Drug intelligence / Profile preview

D14000137

Development stage
Unknown
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Oral
01

Overview

D14000137 is an investigational, orally administered omega-3-carboxylic acid prototype formulation developed by AstraZeneca. It consists of free fatty acids, primarily eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA) derived from fish oil, formulated as a coated capsule. D14000137 was designed to improve the bioavailability of omega-3 fatty acids under both fasted and fed conditions. It acts as an agonist of peroxisome proliferator-activated receptors alpha (PPARα) and gamma (PPARγ), and inhibits diacylglycerol O-acyltransferases (DGAT1 and DGAT2), thereby reducing hepatic triglyceride synthesis and secretion while enhancing fatty acid oxidation. D14000137 was evaluated in a Phase 1 crossover clinical trial (NCT02359045) comparing its bioavailability to other prototype formulations (D1400147 and D14000136) and the reference drug Epanova in healthy subjects for the potential treatment of severe hypertriglyceridemia.

02

Targets

DGAT1 (Diacylglycerol O-acyltransferase 1)DGAT2 (Hepatic diacylglycerol acyltransferase 2)PPARA (Peroxisome proliferator-activated receptor alpha)PPARG (Peroxisome proliferator-activated receptor gamma)

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