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Tariquidar + chemotherapy refers to the combination of tariquidar, a third-generation *P-glycoprotein (Pgp, ABCB1) inhibitor*, with various cytotoxic chemotherapy agents such as vinorelbine, doxorubicin, docetaxel, or etoposide. Tariquidar inhibits the ATPase activity of Pgp, a membrane efflux pump associated with multidrug resistance (MDR) in cancer cells, and at higher concentrations, also inhibits breast cancer resistance protein (BCRP/ABCG2). This inhibition leads to increased intracellular retention and cytotoxicity of chemotherapeutics that are Pgp substrates in tumors expressing Pgp, potentially overcoming resistance. Tariquidar has been studied in both pediatric and adult populations with recurrent, refractory, or metastatic cancers, in various combinations with standard chemotherapies, and is usually administered intravenously prior to chemotherapy infusion.
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