Investigational Drug Details
| Drug ID: | D239 |
| Drug Name: | Niacin |
| Synonyms: | 3-carboxypyridine; 3-Pyridinecarboxylic acid; 3-Pyridylcarboxylic acid; anti-pellagra vitamin; m-pyridinecarboxylic acid; Niacin; Nicotinic acid; pyridine-β-carboxylic acid; β-pyridinecarboxylic acid |
| Type: | Supplement |
| DrugBank ID: | DB00627 |
| DrugBank Description: | Niacin is a B vitamin used to treat vitamin deficiencies as well as hyperlipidemia, dyslipidemia, hypertriglyceridemia, and to reduce the risk of myocardial infarctions. |
| PubChem ID: | 938 |
| CasNo: | 59-67-6 |
| Repositioning for NAFLD: | Yes |
| SMILES: | C(=O)(O)c1cccnc1 |
| Structure: |
|
| InChiKey: | PVNIIMVLHYAWGP-UHFFFAOYSA-N |
| Molecular Weight: | 123.111 |
| DrugBank Targets: | Hydroxycarboxylic acid receptor 3 agonist; Hydroxycarboxylic acid receptor 2 agonist; Nicotinate-nucleotide pyrophosphorylase [carboxylating] binder; Nicotinamide N-methyltransferase binder |
| DrugBank MoA: | Niacin performs a number of functions in the body and so has many mechanisms, not all of which have been fully described. Niacin can decrease lipids and apolipoprotein B (apo B)-containing lipoproteins by modulating triglyceride synthesis in the liver, which degrades apo B, or by modulating lipolysis in adipose tissue. Niacin inhibits hepatocyte diacylglycerol acyltransferase-2. This action prevents the final step of triglyceride synthesis in hepatocytes, limiting available triglycerides for very low density lipoproteins (VLDL). This activity also leads to intracellular degradation of apo B and decreased production of low density lipoproteins, the catabolic product of VLDL. Niacin also inhibits a high density lipoprotein (HDL) catabolism receptor, which increases the levels and half life of HDL. |
| DrugBank Pharmacology: | Niacin is a B vitamin used to treat vitamin deficiencies as well as hyperlipidemia, dyslipidemia, hypertriglyceridemia, and to reduce the risk of myocardial infarctions. Niacin acts to decrease levels of very low density lipoproteins and low density lipoproteins, while increasing levels of high density lipoproteins. Niacin has a wide therapeutic window with usual oral doses between 500mg and 2000mg. Patients with diabetes, renal failure, uncontrolled hypothyroidism, and elderly patients taking niacin with simvastatin or lovastatin are at increased risk of myopathy and rhabdomyolysis. |
| DrugBank Indication: | Niacin is indicated to prevent vitamin deficiencies in pediatric and adult patients receiving parenteral nutrition as part of multivitamin intravenous injections. Niacin oral tablets are indicated as a monotherapy or in combination with simvastatin or lovastatin to treat primary hyperlipidemia and mixed dyslipidemia. It can also be used to reduce the risk of nonfatal myocardial infarctions in patients with a history of myocardial infarction and hyperlipidemia. Niacin is also indicated with bile acid binding resins to treat atherosclerosis in patients with coronary artery disease and hyperlipidemia or to treat primary hyperlipidemia. Finally niacin is indicated to treat severe hypertriglyceridemia. |
| Targets: | NNMT binder |
| Therapeutic Category: | Hypolipidemic drug |
| Clinical Trial Progress: | Phase 2 completed (NCT03850886: Nicotinamide at a dose of 1000 mg daily was tolerable, improved metabolic abnormalities and QOL of diabetic NAFLD patients with no effect on liver fibrosis or steatosis.) |
| Latest Progress: | Under clinical trials |
| Trial ID | Source ID | Phases | Status | Study Results | Start Date | Last Update Posted | |
|---|---|---|---|---|---|---|---|
| L0013 | NCT00262964 | Not applicable | Completed | Has Results | October 2004 | July 11, 2018 | Details |
| L0770 | NCT03850886 | Phase 2 | Not recruiting | No Results Available | 30/01/2019 | 12 December 2020 | Details |
| Target ID | Target Name | GENE | Action | Class | UniProtKB ID | Entry Name |
|---|
| Strategy ID | Strategy | Synonyms | Related Targets | Related Drugs | |
|---|---|---|---|---|---|
| S03 | Anti-fibrosis | fibrosis | Angiotensin Receptor Blocker (ARB); CCR2/CCR5 antagonist; Thyroid receptor β agonist; PEGylated human FGF21 analogue; Monoclonal antibody to lysyl oxidase-like 2 (LOXL2); Galectin-3 inhibitor; FGF19 variant | Losartan; Cenicriviroc; VK-2809; MGL-3196; Pegbelfermin; Simtuzumab; GR-MD-02; NGM282 | Details |
| Article ID | PMID | Source | Title | |
|---|---|---|---|---|
| A01100 | 34869532 | Front Nutr | Clinical Relevance of Vitamins and Carotenoids With Liver Steatosis and Fibrosis Detected by Transient Elastography in Adults. | Details |
| A03768 | 33870623 | Mol Nutr Food Res | Nicotinamide Protects Against Diet-Induced Body Weight Gain, Increases Energy Expenditure, and Induces White Adipose Tissue Beiging. | Details |
| A05022 | 33408299 | J Toxicol Sci | Reduction of fatty liver in rats by nicotinamide via the regeneration of the methionine cycle and the inhibition of aldehyde oxidase. | Details |
| A06028 | 33035588 | Life Sci | Nicotinamide and ascorbic acid nanoparticles against the hepatic insult induced in rats by high fat high fructose diet: A comparative study. | Details |
| A07521 | 32460191 | Biomed Pharmacother | Sodium acetate-mediated inhibition of histone deacetylase alleviates hepatic lipid dysregulation and its accompanied injury in streptozotocin-nicotinamide-induced diabetic rats. | Details |
| A07664 | 32404278 | Biochim Biophys Acta Mol Cell Biol Lipids | Niacin increases diet-induced hepatic steatosis in B6129 mice. | Details |
| A07840 | 32337855 | Mol Syst Biol | The acute effect of metabolic cofactor supplementation: a potential therapeutic strategy against non-alcoholic fatty liver disease. | Details |
| A08277 | 32171275 | BMC Pediatr | Analysis of the dietary factors associated with suspected pediatric nonalcoholic fatty liver disease and potential liver fibrosis: Korean National Health and Nutrition Examination Survey 2014-2017. | Details |
| A09148 | 31858105 | J Nutr | Niacin Ameliorates Hepatic Steatosis by Inhibiting De Novo Lipogenesis Via a GPR109A-Mediated PKC-ERK1/2-AMPK Signaling Pathway in C57BL/6 Mice Fed a High-Fat Diet. | Details |
| A09528 | 31706905 | J Clin Lipidol | Niacin for treatment of nonalcoholic fatty liver disease (NAFLD): novel use for an old drug? | Details |
| A09681 | 31650383 | Mol Biol Rep | High fructose-containing drinking water-induced steatohepatitis in rats is prevented by the nicotinamide-mediated modulation of redox homeostasis and NADPH-producing enzymes. | Details |
| A10090 | 31491949 | Int J Mol Sci | Combined Treatment with L-Carnitine and Nicotinamide Riboside Improves Hepatic Metabolism and Attenuates Obesity and Liver Steatosis. | Details |
| A10462 | 31326093 | Am J Med Sci | Association Between Index of Nutritional Quality and Nonalcoholic Fatty Liver Disease: The Role of Vitamin D and B Group. | Details |
| A10785 | 31195117 | Biochim Biophys Acta Mol Basis Dis | Nicotinamide riboside, an NAD+ precursor, attenuates the development of liver fibrosis in a diet-induced mouse model of liver fibrosis. | Details |
| A11828 | 30718741 | Sci Rep | Dietary Niacin Intake Predicts the Decrease of Liver Fat Content During a Lifestyle Intervention. | Details |
| A12460 | 30446221 | Biochem Biophys Res Commun | Alleviation of fatty liver in a rat model by enhancing N1-methylnicotinamide bioavailability through aldehyde oxidase inhibition. | Details |
| A14423 | 29413998 | Curr Opin Pharmacol | Lipid-lowering treatment in peripheral artery disease. | Details |
| A15157 | 29069580 | Eur J Pharmacol | Nicotinamide prevents sweet beverage-induced hepatic steatosis in rats by regulating the G6PD, NADPH/NADP+ and GSH/GSSG ratios and reducing oxidative and inflammatory stress. | Details |
| A15289 | 28985579 | Eur J Cancer | Metformin and insulin impact on clinical outcome in patients with advanced hepatocellular carcinoma receiving sorafenib: Validation study and biological rationale. | Details |
| A16274 | 28473059 | Nutr Res | Nicotinamide protects hepatocytes against palmitate-induced lipotoxicity via SIRT1-dependent autophagy induction. | Details |