[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: H Yamaguchi, T Kubota, T Takahara, T Takeuchi, T Furukawa, S Kase, K Josui, S Kodaira, K Ishibiki, O Abe
• Journal: Gan to kagaku ryoho. Cancer & chemotherapy (Gan To Kagaku Ryoho) Vol. 18 Issue 7 Pg. 1135-41 (Jun 1991) ISSN: 0385-0684 [Print] Japan
• PMID: 2053772 (Publication Type: Comparative Study, English Abstract, Journal Article)

Chemical References

• Antineoplastic Agents
• Organoplatinum Compounds
• DWA 2114
• KB 5424
• Carboplatin
• Cisplatin

Topics

• 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