin in populations of African descent非洲裔人群中的华法令药物基因组学
  6. Drug-induced QT interval prolongation: does ethnicity of the thorough QT study population matter?药物诱导性QT间期延长:全面QT研究人群的种族有影响吗?
  7. Online learning applied to a course on rational therapeutics: an international comparison between final year students of two medical schools对合理治疗学课程实施的在线学习:两所医科大学最后一年学生之间的国际比较
  8. Double-blind, randomized, placebo-controlled study of safety, tolerability, pharmacokinetics and pharmacodynamics of TAK-683, an investigational metastin analogue in healthy men在健康人中针对研究性metastin类似物——TAK-683——的安全性、耐药性、药代动力学和药效学进行的一项双盲、随机、安慰剂对照研究
  9. Insulin at normal physiological levels does not prolong QTc interval in thorough QT studies performed in healthy volunteers正常生理水平的胰岛素在健康志愿者中进行的全面QT研究中不延长QTc间期
  10. An oral TRPV1 antagonist attenuates laser radiant-heat-evoked potentials and pain ratings from UVB-inflamed and normal skin一种能降低UVB致炎皮肤和正常皮肤激光辐射热诱发电位和疼痛评分的口服TRPV1拮抗剂
  11. Relationship between the receptor occupancy profile and pleiotropic effects of angiotensin II receptor blockers血管紧张素II受体阻断剂受体占有特征与多效作用之间的关系
  12. Low doses of fludrocortisone and hydrocortisone, alone or in combination, on vascular responsiveness to phenylephrine in healthy volunteers健康志愿者单独或联合应用低剂量氟氢可的松和氢化可的松对苯福林血管反应性的作用
  13. The effect of CYP3A inhibitors and inducers on the pharmacokinetics of telaprevir in healthy volunteersCYP3A抑制剂和诱导剂对特拉匹韦在健康志愿者中的药代动力学所起的作用
  14. The pharmacokinetics of darexaban are not affected to a clinically relevant degree by rifampicin, a strong inducer of P-glycoprotein and CYP3A4利福平(P-糖蛋白和CYP3A4的强效诱导剂)对darexaban的药代动力学影响无临床意义
  15. Effect of a herbal extract containing curcumin and piperine on midazolam, flurbiprofen and paracetamol (acetaminophen) pharmacokinetics in healthy volunteers一种含姜黄素和胡椒碱的草药提取物对咪达唑仑、氟比洛芬和扑热息痛(醋氨酚)在健康志愿者中的药代动力学影响
  16. Population pharmacokinetics of unbound mycophenolic acid in adult allogeneic haematopoietic cell transplantation: effect of pharmacogenetic factors未结合麦考酚酸在成人异基因造血干细胞移植中的人群药代动力学:遗传药理学因素的作用
  17. Apixaban, an oral, direct factor Xa inhibitor: single dose safety, pharmacokinetics, pharmacodynamics and food effect in healthy subjects口服Xa因子直接抑制剂——阿哌沙班:健康志愿者单次给药的安全性、药代动力学、药效学和食物作用
  18. Assessment of potential drug interactions by characterization of human drug metabolism pathways using non-invasive bile sampling利用非侵入式胆汁取样鉴定人体药物代谢通路评估潜在的药物相互作用
  19. Effect of peginterferon alfa-2a (40KD) on cytochrome P450 isoenzyme activity聚乙二醇干扰素alfa-2b(40KD)对细胞色素P450同工酶活性的作用
  20. Pharmacokinetics of eribulin mesylate in patients with solid tumours receiving repeated oral rifampicin甲磺酸艾日布林在接受重复剂量口服利福平的实体肿瘤患者中的药代动力学
  21. Association between eIF3a polymorphism and severe toxicity caused by platinum-based chemotherapy in non-small cell lung cancer patients非小细胞肺癌患者中的eIF3a基因多态性与铂类药物化疗导致严重毒性之间的相关性
  22. First-in-man safety and pharmacokinetics of synthetic ozonide OZ439 demonstrates an improved exposure profile relative to other peroxide antimalarials合成性臭氧化物OZ439的首次人类安全性和药代动力学分析表明其暴露特性优于其他过氧化物抗疟药
  23. Effects of atomoxetine on the QT interval in healthy CYP2D6 poor metabolizers阿托莫西汀对健康CYP2D6弱代谢者QT间期的作用

Charles Frost, Jessie Wang, Sunil Nepal, Alan Schuster, Yu Chen Barrett, Rogelio Mosqueda-Garcia, Richard A. Reeves & Frank LaCreta

关于该课题的已知结论
  • 血栓性疾病仍然是西方国家的头号死亡原因,虽然现有的药物能有效降低血栓病相关风险,但它们也存在多种局限性。因此,已经有一些以抑制凝血酶或Xa因子为靶点的新型口服药被开发出来。阿哌沙班(Apixaban)是游离和与凝血酶原结合的Xa因子的一种有高度选择性、高强效性和口服利用度的凝血抑制剂。
本研究的新发现
  • 本报告首次描述了阿哌沙班安全性、耐受性、药代动力学和药效学在人体的评估结果,和食物对阿哌沙班药代动力学的作用。这些结果表明,阿哌沙班50 mg以内的单次口服给药在这个研究人群中可能是安全且通常是耐受良好的。阿哌沙班有线性药代动力学和浓度相关的药效学作用,其暴露不会受标准高脂高热量食物的影响。

Assessment of potential drug interactions by characterization of human drug metabolism pathways using non-invasive bile sampling利用非侵入式胆汁取样鉴定人体药物代谢通路评估潜在的药物相互作用

  1. Top of page
  2. Cannabidiol as potential anticancer drug大麻二酚是潜在的抗癌药物
  3. Is the cardiovascular system a therapeutic target for cannabidiol?心血管系统是大麻二酚的治疗靶点吗?
  4. Cannabidiol for neurodegenerative disorders: important new clinical applications for this phytocannabinoid?以大麻二酚治疗神经退行性疾病:这是这种植物源性大麻素类重要的新临床作用吗?
  5. Pharmacogenomics of warfarin in populations of African descent非洲裔人群中的华法令药物基因组学
  6. Drug-induced QT interval prolongation: does ethnicity of the thorough QT study population matter?药物诱导性QT间期延长:全面QT研究人群的种族有影响吗?
  7. Online learning applied to a course on rational therapeutics: an international comparison between final year students of two medical schools对合理治疗学课程实施的在线学习:两所医科大学最后一年学生之间的国际比较
  8. Double-blind, randomized, placebo-controlled study of safety, tolerability, pharmacokinetics and pharmacodynamics of TAK-683, an investigational metastin analogue in healthy men在健康人中针对研究性metastin类似物——TAK-683——的安全性、耐药性、药代动力学和药效学进行的一项双盲、随机、安慰剂对照研究
  9. Insulin at normal physiological levels does not prolong QTc interval in thorough QT studies performed in healthy volunteers正常生理水平的胰岛素在健康志愿者中进行的全面QT研究中不延长QTc间期
  10. An oral TRPV1 antagonist attenuates laser radiant-heat-evoked potentials and pain ratings from UVB-inflamed and normal skin一种能降低UVB致炎皮肤和正常皮肤激光辐射热诱发电位和疼痛评分的口服TRPV1拮抗剂
  11. Relationship between the receptor occupancy profile and pleiotropic effects of angiotensin II receptor blockers血管紧张素II受体阻断剂受体占有特征与多效作用之间的关系
  12. Low doses of fludrocortisone and hydrocortisone, alone or in combination, on vascular responsiveness to phenylephrine in healthy volunteers健康志愿者单独或联合应用低剂量氟氢可的松和氢化可的松对苯福林血管反应性的作用
  13. The effect of CYP3A inhibitors and inducers on the pharmacokinetics of telaprevir in healthy volunteersCYP3A抑制剂和诱导剂对特拉匹韦在健康志愿者中的药代动力学所起的作用
  14. The pharmacokinetics of darexaban are not affected to a clinically relevant degree by rifampicin, a strong inducer of P-glycoprotein and CYP3A4利福平(P-糖蛋白和CYP3A4的强效诱导剂)对darexaban的药代动力学影响无临床意义
  15. Effect of a herbal extract containing curcumin and piperine on midazolam, flurbiprofen and paracetamol (acetaminophen) pharmacokinetics in healthy volunteers一种含姜黄素和胡椒碱的草药提取物对咪达唑仑、氟比洛芬和扑热息痛(醋氨酚)在健康志愿者中的药代动力学影响
  16. Population pharmacokinetics of unbound mycophenolic acid in adult allogeneic haematopoietic cell transplantation: effect of pharmacogenetic factors未结合麦考酚酸在成人异基因造血干细胞移植中的人群药代动力学:遗传药理学因素的作用
  17. Apixaban, an oral, direct factor Xa inhibitor: single dose safety, pharmacokinetics, pharmacodynamics and food effect in healthy subjects口服Xa因子直接抑制剂——阿哌沙班:健康志愿者单次给药的安全性、药代动力学、药效学和食物作用
  18. Assessment of potential drug interactions by characterization of human drug metabolism pathways using non-invasive bile sampling利用非侵入式胆汁取样鉴定人体药物代谢通路评估潜在的药物相互作用
  19. Effect of peginterferon alfa-2a (40KD) on cytochrome P450 isoenzyme activity聚乙二醇干扰素alfa-2b(40KD)对细胞色素P450同工酶活性的作用
  20. Pharmacokinetics of eribulin mesylate in patients with solid tumours receiving repeated oral rifampicin甲磺酸艾日布林在接受重复剂量口服利福平的实体肿瘤患者中的药代动力学
  21. Association between eIF3a polymorphism and severe toxicity caused by platinum-based chemotherapy in non-small cell lung cancer patients非小细胞肺癌患者中的eIF3a基因多态性与铂类药物化疗导致严重毒性之间的相关性
  22. First-in-man safety and pharmacokinetics of synthetic ozonide OZ439 demonstrates an improved exposure profile relative to other peroxide antimalarials合成性臭氧化物OZ439的首次人类安全性和药代动力学分析表明其暴露特性优于其他过氧化物抗疟药
  23. Effects of atomoxetine on the QT interval in healthy CYP2D6 poor metabolizers阿托莫西汀对健康CYP2D6弱代谢者QT间期的作用

Jackie C. Bloomer, Mike Nash, Alison Webb, Bruce E. Miller, Aili L. Lazaar, Claire Beaumont & William J. Guiney

关于该课题的已知结论
  1. 以一种共用药去抑制药物清除机制会导致受害药物相互作用(victim drug interaction)。理解与药物清除有关的酶类和转运蛋白(这种理解通常来自体外系统)有助于通报药物相互作用的风险。
  2. 对于人类受试者,要将酶和转运蛋白的机制信息导入临床就必须具备药物知识和了解代谢物分泌特征,而通常来说这仅限于临床开发后期应用放射性标记药物后对尿液和粪便进行的代谢研究。
本研究的新发现
  1. 此项临床研究表明可以利用为药物和代谢物分析而采集的人胆汁样本在早期临床开发中通报药物的受害药物相互作用。
  2. 本研究采用非侵入式胆汁取样技术,评估了GSK1325756 —— 一种正被开发用于治疗慢性阻塞性肺病(COPD)的药物——在健康老年受试者中的胆汁处置。研究显示O-葡糖苷酸是胆汁中的主要代谢物,这表明GSK1325756的清除主要由UGT酶介导。
  3. 人胆汁中的氧化代谢物水平相对较低表明CYP酶对GSK1325756的消除影响较小。因此COPD患者联合用药的受害药物相互作用风险很低,这将使即将到来的临床试验对象招募更容易。

Effect of peginterferon alfa-2a (40KD) on cytochrome P450 isoenzyme activity聚乙二醇干扰素alfa-2b(40KD)对细胞色素P450同工酶活性的作用

  1. Top of page
  2. Cannabidiol as potential anticancer drug大麻二酚是潜在的抗癌药物
  3. Is the cardiovascular system a therapeutic target for cannabidiol?心血管系统是大麻二酚的治疗靶点吗?
  4. Cannabidiol for neurodegenerative disorders: important new clinical applications for this phytocannabinoid?以大麻二酚治疗神经退行性疾病:这是这种植物源性大麻素类重要的新临床作用吗?
  5. Pharmacogenomics of warfarin in populations of African descent非洲裔人群中的华法令药物基因组学
  6. Drug-induced QT interval prolongation: does ethnicity of the thorough QT study population matter?药物诱导性QT间期延长:全面QT研究人群的种族有影响吗?
  7. Online learning applied to a course on rational therapeutics: an international comparison between final year students of two medical schools对合理治疗学课程实施的在线学习:两所医科大学最后一年学生之间的国际比较
  8. Double-blind, randomized, placebo-controlled study of safety, tolerability, pharmacokinetics and pharmacodynamics of TAK-683, an investigational metastin analogue in healthy men在健康人中针对研究性metastin类似物——TAK-683——的安全性、耐药性、药代动力学和药效学进行的一项双盲、随机、安慰剂对照研究
  9. Insulin at normal physiological levels does not prolong QTc interval in thorough QT studies performed in healthy volunteers正常生理水平的胰岛素在健康志愿者中进行的全面QT研究中不延长QTc间期
  10. An oral TRPV1 antagonist attenuates laser radiant-heat-evoked potentials and pain ratings from UVB-inflamed and normal skin一种能降低UVB致炎皮肤和正常皮肤激光辐射热诱发电位和疼痛评分的口服TRPV1拮抗剂
  11. Relationship between the receptor occupancy profile and pleiotropic effects of angiotensin II receptor blockers血管紧张素II受体阻断剂受体占有特征与多效作用之间的关系
  12. Low doses of fludrocortisone and hydrocortisone, alone or in combination, on vascular responsiveness to phenylephrine in healthy volunteers健康志愿者单独或联合应用低剂量氟氢可的松和氢化可的松对苯福林血管反应性的作用
  13. The effect of CYP3A inhibitors and inducers on the pharmacokinetics of telaprevir in healthy volunteersCYP3A抑制剂和诱导剂对特拉匹韦在健康志愿者中的药代动力学所起的作用
  14. The pharmacokinetics of darexaban are not affected to a clinically relevant degree by rifampicin, a strong inducer of P-glycoprotein and CYP3A4利福平(P-糖蛋白和CYP3A4的强效诱导剂)对darexaban的药代动力学影响无临床意义
  15. Effect of a herbal extract containing curcumin and piperine on midazolam, flurbiprofen and paracetamol (acetaminophen) pharmacokinetics in healthy volunteers一种含姜黄素和胡椒碱的草药提取物对咪达唑仑、氟比洛芬和扑热息痛(醋氨酚)在健康志愿者中的药代动力学影响
  16. Population pharmacokinetics of unbound mycophenolic acid in adult allogeneic haematopoietic cell transplantation: effect of pharmacogenetic factors未结合麦考酚酸在成人异基因造血干细胞移植中的人群药代动力学:遗传药理学因素的作用
  17. Apixaban, an oral, direct factor Xa inhibitor: single dose safety, pharmacokinetics, pharmacodynamics and food effect in healthy subjects口服Xa因子直接抑制剂——阿哌沙班:健康志愿者单次给药的安全性、药代动力学、药效学和食物作用
  18. Assessment of potential drug interactions by characterization of human drug metabolism pathways using non-invasive bile sampling利用非侵入式胆汁取样鉴定人体药物代谢通路评估潜在的药物相互作用
  19. Effect of peginterferon alfa-2a (40KD) on cytochrome P450 isoenzyme activity聚乙二醇干扰素alfa-2b(40KD)对细胞色素P450同工酶活性的作用
  20. Pharmacokinetics of eribulin mesylate in patients with solid tumours receiving repeated oral rifampicin甲磺酸艾日布林在接受重复剂量口服利福平的实体肿瘤患者中的药代动力学
  21. Association between eIF3a polymorphism and severe toxicity caused by platinum-based chemotherapy in non-small cell lung cancer patients非小细胞肺癌患者中的eIF3a基因多态性与铂类药物化疗导致严重毒性之间的相关性
  22. First-in-man safety and pharmacokinetics of synthetic ozonide OZ439 demonstrates an improved exposure profile relative to other peroxide antimalarials合成性臭氧化物OZ439的首次人类安全性和药代动力学分析表明其暴露特性优于其他过氧化物抗疟药
  23. Effects of atomoxetine on the QT interval in healthy CYP2D6 poor metabolizers阿托莫西汀对健康CYP2D6弱代谢者QT间期的作用

Barbara J. Brennan, Zhi-Xin Xu & Joseph F. Grippo

关于该课题的已知结论
  1. 众所周知干扰素能下调肝脏细胞色素P450 (CYP)系统,从而减少药物代谢。
  2. 已有多项研究评估过干扰素与各种CYP同工酶代谢的药物之间的相互作用,这些研究资料表明,干扰素可降低CYP1A2的活性。
本研究的新发现
  1. 本研究考查了聚乙二醇干扰素(PEG-IFN)alfa-2a对CYP450系统——包括茶碱(CYP1A2)——代谢药物的作用。
  2. 此前已有研究考查过标准IFN或PEG-IFN alfa-2b对CYP450药物代谢酶活性的作用。然而,PEG-IFN alfa-2a的药代动力学、剂量和聚乙二醇化(pegylated)部分不同于标准的IFN和PEG-IFN-alfa-2b。
  3. PEG-IFN alfa-2a (40KD) 对CYP酶系统的任何作用都对接受联合药物治疗的丙型肝炎患者有重要影响。

Pharmacokinetics of eribulin mesylate in patients with solid tumours receiving repeated oral rifampicin甲磺酸艾日布林在接受重复剂量口服利福平的实体肿瘤患者中的药代动力学

  1. Top of page
  2. Cannabidiol as potential anticancer drug大麻二酚是潜在的抗癌药物
  3. Is the cardiovascular system a therapeutic target for cannabidiol?心血管系统是大麻二酚的治疗靶点吗?
  4. Cannabidiol for neurodegenerative disorders: important new clinical applications for this phytocannabinoid?以大麻二酚治疗神经退行性疾病:这是这种植物源性大麻素类重要的新临床作用吗?
  5. Pharmacogenomics of warfarin in populations of African descent非洲裔人群中的华法令药物基因组学
  6. Drug-induced QT interval prolongation: does ethnicity of the thorough QT study population matter?药物诱导性QT间期延长:全面QT研究人群的种族有影响吗?
  7. Online learning applied to a course on rational therapeutics: an international comparison between final year students of two medical schools对合理治疗学课程实施的在线学习:两所医科大学最后一年学生之间的国际比较
  8. Double-blind, randomized, placebo-controlled study of safety, tolerability, pharmacokinetics and pharmacodynamics of TAK-683, an investigational metastin analogue in healthy men在健康人中针对研究性metastin类似物——TAK-683——的安全性、耐药性、药代动力学和药效学进行的一项双盲、随机、安慰剂对照研究
  9. Insulin at normal physiological levels does not prolong QTc interval in thorough QT studies performed in healthy volunteers正常生理水平的胰岛素在健康志愿者中进行的全面QT研究中不延长QTc间期
  10. An oral TRPV1 antagonist attenuates laser radiant-heat-evoked potentials and pain ratings from UVB-inflamed and normal skin一种能降低UVB致炎皮肤和正常皮肤激光辐射热诱发电位和疼痛评分的口服TRPV1拮抗剂
  11. Relationship between the receptor occupancy profile and pleiotropic effects of angiotensin II receptor blockers血管紧张素II受体阻断剂受体占有特征与多效作用之间的关系
  12. Low doses of fludrocortisone and hydrocortisone, alone or in combination, on vascular responsiveness to phenylephrine in healthy volunteers健康志愿者单独或联合应用低剂量氟氢可的松和氢化可的松对苯福林血管反应性的作用
  13. The effect of CYP3A inhibitors and inducers on the pharmacokinetics of telaprevir in healthy volunteersCYP3A抑制剂和诱导剂对特拉匹韦在健康志愿者中的药代动力学所起的作用
  14. The pharmacokinetics of darexaban are not affected to a clinically relevant degree by rifampicin, a strong inducer of P-glycoprotein and CYP3A4利福平(P-糖蛋白和CYP3A4的强效诱导剂)对darexaban的药代动力学影响无临床意义
  15. Effect of a herbal extract containing curcumin and piperine on midazolam, flurbiprofen and paracetamol (acetaminophen) pharmacokinetics in healthy volunteers一种含姜黄素和胡椒碱的草药提取物对咪达唑仑、氟比洛芬和扑热息痛(醋氨酚)在健康志愿者中的药代动力学影响
  16. Population pharmacokinetics of unbound mycophenolic acid in adult allogeneic haematopoietic cell transplantation: effect of pharmacogenetic factors未结合麦考酚酸在成人异基因造血干细胞移植中的人群药代动力学:遗传药理学因素的作用
  17. Apixaban, an oral, direct factor Xa inhibitor: single dose safety, pharmacokinetics, pharmacodynamics and food effect in healthy subjects口服Xa因子直接抑制剂——阿哌沙班:健康志愿者单次给药的安全性、药代动力学、药效学和食物作用
  18. Assessment of potential drug interactions by characterization of human drug metabolism pathways using non-invasive bile sampling利用非侵入式胆汁取样鉴定人体药物代谢通路评估潜在的药物相互作用
  19. Effect of peginterferon alfa-2a (40KD) on cytochrome P450 isoenzyme activity聚乙二醇干扰素alfa-2b(40KD)对细胞色素P450同工酶活性的作用
  20. Pharmacokinetics of eribulin mesylate in patients with solid tumours receiving repeated oral rifampicin甲磺酸艾日布林在接受重复剂量口服利福平的实体肿瘤患者中的药代动力学
  21. Association between eIF3a polymorphism and severe toxicity caused by platinum-based chemotherapy in non-small cell lung cancer patients非小细胞肺癌患者中的eIF3a基因多态性与铂类药物化疗导致严重毒性之间的相关性
  22. First-in-man safety and pharmacokinetics of synthetic ozonide OZ439 demonstrates an improved exposure profile relative to other peroxide antimalarials合成性臭氧化物OZ439的首次人类安全性和药代动力学分析表明其暴露特性优于其他过氧化物抗疟药
  23. Effects of atomoxetine on the QT interval in healthy CYP2D6 poor metabolizers阿托莫西汀对健康CYP2D6弱代谢者QT间期的作用

Lot A. Devriese, Petronella (Els) O. Witteveen, Jantien Wanders, Kenneth Law, Geoff Edwards, Larisa Reyderman, William Copalu, Fuping Peng, Serena Marchetti, Jos H. Beijnen, Alwin D. R. Huitema, Emile E. Voest & Jan H. M. Schellens

关于该课题的已知结论
  • 甲磺酸艾日布林(eribulin mesylate)是一种最近被欧洲药品管理局(European Medicines Agency)批准用作单一疗法的非紫杉烷类微管动力学抑制剂,适用对象是在晚期疾病中至少经过两种化疗方案仍然进展的局部晚期或转移性乳腺癌患者。
  • 人肝微粒体临床前资料表明,艾日布林(eribulin)主要通过体外肝代谢清除,CYP3A4是参与代谢的主要酶。
  • 本研究的目的是探讨重复口服利福平这一典型的CYP3A4强效诱导剂对静脉滴注甲磺酸艾日布林的血浆药代动力学的作用。
本研究的新发现
  • 联合应用利福平对艾日布林单次给药暴露量不起作用。
  • 这些结果表明,甲磺酸艾日布林可以与CYP3A4诱导剂联合应用。

Association between eIF3a polymorphism and severe toxicity caused by platinum-based chemotherapy in non-small cell lung cancer patients非小细胞肺癌患者中的eIF3a基因多态性与铂类药物化疗导致严重毒性之间的相关性

  1. Top of page
  2. Cannabidiol as potential anticancer drug大麻二酚是潜在的抗癌药物
  3. Is the cardiovascular system a therapeutic target for cannabidiol?心血管系统是大麻二酚的治疗靶点吗?
  4. Cannabidiol for neurodegenerative disorders: important new clinical applications for this phytocannabinoid?以大麻二酚治疗神经退行性疾病:这是这种植物源性大麻素类重要的新临床作用吗?
  5. Pharmacogenomics of warfarin in populations of African descent非洲裔人群中的华法令药物基因组学
  6. Drug-induced QT interval prolongation: does ethnicity of the thorough QT study population matter?药物诱导性QT间期延长:全面QT研究人群的种族有影响吗?
  7. Online learning applied to a course on rational therapeutics: an international comparison between final year students of two medical schools对合理治疗学课程实施的在线学习:两所医科大学最后一年学生之间的国际比较
  8. Double-blind, randomized, placebo-controlled study of safety, tolerability, pharmacokinetics and pharmacodynamics of TAK-683, an investigational metastin analogue in healthy men在健康人中针对研究性metastin类似物——TAK-683——的安全性、耐药性、药代动力学和药效学进行的一项双盲、随机、安慰剂对照研究
  9. Insulin at normal physiological levels does not prolong QTc interval in thorough QT studies performed in healthy volunteers正常生理水平的胰岛素在健康志愿者中进行的全面QT研究中不延长QTc间期
  10. An oral TRPV1 antagonist attenuates laser radiant-heat-evoked potentials and pain ratings from UVB-inflamed and normal skin一种能降低UVB致炎皮肤和正常皮肤激光辐射热诱发电位和疼痛评分的口服TRPV1拮抗剂
  11. Relationship between the receptor occupancy profile and pleiotropic effects of angiotensin II receptor blockers血管紧张素II受体阻断剂受体占有特征与多效作用之间的关系
  12. Low doses of fludrocortisone and hydrocortisone, alone or in combination, on vascular responsiveness to phenylephrine in healthy volunteers健康志愿者单独或联合应用低剂量氟氢可的松和氢化可的松对苯福林血管反应性的作用
  13. The effect of CYP3A inhibitors and inducers on the pharmacokinetics of telaprevir in healthy volunteersCYP3A抑制剂和诱导剂对特拉匹韦在健康志愿者中的药代动力学所起的作用
  14. The pharmacokinetics of darexaban are not affected to a clinically relevant degree by rifampicin, a strong inducer of P-glycoprotein and CYP3A4利福平(P-糖蛋白和CYP3A4的强效诱导剂)对darexaban的药代动力学影响无临床意义
  15. Effect of a herbal extract containing curcumin and piperine on midazolam, flurbiprofen and paracetamol (acetaminophen) pharmacokinetics in healthy volunteers一种含姜黄素和胡椒碱的草药提取物对咪达唑仑、氟比洛芬和扑热息痛(醋氨酚)在健康志愿者中的药代动力学影响
  16. Population pharmacokinetics of unbound mycophenolic acid in adult allogeneic haematopoietic cell transplantation: effect of pharmacogenetic factors未结合麦考酚酸在成人异基因造血干细胞移植中的人群药代动力学:遗传药理学因素的作用
  17. Apixaban, an oral, direct factor Xa inhibitor: single dose safety, pharmacokinetics, pharmacodynamics and food effect in healthy subjects口服Xa因子直接抑制剂——阿哌沙班:健康志愿者单次给药的安全性、药代动力学、药效学和食物作用
  18. Assessment of potential drug interactions by characterization of human drug metabolism pathways using non-invasive bile sampling利用非侵入式胆汁取样鉴定人体药物代谢通路评估潜在的药物相互作用
  19. Effect of peginterferon alfa-2a (40KD) on cytochrome P450 isoenzyme activity聚乙二醇干扰素alfa-2b(40KD)对细胞色素P450同工酶活性的作用
  20. Pharmacokinetics of eribulin mesylate in patients with solid tumours receiving repeated oral rifampicin甲磺酸艾日布林在接受重复剂量口服利福平的实体肿瘤患者中的药代动力学
  21. Association between eIF3a polymorphism and severe toxicity caused by platinum-based chemotherapy in non-small cell lung cancer patients非小细胞肺癌患者中的eIF3a基因多态性与铂类药物化疗导致严重毒性之间的相关性
  22. First-in-man safety and pharmacokinetics of synthetic ozonide OZ439 demonstrates an improved exposure profile relative to other peroxide antimalarials合成性臭氧化物OZ439的首次人类安全性和药代动力学分析表明其暴露特性优于其他过氧化物抗疟药
  23. Effects of atomoxetine on the QT interval in healthy CYP2D6 poor metabolizers阿托莫西汀对健康CYP2D6弱代谢者QT间期的作用

Xiaojing Xu, Lifang Han, Li Duan, Yingchun Zhao, Huaping Yang, Boting Zhou, Rui Ma, Ruixia Yuan, Honghao Zhou & Zhaoqian Liu

关于该课题的已知结论
  • 肾毒性和耳毒性都是铂类治疗中的严重毒性,构成了阻碍癌症病人化疗成功的一道障碍。文献已经详实记载了铂类药物治疗方案的巨大个体间变异性。预测严重铂类毒性和反应的潜在生物标记物将显著提高临床疗效。eIF3a在DNA修复通路的活性调节中起着至关重要的作用,并能促进肺癌患者的铂反应。
本研究的新发现
  • 本研究确定了一种新的eIF3a无义突变,其与中国非小细胞肺癌(NSCLC)患者中铂诱导的肾毒性和耳毒性相关。这可能是预先确定有较大铂毒性风险患者的新型有效生物标记物,对NSCLC患者的个体化化疗提供了重要的信息。

First-in-man safety and pharmacokinetics of synthetic ozonide OZ439 demonstrates an improved exposure profile relative to other peroxide antimalarials合成性臭氧化物OZ439的首次人类安全性和药代动力学分析表明其暴露特性优于其他过氧化物抗疟药

  1. Top of page
  2. Cannabidiol as potential anticancer drug大麻二酚是潜在的抗癌药物
  3. Is the cardiovascular system a therapeutic target for cannabidiol?心血管系统是大麻二酚的治疗靶点吗?
  4. Cannabidiol for neurodegenerative disorders: important new clinical applications for this phytocannabinoid?以大麻二酚治疗神经退行性疾病:这是这种植物源性大麻素类重要的新临床作用吗?
  5. Pharmacogenomics of warfarin in populations of African descent非洲裔人群中的华法令药物基因组学
  6. Drug-induced QT interval prolongation: does ethnicity of the thorough QT study population matter?药物诱导性QT间期延长:全面QT研究人群的种族有影响吗?
  7. Online learning applied to a course on rational therapeutics: an international comparison between final year students of two medical schools对合理治疗学课程实施的在线学习:两所医科大学最后一年学生之间的国际比较
  8. Double-blind, randomized, placebo-controlled study of safety, tolerability, pharmacokinetics and pharmacodynamics of TAK-683, an investigational metastin analogue in healthy men在健康人中针对研究性metastin类似物——TAK-683——的安全性、耐药性、药代动力学和药效学进行的一项双盲、随机、安慰剂对照研究
  9. Insulin at normal physiological levels does not prolong QTc interval in thorough QT studies performed in healthy volunteers正常生理水平的胰岛素在健康志愿者中进行的全面QT研究中不延长QTc间期
  10. An oral TRPV1 antagonist attenuates laser radiant-heat-evoked potentials and pain ratings from UVB-inflamed and normal skin一种能降低UVB致炎皮肤和正常皮肤激光辐射热诱发电位和疼痛评分的口服TRPV1拮抗剂
  11. Relationship between the receptor occupancy profile and pleiotropic effects of angiotensin II receptor blockers血管紧张素II受体阻断剂受体占有特征与多效作用之间的关系
  12. Low doses of fludrocortisone and hydrocortisone, alone or in combination, on vascular responsiveness to phenylephrine in healthy volunteers健康志愿者单独或联合应用低剂量氟氢可的松和氢化可的松对苯福林血管反应性的作用
  13. The effect of CYP3A inhibitors and inducers on the pharmacokinetics of telaprevir in healthy volunteersCYP3A抑制剂和诱导剂对特拉匹韦在健康志愿者中的药代动力学所起的作用
  14. The pharmacokinetics of darexaban are not affected to a clinically relevant degree by rifampicin, a strong inducer of P-glycoprotein and CYP3A4利福平(P-糖蛋白和CYP3A4的强效诱导剂)对darexaban的药代动力学影响无临床意义
  15. Effect of a herbal extract containing curcumin and piperine on midazolam, flurbiprofen and paracetamol (acetaminophen) pharmacokinetics in healthy volunteers一种含姜黄素和胡椒碱的草药提取物对咪达唑仑、氟比洛芬和扑热息痛(醋氨酚)在健康志愿者中的药代动力学影响
  16. Population pharmacokinetics of unbound mycophenolic acid in adult allogeneic haematopoietic cell transplantation: effect of pharmacogenetic factors未结合麦考酚酸在成人异基因造血干细胞移植中的人群药代动力学:遗传药理学因素的作用
  17. Apixaban, an oral, direct factor Xa inhibitor: single dose safety, pharmacokinetics, pharmacodynamics and food effect in healthy subjects口服Xa因子直接抑制剂——阿哌沙班:健康志愿者单次给药的安全性、药代动力学、药效学和食物作用
  18. Assessment of potential drug interactions by characterization of human drug metabolism pathways using non-invasive bile sampling利用非侵入式胆汁取样鉴定人体药物代谢通路评估潜在的药物相互作用
  19. Effect of peginterferon alfa-2a (40KD) on cytochrome P450 isoenzyme activity聚乙二醇干扰素alfa-2b(40KD)对细胞色素P450同工酶活性的作用
  20. Pharmacokinetics of eribulin mesylate in patients with solid tumours receiving repeated oral rifampicin甲磺酸艾日布林在接受重复剂量口服利福平的实体肿瘤患者中的药代动力学
  21. Association between eIF3a polymorphism and severe toxicity caused by platinum-based chemotherapy in non-small cell lung cancer patients非小细胞肺癌患者中的eIF3a基因多态性与铂类药物化疗导致严重毒性之间的相关性
  22. First-in-man safety and pharmacokinetics of synthetic ozonide OZ439 demonstrates an improved exposure profile relative to other peroxide antimalarials合成性臭氧化物OZ439的首次人类安全性和药代动力学分析表明其暴露特性优于其他过氧化物抗疟药
  23. Effects of atomoxetine on the QT interval in healthy CYP2D6 poor metabolizers阿托莫西汀对健康CYP2D6弱代谢者QT间期的作用

Joerg J. Moehrle, Stephan Duparc, Christoph Siethoff, Paul L. M. van Giersbergen, J. Carl Craft, Sarah Arbe-Barnes, Susan A. Charman, Maria Gutierrez, Sergio Wittlin & Jonathan L. Vennerstrom

关于该课题的已知结论
  • OZ439是一种合成性过氧化物候选抗疟药,其在体外和动物模型中表现出非常寻常的抗疟疾和药代动力学特性。它在整个无性生殖的疟原虫(Plasmodium falciparum)红细胞期是快速作用的激动剂,其IC50值与临床使用的青蒿素衍生物不相上下。与所有其他合成性过氧化物和半合成性青蒿素衍生物不同的是,OZ439在20 mg/kg的口服剂量下就能完全治愈伯氏疟原虫(Plasmodium berghei)感染的小鼠,显示出有优于一系列当前应用的抗疟药(包括甲氟喹)的疾病预防活性。
本研究的新发现
  • 我们报告了OZ439首次在人类志愿者中的应用。本文罗列了从50至1600 mg单次给药和200–800 mg重复3天给药的耐药性和药代动力学原始资料。这些结果证实了预测的OZ439长时间血浓度,表明其是有单药抗疟疗法适当特征的首个内过氧化物药物。

Effects of atomoxetine on the QT interval in healthy CYP2D6 poor metabolizers阿托莫西汀对健康CYP2D6弱代谢者QT间期的作用

  1. Top of page
  2. Cannabidiol as potential anticancer drug大麻二酚是潜在的抗癌药物
  3. Is the cardiovascular system a therapeutic target for cannabidiol?心血管系统是大麻二酚的治疗靶点吗?
  4. Cannabidiol for neurodegenerative disorders: important new clinical applications for this phytocannabinoid?以大麻二酚治疗神经退行性疾病:这是这种植物源性大麻素类重要的新临床作用吗?
  5. Pharmacogenomics of warfarin in populations of African descent非洲裔人群中的华法令药物基因组学
  6. Drug-induced QT interval prolongation: does ethnicity of the thorough QT study population matter?药物诱导性QT间期延长:全面QT研究人群的种族有影响吗?
  7. Online learning applied to a course on rational therapeutics: an international comparison between final year students of two medical schools对合理治疗学课程实施的在线学习:两所医科大学最后一年学生之间的国际比较
  8. Double-blind, randomized, placebo-controlled study of safety, tolerability, pharmacokinetics and pharmacodynamics of TAK-683, an investigational metastin analogue in healthy men在健康人中针对研究性metastin类似物——TAK-683——的安全性、耐药性、药代动力学和药效学进行的一项双盲、随机、安慰剂对照研究
  9. Insulin at normal physiological levels does not prolong QTc interval in thorough QT studies performed in healthy volunteers正常生理水平的胰岛素在健康志愿者中进行的全面QT研究中不延长QTc间期
  10. An oral TRPV1 antagonist attenuates laser radiant-heat-evoked potentials and pain ratings from UVB-inflamed and normal skin一种能降低UVB致炎皮肤和正常皮肤激光辐射热诱发电位和疼痛评分的口服TRPV1拮抗剂
  11. Relationship between the receptor occupancy profile and pleiotropic effects of angiotensin II receptor blockers血管紧张素II受体阻断剂受体占有特征与多效作用之间的关系
  12. Low doses of fludrocortisone and hydrocortisone, alone or in combination, on vascular responsiveness to phenylephrine in healthy volunteers健康志愿者单独或联合应用低剂量氟氢可的松和氢化可的松对苯福林血管反应性的作用
  13. The effect of CYP3A inhibitors and inducers on the pharmacokinetics of telaprevir in healthy volunteersCYP3A抑制剂和诱导剂对特拉匹韦在健康志愿者中的药代动力学所起的作用
  14. The pharmacokinetics of darexaban are not affected to a clinically relevant degree by rifampicin, a strong inducer of P-glycoprotein and CYP3A4利福平(P-糖蛋白和CYP3A4的强效诱导剂)对darexaban的药代动力学影响无临床意义
  15. Effect of a herbal extract containing curcumin and piperine on midazolam, flurbiprofen and paracetamol (acetaminophen) pharmacokinetics in healthy volunteers一种含姜黄素和胡椒碱的草药提取物对咪达唑仑、氟比洛芬和扑热息痛(醋氨酚)在健康志愿者中的药代动力学影响
  16. Population pharmacokinetics of unbound mycophenolic acid in adult allogeneic haematopoietic cell transplantation: effect of pharmacogenetic factors未结合麦考酚酸在成人异基因造血干细胞移植中的人群药代动力学:遗传药理学因素的作用
  17. Apixaban, an oral, direct factor Xa inhibitor: single dose safety, pharmacokinetics, pharmacodynamics and food effect in healthy subjects口服Xa因子直接抑制剂——阿哌沙班:健康志愿者单次给药的安全性、药代动力学、药效学和食物作用
  18. Assessment of potential drug interactions by characterization of human drug metabolism pathways using non-invasive bile sampling利用非侵入式胆汁取样鉴定人体药物代谢通路评估潜在的药物相互作用
  19. Effect of peginterferon alfa-2a (40KD) on cytochrome P450 isoenzyme activity聚乙二醇干扰素alfa-2b(40KD)对细胞色素P450同工酶活性的作用
  20. Pharmacokinetics of eribulin mesylate in patients with solid tumours receiving repeated oral rifampicin甲磺酸艾日布林在接受重复剂量口服利福平的实体肿瘤患者中的药代动力学
  21. Association between eIF3a polymorphism and severe toxicity caused by platinum-based chemotherapy in non-small cell lung cancer patients非小细胞肺癌患者中的eIF3a基因多态性与铂类药物化疗导致严重毒性之间的相关性
  22. First-in-man safety and pharmacokinetics of synthetic ozonide OZ439 demonstrates an improved exposure profile relative to other peroxide antimalarials合成性臭氧化物OZ439的首次人类安全性和药代动力学分析表明其暴露特性优于其他过氧化物抗疟药
  23. Effects of atomoxetine on the QT interval in healthy CYP2D6 poor metabolizers阿托莫西汀对健康CYP2D6弱代谢者QT间期的作用

Corina Loghin, Harry Haber, Charles M. Beasley, Jr, Prajakti A. Kothare, Lynnette Kauffman, John April, Ling Jin, Albert J. Allen & Malcolm I. Mitchell

关于该课题的已知结论
  • 在开展本研究之前,阿托莫西汀(atomoxetine)对心率校正QT间期(QTc)离散度的影响估计是由以临床各种适当剂量给药、进入临床试验的常规临床人口而得出的结果。
本研究的新发现
  • 本文向临床药理学界报告了最大暴露水平的阿托莫西汀(在TQT研究中接受最大允许剂量的CYP2D6弱代谢受试者)对QTc的潜在影响。