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AR-9281

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

Overview

AR-9281 is a potent, selective, and orally active small molecule inhibitor of soluble epoxide hydrolase (sEH), an enzyme that plays a key role in the cytochrome P450 pathway of arachidonic acid metabolism[2][3][4]. By inhibiting sEH, AR-9281 prevents the breakdown of epoxyeicosatrienoic acids (EETs), which have anti-hypertensive and anti-inflammatory effects. This mechanism enhances EETs' beneficial activities by increasing their levels in the body. Preclinical studies demonstrated that AR-9281 lowers blood pressure, improves vascular function, and reduces renal inflammation and injury in models of hypertension[5]. It was developed as a first-in-class antihypertensive agent with potential additional benefits for cardiovascular disease, diabetes, inflammation, and kidney disease[6]. The drug reached Phase 2 clinical trials for indications including hypertension, type 2 diabetes mellitus, and glucose intolerance but development has since been discontinued[7].

Other names
1-(1-acetyl-piperidine-4-yl)-3-adamantan-1-yl-urea
02

Targets

EPHX2 (Soluble epoxide hydrolase)

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