Naito M, Nakanishi O, Tsuruo T
Institute of Molecular and Cellular Biosciences, University of Tokyo.
Nihon Rinsho. 1997 May;55(5):1122-7.
The emergence of multidrug resistance(MDR) is a major problem in cancer chemotherapy. Many compounds are developed to reverse MDR, and some of them are under clinical trials. Among them, MS-209, a novel quinoline derivative, is one of the most potent MDR reversing agents. MS-209 at 3 microM effectively reverses MDR in various cell lines in vitro. MS-209 directly interacts with P-glycoprotein and inhibits the P-glycoprotein-mediated drug transport. Oral administration of MS-209 combined with anticancer drugs markedly increases the life span of mice bearing MDR tumor cells without causing serious side effects. Thus, MS-209 is an orally active and potent MDR reversing drug without serious side effects.
多药耐药性（MDR）的出现是癌症化疗中的一个主要问题。人们开发了许多化合物来逆转MDR，其中一些正在进行临床试验。其中，新型喹啉衍生物MS-209是最有效的MDR逆转剂之一。3微摩尔的MS-209在体外可有效逆转多种细胞系中的MDR。MS-209直接与P-糖蛋白相互作用，并抑制P-糖蛋白介导的药物转运。口服MS-209联合抗癌药物可显著延长携带MDR肿瘤细胞的小鼠的寿命，且不会引起严重的副作用。因此，MS-209是一种口服活性强且无严重副作用的MDR逆转药物。
