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).
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).
Study Type
INTERVENTIONAL
Allocation
NA
Purpose
TREATMENT
Masking
NONE
Enrollment
20
Apatinib at a dosage of 750mg will be administered daily from day 9 of phase A
Nifedipine at a dosage of 30mg will be administered at day 1 and day 14 of phase A
Nifedipine at a dosage of 3mg will be administered at day 3 and day 16 of phase A
Chinese Medical University First Hospital
Shenyang, Liaoning, China
RECRUITINGArea under the plasma concentration versus time curve (AUC) of warfarin or nifedipine
AUC0\~t of warfarin and nifedipine in the absence or in presence of apatinib will be defined
Time frame: 1 year
Number of participants with treatment-related adverse events as assessed by CTCAE v4.0
to assess safety and tolerability of apatinib combined with warfarin or nifedipine in patients with advanced solid tumors. The vital signs, ECG, laboratory values and adverse events (AE and SAE) were judged according to NCI-CTCAE V4.0 criteria
Time frame: Day 1 to 21 ( Phase A）
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