[Antitumor activity and toxicity of KB-5424 R, a newly developed antitumor platinum compound].

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.
AuthorsH Yamaguchi, T Kubota, T Takahara, T Takeuchi, T Furukawa, S Kase, K Josui, S Kodaira, K Ishibiki, O Abe
JournalGan to kagaku ryoho. Cancer & chemotherapy (Gan To Kagaku Ryoho) Vol. 18 Issue 7 Pg. 1135-41 (Jun 1991) ISSN: 0385-0684 [Print] JAPAN
PMID2053772 (Publication Type: Comparative Study, English Abstract, Journal Article)
Chemical References
  • Antineoplastic Agents
  • Organoplatinum Compounds
  • DWA 2114
  • KB 5424
  • Carboplatin
  • Cisplatin
  • Animals
  • Antineoplastic Agents (adverse effects, chemistry, therapeutic use)
  • Carboplatin (analogs & derivatives, therapeutic use)
  • Cisplatin (therapeutic use)
  • Drug Screening Assays, Antitumor
  • Kidney (drug effects)
  • Male
  • Mice
  • Mice, Inbred BALB C
  • Mice, Inbred C57BL
  • Neoplasm Transplantation
  • Neoplasms, Experimental (drug therapy)
  • Optical Rotation
  • Organoplatinum Compounds (administration & dosage, therapeutic use)
  • Rats
  • Rats, Inbred F344

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