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Description

A cell-permeable pyrazolopyrimidine that selectively inhibits MRP1. It is shown to increase the efficacy of vincristine and etopiside by 10- to 15-fold and 7- to 10-fold, respectively, over either of these two MRP1 substrate drugs alone in murine models of neuroblastoma (syngenic and human xenografts). As opposed to the majority of inhibitors of multidrug transporters, it is demonstrated that Reversan was not toxic by itself nor did it increase the toxicity of chemotherapeutic drug exposure in mice. Therefore, Reversan represents a new class of nontoxic MRP1 inhibitor, which may be a useful research tool for the study of neuroblastoma and other MRP1-overexpressing drug-refractory tumors.