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Titolo:
PHARMACOKINETICS OF CPT-11 IN RHESUS-MONKEYS
Autore:
INABA M; OHNISHI Y; ISHII H; TANIOKA Y; YOSHIDA Y; SUDOH K; HAKUSUI H; MIZUNO N; ITO K; SUGIYAMA Y;
Indirizzi:
JAPANESE FDN CANC RES,CTR CANC CHEMOTHERAPY,TOSHIMA KU,1-37-1 KAMI IKEBUKURO TOKYO 170 JAPAN CENT INST EXPT ANIM,MIYAMAE KU KAWASAKI KANAGAWA 216 JAPAN DAIICHI PHARMACEUT CO LTD,DRUG METAB & ANALYT CHEM RES LAB,EDOGAWA KUTOKYO 134 JAPAN UNIV TOKYO,FAC PHARMACEUT SCI,BUNKYO KU TOKYO 113 JAPAN
Titolo Testata:
Cancer chemotherapy and pharmacology
fascicolo: 2, volume: 41, anno: 1998,
pagine: 103 - 108
SICI:
0344-5704(1998)41:2<103:POCIR>2.0.ZU;2-V
Fonte:
ISI
Lingua:
ENG
Soggetto:
ACTIVE METABOLITE SN-38; CYCLE PHASE SPECIFICITY; IRINOTECAN CPT-11; KINETIC-ANALYSIS; TOPOISOMERASE-I; CANCER; 1-PIPERIDINO)-1-PIPERIDINO>CARBONYLOXYCAMPTOTHECIN; PHARMACODYNAMICS; CARBOXYLESTERASE; CAMPTOTHECIN;
Keywords:
CPT-11; PHARMACOKINETICS; MONKEY;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
21
Recensione:
Indirizzi per estratti:
Citazione:
M. Inaba et al., "PHARMACOKINETICS OF CPT-11 IN RHESUS-MONKEYS", Cancer chemotherapy and pharmacology, 41(2), 1998, pp. 103-108

Abstract

Purpose: To examine the pharmacokinetic relationships between humans and monkeys, we studied the disposition of 1-piperidino)-1-piperidino]carbonyloxycamptothecin (CPT-11) and its active metabolite, 7-ethyl-10-hydroxycamptothecin (SN-38), in rhesus monkeys. Methods: CPT-11 was administered to a total of six monkeys at doses of 3, 7, 15 and 25 mg/kg by intravenous infusion for 10 min and plasma concentrations and pharmacokinetic parameters of CPT-11 determined. Results: Maximum plasma concentrations at 25 mg/kg reached around 10 000 ng/ml, and dropped to500 ng/ml in 8 h. Plasma concentrations of SN-38 remained between 2 and 10 ng/ml. Mean values of systemic clearance, mean residence time and distribution volume at steady state, the major pharmacokinetic parameters for CPT-11, were 13.3 (ml/min per kg), 192 (min) and 2553 (ml/kg), respectively. The initial plasma concentration ratio of lactone to total CPT-11, 76%, declined to about 20% within 75 min, and the final ratio was about 40% at 8 h; the initial ratio of SN-38 was 72%, dropped to 34% within 70 min and finally recovered to 55% at 8 h. Conclusion: Comparison with human data revealed that systemic clearances of CPT-11 and the maximum AUC of SN-38 were not as different between humans and monkeys as between humans and mice, but the metabolic conversion ofCPT-11 into SN-38 in monkeys was significantly lower than in humans.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 03/04/20 alle ore 11:01:53