신규 캄토테신계 항암제 CKD-602의 약물동태 : 흡수

Pharmacokinetic Study of CKD-602, A New Camptothecin Derivative: Absorption

The pharmacokinetics of CKD-602, a new camptothecin anticancer derivative, were studied in mice, rats and dogs following a single or multiple intravenous administration, and the following results were obtained. The blood levels of CKD-602 declined in biphasic fashions with peak plasma levels (C0) of 2.63mcg/ml in mice, 2.27mcg/ml in tumor bearing mice, 2.84mcg/ml in rats at a dose of 20mg/kg, and of 0.02mcg/ml in dogs at a dose of 0.5mg/kg. The plasma half-lives (t1/2beta) were 9.55hr in mice, 9.94hr in tumor bearing mice, 9.98hr in rats and 12.75hr in dogs. AUC of CKD-602 was increased linearly with the dose at a range from 5 to 20mg/kg. Moreover, Cltot and Vdss were also not significantly changed with increasing the dose. On the other hand, after 5 daily intravenous bolus injection of CKD-602 (5mg/kg) in rats, t1/2beta, AUC and MRT of CKD-602 were 11.90hr, 3.19mcg hr/ml, and 11.61hr, respectively, which were slightly higher than after the single bolus injection.