Drug intelligence / Profile preview

tariquidar

Development stage
Phase 3
Lead developer
Xenova Group
Modality
Small Molecules
Administration
Intravenous, Oral
01

Overview

Tariquidar is an anthranilamide derivative and a third-generation P-glycoprotein (P-gp, also known as ABCB1) inhibitor developed to overcome multidrug resistance in cancer. It acts as a potent, specific, noncompetitive inhibitor of P-glycoprotein by binding to the transporter and inhibiting its ATPase activity, thereby blocking the efflux of anticancer drugs from tumor cells. This inhibition increases intracellular concentrations of chemotherapeutic agents and can reverse both intrinsic and acquired drug resistance. Tariquidar may also inhibit breast cancer resistance protein (BCRP/ABCG2). It has been studied primarily as an adjuvant in combination with chemotherapy for refractory or recurrent solid tumors[1][2][3][5][7].

Other names
tariquidarXR9576XR-9576XR 9576
02

Targets

ABCB1 (P-glycoprotein)ABCG2 (ATP-binding cassette sub-family G member 2)

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