Drug intelligence / Profile preview

gw9578

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

Overview

GW9578 is a **synthetic small molecule** that acts as a highly potent and subtype-selective agonist of **peroxisome proliferator-activated receptor alpha (PPARα)**[1][2][5][7][8]. The drug was developed by **GSK Plc** for **endocrinology and metabolic diseases**, predominantly targeting **hyperlipidemia** and related metabolic disorders. GW9578 robustly activates the PPARα nuclear receptor, with an EC50 of 8 nM and exhibits over 250-fold selectivity for PPARα versus other PPAR subtypes[2]. Its primary mechanism is upregulation of fatty acid oxidation and modulation of gene expression involved in lipid metabolism, resulting in potent **lipid-lowering effects** and potential reduction of insulin resistance[3][5][7]. GW9578 also demonstrated effects on appetite suppression and modulated metabolic markers in preclinical models[2]. The development of GW9578 was discontinued and did not reach regulatory approval for any indications[1].

Other names
2-[4-[2-[(2,4-difluorophenyl)carbamoyl-heptylamino]ethyl]phenyl]sulfanyl-2-methylpropanoic acidureido-thioisobutyric acid247923-29-1
02

Targets

PPARA (Peroxisome proliferator-activated receptor alpha)

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