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Quantitative Structure-Activity Relationship, Activity Prediction, and Molecular Dynamics of Non-nucleotide Reverse Transcriptase Inhibitors
Published on: May 9, 2025
Combinations of nucleoside/nucleotide analogues for HIV therapy
Pablo Barreiro1, Teresa García-Benayas, Ana Rendón
1Department of Infectious Diseases, Hospital Carlos III, Madrid, Spain. pbarreiro@v4066.drago.net
Abstract:
Nucleoside and nucleotide analogues are essential for the design of effective antiretroviral regimens. There are currently many options for the selection of such drug backbones, although not all combinations will display optimal results. The concomitant administration of certain drugs should be avoided due to high rates of toxicity (ddl/d4T, ddl/TDF), antagonism (AZT/d4T, 3TC/FTC) and/or a greater risk of virological failure (ddl/TDF, ABC/TDF). The understanding of the plasmatic and intracellular metabolism of nucleoside/nucleotide analogues is crucial for deciding the optimal posology of each drug and the better dual combinations to be selected. Interferences between the pathways involved into the intracellular activation of some nucleoside/nucleotide analogues may help to understand why certain drug combinations should be avoided.
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