卡铂临床前药效及毒理研究

PRECLINICAL STUDIES OF EFFECT AND TOXICITY OF CARBOPLATIN

卡铂(CBDCA)是第二代铂类抗癌新药,本文通过体内、外试验证实它对动物移植性肿瘤S_(180)、W_(256)抑制作用显著。对体外传代细胞系HL—60细胞杀伤作用明显,且有剂量效应关系。 大鼠及家犬长期毒性试验证实CBDCA的剂量限制性毒性反应是骨髓抑制。大鼠外周血检查,给药二周后白细胞首先开始降低,随之有血小板及血红蛋白降低。家犬试验除发现外周血象降低外,并分别在不同试验阶段做骨髓检查,进一步证实CBDCA可使大剂量组动物骨髓红系、粒系、巨核细胞系受到不同程度的抑制。停药后2—4周外周血象及骨髓象均可得到恢复。CBDCA的其他毒副反应均非常轻微,是一个较好的抗癌新药。

Carboplatin is a seconb-gene ration platinum, containg anti-tumor new agent, The antitumour activity was demonstrated in vivo S180, W256 and in vitio cell line HL-60.In the present rats and dogs were used to investigate the toxicity of CBDCA. The drug of dose -limiting toxicity effect was bone marrow inhibition. CBDCA caused depression in the number of leukocytes, platelets and hemoglobin in for high-dose group, which were reversed after stop daministration two to four weeks. In addition, CBDCA has been shown to with little or no nephrotoxicity and less emesis. It appeared to be a valuable drug for the antitumor.