Antiviral Drugs: From Basic Discovery Through Clinical Trials

Cover......Page 1
Frontmatter......Page 2
Copyright......Page 4
Contents......Page 6
Contributors......Page 10
Preface......Page 14
Color plates......Page 15
PART I - HUMAN IMMUNODEFICIENCY VIRUS......Page 31
1: DISCOVERY AND DEVELOPMENT OF ATAZANAVIR......Page 33
2: DISCOVERY AND DEVELOPMENT OF PL-100, A NOVEL HIV-1 PROTEASE INHIBITOR......Page 49
3: DARUNAVIR (PREZISTA, TMC114): FROM BENCH TO CLINIC, IMPROVING TREATMENT OPTIONS FOR HIV-INFECTED PATIENTS......Page 61
4: DISCOVERY AND DEVELOPMENT OF TIPRANAVIR......Page 77
5: TMC278 (RILPIVIRINE): A NEXT-GENERATION NNRTI IN PHASE III CLINICAL DEVELOPMENT FOR TREATMENT-NAIVE PATIENTS......Page 89
6: ETRAVIRINE: FROM TMC125 TO INTELENCE: A TREATMENT PARADIGM SHIFT FOR HIV-INFECTED PATIENTS......Page 101
7: DISCOVERY AND DEVELOPMENT OF TENOFOVIR DISOPROXIL FUMARATE......Page 115
8: DISCOVERY AND DEVELOPMENT OF APRICITABINE......Page 133
9: DISCOVERY AND DEVELOPMENT OF MARAVIROC AND PF-232798: CCR5 ANTAGONISTS FOR THE TREATMENT OF HIV-1 INFECTION......Page 147
10: DISCOVERY OF THE CCR5 ANTAGONIST VICRIVIROC (SCH 417690/SCH-D) FOR THE TREATMENT OF HIV-1 INFECTION......Page 167
11: DISCOVERY AND DEVELOPMENT OF HIV-1 ENTRY INHIBITORS THAT TARGET gp120......Page 179
12: DISCOVERY OF MK-0536: A POTENTIAL SECOND-GENERATION HIV-1 INTEGRASE STRAND TRANSFER INHIBITOR WITH A HIGH GENETIC BARRIER TO MUTATION......Page 193
13: DISCOVERY AND DEVELOPMENT OF HIV INTEGRASE INHIBITOR RALTEGRAVIR......Page 211
14: ELVITEGRAVIR: A NOVEL MONOKETO ACID HIV-1 INTEGRASE STRAND TRANSFER INHIBITOR......Page 227
PART II - HEPATITIS C VIRUS......Page 237
15: DISCOVERY AND DEVELOPMENT OF TELAPREVIR......Page 239
16: DISCOVERY AND DEVELOPMENT OF BILN 2061 AND FOLLOW-UP BI 201335......Page 255
17: INTERVENTION OF HEPATITIS C REPLICATION THROUGH NS3-4A, THE PROTEASE INHIBITOR BOCEPREVIR......Page 269
18: DISCOVERY AND DEVELOPMENT OF THE HCV NS3/4A PROTEASE INHIBITOR DANOPREVIR (ITMN-191/RG7227)......Page 287
19: DISCOVERY AND DEVELOPMENT OF THE HCV PROTEASE INHIBITOR TMC435......Page 303
20: DISCOVERY AND CLINICAL EVALUATION OF THE NUCLEOSIDE ANALOG BALAPIRAVIR (R1626) FOR THE TREATMENT OF HCV INFECTION......Page 317
21: DISCOVERY AND DEVELOPMENT OF PSI-6130/RG7128......Page 335
22: DISCOVERY OF CYCLOPHILIN INHIBITOR NIM811 AS A NOVEL THERAPEUTIC AGENT FOR HCV......Page 347
23: HCV VIRAL ENTRY INHIBITORS......Page 359
PART III - RESPIRATORY SYNCYTIAL VIRUS INHIBITORS......Page 369
24: DISCOVERY OF THE RSV INHIBITOR TMC353121......Page 371
25: DISCOVERY AND DEVELOPMENT OF ORALLY ACTIVE RSV FUSION INHIBITORS......Page 383
26: DISCOVERY AND DEVELOPMENT OF RSV604......Page 397
PART IV - INFLUENZA, HEPATITIS B, AND CYTOMEGALOVIRUSINHIBITORS......Page 413
27: DISCOVERY AND DEVELOPMENT OF INFLUENZA VIRUS SIALIDASE INHIBITOR RELENZA......Page 415
28: DISCOVERY AND DEVELOPMENT OF ENTECAVIR......Page 431
29: BENZIMIDAZOLE RIBONUCLEOSIDES: NOVEL DRUG CANDIDATES FOR THE PREVENTION AND TREATMENT OF CYTOMEGALOVIRUS DISEASES......Page 447
Index......Page 465