Target: P-glycoprotein (Pgp); breast cancer resistance protein (BCRP)
IC50: 193 nM; 250 nM
Elacridar is a potent P-gp (MDR-1) and BCRP inhibitor that has been used to improve the brain distribution of drugs that are substrates of P-gp and BCRP [1]. Pgp and BCRP are expressed in endothelial cells of the blood-brain barrier (BBB), limiting the entry of substrate drugs or toxins into the brain by pumping them back into the blood [2].
In vitro: Elacridar microemulsion was effective in inhibiting P-gp and Bcrp in vitro at an elacridar concentration of 1 μM [3]. Elacridar at 5 μM completely inhibited the polarized sunitinib transport in huABCB1, huABCG2 or muABCG2 cell lines [4].
In vivo: Oral administration of elacridar (100 mg/kg) could completely
IC50: 193 nM; 250 nM
Elacridar is a potent P-gp (MDR-1) and BCRP inhibitor that has been used to improve the brain distribution of drugs that are substrates of P-gp and BCRP [1]. Pgp and BCRP are expressed in endothelial cells of the blood-brain barrier (BBB), limiting the entry of substrate drugs or toxins into the brain by pumping them back into the blood [2].
In vitro: Elacridar microemulsion was effective in inhibiting P-gp and Bcrp in vitro at an elacridar concentration of 1 μM [3]. Elacridar at 5 μM completely inhibited the polarized sunitinib transport in huABCB1, huABCG2 or muABCG2 cell lines [4].
In vivo: Oral administration of elacridar (100 mg/kg) could completely