The history of antiretrovirals: key discoveries over the past 25 years.

Abstract

Within 25 years after zidovudine (3'-azido-2',3'-dideoxythymidine, AZT) was first described as an inhibitor of HIV replication, 25 anti-HIV drugs have been formally approved for clinical use in the treatment of HIV infections: seven nucleoside reverse transcriptase inhibitors (NRTIs): zidovudine, didanosine, zalcitabine, stavudine, lamivudine, abacavir and emtricitabine; one nucleotide reverse transcriptase inhibitor (NtRTI): tenofovir [in its oral prodrug form: tenofovir disoproxil fumarate (TDF)]; four non-nucleoside reverse transcriptase inhibitors (NNRTIs): nevirapine, delavirdine, efavirenz and etravirine; ten protease inhibitors (PIs): saquinavir, ritonavir, indinavir, nelfinavir, amprenavir, lopinavir, atazanavir, fosamprenavir, tipranavir and darunavir; one fusion inhibitor (FI): enfuvirtide; one co-receptor inhibitor (CRI): maraviroc and one integrase inhibitor (INI): raltegravir. These compounds are used in various drug combination (some at fixed dose) regimens so as to achieve the highest possible benefit and tolerability, and to diminish the risk of virus-drug resistance development.

• Authors: Erik De Clercq
• Journal: Reviews in medical virology (Rev Med Virol) Vol. 19 Issue 5 Pg. 287-99 (Sep 2009) ISSN: 1099-1654 [Electronic] England
• PMID: 19714702 (Publication Type: Historical Article, Journal Article)
• Copyright: (c) 2009 John Wiley & Sons, Ltd.

Chemical References

• Anti-HIV Agents
• Drug Combinations

Topics

• Anti-HIV Agents (chemistry, history, therapeutic use)
• Drug Combinations
• Drug Discovery (history, trends)
• HIV Infections (drug therapy, history)
• History, 20th Century
• History, 21st Century
• Humans
• Virus Replication (drug effects)