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fezagepras
- Development stage
- Discontinued
- Lead developer
- Liminal BioSciences
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Fezagepras (also known as PBI-4050 and setogepram) is an orally available small molecule drug that was developed by Liminal BioSciences (formerly ProMetic Life Sciences). It acts as a modulator of fatty acid receptors, specifically functioning as an agonist for Free fatty acid receptor 1 (FFAR1) (GPR40) and an antagonist or inverse agonist for G protein-coupled receptor 84 (GPR84). Fezagepras also modulates peroxisome proliferator-activated receptor alpha (PPAR alpha). The drug was investigated for its anti-fibrotic, anti-inflammatory, antihyperglycemic, and hepatoprotective properties. Its mechanisms include nitrogen scavenging activity via glutamine conjugation and modulation of metabolic pathways relevant to fibrosis and metabolic diseases. Development was discontinued in 2022 after clinical trials showed it was inferior to sodium phenylbutyrate as a nitrogen scavenger[1][2][4][5][6].
- Brand names
- fezagepras
- Other names
- 3-pentylbenzeneacetic acid sodium salt
02
Targets
FFAR1 (Free fatty acid receptor 1)GPR84PPARA (Peroxisome proliferator-activated receptor alpha)
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