Table 5.

Pharmacokinetic analysis of selumetinib (S) and N-desmethyl-selumetinib (NDS).

Dose (mg)	Patients (n)	Agent (S/NDS)	Tmax (h)	Cmax (ng/mL)	AUC0-4h (h*ng/mL)	AUC0-8h (h*ng/mL)	t½ (h)	CL/F (L/h)
100	1-2	S	1.7 ± 0.5 (6)	1453 ± 530 (6)	2903 ± 461 (6)	4265 ± 628 (2)	2.4 ± 0.3 (2)	20.9 ± 3.7 (2)
		NDS	2.0 ± 0.6 (6)	77 ± 32 (6)	171 ± 59 (6)	272 ± 34 (2)	2.9 ± 0.4 (2)	–
125	15-14	S	1.5 ± 0.8 (56)	2115 ± 798 (56)	4270 ± 1470 (56)	6042 ± 2210 (29)	4.3 ± 5.7 (26)	18.7 ± 8.1 (26)
		NDS	1.7 ± 0.8 (56)	101 ± 44 (56)	218 ± 83 (56)	353 ± 124 (29)	4.3 ± 3.3 (26)	–
150	2	SEL	1.5 ± 0.8 (8)	3041 ± 1155 (8)	6073 ± 1540 (8)	6683 ± 729 (4)	7.9 ± 9.1 (3)	14.8 ± 7.6 (8)
		NDS	1.6 ± 0.7 (8)	97 ± 72 (8)	198 ± 119 (8)	264 ± 125 (4)	6.1 ± 5.0 (3)	–