The history of antiretrovirals: key discoveries over the past 25 years.
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.
De Clercq
Erik
E
Department of Microbiology and Immunology, Rega Institute for Medical Research, Katholieke Universiteit Leuven, Leuven, Belgium. erik.declercq@rega.kuleuven.be
D019380:Anti-HIV Agents / Q000737:chemistry / Q000266:history* / Q000627:therapeutic use; D004338:Drug Combinations; D055808:Drug Discovery / Q000266:history* / Q000639:trends; D015658:HIV Infections / Q000188:drug therapy / Q000266:history*; D049673:History, 20th Century; D049674:History, 21st Century; D006801:Humans; D014779:Virus Replication / Q000187:drug effects*
D019380:Anti-HIV Agents; D004338:Drug Combinations