The activity profile of the hexacyclic camptothecin derivative DX-8951f in experimental human colon cancer and ovarian cancer

DX-8951f or exatecan mesylate ((1 S,9 S)-1-amino-9-ethyl-5-fluoro-2,3-dihydro-9-hydroxy-4-methyl-1 H,12 H-benzo[ de]pyrano[3′,4′:6,7]indolizino[1,2- b]quinoline-10-13(9 H,15 H)-dione methanesulfonate dihydrate), is a new water-soluble derivative of camptothecin. We determined the activity of DX-8951...

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Veröffentlicht in:	Biochemical pharmacology 2002-10, Vol.64 (8), p.1267-1277
Hauptverfasser:	van Hattum, Annemarie H, Pinedo, Herbert M, Schlüper, Hennie M.M, Erkelens, Caroline A.M, Tohgo, Akiko, Boven, Epie
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Antigens, CD - biosynthesis Antineoplastic agents Antineoplastic Agents - therapeutic use Antineoplastic Combined Chemotherapy Protocols - therapeutic use ATP Binding Cassette Transporter, Subfamily B, Member 1 - biosynthesis Biological and medical sciences Camptothecin - analogs & derivatives Camptothecin - therapeutic use Cell Division - drug effects Cisplatin - therapeutic use Colon cancer Colonic Neoplasms - pathology Disease Models, Animal DX-8951f Female General aspects Human tumor xenografts Humans Medical sciences Membrane Glycoproteins Mice Mice, Nude Neoplasm Proteins - biosynthesis Neoplasm Transplantation Neoplasms, Experimental - drug therapy Ovarian cancer Ovarian Neoplasms - pathology Pharmacology. Drug treatments Sulfhydryl Reagents - pharmacology Tetraspanin 29 Topoisomerase I inhibitor Tumor Cells, Cultured Vault Ribonucleoprotein Particles - biosynthesis Xenograft Model Antitumor Assays
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Zusammenfassung:	DX-8951f or exatecan mesylate ((1 S,9 S)-1-amino-9-ethyl-5-fluoro-2,3-dihydro-9-hydroxy-4-methyl-1 H,12 H-benzo[ de]pyrano[3′,4′:6,7]indolizino[1,2- b]quinoline-10-13(9 H,15 H)-dione methanesulfonate dihydrate), is a new water-soluble derivative of camptothecin. We determined the activity of DX-8951f in experimental human colon cancer and ovarian cancer, being tumor types sensitive to camptothecins. With the use of the MTT assay, DX-8951f was more potent than SN-38 in four out of five human colon cancer cell lines and three out of four human ovarian cancer cell lines ( P
ISSN:	0006-2952 1873-2968
DOI:	10.1016/S0006-2952(02)01297-2