Antiviral Drugs: From Basic Discovery through Clinical Trials

Copyright © 2011 John Wiley & Sons, Inc.

Antiviral Drugs: From Basic Discovery through Clinical Trials

Editor(s): Wieslaw M. Kazmierski

Published Online: 20 JUN 2011 08:42AM EST

Print ISBN: 9780470455630

Online ISBN: 9780470929353

DOI: 10.1002/9780470929353

About this Book

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About The Product

This book focuses on new small molecule approaches to combat viral infections. The chapters describe the discovery and development from bench through the clinic of relatively recently-approved antiviral drugs and compounds in advanced clinical development. Organized by a virus (such as HIV, HCV, RSV, influenza, HBV and CMV) and written by top academic and industrial authorities in the field, the book provides a unique opportunity to study, understand and apply discovery and development principles and learning without the need for an individual to research, analyze and synthesize all immense sourcing references.  Topics showcase challenges and solutions of issues encountered, offering tremendous experience accumulated over many years of research that will be particularly useful to basic and bench scientists as well as clinicians as they continue discovering and developing new drugs and therapies.

Table of contents

    1. You have free access to this content
      Frontmatter (pages i–xiii)

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      Color Plates (pages c1–c16)

  3. Part I: Human Immunodeficiency Virus - Section I: HIV Protease Inhibitors

    1. Chapter 1

      Discovery and Development of Atazanavir (pages 1–17)

      Awny Farajallah, R. Todd Bunch and Nicholas A. Meanwell

    2. Chapter 2

      Discovery and Development of PL-100, A Novel HIV-1 Protease Inhibitor (pages 19–30)

      Jinzi J. Wu and Joseph Musto

    3. Chapter 3

      Darunavir (Prezista, TMC114): From Bench to Clinic, Improving Treatment Options for HIV-Infected Patients (pages 31–45)

      Marie-Pierre de Béthune, Vanitha Sekar, Sabrina Spinosa-Guzman, Marc Vanstockem, Sandra De Meyer, Piet Wigerinck and Eric Lefebvre

    4. Chapter 4

      Discovery and Development of Tipranavir (pages 47–57)

      Karen R. Romines

  4. Part I: Human Immunodeficiency Virus - Section II: HIV Non-nucleoside Reverse Transcriptase Inhibitors

    1. Chapter 5

      TMC278 (Rilpivirine): A Next-Generation NNRTI in Phase III Clinical Development for Treatment-Naive Patients (pages 59–69)

      Jérôme Guillemont, Katia Boven, Herta Crauwels and Marie-Pierre de Béthune

    2. Chapter 6

      Etravirine: From TMC125 to Intelence: A Treatment Paradigm Shift for HIV-Infected Patients (pages 71–84)

      Koen Andries, Ann Debunne, Thomas N. Kakuda, Michael Kukla, Ruud Leemans, Johan Vingerhoets, Brian Woodfall and Marie-Pierre de Béthune

  5. Part I: Human Immunodeficiency Virus - Section III: HIV Nucleoside Reverse Transcriptase Inhibitors

    1. Chapter 7

      Discovery and Development of Tenofovir Disoproxil Fumarate (pages 85–101)

      Erik De Clercq

    2. Chapter 8

      Discovery and Development of Apricitabine (pages 103–116)

      Susan Cox, John Deadman, Justine Southby and Jonathan Coates

  6. Part I: Human Immunodeficiency Virus - Section IV: HIV Entry Inhibitors

    1. Chapter 9

      Discovery and Development of Maraviroc and PF-232798: CCR5 Antagonists for the Treatment of HIV-1 Infection (pages 117–136)

      Patrick Dorr and Paul Stupple

    2. Chapter 10

      Discovery of the CCR5 Antagonist Vicriviroc (Sch 417690/Sch-D) for the Treatment of HIV-1 Infection (pages 137–147)

      Jayaram R. Tagat, Julie M. Strizki and Lisa M. Dunkle

    3. Chapter 11

      Discovery and Development of HIV-1 Entry Inhibitors That Target gp120 (pages 149–162)

      John F. Kadow, John Bender, Alicia Regueiro-Ren, Yasutsugu Ueda, Tao Wang, Kap-Sun Yeung and Nicholas A. Meanwell

  7. Part I: Human Immunodeficiency Virus - Section V: HIV Integrase Inhibitors

    1. Chapter 12

      Discovery of MK-0536: A Potential Second-Generation HIV-1 Integrase Strand Transfer Inhibitor with a High Genetic Barrier to Mutation (pages 163–180)

      Melissa S. Egbertson, John S. Wai, Mark Cameron and R. Scott Hoerrner

    2. Chapter 13

      Discovery and Development of HIV Integrase Inhibitor Raltegravir (pages 181–195)

      Vincenzo Summa and Paola Pace

    3. Chapter 14

      Elvitegravir: A Novel Monoketo Acid HIV-1 Integrase Strand Transfer Inhibitor (pages 197–205)

      Hisashi Shinkai, Masanori Sato and Yuji Matsuzaki

  8. Part II: Hepatitis C Virus - Section VI: Protease Inhibitors

    1. Chapter 15

      Discovery and Development of Telaprevir (pages 207–224)

      Anne-Laure Grillot, Luc J. Farmer, B. Govinda Rao, William P. Taylor, Ilan S. Weisberg, Ira M. Jacobson, Robert B. Perni and Ann D. Kwong

    2. Chapter 16

      Discovery and Development of BILN 2061 and Follow-Up BI 201335 (pages 225–238)

      Montse Llinàs-Brunet and Peter W. White

    3. Chapter 17

      Intervention of Hepatitis C Replication through NS3-4A, the Protease Inhibitor Boceprevir (pages 239–255)

      Srikanth Venkatraman and F. George Njoroge

    4. Chapter 18

      Discovery and Development of the HCV NS3/4A Protease Inhibitor Danoprevir (ITMN-191/RG7227) (pages 257–271)

      Scott D. Seiwert, Karl Kossen, Lin Pan, Jyanwei Liu and Brad O. Buckman

    5. Chapter 19

      Discovery and Development of the HCV Protease Inhibitor TMC435 (pages 273–286)

      Pierre Raboisson, Gregory Fanning, Herman de Kock, Åsa Rosenquist, René Verloes and Kenneth Simmen

  9. Part II: Hepatitis C Virus - Section VII: HCV Polymerase Nucleoside Inhibitors

    1. Chapter 20

      Discovery and Clinical Evaluation of the Nucleoside Analog Balapiravir (R1626) for the Treatment of HCV Infection (pages 287–304)

      Klaus Klumpp and David B. Smith

    2. Chapter 21

      Discovery and Development of PSI-6130/RG7128 (pages 305–315)

      Phillip A. Furman, Michael J. Otto and Michael J. Sofia

  10. Part II: Hepatitis C Virus - Section VIII: Other HCV Inhibitors

    1. Chapter 22

      Discovery of Cyclophilin Inhibitor NIM811 as a Novel Therapeutic Agent for HCV (pages 317–328)

      Kai Lin

    2. Chapter 23

      HCV Viral Entry Inhibitors (pages 329–337)

      Flossie Wong-Staal, Guohong Liu and Jeffrey McKelvy

  11. Part III: Respiratory Syncytial Virus Inhibitors

    1. Chapter 24

      Discovery of the RSV Inhibitor TMC353121 (pages 339–352)

      Jean-François Bonfanti, Gabriela Ispas, Frans Van Velsen, Wieslawa Olszewska, Tom Gevers and Dirk Roymans

    2. Chapter 25

      Discovery and Development of Orally Active RSV Fusion Inhibitors (pages 353–366)

      Nicholas A. Meanwell, Christopher W. Cianci and Mark R. Krystal

    3. Chapter 26

      Discovery and Development of RSV604 (pages 367–382)

      Joanna Chapman and Stuart Cockerill

  12. Part IV: Influenza, Hepatitis B, and Cytomegalovirus Inhibitors

    1. Chapter 27

      Discovery and Development of Influenza Virus Sialidase Inhibitor Relenza (pages 383–400)

      Robin Thomson and Mark von Itzstein

    2. Chapter 28

      Discovery and Development of Entecavir (pages 401–416)

      Richard Wilber, Bruce Kreter, Marc Bifano, Stephanie Danetz, Lois Lehman-McKeeman, Daniel J. Tenney, Nicholas Meanwell, Robert Zahler and Helena Brett-Smith

    3. Chapter 29

      Benzimidazole Ribonucleosides: Novel Drug Candidates for the Prevention and Treatment of Cytomegalovirus Diseases (pages 417–433)

      Karen K. Biron, Kristjan S. Gudmundsson and John C. Drach

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      Index (pages 435–438)

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