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Niacin

drug
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Also known as Acide nicotiniqueAcido nicotinicoAcidum nicotinicumNiacin component of advicorNiacin component of simcorNiacin extended releaseNiacorNiaspanNiaspan titration starter packNicanginNicolarNicotinic acidNSC-169454Niacin tdNiaspan erNicotinateVitamin b3WampocapSID11112153

Summary

Niacin (CHEMBL573) is an approved small-molecule antilipemic drug (ATC C10AD02) targeting HCAR1, HCAR2, and HCAR3; indicated across 49 conditions including atherosclerosis and anemia.

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: C10AD02 (+2 more)
  • Targets: 3 (HCAR1, HCAR2, HCAR3)
  • Indications: 49 conditions
  • Clinical trials: 111
  • Chemistry: 123.11 Da · C6H5NO2

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL573
NameNiacin
TypeSmall molecule
Max phase4
FDA approvedyes
PubChem CID938
ChEBICHEBI:15940
ATCC10AD02, C04AC01, C10AD52
Molecular formulaC6H5NO2
Molecular weight123.11
InChIKeyPVNIIMVLHYAWGP-UHFFFAOYSA-N

SMILES: C1=CC(=CN=C1)C(=O)O

IUPAC name: pyridine-3-carboxylic acid

ChEBI definition: A pyridinemonocarboxylic acid that is pyridine in which the hydrogen at position 3 is replaced by a carboxy group.

Pharmacological roles (ChEBI): antidote, antilipemic drug, vasodilator agent, EC 3.5.1.19 (nicotinamidase) inhibitor.

Other ChEBI roles (chemical / environmental): metabolite, Escherichia coli metabolite, mouse metabolite, human urinary metabolite, plant metabolite.

Also known as: Acide nicotinique, Acido nicotinico, Acidum nicotinicum, Niacin, Niacin component of advicor, Niacin component of simcor, Niacin extended release, Niacor, Niaspan, Niaspan titration starter pack, Nicangin, Nicolar

Patent coverage: 136,913 distinct patent families (351,963 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 342,387 (97%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

GeneTargetActionpAffinityCancer dependencyUniProt
HCAR1HCA1 receptorAgonist0.6%Q9BXC0
HCAR2HCA2 receptorFull agonist7.20.1%Q8TDS4
HCAR3HCA3 receptorFull agonist6.520.2%P49019

Broader ChEMBL bioactivity targets: 7 (assay-derived). Sample: Amyloid-beta precursor protein, Lysosomal alpha-glucosidase, Aldehyde dehydrogenase 1A1, Hydroxycarboxylic acid receptor 2, Hydroxycarboxylic acid receptor 2, Hydroxycarboxylic acid receptor 3, Hydroxycarboxylic acid receptor 2.

Bioactivity

ChEMBL activities: 58 potent at pChembl ≥ 5 of 63 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
HCAR28.06EC508.71nMCHEMBL_ACT_1984829
HCAR27.84EC5014.5nMCHEMBL_ACT_19115145
HCAR27.75EC5017.6nMCHEMBL_ACT_19115144
HCAR27.68EC5020.75nMCHEMBL_ACT_18423055
HCAR27.68EC5020.7nMCHEMBL_ACT_18423069
HCAR27.57EC5026.92nMCHEMBL_ACT_2692235
HCAR27.57EC5027nMCHEMBL_ACT_3303420
Q9EP667.54EC5029nMCHEMBL_ACT_10903590
Q9EP667.54EC5029nMCHEMBL_ACT_5221928
Q80Z397.48Ki33nMCHEMBL_ACT_962745
Q80Z397.41EC5039nMCHEMBL_ACT_10903583
Q80Z397.41EC5039nMCHEMBL_ACT_5221925
HCAR27.33EC5047nMCHEMBL_ACT_15643548
HCAR27.3Ki50nMCHEMBL_ACT_2244469
HCAR27.29EC5051nMCHEMBL_ACT_10953654
HCAR27.09Ki82nMCHEMBL_ACT_3189346
HCAR27EC5099nMCHEMBL_ACT_10903569
HCAR27EC50100nMCHEMBL_ACT_5221917
HCAR27EC50100nMCHEMBL_ACT_8007969
HCAR26.98Ki104nMCHEMBL_ACT_3189347
HCAR26.92EC50120nMCHEMBL_ACT_1824989
HCAR26.92EC50120nMCHEMBL_ACT_2037630
HCAR26.89IC50130nMCHEMBL_ACT_2483000
HCAR26.85IC50140nMCHEMBL_ACT_2006151
Q9EP666.85IC50140nMCHEMBL_ACT_2006220
HCAR26.85IC50140nMCHEMBL_ACT_2063456
Q9EP666.85IC50140nMCHEMBL_ACT_2417047
HCAR26.85IC50140nMCHEMBL_ACT_2417073
HCAR26.85IC50140nMCHEMBL_ACT_2524923
HCAR26.85IC50140nMCHEMBL_ACT_2721749

Target pathways

Aggregated over 3 target gene(s): HCAR1, HCAR2, HCAR3.

Top Reactome pathways

3 total, by targets touching each:

PathwayTargetsGenes
Hydroxycarboxylic acid-binding receptors3HCAR1, HCAR2, HCAR3
G alpha (i) signalling events3HCAR1, HCAR2, HCAR3
Class A/1 (Rhodopsin-like receptors)1HCAR2

Dominant GO biological processes

GO termTargets
G protein-coupled receptor signaling pathway3
negative regulation of lipid catabolic process3
signal transduction3
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway2
neutrophil apoptotic process1
positive regulation of neutrophil apoptotic process1
positive regulation of adiponectin secretion1
apoptotic process1

Indications & clinical

Indications

49 indications (11 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

IndicationTrial phaseMONDOEFO
atherosclerosis4MONDO:0005311EFO:0003914
anemia4MONDO:0002280EFO:0004272
myocardial infarction4MONDO:0005068EFO:0000612
chronic kidney disease4MONDO:0005300EFO:0003884
iron deficiency anemia4MONDO:0001356HP:0001891
acne4MONDO:0011438EFO:0003894
coronary artery disorder4MONDO:0005010EFO:0001645
cardiovascular disorder4MONDO:0004995EFO:0000319
hyperlipidemia4MONDO:0021187MONDO:0021187
psychotic disorder3MONDO:0005485EFO:0005407
acute coronary syndrome3MONDO:0005542EFO:0005672
carotid artery disorder3MONDO:0005269EFO:0003781
intermittent vascular claudication3MONDO:0005295EFO:0003876
familial hypercholesterolemia3MONDO:0005439EFO:0004911
myocardial ischemia3MONDO:0024644EFO:1001375
cerebral atherosclerosis3MONDO:0006694EFO:1000860
stroke disorder3MONDO:0005098EFO:0000712
type 2 diabetes mellitus3MONDO:0005148MONDO:0005148
tuberculosis3MONDO:0018076MONDO:0018076
heart disorder3MONDO:0005267EFO:0003777
peripheral vascular disease3MONDO:0005294EFO:0003875
HIV infectious disease2MONDO:0005109EFO:0000764
metabolic syndrome X2MONDO:0011565EFO:0000195
obesity disorder2MONDO:0011122EFO:0001073
retinal vein occlusion2MONDO:0006951EFO:1001157
heart failure2MONDO:0005252EFO:0003144
major depressive disorder2MONDO:0002009MONDO:0002009
systolic heart failure2MONDO:0006993EFO:1001207
nicotine dependence2MONDO:0008575EFO:0003768
sickle cell disease2MONDO:0011382MONDO:0011382
neoplasm2MONDO:0005070MONDO:0004992
migraine disorder2MONDO:0005277MONDO:0005277
metabolic dysfunction-associated steatotic liver disease2MONDO:0013209EFO:0003095
depressive disorder2MONDO:0002050MONDO:0002050
obsessive-compulsive disorder1MONDO:0008114EFO:0004242
post-traumatic stress disorder1MONDO:0005146EFO:0001358
non-Hodgkin lymphoma1MONDO:0018908EFO:0005952
glioblastoma1MONDO:0018177EFO:0000519
anxiety1MONDO:0011918EFO:0005230
aortic valve stenosis0MONDO:0042981EFO:0000266

9 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 111.

Phase distribution

PhaseTrials
Not specified26
PHASE423
PHASE222
PHASE317
PHASE111
EARLY_PHASE16
PHASE2/PHASE34
PHASE1/PHASE22

Top trials by phase / activity

NCTPhaseStatusTitle
NCT00079638PHASE4COMPLETEDComparative Efficacy Evaluation of Lipids When Treated With Niaspan & Statin or Other Lipid-Modifying Therapies-COMPELL
NCT00203476PHASE4COMPLETEDA Prospective, Open Label Comparison of Ezetimibe, Niacin, and Colestipol as Adjunct Therapy in Lipid Reduction
NCT00238004PHASE4UNKNOWNThe Low HDL On Six Weeks Statin Therapy (LOW) Study
NCT00298909PHASE4COMPLETEDExercise Versus Niacin in Patients With Coronary Artery Disease (CAD) and Low High-Density Lipoproteins (HDL)
NCT00304993PHASE4COMPLETEDStudy of Niacin and Rosiglitazone in Dysmetabolic Dyslipidemia
NCT00307307PHASE4COMPLETEDCarotid Atherosclerosis Regression at Magnetic Resonance Assessment.
NCT00345657PHASE4COMPLETEDEfficacy Study of Extended-Release Niacin/Lovastatin Versus Usual Care
NCT00346970PHASE4COMPLETEDThe High Density Lipoprotein and Endothelial Function, Niacin and Nitric Oxide Study (The High-Ennd Study)
NCT00590629PHASE4COMPLETEDBenefit of Elevation of HDL-C on Cardiovascular Outcomes in Women
NCT00687076PHASE4COMPLETEDEffectiveness of Intensive Lipid Modification Medication in Preventing the Progression of Peripheral Arterial Disease (The ELIMIT Study)
NCT00712049PHASE4UNKNOWNEffects of Nicotinic Acid Plus Simvastatin Versus Simvastatin Alone on Carotid and Femoral Intima-Media Thickness in Patients With Peripheral Artery Disease (NASCIT)
NCT00715273PHASE4COMPLETEDEvaluate Carotid Artery Plaque Composition by Magnetic Resonance Imaging in People Receiving Cholesterol Medication
NCT00852969PHASE4COMPLETEDNiacin and Endothelial Function in Early CKD
NCT01054508PHASE4COMPLETEDEffect of Tredaptive on Serum Lipoproteins and Inflammatory Markers
NCT01126073PHASE4COMPLETEDNiacin/Laropiprant and Endothelial Function
NCT01239992PHASE4TERMINATEDEffect of Niacin/Laropiprant on Postprandial Lipoprotein Metabolism in Patients With Dyslipoproteinemia
NCT01321034PHASE4COMPLETEDEffect of Niacin in the Lipoprotein (a) Concentration
NCT01450410PHASE4TERMINATEDNicotinic Acid Composition of HDL and Arterial Endothelium Function in Premature Coronary Heart Disease and High HDL
NCT01683656PHASE4TERMINATEDER Niacin/Laropiprant Impact on Cardiovascular Markers and Atheroprogression in HIV-infected Individuals on cART
NCT01921010PHASE4COMPLETEDBenefit of Elevation of HDL-C in Women
NCT01942291PHASE4COMPLETEDShort-term Effect of Extended-release Niacin on Endothelial Function.
NCT02642159PHASE4COMPLETEDEfficacy and Safety of Alirocumab Versus Usual Care on Top of Maximally Tolerated Statin Therapy in Patients With Type 2 Diabetes and Mixed Dyslipidemia (ODYSSEY DM-Dyslipidemia)
NCT03163576PHASE4UNKNOWNThe Efficacy of Niacin on Hyperphosphatemia in Patients Undergoing Haemodialysis
NCT05398484PHASE2/PHASE3RECRUITINGPsilocybin Therapy in Advanced Cancer
NCT06406140PHASE2/PHASE3ENROLLING_BY_INVITATIONStudy the Effect of Niacin on Lipoprotein (a) Concentration and Hyperphosphatemia in Hemodialysis Patients
NCT00000482PHASE3COMPLETEDCoronary Drug Project
NCT00000512PHASE3COMPLETEDFamilial Atherosclerosis Treatment Study
NCT00000539PHASE3COMPLETEDArterial Disease Multifactorial Intervention Trial (ADMIT)
NCT00000553PHASE3COMPLETEDHDL-Atherosclerosis Treatment Study (HATS)
NCT00000599PHASE3COMPLETEDCholesterol-Lowering Atherosclerosis Study (CLAS)
NCT00062556PHASE3COMPLETEDEffect of Niacin ER/Lovastatin on Peak Walking Time & Claudication Onset Time in Patients With Intermittent Claudication
NCT00071266PHASE3COMPLETEDThe Dose Response of Niacin ER/Lovastatin on Peak Walking Time (PWT) in Patients With Intermittent Claudication - TROPIC
NCT00082251PHASE3COMPLETEDSafety & Efficacy of a Combination Niacin ER/Simvastatin in Patients With Dyslipidemia: A Dose-Ranging Study - SEACOAST
NCT00127218PHASE3COMPLETEDHigh-Density Lipoprotein (HDL) Cholesterol Increased Plaque Stabilization in the Elderly
NCT00170404PHASE3COMPLETEDTB Nutrition, Immunology and Epidemiology
NCT00378833PHASE3COMPLETEDTolerability of MK0524A Versus Niacin Extended-Release (0524A-054)
NCT00493064PHASE2/PHASE3COMPLETEDTo Study the Effectiveness and Safety of Niacin and a Topical Steroid Eye Drop to Treat Retinal Vein Occlusions
NCT00500045PHASE2/PHASE3TERMINATEDRetrospective Study of the Effectiveness and Safety of Niacin and Steroid Eye Drops for Retinal Vein Occlusions
NCT00536510PHASE3COMPLETEDEffect of MK0524A on Cholesterol Levels (0524A-048)
NCT01368328PHASE3UNKNOWNEffect of the Chromium Nicotinate on Type 2 Diabetes

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 0 clinical and 4 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

47 molecules share ≥1 primary target. Top 47 by shared-target count:

MoleculeSourceStatusShared targets
ACIFRANChEMBLPhase 2HCAR2, HCAR3
SCH-900271ChEMBLPhase 2HCAR2, HCAR3
ACIPIMOXChEMBLPhase 4 (approved)HCAR2
DIMETHYLChEMBLPhase 4 (approved)HCAR2
MONOMETHYLChEMBLPhase 4 (approved)HCAR2
5-FLUORONICOTINIC ACIDChEMBLPhase 3HCAR2
Aclidinium BromidePubChemApprovedHCAR2
AllopurinolPubChemApprovedHCAR2
AlprazolamPubChemApprovedHCAR2
AmitriptylinePubChemApprovedHCAR2
BeclomethasonePubChemApprovedHCAR2
Beclomethasone DipropionatePubChemApprovedHCAR2
BelzutifanPubChemApprovedHCAR2
CarisoprodolPubChemApprovedHCAR2
CelecoxibPubChemApprovedHCAR2
cephalexinPubChemApprovedHCAR2
CetirizinePubChemApprovedHCAR2
Cinnamic AcidPubChemApprovedHCAR2
CitalopramPubChemApprovedHCAR2
ClindamycinPubChemApprovedHCAR2
ClonazepamPubChemApprovedHCAR2
ClonidinePubChemApprovedHCAR2
DesloratadinePubChemApprovedHCAR2
DiazepamPubChemApprovedHCAR2
DiltiazemPubChemApprovedHCAR2
FamciclovirPubChemApprovedHCAR2
FenofibratePubChemApprovedHCAR2
FluconazolePubChemApprovedHCAR2
Fluticasone PropionatePubChemApprovedHCAR2
GemfibrozilPubChemApprovedHCAR2
GuaifenesinPubChemApprovedHCAR2
HydroxyzinePubChemApprovedHCAR2
Isosorbide MononitratePubChemApprovedHCAR2
lactic acid, l-PubChemApprovedHCAR1
LamotriginePubChemApprovedHCAR2
LorazepamPubChemApprovedHCAR2
MeclizinePubChemApprovedHCAR2
MetforminPubChemApprovedHCAR2
MetoclopramidePubChemApprovedHCAR2
NifedipinePubChemApprovedHCAR2
oxybatePubChemApprovedHCAR1
PantoprazolePubChemApprovedHCAR2
PimozidePubChemApprovedHCAR2
PropoxyphenePubChemApprovedHCAR2
ValacyclovirPubChemApprovedHCAR2
VerapamilPubChemApprovedHCAR2
ZidovudinePubChemApprovedHCAR2

About this page

Generated deterministically by Sugi Atlas from primary biomedical databases via BioBTree. Every record on this page traces to a primary source.

Generated
Atlas version
v1.1.2
BioBTree
v2.0.2

Sources 30

This page pulls from 30 datasets indexed by BioBTree:

chebichembl_activitychembl_moleculechembl_targetcivic_evidenceclingen_dosageclinical_trialsdepmapefoensemblentrezgogoparentgtopdbgtopdb_interactiongtopdb_ligandhgncmeshmondomsigdbpatent_compoundpharmgkbpharmgkb_guidelinepubchempubchem_activityreactomereactomeparentrefseqtranscriptuniprot