Drug intelligence / Profile preview

niacin extended-release + aspirin

Development stage
Phase 3
Lead developer
Abbott
Modality
Small Molecules
Administration
Oral
01

Overview

**Niacin extended-release + aspirin** is a combination regimen where *niacin extended-release* (nicotinic acid, formulated for slow release) is administered along with *aspirin* (acetylsalicylic acid) to treat dyslipidemia. The primary rationale for this combination is that niacin improves lipid profiles—lowering LDL cholesterol and triglycerides while raising HDL cholesterol—but is often poorly tolerated due to prostaglandin D2–mediated flushing as a side effect. Aspirin mitigates this side effect by inhibiting cyclooxygenase (COX), thereby reducing prostaglandin synthesis and the severity, duration, and incidence of flushing. This combination does not represent a proprietary co-formulated drug approved as a single product but refers to use of both agents together as part of a therapeutic strategy[1][3]. - **Mechanism of Action:** - Niacin is a lipid-modifying agent that inhibits hepatic diacylglycerol acyltransferase-2, reduces VLDL synthesis, decreases LDL, and increases HDL. It is also a potent agonist of the GPR109A receptor, leading to sequence of prostaglandin D2 release and flushing. - Aspirin is an irreversible cyclooxygenase inhibitor (primarily COX-1), blocking prostaglandin D2 formation, thereby reducing niacin-induced flushing without interfering with the lipid benefit[1][3].

Other names
niacin ER + aspirinniacin extended-release plus aspirinextended-release niacin + aspirin
02

Targets

PGHS-1 (Prostaglandin G/H Synthase 1)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)DGAT2 (Hepatic diacylglycerol acyltransferase 2)HCAR2 (Hydroxycarboxylic acid receptor 2)

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