tcsc1112 Elacridar

Elacridar is a potent P-glycoprotein (Pgp) and BCRP inhibitor.

IC50 & Target: P-glycoprotein (Pgp), BCRP^[1]

In Vitro: Elacridar inhibits P-glycoprotein (P-gp) labeling by [³H]azidopine with a IC₅₀ of 0.16 μM^[2]. In Caki-1 and ACHN cells, elacridar (2.5 μM) significantly ihibits the cell growth. The P-glycoprotein activity is found to be inhibited by elacridar. The combination of elacridar and sunitinib lead to a significant reduction in ABC Sub-family B Member 2 (ABCG2) expression in 786-O cells^[3].

In Vivo: Oral co-administration of elacridar (100 mg/kg, p.o.) and crizotinib increases the plasma and brain concentrations and brain-to-plasma ratios of crizotinib in wild-type mice, equaling the levels in Abcb1a/1b; Abcg2^-/- mice^[1]. In friend leukemia virus stain B mice, the brain-to-plasm partition coefficient (Kp, brain) of elacridar is 0.82, 0.43, and 4.31 after intravenous (2.5 mg/kg), intraperitoneal (100 mg/kg), and oral (100 mg/kg) treatment, respectively^[4]. In Mrp4(-/-) mice, elacridar fully inhibits P-gp mediated transport of topotecan, without siginificant effects on Bcrp1-mediated transport^[5].