Encequidar (mesylate)

849675-87-2

C39H40N6O10S

H2O

Membrane Transporter/Ion Channel

Encequidar mesylate (HM30181 mesylate) is a competitive and potent P-glycoprotein inhibitor. IC50 & Target: P-glycoprotein^[1][2]. In Vitro: Compared with control (0 nM Encequidar (HM30181)), paclitaxel potently inhibits the survival of K1735 cells by about 65% at 100 nM and 72% at 1000 nM in a dose-dependent manner. Encequidar (HM30181) does not make any significant changes in the survival of K1735 cells. In contrast, bEnd.3 cells do not show any decreases in survival by the paclitaxel treatment without Encequidar (HM30181). However, treatment of 0.1 or 1 nM Encequidar (HM30181) lead to 20 and 42% inhibition of survival at the 100 nM and 1000 nM paclitaxel treatment, respectively^[2]. In Vivo: The plasma concentrations of Encequidar (HM30181) are higher for the simultaneous administration with the microcapsule than with the powder; providing significant differences from 1 to 2 h. The microcapsule has about a 1.7-fold faster T_max and a 1.6-fold higher AUC value compared with the powder (2.5+/-0.6 vs. 4.3+/-0.9 h; 107.7+/-20.1 vs. 64.3+/-18.0 h ng/mL). The faster and overall improved absorption of Encequidar (HM30181) in microcapsule form might be due to the remarkable enhancement of the aqueous solubility and dissolution resulting from its crystalline conversion to the amorphous form and particle size reduction^[1].