Elacridar is a dual inhibitor of P-glycoprotein (MRP-1, ABCB1) and breast cancer resistance protein (BCRP, ABCG2). It maximally inhibits P-glycoprotein in isolated human peripheral blood leukocytes at 200 nM. Elacridar blocks the activity of P-glycoprotein at the blood-brain barrier, altering the pharmacokinetics of certain drugs in the brain. This compound is effective against both human BCRP and the mouse homolog, Bcrp1.
