Antiviral Drugs: From Basic Discovery Through Clinical TrialsISBN: 978-0-470-45563-0
Hardcover
480 pages
August 2011
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PREFACE xiii
PART I HUMAN IMMUNODEFICIENCY VIRUS
Section I HIV Protease Inhibitors
1 Discovery and Development of Atazanavir 3
Awny Farajallah, R. Todd Bunch, and Nicholas A. Meanwell
2 Discovery and Development of PL-100, A Novel HIV-1 Protease
Inhibitor 19
Jinzi J. Wu and Joseph Musto
3 Darunavir (Prezista, TMC114): From Bench to Clinic, Improving
Treatment Options for HIV-Infected Patients 31
Marie-Pierre de Bethune, Vanitha Sekar, Sabrina Spinosa-Guzman,
Marc Vanstockem, Sandra De Meyer, Piet Wigerinck, and Eric
Lefebvre
4 Discovery and Development of Tipranavir 47
Karen R. Romines
Section II HIV Non-nucleoside Reverse Transcriptase Inhibitors
5 TMC278 (Rilpivirine): A Next-Generation NNRTI in Phase III Clinical
Development for Treatment-Naive Patients 59
Jerome Guillemont, Katia Boven, Herta Crauwels, and Marie-Pierre
de Bethune
6 Etravirine: From TMC125 to Intelence: A Treatment Paradigm
Shift for HIV-Infected Patients 71
Koen Andries, Ann Debunne, Thomas N. Kakuda, Michael Kukla, Ruud
Leemans, Johan Vingerhoets, Brian Woodfall, and Marie-Pierre de
B´ethune
Section III HIV Nucleoside Reverse Transcriptase Inhibitors
7 Discovery and Development of Tenofovir Disoproxil Fumarate
85
Erik De Clercq
8 Discovery and Development of Apricitabine 103
Susan Cox, John Deadman, Justine Southby, and Jonathan
Coates
Section IV HIV Entry Inhibitors
9 Discovery and Development of Maraviroc and PF-232798: CCR5
Antagonists for the Treatment of HIV-1 Infection 117
Patrick Dorr and Paul Stupple
10 Discovery of the CCR5 Antagonist Vicriviroc (Sch
417690/Sch-D) for the Treatment of HIV-1 Infection 137
Jayaram R. Tagat, Julie M. Strizki, and Lisa M. Dunkle
11 Discovery and Development of HIV-1 Entry Inhibitors That
Target gp120 149
John F. Kadow, John Bender, Alicia Regueiro-Ren, Yasutsugu Ueda,
Tao Wang, Kap-Sun Yeung, and Nicholas A. Meanwell
Section V HIV Integrase Inhibitors
12 Discovery of MK-0536: A Potential Second-Generation HIV-1
Integrase Strand Transfer Inhibitor with a High Genetic Barrier to
Mutation 163
Melissa S. Egbertson, John S. Wai, Mark Cameron, and R. Scott
Hoerrner
13 Discovery and Development of HIV Integrase Inhibitor
Raltegravir 181
Vincenzo Summa and Paola Pace
14 Elvitegravir: A Novel Monoketo Acid HIV-1 Integrase Strand
Transfer Inhibitor 197
Hisashi Shinkai, Masanori Sato, and Yuji Matsuzaki
PART II HEPATITIS C VIRUS
Section VI Protease Inhibitors
15 Discovery and Development of Telaprevir 209
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
16 Discovery and Development of BILN 2061 and Follow-up BI
201335 225
Montse Llinas-Brunet and Peter W. White
17 Intervention of Hepatitis C Replication Through NS3-4A, the
Protease Inhibitor Boceprevir 239
Srikanth Venkatraman and F. George Njoroge
18 Discovery and Development of the HCV NS3/4A Protease
Inhibitor Danoprevir (ITMN-191/RG7227) 257
Scott D. Seiwert, Karl Kossen, Lin Pan, Jyanwei Liu, and Brad O.
Buckman
19 Discovery and Development of the HCV Protease Inhibitor
TMC435 273
Pierre Raboisson, Gregory Fanning, Herman de Kock, Asa
Rosenquist, Rene Verloes, and Kenneth Simmen
Section VII HCV Polymerase Nucleoside Inhibitors
20 Discovery and Clinical Evaluation of the Nucleoside Analog
Balapiravir (R1626) for the Treatment of HCV Infection 287
Klaus Klumpp and David B. Smith
21 Discovery and Development of PSI-6130/RG7128 305
Phillip A. Furman, Michael J. Otto, and Michael J. Sofia
Section VIII Other HCV Inhibitors
22 Discovery of Cyclophilin Inhibitor NIM811 as a Novel
Therapeutic Agent for HCV 317
Kai Lin
23 HCV Viral Entry Inhibitors 329
Flossie Wong-Staal, Guohong Liu, and Jeffrey McKelvy
PART III RESPIRATORY SYNCYTIAL VIRUS INHIBITORS
24 Discovery of the RSV Inhibitor TMC353121 341
Jean-Francois Bonfanti, Gabriela Ispas, Frans Van Velsen,
Wieslawa Olszewska, Tom Gevers, and Dirk Roymans
25 Discovery and Development of Orally Active RSV Fusion
Inhibitors 353
Nicholas A. Meanwell, Christopher W. Cianci, and Mark R.
Krystal
26 Discovery and Development of RSV604 367
Joanna Chapman and G. Stuart Cockerill
PART IV INFLUENZA, HEPATITIS B, AND CYTOMEGALOVIRUS INHIBITORS
27 Discovery and Development of Influenza Virus Sialidase
Inhibitor Relenza 385
Robin Thomson and Mark von Itzstein
28 Discovery and Development of Entecavir 401
Richard Wilber, Bruce Kreter, Marc Bifano, Stephanie Danetz,
Lois Lehman-McKeeman, Daniel J. Tenney, Nicholas Meanwell, Robert
Zahler, and Helena Brett-Smith
29 Benzimidazole Ribonucleosides: Novel Drug Candidates for the
Prevention and Treatment of Cytomegalovirus Diseases 417
Karen K. Biron, Kristjan S. Gudmundsson, and John C.
Drach
INDEX 435