Table 4. Pharmacokinetic parameters of TKIs used in the estimation of AUC changes.

Drugs		Axitinib	Imatinib	Lapatinib	Vandetanib
Dose (mg)		5	400	1250	300
Dosing Interval (hr)		12	24	24	24
Cmax (μM)		0.16	4.41	4.2	3.32
Absorption Rate Constant (ka, h-1)		0.523	1.64	0.7	0.3
Fraction absorbed (Fa)		0.88	1	0.73	0.935
Plasma Unbound Fraction (fu,p)		0.01	0.05	0.01	0.06
Oral CL (L/h)		45	11.2	114	13.2
t1/2 (h)		3.2	22	24	456
Calculated Concentrations	Iav (μM)	0.024	2.52	0.79	1.99
	Imax,u (μM)	0.00067	0.18	0.011	0.12
	Iin,u (μM)	0.00086	0.7	0.12	0.23
References		17,40,45	38,39,46	41,42	43,44