Antiviral Drugs - From Basic Discov. Through Clin. Trials - W. Kazmierski (Wiley, 2011) WW PDF
Preview Antiviral Drugs - From Basic Discov. Through Clin. Trials - W. Kazmierski (Wiley, 2011) WW
P1: TIX/XYZ P2: ABC JWBS061-FM JWBS061-Kazmierski May 24, 2011 17:18 Printer Name: Yet to Come ANTIVIRAL DRUGS i P1: TIX/XYZ P2: ABC JWBS061-FM JWBS061-Kazmierski May 24, 2011 17:18 Printer Name: Yet to Come ANTIVIRAL DRUGS From Basic Discovery Through Clinical Trials Edited by WIESLAW M. KAZMIERSKI, Ph.D. A JOHN WILEY & SONS, INC., PUBLICATION iii P1: TIX/XYZ P2: ABC JWBS061-FM JWBS061-Kazmierski May 24, 2011 17:18 Printer Name: Yet to Come Copyright C⃝ 2011 by John Wiley & Sons, Inc. All rights reserved. Published by John Wiley & Sons, Inc., Hoboken, New Jersey. Published simultaneously in Canada. No part of this publication may be reproduced, stored in a retrieval system, or transmitted in any form or by any means, electronic, mechanical, photocopying, recording, scanning, or otherwise, except as permitted under Section 107 or 108 of the 1976 United States Copyright Act, without either the prior written permission of the Publisher, or authorization through payment of the appropriate per-copy fee to the Copyright Clearance Center, Inc., 222 Rosewood Drive, Danvers, MA 01923, (978) 750-8400, fax (978) 750-4470, or on the web at www.copyright.com. Requests to the Publisher for permission should be addressed to the Permissions Department, John Wiley & Sons, Inc., 111 River Street, Hoboken, NJ 07030, (201) 748-6011, fax (201) 748-6008, or online at ttp://www.wiley.com/go/permission. Limit of Liability/Disclaimer of Warranty: While the publisher and author have used their best efforts in preparing this book, they make no representations or warranties with respect to the accuracy or completeness of the contents of this book and specifically disclaim any implied warranties of merchantability or fitness for a particular purpose. No warranty may be created or extended by sales representatives or written sales materials. The advice and strategies contained herein may not be suitable for your situation. You should consult with a professional where appropriate. Neither the publisher nor author shall be liable for any loss of profit or any other commercial damages, including but not limited to special, incidental, consequential, or other damages. For general information on our other products and services or for technical support, please contact our Customer Care Department within the United States at (800) 762-2974, outside the United States at (317) 572-3993 or fax (317) 572-4002. Wiley also publishes its books in a variety of electronic formats. Some content that appears in print may not be available in electronic formats. For more information about Wiley products, visit our web site at www.wiley.com. Library of Congress Cataloging-in-Publication Data: Antiviral drugs: from basic discovery through clinical trials / edited by Wieslaw M. Kazmierski. p. ; cm. Includes bibliographical references and index. ISBN 978-0-470-45563-0 (cloth) 1. Antiviral agents. I. Kazmierski, Wieslaw M. [DNLM: 1. Antiviral Agents–therapeutic use. 2. Clinical Trials as Topic. 3. Drug Discovery. 4. Drug Evaluation. QV 268.5 A63347 2011] RM411.A5753 2011 615′.7924–dc22 2010025372 Printed in Singapore oBook ISBN: 9780470929353 ePDF ISBN: 9780470929346 ePub ISBN: 9780470934685 10 9 8 7 6 5 4 3 2 1 iv wwwwwww P1: TIX/XYZ P2: ABC JWBS061-FM JWBS061-Kazmierski May 24, 2011 17:18 Printer Name: Yet to Come CONTENTS CONTRIBUTORS ix 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 B´ethune, 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 J´erˆome Guillemont, Katia Boven, Herta Crauwels, and Marie-Pierre de B´ethune 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 v P1: TIX/XYZ P2: ABC JWBS061-FM JWBS061-Kazmierski May 24, 2011 17:18 Printer Name: Yet to Come vi CONTENTS 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 Llin`as-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 P1: TIX/XYZ P2: ABC JWBS061-FM JWBS061-Kazmierski May 24, 2011 17:18 Printer Name: Yet to Come CONTENTS vii 19 Discovery and Development of the HCV Protease Inhibitor TMC435 273 Pierre Raboisson, Gregory Fanning, Herman de Kock, ˚Asa Rosenquist, Ren´e 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-Franc¸ois 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 wwwwwww P1: TIX/XYZ P2: ABC JWBS061-FM JWBS061-Kazmierski May 24, 2011 17:18 Printer Name: Yet to Come CONTRIBUTORS Koen Andries, Johnson & Johnson Pharmaceutical Re- search and Development, Beerse, Belgium John Bender, Bristol-Myers Squibb Company Research and Development, Wallingford, Connecticut Marc Bifano, Bristol-Myers Squibb Company Research and Development, Wallingford, Connecticut Karen K. Biron, Pathfinder Pharmaceuticals, Inc., Durham, North Carolina Jean-Franc¸ois Bonfanti, Janssen R&D, Janssen-Cilag, Johnson & Johnson, Val de Reuil, France Katia Boven, Tibotec, Inc., Titusville, New Jersey Helena Brett-Smith, Bristol-Myers Squibb Company Re- search and Development, Wallingford, Connecticut Brad O. Buckman, InterMune, Inc., Brisbane, California R. Todd Bunch, Bristol-Myers Squibb Company, Evansville, Indiana Mark Cameron, Merck Research Laboratories, West Point, Pennsylvania Joanna Chapman, Arrow Therapeutics, Ltd., London, UK Christopher W. Cianci, Bristol-Myers Squibb Company Research and Development, Wallingford, Connecticut Jonathan Coates, Avexa Ltd., Richmond, Victoria, Aus- tralia G. Stuart Cockerill, Arrow Therapeutics, Ltd., London, UK Susan Cox, Avexa Ltd., Richmond, Victoria, Australia Herta Crauwels, Tibotec BVBA, Beerse, Belgium Stephanie Danetz, Bristol-Myers Squibb Company Re- search and Development, Wallingford, Connecticut John Deadman, Avexa Ltd., Richmond, Victoria, Australia Marie-Pierre de B´ethune, Tibotec BVBA, Beerse, Bel- gium Ann Debunne, Johnson & Johnson Pharmaceutical Re- search and Development, Beerse, Belgium Erik De Clercq, Rega Institute for Medical Research, Leuven, Belgium Herman de Kock, Tibotec BVBA, Beerse, Belgium Sandra De Meyer, Tibotec BVBA, Beerse, Belgium Patrick Dorr, Abbott Laboratories, Berkshire, UK John C. Drach, School of Dentistry, University of Michi- gan, Ann Arbor, Michigan Lisa M. Dunkle, Merck Research Laboratories, Kenilworth, New Jersey Melissa S. Egbertson, Merck Research Laboratories, West Point, Pennsylvania Gregory Fanning, Tibotec BVBA, Beerse, Belgium Awny Farajallah, Bristol-Myers Squibb Company, Plains- boro, New Jersey Luc J. Farmer, Vertex Pharmaceuticals, Inc., Cambridge, Massachusetts Phillip A. Furman, Pharmasset, Inc., Princeton, New Jersey Tom Gevers, Tibotec BVBA, Beerse, Belgium ix
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