Pharmacokinetics of asciminib in the presence of CYP3A or P‐gp inhibitors, CYP3A inducers, and acid‐reducing agents

• Published in: Clinical and translational science Vol. 15; no. 7; pp. 1698 - 1712
• Main Authors: Hoch, Matthias, Huth, Felix, Sato, Masahiko, Sengupta, Tirtha, Quinlan, Michelle, Dodd, Stephanie, Kapoor, Shruti, Hourcade‐Potelleret, Florence
• Format: Journal Article
• Language: English
• Published: United States John Wiley & Sons, Inc 01.07.2022; John Wiley and Sons Inc; Wiley
• Subjects: Antacids; Antibiotics; Antifungal agents; Binding sites; Bioavailability; Bosutinib; Clarithromycin; Cyclodextrin; Cyclodextrins; Cytochrome P-450; Drug dosages; Drug interactions; Enrollments; Itraconazole; Mutation; Pharmacokinetics; Plasma; Quinidine; Reducing agents; Rifampin

Asciminib is a first‐in‐class inhibitor of BCR::ABL1, specifically targeting the ABL myristoyl pocket. Asciminib is a substrate of CYP3A4 and P‐glycoprotein (P‐gp) and possesses pH‐dependent solubility in aqueous solution. This report summarizes the results of two phase I studies in healthy subjects...