Product Overview
Elacridar is an inhibitor of breast cancer resistance protein (BCRP) and P-glycoprotein (P-GP) that has been used to improve the brain distribution of drugs. Recent studies have revealed that elacridar could probably be the substrate of these multidrug transporters (MDTs). Recent studies had shown that elacridar and taxanes co-administrated orally could increase plasma concentrations of docetaxel (four-fold) and paclitaxel (10.7-fold) in mice. Co-administration of elacridar with taxanes and ritonavir could lead to a further increase in plasma concentrations of docetaxel (37.4-fold) and paclitaxel (31.9-fold). Besides, co-administration of elacridar with taxanes and ritonavir could potently increase taxanes concentration in the brain, but not increase the brain penetration of the taxanes. Elacridar co-administrated orally with crizotinib has shown to increase the crizotinib concentrations in plasma and brain as well as increase the brain-to-plasma ratios of crizotinib, indicating that co-administration of crizotinib with elacridar could increase oral availability of crizotinib and delivery of crizotinib to the brain. Apart from these, the uptake of elacridar at nanomolar doses in mouse brain was proved to be limited by Pgp-and Bcrp1-induced efflux at the blood-brain barrier. In vitro, Elacridar was indicated a low intracellular accumulation at nanomolar concentrations and a high intracellular accumulation at micromolar concentrations in Pgp-and Bcrp1-overexpressing cell lines.
Synonyms
GF 120918A; GF120918A; GF-120918A
Molecular Formula
C34H34ClN3O5
Chemical Name
N-[4-[2-(6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)ethyl]phenyl]-5-methoxy-9-oxo-10H-acridine-4-carboxamide; hydrochloride
Solubility
Soluble in DMSO > 10 mM
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request
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