Drug intelligence / Profile preview

farglitazar

Development stage
Phase 2
Lead developer
GSK
Modality
Small Molecules
Administration
Oral
01

Overview

Farglitazar is a small molecule drug developed as a selective peroxisome proliferator–activated receptor gamma (PPARγ) agonist. It is an L‑tyrosine derivative with hypoglycemic and lipid-lowering activity. Farglitazar was investigated for the treatment of type 2 diabetes mellitus and hepatic fibrosis due to its ability to improve glycemic control and modulate lipid metabolism. The drug acts primarily by activating PPARγ receptors—nuclear hormone receptors involved in glucose and lipid homeostasis—which leads to increased insulin sensitivity. Farglitazar also influences renal sodium and water reabsorption by stimulating epithelial sodium channels (ENaC) and Na,K‑ATPase systems in the distal nephron[1][3][4][6]. Development was discontinued after reaching phase 3 trials for type 2 diabetes mellitus and phase 2 trials for liver fibrosis[5].

Other names
farglitazar [USAN]farglitazar [INN]N-(2-benzoylphenyl)-O-[2-(5-methyl-2-phenyl-4-oxazolyl)ethyl]-L-tyrosineL-tyrosine N-(2-benzoylphenyl)-O-[2-(5-methyl-2-phenyl-4-oxazolyl)ethyl]UNII-3433GY7132UNII3433GY7132UNII 3433GY7132
02

Targets

PPARG (Peroxisome proliferator-activated receptor gamma)PPARA (Peroxisome proliferator-activated receptor alpha)

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