Dl. Slate et al., RS-33295-198 - A NOVEL, POTENT MODULATOR OF P-GLYCOPROTEIN-MEDIATED MULTIDRUG-RESISTANCE, Anticancer research, 15(3), 1995, pp. 811-814
A novel multidrug resistance modulator; RS-33295-198, circumvented dru
g resistance in human, mouse, and Chinese hamster cell lines overexpre
ssing P-glycoprotein. It enhanced the antiproliferative activity of do
xorubicin, vincristine, etoposide, and paclitaxel and increased doxoru
bicin retention in multidrug-resistant hamster CH(R)C5 cells. RS-33295
-198 modulated doxorubicin resistance in a murine P388/ADR leukemia mo
del when administered ip via continuous minipump delivery, ip by bolus
injection and orally; it also improved the efficacy of vincristine to
ward P388/VCR leukemia when given ip or po. RS-33295-198 showed weak a
ctivity in enhancing doxorubicin efficacy against a multidrug-resistan
t human sarcoma xenograft.