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Quantitative Structure-Activity Relationship, Activity Prediction, and Molecular Dynamics of Non-nucleotide Reverse Transcriptase Inhibitors
Published on: May 9, 2025
Apricitabine: a nucleoside reverse transcriptase inhibitor for HIV infection
Monica M Gaffney1, Paul P Belliveau, Linda M Spooner
1Department of Pharmacy Practice, School of Pharmacy Worcester/Manchester, Massachusetts College of Pharmacy and Health Sciences, Worcester, MA 01608, USA. Monica.gaffney@mcphs.edu
The Annals of Pharmacotherapy
|September 10, 2009
Summary
Apricitabine, a novel nucleoside reverse transcriptase inhibitor, shows promise for HIV-1 treatment. It effectively reduces viral load and is well-tolerated, even against resistant strains.
Area of Science:
- Pharmacology and virology
- Drug development for infectious diseases
Background:
- Human Immunodeficiency Virus type 1 (HIV-1) infection remains a significant global health challenge.
- Development of novel antiretroviral therapies is crucial, particularly for managing drug-resistant strains.
- Nucleoside reverse transcriptase inhibitors (NRTIs) are a cornerstone of HIV-1 treatment.
Purpose of the Study:
- To review the pharmacology, pharmacokinetics, efficacy, and safety of apricitabine.
- To assess the potential role of apricitabine in HIV-1 treatment regimens.
Main Methods:
- Comprehensive literature search of PubMed (1966-June 2009) using terms: apricitabine, SPD754, AVX754.
- Inclusion of all English-language in vitro and in vivo studies, with preference for human data.
- Information also sourced from the drug manufacturer.
Main Results:
- Apricitabine is an orally administered prodrug, intracellularly phosphorylated to its active form, inhibiting reverse transcription.
- Demonstrated antiretroviral activity against drug-resistant HIV-1 strains in vitro and in vivo.
- Achieved significant plasma viral load reduction in clinical studies; well-tolerated with low mitochondrial toxicity potential.
- Common adverse events include headache and rhinitis; no resistance development observed in clinical studies to date.
Conclusions:
- Apricitabine exhibits activity against lamivudine- or emtricitabine-resistant HIV-1 strains.
- Its favorable tolerability profile suggests potential as a second-line treatment option.
- Further Phase 2 and 3 studies are ongoing to establish its role in HIV-1 management.
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