Activity of CPT-11 (irinotecan hydrochloride), a topoisomerase I inhibitor, against human tumor colony-forming units.
CPT-11 (irinotecan hydrochloride, 7-ethyl-10-[4-(piperidino)-1-piperidino] carbonyloxy-camptothecin) is a semisynthetic camptothecin derivative developed in Japan. The inhibitory activity of CPT-11 against human tumor colony-forming units from freshly explanted human tumors was explored using a soft agar cloning system. Final CPT-11 concentrations of 0.3-3.0 micrograms/ml were used for a 1 h exposure. At a concentration of 3.0 micrograms/ml antitumor activity was seen against colorectal, ovarian, nonsmall-cell lung, breast cancer and mesothelioma colony-forming units. CPT-11 should have activity against a broad spectrum of tumors in patients.
Shimada
Y
Y
Department of Medical Oncology, National Cancer Center Hospital, Tokyo, Japan.
Rothenberg
M
M
Hilsenbeck
S G
SG
Burris
H A
HA
Degen
D
D
Von Hoff
D D
DD
D000970:Antineoplastic Agents / Q000494:pharmacology*; D002166:Camptothecin / Q000031:analogs & derivatives* / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D000077146:Irinotecan; D014411:Neoplastic Stem Cells / Q000187:drug effects*; D059004:Topoisomerase I Inhibitors
D000970:Antineoplastic Agents; D059004:Topoisomerase I Inhibitors; D000077146:Irinotecan; D002166:Camptothecin