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

PubMedJournal of nutritional science and vitaminology2026-08-30

Orally Administered Vitamin D Ameliorates Cognitive Decline in Early Stage of Vitamin D Deficiency.

Furukawa Taichi T, Ogiwara Maiko M, Ohinata Kousaku K

Vitamin D (VD) deficiency has been associated with cognitive impairment; however, the mechanisms underlying this relationship remain unclear. In this study, we examined the impact of dietary VD deficiency on cognitive function and explored the potential involvement of gastrointestinal signaling pathways independently of changes in circulating VD levels. Mice fed a VD-deficient (VD-Def) diet exhibited impaired cognitive performance in behavioral tests, including the novel object recognition test and the object location test, despite unchanged circulating 25-hydroxyvitamin D [25(OH)D] levels. Notably, this cognitive impairment was ameliorated by oral, but not intraperitoneal, administration of VD, indicating a route-dependent effect. Furthermore, the cognitive improvement induced by oral VD was abolished by oral administration of methyllycaconitine, an α7 nicotinic acetylcholine receptor (α7nAChR) antagonist, whereas intraperitoneal administration had no effect. These findings suggest that α7nAChRs via the gastrointestinal tract are required for the cognitive benefits of orally administered VD. Collectively, our results demonstrate that VD deficiency can impair cognitive function independently of systemic VD depletion and metabolic changes, and highlight a previously unrecognized role of gastrointestinal cholinergic signaling in mediating the cognitive effects of VD.

PMID 42669525
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PubMedThe journal of allergy and clinical immunology. Global2026-08-30

ALOX15-driven ω-6 fatty acid metabolism promotes type 2 inflammation in eosinophilic chronic rhinosinusitis with nasal polyps.

Sakashita Masafumi M, Kidoguchi Masanori M, Imoto Yoshimasa Y, Sato Yohei Y et al.

Local lipid metabolism contributes to immune homeostasis in the nasal mucosa and the pathogenesis of chronic rhinosinusitis. However, lipid mediator networks underlying eosinophilic chronic rhinosinusitis (ECRS) remain poorly defined. To characterize fatty acid-derived lipid mediator profiles in nasal polyps (NPs) from patients with and without ECRS and identify pathways associated with eosinophilic inflammation. Lipidomic profiling was performed using LC-MS/MS on NP tissues from patients with ECRS (n = 4) and without ECRS (n = 4). A total of 158 ω-6 and ω-3 fatty acid-derived lipid mediators were quantified. Arachidonate 15-lipoxygenase (ALOX15) pathway activity was evaluated by quantitative PCR and ELISA. ECRS NPs displayed a distinct lipidomic signature compared with non-ECRS NPs. ECRS NPs exhibited increased levels of proinflammatory ω-6 fatty acid metabolites, including 15-hydroxyeicosatetraenoic acid (15-HETE) and 13-hydroxyoctadecadienoic acid, along with elevated ALOX15 pathway products and higher ALOX15 mRNA expression. Anti-inflammatory specialized proresolving mediators, such as lipoxin A4, were also elevated within the ω-6 pathway, and lipoxin A4 levels correlated with 15-HETE levels. These patterns indicate the concurrent activation of pro- and anti-inflammatory pathways, with a predominance of ALOX15-driven ω-6 metabolites in ECRS. In contrast, the ω-3 fatty acid pathway showed only modest increases in 14,15-DiHETE and resolvin D2, suggesting a limited compensatory resolution response compared with the robust ALOX15-dependent ω-6 activity. ECRS NPs exhibit a skewed lipid mediator profile characterized by enhanced ALOX15-dependent ω-6 metabolism and insufficient resolution activity. This imbalance may underlie persistent type 2 inflammation in ECRS and suggests that targeting the 15-lipoxygenase pathway may offer therapeutic benefits.

PMID 42668469
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PubMedFood chemistry: X2026-08-30

Effect of solid-state fermentation on the release and antioxidant activity of soluble polyphenols from wheat bran.

Tian Xiaomin X, Guo Yuqiu Y, Sun Linlin L, Chen Lirong L et al.

Using wheat bran as substrate, four solid-state fermentation methods were compared for soluble polyphenol release. The effect of Bio-enzymatic synergy (BES) is the most significant, producing 4.85 mg GAE/g of total phenolic substances, which is 45.77% higher than the control group (CK). LC-MS analysis revealed that ferulamide and 2,4,6-trihydroxybenzoic acid predominated in positive ion mode, while salicylic acid dominated in negative mode. Notably, salicylic acid was found almost exclusively in ester-bound and glycoside-bound fractions (>88%), indicating its release requires cleavage of covalent linkages to cell wall components. The release of salicylic acid results from the synergistic action of Bio-enzymatic synergy and alkaline hydrolysis. Both in vitro and in vivo assays confirmed that BES-released polyphenols enhanced antioxidant activity, reducing ROS and MDA levels while increasing GSH-Px activity and extending C. elegans lifespan. These findings provide a mechanistic basis for developing targeted fermentation-enzymatic processes to produce functional wheat bran extracts.

PMID 42668496
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PubMedFood chemistry: X2026-08-30

Comprehensive analysis of the effects of foliar application of the synthetic strigolactone analog GR24 during the growth period on postharvest quality and metabolic indicators of pak choi.

Ma Yufeng Y, Cai Qitong Q, Wang Cheng C, Liu Yang Y et al.

Strigolactones (SLs) regulate plant growth and metabolism, but their concentration-dependent effects on leafy vegetable quality remain unclear. We investigated how the synthetic SL analog GR24 affects physiological and metabolic processes in pak choi (Brassica rapa subsp. chinensis). Mantel correlation analysis and partial least squares structural equation modeling (PLS-SEM) revealed distinct response patterns. The 1 μmol·L-1 treatment (T2) enhanced photosynthesis, carbon‑nitrogen assimilation, mineral accumulation, and GA3, ZT, ABA, and JA levels, whereas the 10 μmol·L-1 treatment (T3) promoted carotenoid and phenolic accumulation, including rutin, ferulic acid, and caffeic acid. Multivariate analysis linked phenolic acid accumulation mainly to nitrogen and amino acid metabolism, with additional associations with P status. Overall, T2 broadly enhanced primary metabolism and nutrition, whereas T3 favored secondary and antioxidant-related metabolism, providing a framework for optimizing GR24 application in high-quality leafy vegetable production.

PMID 42668560
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PubMedInternational journal of pharmaceutics: X2026-08-30

Optimizing nucleic acid delivery using PF14 peptide and lipid nanoparticle systems.

Daniele Delia D, Hein Zaw Myo ZM, Saher Osama O, El-Serafi Ibrahim I

Nucleic acid-based therapeutics are a rapidly expanding class of precision medicines capable of directly modulating gene expression. However, their clinical application is limited by challenges in cellular delivery, including large molecular size, hydrophilicity, and susceptibility to enzymatic degradation. To address these barriers, advanced delivery platforms such as cell-penetrating peptides and lipid nanoparticles (LNPs) have been developed. This study evaluates two delivery systems: the cell-penetrating peptide PepFect-14 (PF14) and LNP formulations, for enhancing nucleic acid delivery and cellular uptake. PF14 facilitates intracellular transport through peptide-nucleic acid complex formation, while LNPs protect cargo from degradation and can promote endosomal escape. Their performance was assessed under different conditions using luciferase-based reporter systems in HeLa cells. PF14-mediated delivery of the splice-switching oligonucleotide ON-705 in HeLa 705 cells showed efficient splice correction, with activity increasing in a dose- and molar ratio- dependent manner, reaching a plateau at a 1:10 ratio. Delivery efficiency was significantly influenced by formulation conditions, with Opti-MEM outperforming standard media and sugar-based buffers. Polymer excipients also affected activity as PVA18, PVA40, and PVP40 enhanced performance, while low molecular weight PVP reduced efficacy. In parallel, LNP-mediated delivery of luciferase mRNA in wild-type HeLa cells demonstrated robust, dose-dependent protein expression. Both systems maintained high cell viability (80-100%). Overall, these findings highlight the importance of formulation optimization in improving nucleic acid delivery and provide practical insights for enhancing peptide- and lipid-based therapeutic platforms.

PMID 42668503
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PubMedMolecular therapy. Oncology2026-08-30

StagX1, an isoquinolinone compound, selectively targets CES1-positive Ewing sarcoma cells as a potential therapeutic agent.

Zhang Nenggang N, Gilbertson Scott R SR, Li Feng F, Pati Debananda D

StagX1 {ethyl 2-[[2-[2-[(2,3-dihydro-1,4-benzodioxin-6-yl)amino]-2-oxoethyl]-1,2-dihydro-1-oxo-5-isoquinolinyl]oxy]propanoate} is a derivative of isoquinolinone, possessing an ethyl propionate. StagX1 exhibits growth-inhibitory activity in multiple Ewing sarcoma cell lines. To advance StagX1 as a potential lead, we conducted experiments to examine its metabolism and stability in tissue culture media, plasma, liver microsomes, cells and mice. Our studies demonstrate that StagX1 is metabolically unstable and undergoes rapid hydrolysis to its corresponding acid metabolite (StagX1-acid) through cleavage of the ethyl ester group. We identified carboxylesterase 1 (CES1) as the primary enzyme responsible for this conversion. Notably, cells expressing CES1 are sensitive to StagX1, whereas CES1-deficient cells show minimal response, indicating that metabolic activation is required for its activity. In contrast, StagX1-acid is metabolically stable. These findings suggest that StagX1 functions as a prodrug that is enzymatically converted to its active metabolite, StagX1-acid, within cells. This metabolic conversion likely underlies its mechanism of action and contributes to its selective anticancer activity in Ewing sarcoma. Our findings provide insight into the metabolism of StagX1 and the role of CES1 in mediating its effects and demonstrate that StagX1 is a promising compound with growth inhibitory effects in CES1 positive Ewing sarcoma cells.

PMID 42668658
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