A Study Evaluating the Effects of Itraconazole or Rifampin on the Pharmacokinetic Characteristics of Rocbrutinib Tablet
brief summary
This is a phase I, open-label, two-part, fixed-sequence drug interaction study conducted to evaluate the effects of concomitant use of the potent CYP3A4 inhibitor itraconazole or the CYP3A4 inducer rifampin on the pharmacokinetics of Rocbrutinib in healthy subjects.
detailed description
This study evaluated the changes in the pharmacokinetic profiles of Rocbrutinib under maximal CYP3A inhibition and induction conditions by investigating the co-administration of Rocbrutinib with potent CYP3A inhibitors or inducers at steady state, compared with Rocbrutinib administered alone.
To assess the potential clinical inhibition of OATP1B by Rocbrutinib, blank plasma samples were collected prior to Rocbrutinib administration and 24-hour plasma samples were collected post-administration. The concentration of coproporphyrin I (CP-I) in these samples was detected and analyzed.
Furthermore, the effect of P-gp inhibitors on the drug absorption of Rocbrutinib (when acting as a substrate) was evaluated by investigating two scenarios: co-administration of a single dose of Rocbrutinib with a single dose of the P-gp inhibitor rifampicin, and co-administration of a single dose of Rocbrutinib with the P-gp inhibitor itraconazole at steady state.
official title
A Phase I, Open-label, Two-part, Fixed-sequence Drug Interaction Study to Evaluate the Effects of Concomitant Use of the CYP3A4 Inhibitor Itraconazole or the CYP3A4 Inducer Rifampin on the Pharmacokinetics of Rocbrutinib in Healthy Subjects