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Quantitative Structure-Activity Relationship, Activity Prediction, and Molecular Dynamics of Non-nucleotide Reverse Transcriptase Inhibitors

Quantitative Structure-Activity Relationship, Activity Prediction, and Molecular Dynamics of Non-nucleotide Reverse Transcriptase Inhibitors

Published on: May 9, 2025

Abacavir-based therapy does not affect biological mechanisms associated with cardiovascular dysfunction.

Esteban Martínez¹, María Larrousse, Daniel Podzamczer

¹Infectious Diseases Unit, Hospital Clínic-Institut d'Investigacions Biomèdiques August Pi i Sunyer, University of Barcelona, C/Villarroel 170, 08036 Barcelona, Spain. esteban@fundsoriano.es

AIDS (London, England)

|December 17, 2009

Summary

Switching to abacavir/lamivudine therapy increased total and LDL cholesterol compared to tenofovir/emtricitabine. However, this HIV treatment did not significantly impact cardiovascular biomarkers, inflammation, or insulin resistance.

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Published on: October 26, 2018

Area of Science:

HIV/AIDS research
Cardiovascular health in HIV
Pharmacological studies

Background:

Antiretroviral therapy is crucial for managing HIV infection.
Nucleoside reverse transcriptase inhibitors (NRTIs) form a cornerstone of HIV treatment regimens.
Understanding the long-term effects of different NRTI backbones on cardiovascular health is essential.

Purpose of the Study:

To evaluate the impact of switching to abacavir/lamivudine versus tenofovir/emtricitabine on plasma lipids.
To assess changes in key cardiovascular biomarkers following the switch in nucleoside backbones.
To determine if abacavir-containing therapy influences inflammation, endothelial function, or coagulation in HIV-infected individuals.

Main Methods:

A sub-study of the BICOMBO trial randomized participants to abacavir/lamivudine or tenofovir/emtricitabine.
Fasting lipids and cardiovascular biomarkers were measured at baseline and 48 weeks.
Biomarkers included hsCRP, MCP-1, IL-6, TNF-alpha, ICAM-1, VCAM-1, selectins, adiponectin, insulin, and D-dimer.

Main Results:

Abacavir/lamivudine significantly increased total cholesterol (6.5%) and LDL cholesterol (8.6%) compared to tenofovir/emtricitabine.
No significant differences were observed in inflammatory markers (hsCRP, IL-6, TNF-alpha), endothelial dysfunction markers (ICAM-1, VCAM-1, selectins), or coagulation markers (D-dimer).
Changes in adiponectin and insulin levels did not significantly differ between the two treatment groups.

Conclusions:

Initiating abacavir/lamivudine therapy leads to higher total and LDL cholesterol levels compared to tenofovir/emtricitabine.
Abacavir/lamivudine did not induce significant inflammation, endothelial dysfunction, insulin resistance, or hypercoagulability.
These findings suggest a specific lipid profile alteration with abacavir/lamivudine without broader adverse cardiovascular effects in virologically suppressed HIV patients.