Target intelligence / Profile preview

Nicotinic acid (Niacin)

Target
Niacin
Molecular classification
Small molecule (vitamin), Other (nutrient; drug; not a receptor/enzyme/target protein)
01

Overview

Nicotinic acid (niacin) is a water-soluble B vitamin (vitamin B3), essential for synthesis of the coenzymes NAD and NADP, which play critical roles in cellular energy metabolism, redox reactions, and DNA repair. Deficiency results in pellagra, while pharmacological doses are used mainly for their lipid-modifying effects, reducing LDL and triglycerides and elevating HDL cholesterol. Niacin itself is not a classical target (such as a receptor or enzyme) but is a nutrient and a therapeutic agent. It is rapidly absorbed and converted to active coenzyme forms, and can cause side effects such as flushing and hepatotoxicity at high doses[1][2][3][5][6].\n\nNote: \nIf you are seeking information on a *receptor* or *protein target* for niacin, the canonical form is *Hydroxycarboxylic acid receptor 2 (GPR109A)*, also called the \"niacin receptor\"[3]. Niacin as listed is the active molecule/drug, not the target.

Other names
Vitamin B3Nicotinic acidNiacinamide (different related form)Pyridine-3-carboxylic acidAntipellagra vitaminVitamin PP3-Picolinic acidNicotine acidNiacNicotinamideVB3
02

Mechanism of action

As a lipid therapy: Niacin inhibits hepatic diacylglycerol acyltransferase 2, lowering VLDL, LDL, and increasing HDL via direct and indirect action on hepatic metabolism\nAs a vitamin: Used in cellular metabolism, main mechanism is acting as NAD/NADP precursor to support redox reactions\nMay also activate GPR109A (niacin receptor), mediating therapeutic and side effects

03

Biological functions

Precursor for synthesis of coenzymes NAD and NADPParticipates in oxidation-reduction reactions (energy metabolism)Regulates lipid metabolism (reduces LDL/triglycerides; increases HDL cholesterol)AntioxidantModulates DNA repair
04

Disease associations

Deficiency causes pellagra (dermatitis, diarrhea, dementia, death)Used therapeutically for dyslipidemia, hyperlipidemia, hypertriglyceridemia, cardiovascular disease risk reductionResearch interest in cancer, Crohn's disease, and other inflammatory conditions
05

Safety considerations

Skin flushing (common and dose-dependent)Hepatotoxicity at high doses (monitor liver function)Hyperglycemia; worsen insulin resistanceGastrointestinal disturbancesIncrease in uric acid; gout riskPossible muscle toxicity, especially when combined with statins
06

Interacting drugs

Niacin (brand: Niaspan, Niacor, Advicor, Simcor)

2 more in the full profile.

07

Biomarkers

NAD/NADP levelsUrinary N1-methylnicotinamide and oxidized metabolites (N1-methyl-2-pyridone-5-carboxamide), used to monitor niacin deficiencyLDL, HDL, triglyceride levels (clinical endpoints for cardiovascular risk)Skin flushing reaction (clinical sign of niacin intake)

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