抗肿瘤药Oxaliplatin

• 作 者: 奚刚强
• 出 处: 国外医药.合成药.生化药.制剂分册
• 发表日期: 1990年05期
• 关键词: 顺铂 卡波铂 交叉耐药性 肾脏毒性 碳铂 临床试用 环己烷 Rosenberg 胃肠道 二硝基

自1969年Rosenberg等发现顺铂的抗肿瘤活性以来,世界上许多研究人员为制备优良的铂复合物,改善顺铂的严重毒性作用(如肾脏毒性、胃肠道毒性、血液毒性、骨髓抑制以及周围神经毒性)进行了各种探索。碳铂(卡波铂)已在英国上市。但它对耐受顺铂的肿瘤有交叉耐药性。新研制的本品正在法国进行Ⅰ期与Ⅱ期临床试用中。合成由二硝基-(1 R,2 R-环己烷二胺铂复合体与草酸钠在水中反应而成[Ganm1980,71(5):637]

Since Rosenberg et al. Discovered the anti-tumor activity of cisplatin in 1969, many researchers all over the world have made great efforts to improve the platinum toxicity, such as nephrotoxicity, gastrointestinal toxicity, hematotoxicity, myelosuppression, Peripheral neurotoxicity) conducted a variety of exploration. Carbon platinum (carboplatin) has been listed in the UK. But it is cross-resistant to cisplatin-resistant tumors. The newly developed product is being carried out in France Ⅰ and Ⅱ clinical trials. Synthesis of dinitro- (1 R, 2 R-cyclohexanediamine platinum complex with sodium oxalate in water [Ganm 1980, 71 (5): 637]