Overcoming Time-Dependent Inhibition (TDI) of Cytochrome P450 3A4 (CYP3A4) Resulting from Bioactivation of a Fluoropyrimidine Moiety

Overcoming Time-Dependent Inhibition (TDI) of Cytochrome P450 3A4 (CYP3A4) Resulting from Bioactivation of a Fluoropyrimidine Moiety Fluorine Substitution Can Block CYP3A4 Metabolism-Dependent Inhibition:  Identification of (S)-N-[1-(4-Fluoro-3- morpholin-4-ylphenyl)ethyl]-3- (4-fluorophenyl)acrylamide as an Orally Bioavailable KCNQ2 Opener Devoid of CYP3A4 Metabolism-Dependent Inhibition Mechanism-Based Inactivation (MBI) of Cytochrome P450 Enzymes: Structure–Activity Relationships and Discovery Strategies To Mitigate Drug–Drug Interaction Risks Design and synthesis of a new fluorescent probe for cytochrome P450 3A4 (CYP 3A4) Sequential Metabolism of AMG 487, a Novel CXCR3 Antagonist, Results in Formation of Quinone Reactive Metabolites That Covalently Modify CYP3A4 Cys239 and Cause Time-Dependent Inhibition of the Enzyme Structure–activity studies on seco-pancratistatin analogs: Potent inhibitors of human cytochrome P450 3A4 A Refined Cytochrome P450 IC50 Shift Assay for Reliably Identifying CYP3A Time-Dependent Inhibitors Mechanism-Based Inactivation of Cytochrome P450 3A4 by Mibefradil through Heme Destruction Cytochrome P450 Enzymes Mechanism Based Inhibitors: Common Sub-Structures and Reactivity Development of a cell viability assay to assess drug metabolite structure–toxicity relationships