Reversible, Time-Dependent Inhibition of CYP3A-Mediated Metabolism of Midazolam and Tacrolimus by Telaprevir in Human Liver Microsomes

• Main Authors: Brian Chapron (Author), Linda Risler (Author), Brian Phillips (Author), Carol Collins (Author), Kenneth Thummel (Author), Danny Shen (Author)
• Format: Book
• Published: Frontiers Media S.A., 2015-03-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.

Purpose  Telaprevir inhibits CYP3A resulting in drug-drug interactions (DDI) of unprecedented magnitude. We investigated the mechanisms by which telaprevir inhibits the oxidation of midazolam and tacrolimus in human liver microsomes (HLM). Methods  We performed a static mechanistic DDI prediction to...