title: [Antitumor activity and toxicity of KB-5424 R, a newly developed antitumor platinum compound].
abstract: KB-5424 (ab-(3-aminopyrrolidine)-cd-[glycolato (2-)-0, 0'] platinum (II) is a newly developed antitumor platinum compound which was synthesized at Kanebo Institute for Cancer Research. When the antitumor activity of KB-5424 was evaluated using several rodent tumors, no significant differences were observed between the antitumor activities of KB-5424, cisplatin (CDDP) and DWA-2114 R (DWA). KB-5424 was divided into two kinds of optical isomers, KB-5424 R and KB-5424 S, of which antitumor activity was compared each other. The maximum increased life span (ILSmax) on L 1210 of KB-5424 R was almost equal to that of CDDP and better than those of KB-5424 S and carboplatin (CBDCA). The antitumor activity of KB-5424 R on a human tumor xenograft MX-1 was almost identical to those of CDDP and CBDCA and better than that of DWA. Since the nephrotoxicity of KB-5424 R was significantly reduced comparing with CDDP, this newly developed antitumor platinum compound was thought to be a promising agent for the clinical application.
authors.affiliation: Dept. of Surgery, School of Medicine, Keio University.
authors.forename: H
authors.initials: H
authors.lastname: Yamaguchi
authors.forename: T
authors.initials: T
authors.lastname: Kubota
authors.forename: T
authors.initials: T
authors.lastname: Takahara
authors.forename: T
authors.initials: T
authors.lastname: Takeuchi
authors.forename: T
authors.initials: T
authors.lastname: Furukawa
authors.forename: S
authors.initials: S
authors.lastname: Kase
authors.forename: K
authors.initials: K
authors.lastname: Josui
authors.forename: S
authors.initials: S
authors.lastname: Kodaira
authors.forename: K
authors.initials: K
authors.lastname: Ishibiki
authors.forename: O
authors.initials: O
authors.lastname: Abe
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000009:adverse effects / Q000737:chemistry / Q000627:therapeutic use*; D016190:Carboplatin / Q000031:analogs & derivatives / Q000627:therapeutic use; D002945:Cisplatin / Q000627:therapeutic use; D004354:Drug Screening Assays, Antitumor; D007668:Kidney / Q000187:drug effects; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D008810:Mice, Inbred C57BL; D009368:Neoplasm Transplantation; D009374:Neoplasms, Experimental / Q000188:drug therapy*; D009904:Optical Rotation; D009944:Organoplatinum Compounds / Q000008:administration & dosage / Q000627:therapeutic use*; D051381:Rats; D011916:Rats, Inbred F344
chemical_list: D000970:Antineoplastic Agents; D009944:Organoplatinum Compounds; C058816:DWA 2114; C069360:KB 5424; D016190:Carboplatin; D002945:Cisplatin