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- W1999816621 endingPage "58" @default.
- W1999816621 startingPage "39" @default.
- W1999816621 abstract "Twenty-five years ago, nucleoside analog 3′-azidothymidine (AZT) was shown to efficiently block the replication of HIV in cell culture. Subsequent studies demonstrated that AZT acts via the selective inhibition of HIV reverse transcriptase (RT) by its triphosphate metabolite. These discoveries have established the first class of antiretroviral agents: nucleoside and nucleotide reverse transcriptase inhibitors (NRTIs). Over the years that followed, NRTIs evolved into the main component of antiretroviral drug combinations that are now used for the treatment of all populations of HIV infected patients. A total of thirteen NRTI drug products are now available for clinical application: eight individual NRTIs, four fixed-dose combinations of two or three NRTIs, and one complete fixed-dose regimen containing two NRTIs and one non-nucleoside RT inhibitor. Multiple NRTIs or their prodrugs are in various stages of clinical development and new potent NRTIs are still being identified through drug discovery efforts. This article will review basic principles of the in vitro and in vivo pharmacology of NRTIs, discuss their clinical use including limitations associated with long-term NRTI therapy, and describe newly identified NRTIs with promising pharmacological profiles highlighting those in the development pipeline. This article forms part of a special issue of Antiviral Research marking the 25th anniversary of antiretroviral drug discovery and development, volume 85, issue 1, 2010." @default.
- W1999816621 created "2016-06-24" @default.
- W1999816621 creator A5030919816 @default.
- W1999816621 creator A5035169875 @default.
- W1999816621 date "2010-01-01" @default.
- W1999816621 modified "2023-10-18" @default.
- W1999816621 title "Nucleoside and nucleotide HIV reverse transcriptase inhibitors: 25 years after zidovudine" @default.
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