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. 2019 Dec 23;59(5):531–544. doi: 10.1007/s40262-019-00855-0
Upadacitinib exhibits dose-proportional pharmacokinetics and biphasic elimination with a terminal half-life of 9–14 h following administration of the extended-release formulation.
Strong CYP3A4 inhibitors increase upadacitinib exposure by 75%. Strong inducers of CYP3A4 reduce upadacitinib exposure by approximately half. No dosage adjustment is required for concomitant medications when administered with upadacitinib based on drug-interaction studies.
Mild, moderate, and severe renal impairment as well as mild and moderate hepatic impairment had no clinically relevant effect on upadacitinib systemic exposures (< 45% increase in AUC or Cmax relative to subjects with normal renal/hepatic function).
Body weight, sex, race, ethnicity, and age did not have a clinically relevant effect on the upadacitinib AUC or Cmax.