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Quantitative Structure-Activity Relationship, Activity Prediction, and Molecular Dynamics of Non-nucleotide Reverse Transcriptase Inhibitors
Published on: May 9, 2025
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Approved HIV reverse transcriptase inhibitors in the past decade.
Guangdi Li1, Yali Wang1, Erik De Clercq2
1Hunan Provincial Key Laboratory of Clinical Epidemiology, Xiangya School of Public Health, Central South University, Changsha 410078, China.
Acta Pharmaceutica Sinica. B
|July 18, 2022
Summary
This review covers recent HIV reverse transcriptase inhibitors, crucial for HIV treatment and prevention. It details their discovery, effects, and clinical success, highlighting future drug development needs.
Area of Science:
- Virology
- Pharmacology
- Drug Discovery
Background:
- HIV reverse transcriptase (RT) inhibitors are vital for highly active antiretroviral therapies (HAARTs) and pre-exposure prophylaxis.
- A comprehensive review of RT inhibitors approved in the last decade, covering their discovery, pharmacology, and clinical efficacy, is currently lacking.
Purpose of the Study:
- To provide a comprehensive review of HIV reverse transcriptase inhibitors approved in the past decade.
- To discuss their drug discovery, pharmacology, and clinical efficacy based on randomized controlled trials.
- To highlight novel RT inhibitors and future directions in antiretroviral drug development.
Main Methods:
- Comprehensive literature review of HIV reverse transcriptase inhibitors approved in the last ten years.
- Analysis of drug discovery pathways, pharmacological profiles, and clinical efficacy data from randomized controlled trials.
- Identification and discussion of novel investigational RT inhibitors.
Main Results:
- Detailed review of approved RT inhibitors including tenofovir alafenamide, rilpivirine, doravirine, dapivirine, azvudine, and elsulfavirine.
- Summary of their drug discovery, pharmacology, and clinical efficacy in randomized controlled trials.
- Highlighting of novel RT inhibitors such as islatravir, MK-8504, MK-8507, MK8583, IQP-0528, and MIV-150.
Conclusions:
- Recent advancements in HIV reverse transcriptase inhibitors have significantly impacted HIV treatment and prevention.
- Future research should focus on developing next-generation inhibitors with improved pharmacokinetic properties and activity against drug-resistant strains.
- Continued innovation in antiretroviral therapy is essential for combating the evolving HIV epidemic.
Keywords:
3TC, (−)-2′,3′-dideoxy-3′-thiacytidine (common name, lamivudine)ABC, abacavirATV, atazanavirAZT, 3′-azido-3′-deoxy-thymidine (common name, zidovudine)BIC, bictegravirCAB, cabotegravirCC50, the 50% cytotoxic concentrationCOBI, cobicistatClinical efficacyDOR, doravirineDPV, dapivirineDRV, darunavirDTG, dolutegravirEACS, European AIDS Clinical SocietyEC50, half maximal effective concentrationEFV, efavirenzESV, elsulfavirineEVG, elvitegravirF, bioavailabilityFDA, US Food and Drug AdministrationFTC, (−)-2′,3′-dideoxy-5-fluoro-3′-thiacytidine (common name, emtricitabine)HAARTHAART, highly active antiretroviral therapyHIV treatmentHIV, human immunodeficiency virusIAS-USA, International Antiviral Society-USAIC50, half maximal inhibitory concentrationMSM, men who have sex with menNNRTINNRTI, non-nucleoside reverse transcriptase inhibitorNRTINRTI, nucleoside/nucleotide reverse transcriptase inhibitorRPV, rilpivirineTAF, tenofovir alafenamideTDF, tenofovir disoproxil fumaratet1/2, elimination half-lifeMore Related Videos
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