Article
A Population Pharmacokinetic Approach to Understand the Effect of Efavirenz on CYP3A Activity in Healthy Volunteers Using Midazolam as a Probe.
CPT: pharmacometrics & systems pharmacology - 1 Dec 2025
Collins Kimberly S, Aruldhas Blessed W, Metzger Ingrid F, Lu Jessica B L, Heathman Michael A, Quinney Sara K, Desta Zeruesenay
Abstract excerpt
Efavirenz induces and inhibits multiple drug-metabolizing enzymes, contributing to significant drug-drug interactions. This study quantified the impact of multiple doses of efavirenz on CYP3A activity via midazolam metabolism using a population pharmacokinetic approach. Healthy volunteers received 1 mg midazolam orally in two sessions: first with a single 600 mg efavirenz dose and then after chronic efavirenz...
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