신규 캄토테신계 항암제 CKD-602의 약물동태 : 분포, 대사 및 배설

• 영문명: Pharmacokinetic Study of CKD-602, A New Camptothecin Derivative: Distribution, Metabolism and Excretion
• 발행기관: 대한약학회
• 저자명: 이주몽(Ju Mong Lee) 이준희(Jun Hee Lee) 김준겸(Joon Kyum Kim) 신희종(Hee Jong Shin) 이형기(Hyung Ki Lee) 이상준(Sang Joon Lee) 홍청일(Chung Il Hong)
• 간행물 정보: 『약학회지』제42권 제4호 (1998년), 437~446쪽, 전체 10쪽
• 주제분류: 의약학 > 기타의약학
• 파일형태: PDF
• 발행일자: 1998.08.31

영문 초록

The distribution, metabolism and excretion of CKD-602{20(S)-7-[2-(N-Isopropylamino)ethyl]camptothecin HCI), a new camptothecin derivative, were investigated in rats after a single administration of CKD-602. 1. The tissue levels of CKD-602 given to mice by the intravenous route at a dose of 20mg/kg were the highest in intestine, followed in descending order by kidney, liver, stomach,lung, heart, spleen and plasma. The concentrations of CKD-602 after 24hrs decreased to less than 2% of the peak level in most tissues except the skin. The urinary and fecal excretion of CKD-602 were 47.6% and 44.4% of the administered dose, respectively, with 0.7% remaining in the rinse. 2. After administration of CKD-602 at 10mg/kg in rats, metabolism of this compound was examined in plasma, urine, and feces. The plasma samples were collected for 24hr, urinary and fecal samples for 72hr. While any peak of CKD-602 in HPLC chromatograms was not detected from plasma and urine it was detected in feces (peaks, 9.8 min). However, additional peak area was about 0.5% of the peak area of parent CKD-602. Therefore, CKD-602 may be eliminated with the parent form and rarely metabolized in the body. 4. After I.v. administration of CKD-602 at 10mg/kg in rats, urinary and fecal excretions were examined for 72hrs post dose period. 87% of total urinary excretion of CKD-602 was excreted within 8hr after administration, 53%, and 32% of total fecal excreted amounts were determined in 0-24 hr and 24-48hr periods, respectively. The total excretion amounts of CKD-602 into urine and feces were 94% of the administered dose.

키워드

CKD-602 Camptothecin derivatives pharmacokinetics distribution metabolism excretion.