Background:

Dofequidar fumarate is a multidrug-resistant (MDR) - reversal agent [1].

Dofequidar fumarate is a quinoline derivative and has highly potent reversing effect on multidrug-resistant tumor cells. It prevents the transport of antitumor drugs through interacting with the drug-efflux pump P-glycoprotein directly and thereby reverses MDR. In vincristine (VCR)-resistant P388/VCR cells and Adriamycin (ADM)- resistant P388/ADM cells, dofequidar fumarate at 1μM and 3μM can completely reverse the drug resistance. It also shows significant effects on the MDR K562 cells. Furthermore, in mice model bearing HCT-15 xenografts, combination therapy of dofequidar fumarate and docetaxel induces remarkable tumor growth inhibition. Dofequidar fumarate also shows significant reversing effect in MCF-7/ADM-bearing mice [1, 2].

参考文献:
[1] Sato W, Fukazawa N, Nakanishi O, et al. Reversal of multidrug resistance by a novel quinoline derivative, MS-209. Cancer chemotherapy and pharmacology, 1995, 35(4): 271-277.
[2] Naito M, Matsuba Y, Sato S, et al. MS-209, a quinoline-type reversal agent, potentiates antitumor efficacy of docetaxel in multidrug-resistant solid tumor xenograft models. Clinical cancer research, 2002, 8(2): 582-588.