Brock N, Stekar J, Pohl J, Niemeyer U, Scheffler G
Arzneimittelforschung. 1979;29(4):659-61.
The urotoxicity of oxazaphosphorine cytostatics is not based on their alkylating activity but on the presence of acrolein, which is spontaneously formed in the urine from the primary metabolites eliminated via the kidneys. Thus, acrolein proved to be the causative factor in the urotoxicity of oxazaphosphorines. The mechanism of action of the uroprotector sodium 2-mercaptoethane-sulfonate (mesnum, Mitexan) is mainly based on the formation of a non-toxic additive compound with acrolein.
氮杂磷三环类细胞抑制剂的尿路毒性并非基于其烷基化活性,而是基于丙烯醛的存在,丙烯醛是通过肾脏排出的主要代谢产物在尿液中自发形成的。因此,丙烯醛被证明是氮杂磷三环类药物尿路毒性的致病因素。尿路保护剂2-巯基乙烷磺酸钠(美司钠,Mitexan)的作用机制主要基于与丙烯醛形成无毒加成化合物。