Antiretroviral drugs

被引:142
作者
De Clercq, Erik [1 ]
机构
[1] Katholieke Univ Leuven, Rega Inst Med Res, B-3000 Louvain, Belgium
关键词
REVERSE-TRANSCRIPTASE INHIBITORS; RESISTANT HIV-1 INFECTION; TREATMENT-NAIVE PATIENTS; RALTEGRAVIR RESISTANCE; COMBINATION THERAPY; IN-VIVO; VIRUS; MUTATIONS; DISCOVERY; INVITRO;
D O I
10.1016/j.coph.2010.04.011
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
In October 2010, it will be exactly 25 years ago that the first antiretroviral drug, AZT (zidovudine, 3'-azido-2',3'dideoxythymidine), was described. It was the first of 25 antiretroviral drugs that in the past 25 years have been formally licensed for clinical use. These antiretroviral drugs fall into seven categories [nucleoside reverse transcriptase inhibitors (NRTIs), nucleotide reverse transcriptase inhibitors (NtRTIs), non-nucleoside reverse transcriptase inhibitors (NNRTIs), protease inhibitors (Pls), fusion inhibitors (Fls), co-receptor inhibitors (CRIs) and integrase inhibitors (INIs). The INIs (i.e. raltegravir) represent the most recent advance in the search for effective and selective anti-HIV agents. Combination of several anti-HIV drugs [often referred to as highly active antiretroviral therapy (HAART)] has drastically altered AIDS from an almost uniformly fatal disease to a chronic manageable one.
引用
收藏
页码:507 / 515
页数:9
相关论文
共 44 条
[32]   3'-AZIDO-3'-DEOXYTHYMIDINE (BW A509U) - AN ANTIVIRAL AGENT THAT INHIBITS THE INFECTIVITY AND CYTOPATHIC EFFECT OF HUMAN LYMPHOTROPIC-T VIRUS TYPE-III LYMPHADENOPATHY-ASSOCIATED VIRUS INVITRO [J].
MITSUYA, H ;
WEINHOLD, KJ ;
FURMAN, PA ;
STCLAIR, MH ;
LEHRMAN, SN ;
GALLO, RC ;
BOLOGNESI, D ;
BARRY, DW ;
BRODER, S .
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1985, 82 (20) :7096-7100
[33]   AIDS: lessons learnt and myths dispelled [J].
Piot, Peter ;
Kazatchkine, Michel ;
Dybul, Mark ;
Lob-Levyt, Julian .
LANCET, 2009, 374 (9685) :260-263
[34]   Selective-Advantage Profile of Human Immunodeficiency Virus Type 1 Integrase Mutants Explains In Vivo Evolution of Raltegravir Resistance Genotypes [J].
Quercia, Romina ;
Dam, Elisabeth ;
Perez-Bercoff, Danielle ;
Clavel, Francois .
JOURNAL OF VIROLOGY, 2009, 83 (19) :10245-10249
[35]   The Challenge of Finding a Cure for HIV Infection [J].
Richman, Douglas D. ;
Margolis, David M. ;
Delaney, Martin ;
Greene, Warner C. ;
Hazuda, Daria ;
Pomerantz, Roger J. .
SCIENCE, 2009, 323 (5919) :1304-1307
[36]  
Shimura Kazuya, 2009, Antiviral Chemistry & Chemotherapy, V20, P79, DOI 10.3851/IMP1397
[37]   Evolution of raltegravir resistance during therapy [J].
Sichtig, Nadine ;
Sierra, Saleta ;
Kaiser, Rolf ;
Daeumer, Martin ;
Reuter, Stefan ;
Schuelter, Eugen ;
Altmann, Andre ;
Faetkenheuer, Gerd ;
Dittmer, Ulf ;
Pfister, Herbert ;
Esser, Stefan .
JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY, 2009, 64 (01) :25-32
[38]   Raltegravir with optimized background therapy for resistant HIV-1 infection [J].
Steigbigel, Roy T. ;
Cooper, David A. ;
Kumar, Princy N. ;
Eron, Joseph E. ;
Schechter, Mauro ;
Markowitz, Martin ;
Loutfy, Mona R. ;
Lennox, Jeffrey L. ;
Gatell, Jose M. ;
Rockstroh, Jurgen K. ;
Katlama, Christine ;
Yeni, Patrick ;
Lazzarin, Adriano ;
Clotet, Bonaventura ;
Zhao, Jing ;
Chen, Joshua ;
Ryan, Desmond M. ;
Rhodes, Rand R. ;
Killar, John A. ;
Gilde, Lucinda R. ;
Strohmaier, Kim M. ;
Meibohm, Anne R. ;
Miller, Michael D. ;
Hazuda, Daria J. ;
Nessly, Michael L. ;
DiNubile, Mark J. ;
Isaacs, Robin D. ;
Nguyen, Bach-Yen ;
Teppler, Hedy .
NEW ENGLAND JOURNAL OF MEDICINE, 2008, 359 (04) :339-354
[39]   Discovery of Raltegravir, a potent, selective orally bioavailable HIV-integrase inhibitor for the treatment of HIV-AIDS infection [J].
Summa, Vincenzo ;
Petrocchi, Alessia ;
Bonelli, Fabio ;
Crescenzi, Benedetta ;
Donghi, Monica ;
Ferrara, Marco ;
Fiore, Fabrizio ;
Gardelli, Cristina ;
Paz, Odalys Gonzalez ;
Hazuda, Daria J. ;
Jones, Philip ;
Kinzel, Olaf ;
Laufer, Ralph ;
Monteagudo, Edith ;
Muraglia, Ester ;
Nizi, Emanuela ;
Orvieto, Federica ;
Pace, Paola ;
Pescatore, Giovanna ;
Scarpelli, Rita ;
Stillmock, Kara ;
Witmer, Marc V. ;
Rowley, Michael .
JOURNAL OF MEDICINAL CHEMISTRY, 2008, 51 (18) :5843-5855
[40]   Raltegravir, etravirine and r-darunavir combination in adolescents with multidrug-resistant virus [J].
Thuret, Isabelle ;
Chaix, Marie-Laure ;
Tamalet, Catherine ;
Reliquet, Veronique ;
Firtion, Ghislaine ;
Tricoire, Joelle ;
Rabaud, Christian ;
Frange, Pierre ;
Aumaitre, Hugues ;
Blanche, Stephane .
AIDS, 2009, 23 (17) :2364-2366