Drug intelligence / Profile preview

tariquidar + chemotherapy

Development stage
Unknown
Lead developer
Xenova
Modality
Small Molecules
Administration
Intravenous
01

Overview

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.

02

Targets

ABCB1 (P-glycoprotein)ABCG2 (Breast cancer resistance protein)

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