Drug Database
NI

nicotinic acid (nicotinic acid ER / Niaspanor / Niaspan)

✓ Approved

Merck KGaA · HCAR2 · Small Molecule

What is nicotinic acid?

nicotinic acid is a small molecule developed by Merck KGaA. It is approved for therapeutic indications via oral (po).

Drug Profile

Brand Namesnicotinic acid ER, Niaspanor, Niaspan
CompanyMerck KGaA
Drug ClassSmall Molecule
Molecular TargetHCAR2
RouteOral (PO)
StatusApproved
Sources: ClinicalTrials.gov, Merck KGaA

Mechanism of Action

Molecular Targets

nicotinic acid acts on 1 molecular target:

HCAR2hydroxycarboxylic acid receptor 2 (NIACR1, GPR109A)
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Therapeutic Indications

nicotinic acid is developed for 8 unique indications across 4 therapeutic areas.

Therapeutic AreaConditionPhase
Vascular disordersArteriosclerosis✓ Approved
Metabolism and nutrition disordersHypercholesterolaemia✓ Approved
Metabolism and nutrition disordersHypertriglyceridaemia✓ Approved
Cardiac disordersMyocardial infarction✓ Approved
Metabolism and nutrition disordersDyslipidaemia✓ Approved

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Related Research Articles

PubMedBMC microbiology2026-11-11

Gut microbiome and metabolite profiling in term SGA infants: a multi-omics approach to physical development.

Li Shushu S, Yu Ziwei Z, Jin Yanyu Y, Ma Ke K et al.

Early-life gut microbial composition and fecal metabolic profiles may be altered in infants born small for gestational age (SGA), but evidence specifically concerning term SGA infants remains limited. To characterize gut microbial composition, predicted microbial functions, and fecal metabolite profiles in term SGA infants and explore their associations with early growth. This prospective nested case-control study included 62 term infants (31 SGA and 31 appropriate for gestational age [AGA]). Fecal samples were collected at 3 months. Untargeted metabolomics was performed in the full cohort, and shotgun metagenomic sequencing was conducted in a nested subset of 20 infants (10 SGA and 10 AGA). Differential taxa, KEGG orthologs (KOs), metabolites, and cross-omics correlations were analyzed. Alpha diversity did not differ significantly between groups, whereas microbial composition and species-level abundance patterns differed between SGA and AGA infants. Functional analysis identified 135 differential KOs, including 36 with higher and 99 with lower abundance in the SGA group. These KOs were mapped to 25 metabolic pathways, including galactose, butanoate, D-amino acid, aromatic amino acid, fructose-mannose, pyruvate, propanoate, and lipid metabolism. Twelve fecal metabolite features differed between groups, including 5'-methylthioadenosine, taurocholate, β-alanine, and 17α-hydroxypregnanolone. Exploratory integration identified connections among microbial species, KOs, and metabolites. Several microbial and metabolite features showed nominal associations with 6-month growth indices, but most cross-omics and metabolite-growth associations did not remain significant after false discovery rate correction. Term SGA infants showed differences in gut microbial composition, predicted metabolic potential, and fecal metabolite profiles at 3 months. Associations with subsequent growth were exploratory and require validation in larger longitudinal studies.

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PubMedAnalytical chemistry2026-11-11

Nanopore Identification of Nicotine in Cigarette Tobacco and Its Smoke.

Wang Yifan Y, Dai Xinyi X, Zhao Lulu L, Qian Lu L et al.

Smoking poses a severe threat to global public health. Nicotine, as the predominant addictive constituent existing in both tobacco matrices and inhaled smoke, requires direct and reliable detection for health risk evaluation and tobacco quality control. In this work, we developed a single-molecule nicotine detection system using a nickel-functionalized Mycobacterium smegmatis porin A (MspA) nanopore. Structural analogues of nicotine, including cotinine, nicotinic acid, anatabine, and nornicotine, are also detectable with the same sensing system and can be readily distinguished from nicotine. With the assistance of machine learning, a cross-validation accuracy of 90.85% was achieved for the five analytes. Leveraging the metal coordination chemistry and machine learning algorithm, this system achieves specific identification of nicotine within complex matrices. With a calibrated standard curve, this method enables quantitative analysis of nicotine in tobacco samples. When combined with a smoke collection device, the system successfully detected nicotine in real cigarette smoke, demonstrating great potential for environmental smoke exposure evaluation and on-site field screening.

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PubMedFrontiers in chemistry2026-11-11

Mass spectrometry-based affinity capture of peptide ligands from complex venom mixtures.

Freuville Lou L, Fourmy Rudy R, Violette Aude A, Brans Alain A et al.

Animal venoms constitute a rich source of bioactive peptides targeting membrane receptors, including G protein-coupled receptors (GPCRs) and ligand-gated ion channels. However, identifying receptor-binding ligands directly from complex venom mixtures remains analytically challenging because venoms are highly diverse and conventional screening approaches have limited throughput. Here, we present a membrane-based affinity-capture workflow coupled to mass spectrometry to recover known receptor ligands and prioritize additional venom toxins for validation. The methodology combines native membrane preparations, label-free affinity capture, MALDI-TOF mass spectrometry, and LC-MS/MS-based proteomic identification within a single analytical workflow. Its performance was demonstrated using two pharmacologically distinct membrane receptor families: the human vasopressin type 2 receptor, a G protein-coupled receptor, and the muscle-type nicotinic acetylcholine receptor, a ligand-gated ion channel. The workflow recovered known ligands spanning endogenous peptides and disulfide-rich venom toxins and documented AVP-dependent changes in toxin recovery. Direct comparison of bound fractions obtained with nAChR-rich Torpedo membranes and control CHO membranes further identified toxins preferentially retained by each membrane preparation. By combining receptor-guided affinity selection with direct molecular identification, this strategy provides a versatile analytical platform for investigating ligand-receptor interactions and prioritizing bioactive peptides from highly complex natural mixtures. Beyond venom research, the approach is readily adaptable to other membrane receptors and molecular libraries for ligand discovery. Proteomic data are available via ProteomeXchange with identifier PXD084762.

PMID 43011242
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PubMedHistology and histopathology2026-11-11

Glycyrrhetinic acid alleviates LPS-induced acute lung injury and is associated with modulation of Keap1-Nrf2 signaling and ferroptosis.

Zheng Xiaona X, Zhao Liang L, Ye Ming M, Guo Qingwei Q et al.

Glycyrrhetinic acid, a substance extracted from licorice, has several pharmacological activities, such as anti-inflammatory and antioxidant effects and antiviral properties. Acute lung injury (ALI) represents a significant contributor to morbidity and mortality associated with respiratory disorders, marked by the presence of lung edema, interstitial neutrophilic infiltration, and dysfunction of intravascular and endothelial barriers, ultimately leading to respiratory failure. The present study aimed to investigate the effects of glycyrrhetinic acid on LPS-induced ALI. Glycyrrhetinic acid pretreatment significantly attenuated LPS-induced pulmonary edema, inflammatory cell infiltration, and alveolar wall thickening, while reducing proinflammatory cytokines (TNF-α, IL-1β) in BALF and serum. The transcriptomics analysis predicted that the ferroptosis pathways might be involved in the underlying mechanism of glycyrrhetinic acid against ALI, with validation experiments demonstrating glycyrrhetinic acid-mediated restoration of ferroptosis markers. Mechanistically, glycyrrhetinic acid suppressed Keap1 expression and activated Nrf2, enhancing antioxidant responses and inhibiting lipid peroxidation. These findings suggest that glycyrrhetinic acid may modulate inflammation and ferroptosis, with Keap1-Nrf2 signaling potentially contributing to its protective effects. The study suggests that targeting ferroptosis may represent a potential strategy for ALI management, with glycyrrhetinic acid emerging as a promising pharmacological candidate.

PMID 43012100
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PubMedJournal of agricultural and food chemistry2026-11-11

Organ-Specific Regulation of Folic Acid Bioavailability by Bioactive Small Molecules from Whole Wheat Steamed Buns.

Qi Yan Y, Zheng Renrui R, Huang Zhuohang Z, Yin Jiahong J et al.

The in vivo conversion of folic acid (FA) to its bioactive form is inefficient, and unmetabolized FA poses health concerns. This study investigates the regulatory mechanisms of active small molecules derived from whole wheat on FA intestinal absorption, liver metabolism, and brain accumulation. UPLC-Q-TOF-MS/MS was used to identify active constituents, combined with network pharmacology and molecular docking for target prediction, and a 48 day mouse study with multitissue quantification of FA and 5-methyltetrahydrofolate (5-MTHF). Network pharmacology revealed enrichment in endocytosis, organic acid transport, and blood-brain barrier pathways; molecular docking showed differential affinities for proton-coupled folic acid transporter, reduced folic acid carrier, folic acid receptor alpha, DHFR, and MTHFR. Animal studies confirmed that quercetin promoted intestinal absorption; D-calcium pantothenate enhanced liver 5-MTHF conversion; ferulic acid elevated circulating FA; and δ-tocopherol mediated brain-targeted accumulation of total folate (predominantly FA). These findings demonstrate that whole wheat-derived small molecules exert node-specific regulatory effects on folate metabolism, offering insights for developing FA-fortified foods.

PMID 43012697
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PubMedMaterials horizons2026-11-11

Thermoresponsive control of catalyst accessibility enables inverse temperature dependence of aminofluoroazobenzene thermal back reaction.

Nagano Mizuki M, Nagai Yuki Y, Kobayashi Yoichi Y

Controlling the thermal back reaction dynamics in photochromic reactions is important for designing photofunctional materials. The thermal back reactions are generally promoted at higher temperatures, but overcoming such typical temperature dependence leads to the development of unprecedented smart materials. Herein, we report the widely tunable acid-catalyzed thermal back reactions of p-amino-o-fluoroazobenzenes (AFABs) and a strategy to realize lower-temperature-favored thermal back reactions based on the acid responsiveness. AFABs exhibit tunable cis half-lives, ranging from days to seconds in the presence of acid catalysts, and their acid susceptibility can be modulated by the degree of fluorination. As the solvent for an AFAB, a glycol ether/water mixture, which exhibits lower critical solution temperature (LCST)-type phase separation, is used, allowing thermoresponsive control of a hydrophilic acid catalyst and thereby the lower-temperature-favored thermal back reaction. Our strategy could be applied to other acid-catalyzed photochromic compounds, contributing to the generation of cooling-responsive photofunctional materials.

PMID 43012404
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