Drug intelligence / Profile preview

ARI-3037MO

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

Overview

ARI-3037MO is a novel, orally active structural analog of niacin (nicotinic acid) developed for the treatment of dyslipidemia and related cardiovascular diseases. It acts as an agonist at hydroxycarboxylic acid receptor 3 (HCAR3) and nicotinic acid receptor (HCAR2), as well as an inhibitor of diacylglycerol O-acyltransferase 2 (DGAT2). In preclinical and early clinical studies, ARI-3037MO demonstrated significant lipid-modifying effects, including reductions in total cholesterol, LDL-cholesterol, triglycerides, and free fatty acids. It also increased HDL-cholesterol fractions—potentially through upregulation of liver Apo-A1 and ATP-binding cassette transporter A1 (ABCA1)—and was more effective than niacin at reducing pro-atherogenic lipoproteins in animal models. Clinical trials have shown that ARI-3037MO is well tolerated without typical niacin-associated side effects such as flushing or adverse skin reactions. The drug is being evaluated primarily for severe hypertriglyceridemia and dyslipidemia[1][5][7].

02

Targets

HCAR3 (Hydroxycarboxylic acid receptor 3)DGAT2 (Hepatic diacylglycerol acyltransferase 2)HCAR2 (Hydroxycarboxylic acid receptor 2)

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