NCT07374224

A Study Evaluating the Effects of Itraconazole or Rifampin on the Pharmacokinetic Characteristics of Rocbrutinib Tablet

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

• Status: Recruiting
• Phase: Phase 1
• Study type: Interventional
• Enrollment: 28 (estimated)
• Sponsor: Guangzhou Lupeng Pharmaceutical Company LTD. · Industry
• Sex: All
• Age: 18 Years – 45 Years
• Healthy volunteers: Accepted

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.

Conditions

• Clinical Pharmacology

Interventions

Type	Name	Description
DRUG	Rocbrutinib tablets	Dosage form: tablets Specification: 100 mg Dosage and administration: 100mg or 200mg, single dose, taken on the designated day according to the treatment plan. Dosage schedule: Depending on the cohort, subjects will need to take Rocbrutinib 2 times (inhibitor cohort) or 3 times (inducer cohort) during the study period.
DRUG	Itraconazole capsules	Dosage form: Capsules Specifications: 0.1g Dosage and administration: Take 400 mg (4\*100 mg capsules) on Day 5, followed by 200 mg (2 100 mg capsules) once daily (QD) from Day 6 to Day 12. Duration of medication: The medication was administered for a total of 8 days during the study period.
DRUG	Rifampicin capsules	Dosage form: Capsules Specifications: 0.15g Dosage and administration: Day 4-Day 12, take 600 mg (4 150 mg capsules) once daily (QD). Duration of medication: The medication was administered for a total of 9 days during the study period.

Timeline

• Start date: 2026-03-05
• Primary completion: 2026-06-30
• Completion: 2026-08-30
• First posted: 2026-01-28
• Last updated: 2026-03-09

Locations

1 site across 1 country: China

Regulatory

• FDA-regulated drug study