Effects of Apatinib on the Pharmacokinetics of Nifedipine and Warfarin in Patients with Advanced Solid Tumors

Figures & data

Figure 1 Study design.

Figure 2 Mean (standard deviation) plasma concentration-time profiles of nifedipine following a single oral administration of 30 mg nifedipine alone or in combination with 750 mg apatinib in patients with advanced solid tumors.

Table 1 Pharmacokinetic Parameters of Nifedipine and S-Warfarin Following a Single Oral Administration of 30 mg Nifedipine/3 mg Warfarin Alone or in Combination with 750 mg Apatinib in Patients with Advanced Solid Tumors

Analyte	Parameter	Unit	Summary Statistics	Alone	+ Apatinib	Ratio	90% CI of Ratio
				N=23	N=20	N=20	N=20
Nifedipine	Tmax	h	Median (range)	24.0 (4.00–36.0)	24.0 (6.00–48.0)
	Cmax	ng/mL	GMean (CV%)	23.2 (45.5)	36.6 (38.0)	1.64	1.34–2.01
	AUC0–48h	h×ng/mL	GMean (CV%)	590 (56.2)	1060 (41.1)	1.83	1.46–2.31
	AUC0–36h	h×ng/mL	GMean (CV%)	489 (53.4)	851 (38.6)	1.80	1.45–2.23
S-Warfarin	Tmax	h	Median (range)	0.500 (0.500–3.00)	1.00 (0.500–3.00)
	Cmax	ng/mL	GMean (CV%)	194 (21.2)	234 (19.2)	1.24	1.10–1.39
	AUC0-t	h×ng/mL	GMean (CV%)	4210 (25.5)	7980 (25.8)	1.92	1.68–2.18
	AUC0-∞	h×ng/mL	GMean (CV%)	5190 (26.8)	12600 (35.0)
	t1/2z	h	Mean (SD)	51.2 (11.5)	86.7 (25.2)
	Vz/F	L	Mean (SD)	43.4 (11.8)	29.7 (7.89)
	CL/F	mL/h	Mean (SD)	596 (146)	249 (72.6)

Figure 3 Mean (standard deviation) plasma concentration–time profiles of S-warfarin following a single oral administration of 3 mg warfarin alone or in combination with 750 mg apatinib in patients with advanced solid tumors.