Dorr R T, Alberts D S, Soble M
Cancer Chemother Pharmacol. 1986;16(2):91-4. doi: 10.1007/BF00256155.
Cisplatin and L-PAM are DNA-crosslinking anticancer agents which have not been systematically studied for vesicant potential. Mitoxantrone is a new active anthracene-based, DNA intercalator which is undergoing widespread clinical testing for antitumor efficacy in man. These three agents were tested for vesicant activity in dehaired BALB/c mice given ID injections equivalent to human clinical doses. Neither cisplatin (up to 150 mg/m2) nor L-PAM (up to 71 mg/m2) produced any skin necrosis in the mice. The L-PAM solvent (acid/alcohol in propylene glycol) was ulcerogenic if injected undiluted. Mitoxantrone (up to 14 mg/m2) was not ulcerogenic in the mice, although the skin site retained a blue drug discoloration for several weeks. It is concluded that in clinically relevant doses, cisplatin, L-PAM, and mitoxantrone are not vesicants.
顺铂和左旋苯丙氨酸氮芥是DNA交联抗癌剂，尚未对其发泡剂潜力进行系统研究。米托蒽醌是一种新型的基于蒽的活性DNA嵌入剂，正在广泛进行人体抗肿瘤疗效的临床试验。对脱毛的BALB/c小鼠进行皮内注射，给予相当于人类临床剂量的这三种药物，测试其发泡活性。顺铂（高达150mg/m²）和左旋苯丙氨酸氮芥（高达71mg/m²）均未在小鼠中引起任何皮肤坏死。左旋苯丙氨酸氮芥的溶剂（丙二醇中的酸/醇）如果未经稀释注射会引起溃疡。米托蒽醌（高达14mg/m²）在小鼠中不会引起溃疡，尽管皮肤部位会有数周保留蓝色药物变色。结论是，在临床相关剂量下，顺铂、左旋苯丙氨酸氮芥和米托蒽醌不是发泡剂。
