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ONT-093 is an orally bioavailable small molecule inhibitor of P-glycoprotein (P-gp), a membrane transporter protein that contributes to multidrug resistance in cancer by actively exporting chemotherapeutic agents from tumor cells. By inhibiting P-gp ATPase activity at nanomolar concentrations, ONT-093 increases the intracellular concentration of various chemotherapeutic drugs and can reverse drug resistance in preclinical models. It has been studied primarily for its potential to enhance the efficacy of chemotherapy in cancers exhibiting multidrug resistance. In phase I clinical trials combined with paclitaxel, ONT-093 was generally well tolerated at biologically active serum concentrations[1][3][6][8].
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