Table 6.

Summary of pharmacokinetics parameters of irinotecan and its metabolites

	Dose level	Irinotecan dose (mg/m2)	No. of patients	Pharmacokinetic variables
				Cmax (ng/ml)		AUC (ng h/ml)		Metabolite:irinotecan AUC ratio		T1/2 (h)
				Dl	D8	Dl	D8	Dl	D8	Dl	D8
Irinotecan	1, 2, and 3	60	10	1,060 ± 294	1,203 ± 405	5,534 ± 2,187 (n = 7)	6,567 ± 4,466			5.9 ± 1.8 (n = 7)	8.5 ± 8.7
	4	90	5	1,018 ± 113	916 ± 351	5,525 ± 1,465	4,943 ± 1,512			10.2 ± 6.0	13.9 ± 7.1
	All		15							7.9 ±4.6 (n = 12)	10.4 ± 8.3
SN-38	1, 2, and 3	60	10	40 ± 24	30 ± 24	572 ± 515	345 ± 247	0.12 ±0.07 (n = 7)	0.05 ± 0.03 (n = 8)	11.4 ± 8.2	18.2 ± 17.2 (n = 8)
	4	90	5	24 ± 8	23 ± 11	446 ± 192 (n = 3)	461 ± 349	0.09 ± 0.06 (n = 3)	0.08 ± 0.05	32.6 ± 22.7 (n = 3)	42.4 ± 27.5
	All		15					0.11 ±0.07 (n = 10)	0.06 ± 0.04 (n = 13)	16.7 ± 15.3 (n = 12)	28.3 ± 24.3 (n = 13)
APC	1, 2, and 3	60	10	223 ± 144	176 ± 127	2,507 ± 1,384	1,650 ± 1,344	0.52 ± 0.26 (n = 7)	0.31 ± 0.23	7.3 ± 2.2	6.7 ± 2.3
	4	90	5	129 ± 60	115 ± 58	2,327 ± 1,494 (n = 4)	1,948 ± 1,647	0.38 ± 0.18 (n = 4)	0.35 ± 0.24	13.9 ± 7.3 (n = 4)	13.9 ± 11.4
	All		15					0.47 ± 0.23 (n = 11)	0.32 ± 0.22	9.3 ± 5.2 (n = 13)	9.3 ± 7.5
SN-38G	1, 2, and 3	60	10	372 ± 165 (n = 4)	473 ± 164 (n = 3)	4,213 ± 298 (n = 3)	3,419 ± 724 (n = 3)	0.70 ± 0.22 (n = 3)	0.50 ± 0.12 (n = 3)	6.0 ± 2.9 (n = 3)	5.0 ± 1.2 (n = 3)
	4	90	5	151 (n = 1)	186, 214 (n = 2)	(n = 0)	2,671, 4,944 (n = 2)	(n = 0)	0.56, 0.79 (n = 2)	(n = 0)	7.7, 17.8 (n = 2)
	All		15					0.70 ± 0.22 (n = 3)	0.57 ± 0.15 (n = 5)	6.0 ± 2.9 (n = 3)	8.1 ± 5.6 (n = 5)

Values ar e reported as the mean ± standard deviation. Actual value are reported when n < 2

AUC area under the concentration-time curve, C_max maximal plasma concentration, T_1/2 terminal half-life