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nicotinic acid (nicotinic acid ER / Niaspanor / Niaspan)

✓ Approved

Merck KGaA · HCAR2 · 小分子

什么是 nicotinic acid？

nicotinic acid 是一种小分子，由Merck KGaA研发。该药已获批，用于治疗相关适应症，给药途径：Oral (PO)。

药物档案

商品名nicotinic acid ER, Niaspanor, Niaspan
公司Merck KGaA
药物类别小分子
分子靶点HCAR2
给药途径Oral (PO)
状态Approved
来源： ClinicalTrials.gov, Merck KGaA

作用机制

分子靶点

nicotinic acid 作用于 1 个分子靶点：

HCAR2hydroxycarboxylic acid receptor 2 (NIACR1, GPR109A)
需要更深入的分析？Noah AI 可解释复杂机制并与同类药物比较。

治疗适应症

nicotinic acid 针对 8 个适应症，涉及 4 个治疗领域。

治疗领域疾病/病症分期
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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相关研究文献

PubMedFrontiers in cellular and infection microbiology2026-09-11

Brucellar spondylitis is associated with disturbance in gut microbiota and histamine metabolism associated inflammation.

Ma Zongjun Z, Bai Xiaoyan X, Tian Jun J, Yao Chenfei C et al.

The pathogenesis of brucellar spondylitis (BLS) has traditionally been considered to be primarily limited to local osteoarticular lesions. With the proposal of the "gut-spine axis" concept, the role of intestinal microecological dysbiosis in inflammatory spinal diseases has attracted in an increase of attention. The overactivated inflammatory cytokine network not only mediates bone destruction and intervertebral disc damage, but also forms a bidirectional interaction with gut microbiota dysbiosis through the "gut-spine axis," collectively driving disease progression. However, the inflammatory mechanism by which gut microbiota participates in the pathological process of BLS remains largely unclear. This study recruited 20 BLS patients and 20 healthy donors. Multi-omics analysis including metagenomics, untargeted metabolomics, and targeted short-chain fatty acids (SCFAs) analysis, were used to compare the structural differences in gut microbiota between the two groups and screen for signature differential bacterial species. Plasma levels of histamine and histidine decarboxylase were measured by ELISA to clarify the role of differential histidine metabolic pathway in the disease. Additionally, plasma levels of lipopolysaccharide (LPS) and inflammatory cytokines (IL-1β, IL-6, IL-10, IL-17A, TNF-α) were detected by ELISA. The correlation between gut microbiota and inflammatory indicators was further analyzed. Compared to the healthy control group, the α-diversity of the gut microbiota in BLS patients was significantly reduced, with the microbial community structure exhibiting increased homogeneity. Beta diversity analysis revealed significant differences, suggesting that disease progression is associated with an overall imbalance in the gut microbiota and the deterioration of its specific structural composition. At the phylum level, the abundances of Actinomycetota, unclassified_d_Viruses, and Fusobacteriota were significantly increased in the gut microbiota of BLS patients compared to the control group, while the abundances of Bacillota and Pseudomonadota were significantly decreased. Further analysis revealed that, compared to the control group, the generic abundance of Enterococcus was significantly increased, while the proportions of Blautia, Faecalibacterium, Ruminococcus, Agathobacter, Roseburia, Clostridium, Eubacterium, Alistipes and Anaerobutyricum were significantly decreased. At the species level, the abundances of Enterococcus sp and Enterococcus-faecium were increased, whereas Blautia sp, Ruminococcus sp, Faecalibacterium sp, Faecalibacterium prausnitzii, Agathobacter rectalis, Eubacterium sp, Agathobacter sp, and Roseburia sp were decreased. Furthermore, untargeted metabolomics revealed that metabolites were enriched in the histidine metabolic pathway, and the levels of SCFAs including butyrate, isobutyrate, valerate, and 4-methylvalerate in the intestinal contents were reduced in BLS. Functional KEGG profiling revealed that key KOs involved in butyrate synthesis (e.g., K00074, K00172, K01640) and transport were globally downregulated in the patient group, whereas histidine decarboxylase KOs (K01693, K11755, K19787) that convert histidine to pro-inflammatory histamine were significantly enriched. The loss of butyrate-producing symbionts led to SCFAs deficiency and mucosal barrier disruption, creating ecological niches for facultatively anaerobic Enterococcus, which further exacerbated local inflammation via proteolytic fermentation and histamine production. Compared with the control group, BLS patients showed decreased plasma levels of IL-10, while levels of IL-1β, IL-6, IL-17A, and TNF-α were increased, and LPS levels were elevated. In addition, significantly elevated plasma pro-inflammatory LPS levels in patients with BLS suggest disruption of intestinal integrity and permeability. Correlation analysis indicated a close relationship between gut microbiota and inflammation. BLS is associated with gut microbiota dysbiosis and alterations in microbial metabolites, which may be linked to inflammatory responses and histamine metabolism. The differential microbial taxa identified in this study could be developed into a stool-based non-invasive diagnostic panel to facilitate early differentiation of BLS from other spinal disorders. Furthermore, restoring gut microbial balance through probiotic supplementation or dietary modulation may represent a promising adjunctive strategy to enhance the efficacy of standard antibiotic therapy and reduce disease recurrence.

PMID 42723989
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PubMedNature reviews. Disease primers2026-09-11

Toxidromes.

Roberts Darren M DM, Nic Ionmhain Úna Ú, Trakulsrichai Satariya S, Peter John Victor JV et al.

Poisoning is an important and prevalent concern, occurring owing to many drugs, chemicals or natural poisons. Prompt diagnosis and treatment optimize outcomes. Initial management involves concurrently assessing the history of exposure, performing a clinical examination and resuscitation when required. The integration of symptoms and clinical signs, and possibly investigations and/or the response to an antidote, can enable the identification of a potential toxidrome. Toxidromes are important in the assessment and management of patients with poisoning. Each toxidrome may be caused by a particular group of poisons, so diagnosis of a toxidrome may indicate what a patient was exposed to, guiding further clinical assessment and management. Identifying a toxidrome can be especially informative when a history cannot be obtained, for example in patients who are drowsy or extremely agitated. Additionally, a toxidrome may help to confirm the accuracy of the history of exposure, when this is available, facilitating further assessment and management. Classic poisoning-related toxidromes include the opioid, sympathomimetic, serotonergic, antimuscarinic, muscarinic and nicotinic toxidromes. Other toxidromes that are common and require careful clinical consideration include bradycardia with hypotension, 'knockdown', mushroom poisoning, neuroleptic malignant and uncoupling of oxidative phosphorylation syndromes. Multiple toxidromes can occur together following exposure to certain single xenobiotics or to multiple xenobiotics, which can complicate clinical decision-making. Future directions include refining diagnostic tools including bedside and/or laboratory investigations to complement clinical assessments, improving access to region-specific toxidrome data, and developing targeted therapies to enhance outcomes and address current gaps in care.

PMID 42722690
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PubMedPhysiological reports2026-09-11

Fatty acid species differentially regulate macrophage polarization and oxidative stress with secondary effects on macrophage-HSC crosstalk.

Nakanishi Koichi K, Shinkawa Hiroji H, Takemura Shigekazu S, Nakagawa Kanako K et al.

Metabolic dysfunction-associated steatohepatitis (MASH) is characterized by lipid accumulation, inflammation, and fibrosis. Macrophage-hepatic stellate cell (HSC) communication plays a key role in fibrogenesis; however, how fatty acid species influence macrophage polarization remains unclear. Bone marrow-derived macrophages (BMDMs) were polarized toward M1 or M2 phenotypes in the presence of palmitic acid (PA), oleic acid (OA), or palmitoleic acid (PO). Polarization markers, reactive oxygen species (ROS), and peroxisome proliferator-activated receptor gamma (PPARγ) expression were analyzed by RT-qPCR, Western blotting, and chemiluminescence. Primary HSCs were exposed to fatty acids or conditioned media from treated macrophages. PA enhanced selected inflammatory macrophage responses and increased ROS production under M1-polarizing conditions. OA enhanced ROS production in M1 macrophages and suppressed several M2-associated markers, whereas PO reduced inflammatory responses and ROS under M1-polarizing conditions. Direct fatty acid exposure did not significantly alter HSC activation markers. Conditioned media from polarized macrophages, particularly M1 macrophages, reduced α-SMA and cytoglobin protein expression in HSCs, while fatty acid-specific effects were modest and marker-dependent. Fatty acid species differentially modulate macrophage polarization and redox activity, partly in association with PPARγ signaling. These macrophage changes may secondarily affect macrophage-HSC communication and stellate cell redox-related responses, providing insight into lipid regulation of immune-stromal interactions in the liver.

PMID 42723224
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PubMedFrontiers in plant science2026-09-11

Comparison of heavy metal contents, fatty acid composition, and palinological characteristics of two different Hypericum species growing in mining-impacted area.

Ahıskalı Mihriban M

This study comparatively evaluated heavy metal (Al, Cd, Cr, Fe, and Mn) concentrations, fatty acid composition, and palynological characteristics in Hypericum scabrum and Hypericum lydium samples collected from mining-impacted and reference sites of an iron ore operation. Plant samples of H. scabrum and H. lydium were collected from mining-impacted and reference sites in Bingöl Province, Türkiye. Heavy metal concentrations, fatty acid composition, and pollen morphological characteristics were analyzed using ICP-MS, gas chromatography, and light microscopy, respectively. Translocation factor (TF) and statistical analyses were also performed. In both species, Al, Cr, Fe, and Mn accumulation was markedly increased in the mining area, whereas the increase in Cd remained relatively limited with statistically significant differences between sites. Translocation factor (TF) analyses revealed higher values for most metals in the mining area; notably, H. lydium exhibited a greater translocation capacity for Fe and Mn. In contrast, TF values for Cr remained below 1 in both species, indicating its retention at the root level. Mining conditions were found to markedly alter the fatty acid composition in both Hypericum species, particularly affecting the balance between saturated and unsaturated fatty acids. Under heavy metal stress, total saturated fatty acids (ΣTSFA; particularly palmitic acid (C16:0) and stearic acid (C18:0)) increased in the mining area, whereas total unsaturated fatty acids (ΣTUSFA; oleic acid (C18:1), linoleic acid (C18:2), and α-linolenic acid (C18:3)) were higher under non-mining conditions. From a palynological perspective, the increased metal load preserved morphological integrity in the pollen of H. scabrum, whereas it caused pronounced changes in the P/E ratio and pollen shape in H. lydium, with statistically significant differences observed. Overall, the findings suggest that mining-related heavy metal stress influences metal accumulation, fatty acid composition, and pollen characteristics in Hypericum species, although the magnitude and nature of these effects differ between H. scabrum and H. lydium. These species-specific differences indicate that the two species exhibit distinct physiological and morphological responses to heavy metal stress, contributing to a better understanding of plant-heavy metal interactions in mining ecosystems.

PMID 42723791
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PubMedCureus2026-09-11

Efficacy of Sublingual Misoprostol Versus Intravenous Tranexamic Acid in Reducing Blood Loss Among Full-Term Pregnant Women Undergoing Primary Lower Segment Caesarean Section: A Randomized Controlled Trial.

Basavaraj Nikhitha N, B Ashwini A, Pushpa Kotur K

Postpartum hemorrhage remains a major cause of maternal morbidity and mortality, with caesarean section being associated with increased intraoperative blood loss. Pharmacological agents such as misoprostol and tranexamic acid have been used prophylactically to reduce blood loss during lower segment caesarean section (LSCS); however, evidence directly comparing their efficacy is limited. This study aimed to compare the efficacy and safety of sublingual misoprostol and intravenous tranexamic acid in reducing intraoperative blood loss during primary LSCS. This hospital-based, open-label, randomized controlled trial included 140 women with singleton term pregnancies undergoing primary LSCS. Participants were randomized equally to receive either 600 µg sublingual misoprostol or 1 g intravenous tranexamic acid immediately before skin incision. The primary outcome was intraoperative blood loss measured using a standardized gravimetric method. Secondary outcomes included postoperative fall in haemoglobin, requirement for additional uterotonic agents or blood transfusion, and adverse drug effects. Baseline demographic and obstetric characteristics were comparable between the two groups. Mean intraoperative blood loss was significantly lower in the misoprostol group than in the tranexamic acid group (316.0 ± 158.0 mL vs. 518.5 ± 233.1 mL; p < 0.001). Women receiving misoprostol also had a significantly smaller postoperative fall in haemoglobin and required fewer additional uterotonic agents (2 (2.9%) vs. 11 (15.7%); p = 0.009) and blood transfusions (1 (1.4%) vs. 9 (12.9%); p = 0.016). Fever and shivering were more common with misoprostol, whereas hypotension occurred more frequently in the tranexamic acid group (all p < 0.05). Sublingual 600 µg misoprostol was more effective than 1 g intravenous tranexamic acid in reducing intraoperative blood loss during primary LSCS. It was associated with a smaller postoperative decline in haemoglobin and a reduced need for additional uterotonic agents and blood transfusion, while maintaining an acceptable safety profile. These findings support the use of sublingual misoprostol as an effective and economical option for preventing excessive blood loss during primary LSCS.

PMID 42724954
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PubMedJournal of microbiology and biotechnology2026-09-11

Local Suppression of Dgat2 Augments Fatty Acid Oxidation in Skeletal Muscle in High-Fat Diet-Fed Mice.

Jiyun Yeo Y, Park Ju Young JY, Kwon Min Gyeong MG, Kim Eun Seong ES et al.

Diacylglycerol acyltransferase 2 (DGAT2) codes an enzyme which synthesize triglyceride by esterifying fatty acid to last portion of diacylglycerol backbone, and contributes to intramyocellular lipid metabolism. Small interfering RNA (siRNA)-mediated knockdown of Dgat2 was previously shown to reduce AKT phosphorylation and glucose uptake, decrease fatty acid partitioning into triglycerides, and increase free fatty acid release and oxidation in skeletal muscle cells. The current study aimed to determine whether Dgat2 knockdown affects lipid and glucose metabolism in glycolytic muscle (GM) and oxidative muscle (OM) under high-fat diet conditions, consistent with our previous in vitro findings. Male C57BL/6J mice were fed high-fat diet, and treated with Dgat2 or control-siRNA, and the effects were compared in different muscle types. Muscle Dgat2 suppression reduced intramuscular triglyceride content by up to 38.2% whereas increased circulating triglyceride levels. In addition, decreased Gpat3 mRNA levels supported a reduction in lipid esterification capacity. Dgat2 suppression increased the integration of C14-tagged fatty acids into acid-soluble metabolites, and altered gene expressions related to glucose utilization; GLUT4 protein were decreased and Pdk2 mRNA increased in both GM and OM fibers. GM exhibited decreased AKT phosphorylation about 50%, whereas OM showed no change in AKT phosphorylation. Noticeably OM exhibited reduced Hk2 and glycogen accumulation. Together, these findings suggest that muscle Dgat2 inhibition redirects fatty acid channeling from triglyceride storage toward oxidation in vivo, with accompanying changes in glucose metabolism-related markers. These results extend our previous cell-based findings to a more physiologically relevant setting, while highlighting distinct response patterns in GM and OM.

PMID 42723533
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