Drug intelligence / Profile preview

FR139317

Development stage: Preclinical
Lead developer: Astellas Pharma
Modality: Small Molecules
Administration: Intravenous, Intraperitoneal, Subcutaneous, Intracisternal, Oral

Overview

FR139317 is a highly potent and selective small molecule antagonist of the endothelin ETA receptor. Developed by Fujisawa Pharmaceutical Co., Ltd., this compound has been extensively utilized in preclinical research to elucidate the physiological and pathophysiological roles of endothelin ETA receptors. Studies in various animal models have explored its potential in conditions such as pulmonary hypertension, congestive heart failure, cerebral vasospasm, and the inhibition of neointimal thickening. Its mechanism of action involves blocking the ETA receptor, thereby counteracting the vasoconstrictive and proliferative effects mediated by endothelin-1.

Other names: FR139,317

Targets

EDNRB (Endothelin receptor type B)EDNRA (Endothelin receptor type A)

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