Effects of Strong CYP2C8 or CYP3A Inhibition and CYP3A Induction on the Pharmacokinetics of Brigatinib, an Oral Anaplastic Lymphoma Kinase Inhibitor, in Healthy Volunteers

• Published in: Clinical pharmacology in drug development Vol. 9; no. 2; pp. 214 - 223
• Main Authors: Tugnait, Meera, Gupta, Neeraj, Hanley, Michael J., Sonnichsen, Daryl, Kerstein, David, Dorer, David J., Venkatakrishnan, Karthik, Narasimhan, Narayana
• Format: Journal Article
• Language: English
• Published: United States Wiley Subscription Services, Inc 01.02.2020; John Wiley and Sons Inc
• Subjects: Antifungal agents; brigatinib; CYP2C8; CYP3A; Cytochrome; Drug therapy; drug‐drug interactions; induction; inhibition; Inhibitor drugs; Lymphoma; non–small cell lung cancer; Original Manuscript; Pharmacokinetics; non-small cell lung cancer; CYP3A; brigatinib; CYP2C8; drug-drug interactions; induction; inhibition

In vitro data support involvement of cytochrome P450 (CYP)2C8 and CYP3A4 in the metabolism of the anaplastic lymphoma kinase inhibitor brigatinib. A 3‐arm, open‐label, randomized, single‐dose, fixed‐sequence crossover study was conducted to characterize the effects of the strong inhibitors gemfibroz...