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Nicotinic acid (niacin)
Nicotinic acid activates GPR109A receptors on immune cells and adipocytes to reduce lipolysis, decrease free fatty acid release, and lower triglycerides and LDL cholesterol while raising HDL cholesterol.
Nicotinic acid activates GPR109A receptors on immune cells and adipocytes to reduce lipolysis, decrease free fatty acid release, and lower triglycerides and LDL cholesterol while raising HDL cholesterol. Used for Dyslipidemia and hypercholesterolemia, Hypertriglyceridemia, Pellagra (niacin deficiency).
At a glance
| Generic name | Nicotinic acid (niacin) |
|---|---|
| Also known as | Niaspan |
| Sponsor | Charite University, Berlin, Germany |
| Drug class | Lipid-modifying agent; B vitamin |
| Target | GPR109A (HM74A receptor) |
| Modality | Small molecule |
| Therapeutic area | Cardiovascular |
| Phase | FDA-approved |
Mechanism of action
Nicotinic acid (niacin) is a B vitamin that acts as a ligand for the G-protein coupled receptor GPR109A, primarily on adipocytes and immune cells. This activation suppresses hormone-sensitive lipase, reducing the breakdown of triglycerides and the release of free fatty acids into circulation. The net effect is decreased hepatic VLDL production, lowered triglycerides and LDL cholesterol, and increased HDL cholesterol levels.
Approved indications
- Dyslipidemia and hypercholesterolemia
- Hypertriglyceridemia
- Niacin deficiency (pellagra)
Common side effects
- Flushing and skin reactions
- Pruritus
- Gastrointestinal upset (nausea, dyspepsia)
- Hyperglycemia
- Hepatotoxicity
- Gout exacerbation
Key clinical trials
- Riluzole and Sorafenib Tosylate in Treating Patients With Advanced Solid Tumors or Melanoma (PHASE1)
- Effect of Nicotinamide Riboside on Ketosis, Fat Oxidation & Metabolic Rate (NA)
- Bortezomib, Sorafenib Tosylate, and Decitabine in Treating Patients With Acute Myeloid Leukemia (PHASE1)
- Effects of Nicotinamide Riboside on Bioenergetics and Oxidative Stress in Mild Cognitive Impairment/Alzheimer's Dementia (EARLY_PHASE1)
- Sorafenib and Cyclophosphamide/Topotecan in Patients With Relapsed and Refractory Neuroblastoma (PHASE1)
- Nicotinamide Riboside Oral Supplementation in Macula Off Retinal Detachment (PHASE4)
- MRD-guided Maintenance Post-HCT: Gilteritini vs Sorafenib (PHASE3)
- Study of Durvalumab and Tremelimumab as First-line Treatment in Patients With Advanced Hepatocellular Carcinoma (PHASE3)
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Nicotinic acid (niacin) CI brief — competitive landscape report
- Nicotinic acid (niacin) updates RSS · CI watch RSS
- Charite University, Berlin, Germany portfolio CI