Drug intelligence / Profile preview

elacridar

Development stage
Discontinued
Lead developer
GSK
Modality
Small Molecules
Administration
Oral
01

Overview

Elacridar is an investigational small molecule that acts as a potent, noncompetitive inhibitor of the ATP-binding cassette (ABC) transporters P-glycoprotein (ABCB1) and breast cancer resistance protein (BCRP/ABCG2). It was developed as an oral bioenhancer to overcome multidrug resistance in tumors by inhibiting drug efflux pumps, thereby increasing the bioavailability and efficacy of coadministered chemotherapeutic agents. Elacridar has been studied primarily in preclinical and early clinical settings for its ability to resensitize resistant cancer cells to drugs such as docetaxel. As of 2007, development appears to have been discontinued and it is not approved for any indication[1][2][3][7].

Other names
elacridar hydrochlorideelacridar HCl
02

Targets

ABCG2 (ATP-binding cassette sub-family G member 2)ABCB1 (P-glycoprotein)

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