Elacridar (GF120918)

Description: Elacridar (formerly GW-120918; GF-120918; GG-918; GW-0918; GF120918; GF120918; GW0918; GG918) is a 3rd generationl and potent P-glycoprotein (P-gp or MDR-1) and BCRP inhibitor that has the potential to overcome P-gp-mediated multidrug resistance (MDR) of the cytotoxic drugs such as doxorubicin. Elacridar has been used both in vitro and in vivo as a tool inhibitor of P-gp to investigate the role of transporters in the disposition of various test molecules. In vitro, GF120918A demonstrated high plasma protein binding across species, although a definitive protein binding evaluation was precluded by poor recovery, particularly in buffer and in mouse, rat, and dog plasma.

References: Int J Cancer. 2014 Mar 15; 134(6):1484-94; Drug Metab Dispos. 2012 Aug; 40(8):1612-9; Clin Cancer Res. 2007 Nov 1; 13(21):6440-9.

Related CAS#:143851-98-3 (HCl); 143664-11-3 (Elacridar)