Drug intelligence / Profile preview

GW590735

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

Overview

GW590735 is a potent and selective small molecule agonist of peroxisome proliferator–activated receptor alpha (PPARα), a nuclear hormone receptor that regulates genes involved in lipid metabolism. By activating PPARα (EC50 = 4 nM), GW590735 increases high-density lipoprotein (HDL) cholesterol and decreases low-density lipoprotein (LDL), very-low-density lipoprotein (VLDL), and triglycerides. It was developed for the treatment of dyslipidemia and other metabolic disorders but did not progress beyond phase II clinical trials due to discontinuation of development. The compound exhibits at least 500-fold selectivity for PPARα over PPARγ and PPARδ[2][5][7].

Other names
343321-96-0Propanoic acid 2-methyl-2-(4-((((4-methyl-2-(4-(trifluoromethyl)phenyl)-5-thiazolyl)carbonyl)amino)methyl)phenoxy)-2-methyl-2-{4-[({4-methyl-2-[4-(trifluoromethyl)phenyl]-1,3-thiazol-5-yl}formamido)methyl]phenoxy}propanoic acid
02

Targets

PPARA (Peroxisome proliferator-activated receptor alpha)

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