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Tariquidar is a potent inhibitor of P-glycoprotein (Pgp), a 170-kDa transmembrane protein acting as a drug efflux pump to actively transport structurally unrelated compounds out of cells, that noncompetitively inhibits the basal the activity of ATPase associated with Pgp. Tariquidar contains a tertiary amine, dimethoxyphenyl group and amide group in its chemical structure, which contribute to its inhibition against Pgp. Results of in vitro assays of three different models have shown that Tariquidar inhibits Pgp with 50% inhibition concentration IC50 values ranging from 15 to 223 nM. However, the inhibition by tariquidar is Pgp-specific and attenuated in tumor cell lines, where multidrug resistance is mediated by multidrug resistance-associated protein.

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