Zosuquidar (hydrochloride)

Zosuquidar is a modulator of P-glycoprotein (P-gp; K_i = 59 nM).¹ It restores the sensitivity of P-gp-expressing cancer cells to vinblastine (Item No. 11762), doxorubicin (Item No. 15007), etoposide (Item No. 12092), and paclitaxel (Item No. 10461) when used at 0.1 µM.¹ It less potently inhibits cytochrome P450 (CYP) isoforms CYP3A, CYP2D6, and CYP2C9 (K_is = 3.8, 25, and 12 µM, respectively).² Zosuquidar does not modulate multidrug resistance-associated protein 1 (MRP-1). Zosuquidar significantly enhances the efficacy of chemotherapeutics in mice implanted with P-gp-expressing tumors.¹ Through its effects on P-gp, zosuquidar enhances the distribution of P-gp substrates through the blood-brain barrier into the brain.^3,4

WARNING This product is not for human or veterinary use.

1. Dantzig, A.H., Shepard, R.L., Cao, J., et al. Reversal of P-glycoprotein-mediated multidrug resistance by a potent cyclopropyldibenzosuberane modulator, LY335979. Cancer Res. 56(18), 4171-4179 (1996).

2. Dantzig, A.H., Shepard, R.L., Law, K.L., et al. Selectivity of the multidrug resistance modulator, LY335979, for P-glycoprotein and effect on cytochrome P-450 activities. J. Pharmacol. Exp. Ther. 290(2), 854-862 (1999).

3. Choo, E.F., Leake, B., Wandel, C., et al. Pharmacological inhibition of P-glycoprotein transport enhances the distribution of HIV-1 protease inhibitors into brain and testes. Drug Metab. Dispos. 28(6), 655-660 (2000).

4. Liu, F., Wang, X., Li, Z., et al. P-Glycoprotein (ABCB1) limits the brain distribution of YQA-14, a novel dopamine D₃ receptor antagonist. Chem. Pharm. Bull. (Tokyo) 63(7), 512-518 (2015).