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Quantitative Structure-Activity Relationship, Activity Prediction, and Molecular Dynamics of Non-nucleotide Reverse Transcriptase Inhibitors
Published on: May 9, 2025
Etravirine
Bettina M Knoll1, Sandro Vento, Zelalem Temesgen
1Division of Infectious Diseases, Mayo Clinic, Rochester, Minnesota 55905, USA.
Abstract:
Etravirine, formerly known as TMC 125, is a novel non-nucleoside reverse transcriptase inhibitor (NNRTI) with potent activity against HIV resistant to currently licensed NNRTIs. It is in its final stage of clinical development and has received fast-track status for review by the U.S. Food and Drug Administration (FDA). In randomized placebo-controlled trials in treatment-experienced patients with confirmed NNRTI resistance, it has shown virological efficacy superior to the control arms with comparable rates of adverse events with the exception of rash. Because of its effect on the cytochrome P450 system, there are significant drug interaction issues that will need to be taken into consideration with its use.
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