NCT03245307

A Study To Test The Effect Of Apatinib On P450 Enzymes

A Single-center, Open-Label, Drug Interaction Study to Determine the Effects of Apatinib on the Metabolism of CYP3A4/5 and CYP2C9 Probe Drugs in Patients With Solid Tumors

• Status: Unknown
• Phase: Phase 1
• Study type: Interventional
• Enrollment: 20 (estimated)
• Sponsor: Jiangsu HengRui Medicine Co., Ltd. · Industry
• Sex: All
• Age: 18 Years – 70 Years
• Healthy volunteers: Not accepted

Summary

Apatinib, an oral inhibitor of vascular endothelial growth factor receptor 2（VEGFR-2）, inhibits multiple cytochrome P450 (CYP450) enzymes in vitro. This study in patients with advanced cancer evaluated the effect of Apatinib on CYP450 function by comparing the pharmacokinetics of CYP-specific probe drugs in the presence and absence of Apatinib. The probes used included Nifedipine (CYP3A specific), warfarin (CYP2C9 specific).

Detailed description

This open-label study consists of a drug interaction phase that (part A) and a drug-continuation phase (part B). Patients will receive CYP450-probe drugs, and PK assessments will be performed before apatinib-administration and aſter once-daily administration of apatinib for 5 days (the predicted time point when steady-state plasma apatinib concentrations will have been achieved).

Conditions

• Cytochrome P450 Interaction

Interventions

Type	Name	Description
DRUG	Apatinib	Apatinib at a dosage of 750mg will be administered daily from day 9 of phase A
DRUG	Nifedipine GTIS	Nifedipine at a dosage of 30mg will be administered at day 1 and day 14 of phase A
DRUG	Warfarin Potassium	Nifedipine at a dosage of 3mg will be administered at day 3 and day 16 of phase A

Timeline

• Start date: 2017-08-22
• Primary completion: 2018-04-30
• Completion: 2018-09-30
• First posted: 2017-08-10
• Last updated: 2018-02-07

Locations

1 site across 1 country: China