Assessment of the Effects of Inhibition or Induction of CYP2C19 and CYP2C9 Enzymes, or Inhibition of OAT3, on the Pharmacokinetics of Abrocitinib and Its Metabolites in Healthy Individuals

• Published in: European journal of drug metabolism and pharmacokinetics Vol. 47; no. 3; pp. 419 - 429
• Main Authors: Wang, Xiaoxing, Dowty, Martin E., Wouters, Ann, Tatulych, Svitlana, Connell, Carol A., Le, Vu H., Tripathy, Sakambari, O’Gorman, Melissa T., Winton, Jennifer A., Yin, Natalie, Valdez, Hernan, Malhotra, Bimal K.
• Format: Journal Article
• Language: English
• Published: Cham Springer International Publishing 01.05.2022
• Subjects: Adult; Area Under Curve; Biomedical and Life Sciences; Biomedicine; Clinical Trials, Phase I as Topic; Cytochrome P-450 CYP2C19 - metabolism; Cytochrome P-450 CYP2C9 - metabolism; Cytochrome P-450 Enzyme System - metabolism; Drug Interactions; Fluconazole - pharmacology; Fluvoxamine; Human Physiology; Humans; Medical Biochemistry; NCT; NCT03634345; NCT03637790; NCT03937258; Original; Original Research Article; Pharmaceutical Sciences/Technology; Pharmacology/Toxicology; Pharmacy; Probenecid; Pyrimidines; Rifampin; Sulfonamides

Background and Objective Abrocitinib is a Janus kinase 1-selective inhibitor for the treatment of moderate-to-severe atopic dermatitis. Abrocitinib is eliminated primarily by metabolism involving cytochrome P450 (CYP) enzymes. Abrocitinib pharmacologic activity is attributable to the unbound concent...