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Updated: Jul 9, 2026

Quantitative Structure-Activity Relationship, Activity Prediction, and Molecular Dynamics of Non-nucleotide Reverse Transcriptase Inhibitors
Published on: May 9, 2025
Comparison of the induction of P-glycoprotein activity by nucleotide, nucleoside, and non-nucleoside reverse
Johanna Weiss1, Nicola Weis, Nahal Ketabi-Kiyanvash
1Department of Internal Medicine VI, Clinical Pharmacology and Pharmacoepidemiology, University of Heidelberg, Im Neuenheimer Feld 410, D-69120 Heidelberg, Germany. johanna.weiss@med.uni-heidelberg.de
Abstract:
Combination therapy against human immunodeficiency virus (HIV)-infection is complicated by drug-drug interactions between antiretrovirals and also between anti-HIV drugs and drugs used to treat co-morbidity. P-glycoprotein represents one important site for drug interactions and induction of its function could reduce the effectiveness of drugs that are P-glycoprotein substrates. We therefore investigated induction of P-glycoprotein function in LS180 cells by non-nucleoside and nucleoside reverse transcriptase inhibitors (NNRTIs and NRTIs) and tenofovir as essential components of antiretroviral combination therapy. P-glycoprotein activity was increased by all NNRTIs and some NRTIs with delavirdine (5.3-fold at 100 muM) having the largest effect.
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