Effects of Rifampin on the Pharmacokinetics of a Single Dose of Istradefylline in Healthy Subjects.

ABSTRACT: Istradefylline, a selective adenosine A_2A inhibitor, is under development for the treatment of Parkinson's disease. The effect of oral steady-state rifampin 600 mg/day, a potent cytochrome P450 (CYP) 3A4 inducer, on the disposition of a single oral dose of istradefylline 40 mg was determined in a crossover study in 20 healthy subjects by measuring plasma concentrations of istradefylline and its M1 and M8 metabolites and their derived pharmacokinetic parameters. Based on the geometric mean ratio of log-transformed data, rifampin reduced istradefylline exposure: C_max , 0.55 (90%CI, 0.49-0.62); AUC_last , 0.21 (90%CI, 0.19-0.22); and AUC_inf , 0.19 (90%CI, 0.18-0.20), indicating nonequivalence. These changes were primarily because of the effect of rif

SUBMITTER: Mukai M 

PROVIDER: S-EPMC5811788 | biostudies-literature | 2018 Feb

REPOSITORIES: biostudies-literature