A Study To Test The Effect Of Apatinib On P450 Enzymes

Conditions

• Cytochrome P450 Interaction

Eligibility Criteria

Sex

ALL

Age

18 Years - 70 Years

Healthy Volunteers

Not accepted

Interventions

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

Study Details

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).

Key Dates

Start date

Aug 22, 2017

Status verified

Jul 2017

Primary completion

Apr 30, 2018

Completion

Sep 30, 2018

Study Design

Enrollment

20 participants (estimated)

Allocation

NA

Intervention model

SINGLE_GROUP

Primary purpose

TREATMENT

Arms

• Experimental: Treament
  In phase A, subjects receiving a single 30 mg oral dose of Nifedipine controlled-release tablets and wash-out for 2 days,a single 3 mg oral dose of warfarin tablets and wash-out for 12 days, then apatinib 750 mg once daily with a single 30 mg oral dose of Nifedipine controlled-release tablets co-administered on day 6 ,a a single 3 mg oral dose of warfarin tablets co-administered on day 9.

Primary Outcome Measure

Area under the plasma concentration versus time curve (AUC) of warfarin or nifedipine [ Time Frame: 1 year ]