Elacridar (maleate)

Elacridar maleate is an orally active P-glycoprotein (Pgp) and breast cancer resistance protein (BCRP) inhibitor. Elacridar maleate can be used to examine the influence of efflux transporters on drug distribution to brain and the research of cancer^[1][2]. In Vitro: Elacridar maleate (0.001-1 μM; 2 h) inhibits cell viability of 786-O cells^[2].
Elacridar maleate (5 μM; 24 h) affects P-glycoprotein and ABCG2 protein expression levels in MCF-7 and 786-O cell lines^[2].
Elacridar maleate (5 μM; 24 h) affects ^99mTc-MIBI intracellular accumulation in MCF-7 and 786-O cells^[2]. In Vivo: Elacridar maleate (100 mg/kg; i.p. once) shows different distribution in brain and plasma^[1].
Plasma Pharmacokinetic Parameters of Elacridar maleate in mice^[1].

	Mice PO 100 mg/kg	Mice IP 100 mg/kg	Mice IV 2.5 mg/kg
CL/F (ml/min)	2.05	33.2	0.46
Vd/F (liter)	3.5	12.3	0.17
t1/2 (h)	20	4.3	4.4
AUC0-inf (μg•min/ml)	1460	90.3	161.4
F	0.22	0.013	1