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Dr. Stefan Peukert, Dr. Feng He, Miao Dai, Rui Zhang, Yingchuan Sun, Dr. Karen Miller-Moslin, Michael McEwan, Dr. Bharat Lagu, Kate Wang, Dr. Naeem Yusuff, Aaron Bourret, Arun Ramamurthy, Dr. Wieslawa Maniara, Adam Amaral, Anthony Vattay, Anlai Wang, Ribo Guo, Jing Yuan, John Green, Dr. Juliet Williams, Dr. Silvia Buonamici, Dr. Joseph F. Kelleher III and Dr. Marion Dorsch Discovery of NVP-LEQ506, a Second-Generation Inhibitor of Smoothened ChemMedChem 8

Version of Record online: 2 JUL 2013 | DOI: 10.1002/cmdc.201300217

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First disclosure: Continued optimization provided a novel type of Smoothened (Smo) antagonist based on a pyridazine core. The compound, NVP-LEQ506, currently in phase I clinical trials, combines high intrinsic potency and good pharmacokinetic properties resulting in excellent efficacy in rodent tumor models of medulloblastoma. Activity against a Smo mutant conferring resistance observed in a previous clinical trial with a competitor compound suggests additional therapeutic potential.

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