Pharmacokinetics and enhanced bioavailability of candidate cancer preventative agent, SR13668 in dogs and monkeys

Purpose SR13668 (2,10-dicarbethoxy-6-methoxy-5,7-dihydro-indolo-(2,3-b)carbazole), is a new candidate cancer chemopreventive agent under development. It was designed using computational modeling based on a naturally occurring indole-3-carbinol and its in vivo condensation products. It showed promisi...

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Veröffentlicht in:	Cancer chemotherapy and pharmacology 2010-05, Vol.65 (6), p.1109-1116
Hauptverfasser:	Kapetanovic, Izet M, Muzzio, Miguel, Hu, Shu-Chieh, Crowell, James A, Rajewski, Roger A, Haslam, John L, Jong, Ling, McCormick, David L
Format:	Artikel
Sprache:	eng
Schlagworte:	Administration, Oral Animals Antineoplastic agents Antineoplastic Agents - blood Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacokinetics Area Under Curve Biological and medical sciences Biological Availability Cancer Research Carbazoles - blood Carbazoles - chemistry Carbazoles - pharmacokinetics Chromatography, High Pressure Liquid Dogs Drug Screening Assays, Antitumor Fasting Glycerides Injections, Intravenous Macaca fascicularis Male Medical sciences Medicine Medicine & Public Health Metabolic Clearance Rate Molecular Structure Oncology Organic Chemicals - chemistry Original Article Pharmacology. Drug treatments Pharmacology/Toxicology Polyethylene Glycols - chemistry
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Zusammenfassung:	Purpose SR13668 (2,10-dicarbethoxy-6-methoxy-5,7-dihydro-indolo-(2,3-b)carbazole), is a new candidate cancer chemopreventive agent under development. It was designed using computational modeling based on a naturally occurring indole-3-carbinol and its in vivo condensation products. It showed promising anti-cancer activity and its preclinical toxicology profile (genotoxicity battery and subchronic rat and dog studies) was unremarkable. However, it exhibited a very poor oral bioavailability (
ISSN:	0344-5704 1432-0843
DOI:	10.1007/s00280-009-1116-4