Yamaguchi H, Kubota T, Takahara T, Takeuchi T, Furukawa T, Kase S, Josui K, Kodaira S, Ishibiki K, Abe O
Dept. of Surgery, School of Medicine, Keio University.
Gan To Kagaku Ryoho. 1991 Jun;18(7):1135-41.
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.
KB - 5424（α -（3 - 氨基吡咯烷）-γ，δ - [乙醇酸根合（2 -）-O，O']铂（II））是佳丽宝癌症研究所新开发的一种抗肿瘤铂化合物。当使用几种啮齿动物肿瘤评估KB - 5424的抗肿瘤活性时，未观察到KB - 5424、顺铂（CDDP）和DWA - 2114 R（DWA）的抗肿瘤活性之间存在显著差异。KB - 5424分为两种旋光异构体，KB - 5424 R和KB - 5424 S，并对它们的抗肿瘤活性进行了相互比较。KB - 5424 R对L1210的最大寿命延长率（ILSmax）几乎与顺铂相等，且优于KB - 5424 S和卡铂（CBDCA）。KB - 5424 R对人肿瘤异种移植MX - 1的抗肿瘤活性几乎与顺铂和卡铂相同，且优于DWA。由于与顺铂相比，KB - 5424 R的肾毒性显著降低，这种新开发的抗肿瘤铂化合物被认为是一种有临床应用前景的药物。
