Drug intelligence / Profile preview

GSK2256294

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

Overview

GSK2256294 is a potent, reversible small molecule inhibitor of soluble epoxide hydrolase (sEH), an enzyme that metabolizes epoxyeicosatrienoic acids (EETs), which are endogenous regulators of vascular function and inflammation. By inhibiting sEH, GSK2256294 increases EET levels and the EET-to-DHET ratio in serum. The drug has demonstrated sustained inhibition of sEH activity in plasma, muscle, and adipose tissue in humans. It has been investigated for potential therapeutic use in conditions involving endothelial dysfunction or abnormal tissue repair such as chronic obstructive pulmonary disease (COPD), insulin resistance/prediabetes, wound healing disorders, and subarachnoid hemorrhage (SAH). Clinical studies have shown it to be well tolerated with no significant adverse events reported[1][5][8].

Other names
UNII-L33EX3XR0TUNII-L-33EX3XR0TUNII-L 33EX3XR0TL33EX3XR0TL-33EX3XR0TL 33EX3XR0TN-((4-cyano-2-(trifluoromethyl)phenyl)methyl)-3-((4-methyl-6-(methylamino)-1,3,5-triazin-2-yl)amino)cyclohexanecarboxamidecis-N-((4-Cyano-2-(trifluoromethyl)phenyl)methyl)-3-((4-methyl-6-(methylamino)-1,3,5-triazin-2-yI)amino)cyclohexanecarboxamide
02

Targets

EPHX2 (Soluble epoxide hydrolase)

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