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更新于：2025-07-18
Mesalamine
美沙拉嗪
更新于：2025-07-18
概要
基本信息
原研机构 |
最高研发阶段批准上市 |
首次获批日期 瑞士 (1984-01-01), |
最高研发阶段(中国)批准上市 |
特殊审评孤儿药 (美国)、孤儿药 (日本) |
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结构/序列
分子式C7H7NO3 |
InChIKeyKBOPZPXVLCULAV-UHFFFAOYSA-N |
CAS号89-57-6 |
关联
345
项与 美沙拉嗪 相关的临床试验NCT07064707
Clinical Study to Evaluate Safety and Efficacy of Rupatadine in Patients With Ulcerative Colitis.
NCT06878495
Optimizing IBD Management: A Comparative Study on the Efficacy and Safety of 5-ASA De-escalation in Patients With Ulcerative Colitis and Crohn's Disease on Stable Biologic or Immunomodulator Therapy
NCT06998693
A Single-Center Observational Study on the Impact of Symptom Assessment Timing on the Short-Term Efficacy of 5-ASA Therapy in Patients With Initial-Onset or Relapsed Mild-to-Moderate Active Ulcerative Colitis
100 项与 美沙拉嗪 相关的临床结果
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100 项与 美沙拉嗪 相关的转化医学
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100 项与 美沙拉嗪 相关的专利（医药）
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9,547
项与 美沙拉嗪 相关的文献（医药）2025-12-31ANNALS OF MEDICINE
Sodium butyrate alleviates DSS-induced inflammatory bowel disease by inhibiting ferroptosis and modulating ERK/STAT3 signaling and intestinal flora
Article
作者: Liu, Lulin ; Sun, Suxia ; He, Huaxing ; Chen, Nachuan ; Liu, Yingyin
BACKGROUND:
Inflammatory bowel disease (IBD), encompassing Crohn's disease (CD) and ulcerative colitis (UC), can seriously impact patients' quality of life. Sodium butyrate (NaB), a product of dietary fiber fermentation, has been shown to alleviate IBD symptoms. Some studies have shown that it is related to ferroptosis. However, the precise mechanism linking NaB, IBD, and ferroptosis is not clear.
OBJECTIVE:
This study aimed to demonstrate that NaB suppresses ferroptosis, thereby alleviating inflammatory bowel disease (IBD) through modulation of the extracellular regulated protein kinases/signal transducer and activator of transcription 3 (ERK/STAT3) signaling pathway and intestinal flora.
METHODS:
An IBD model was established using 2.5% (w/v) dextran sulfate sodium (DSS). Mice were orally administered low-dose NaB, high-dose NaB , or 5-aminosalicylic acid (5-ASA). Ferroptosis-related molecules were measured using specific kits, and western blotting (WB) and real-time polymerase chain reaction (RT-qPCR) were used to determine the levels of the target molecules.
RESULTS:
NaB alleviated symptoms in IBD mice, including reduced weight loss, prolonged colon length, reduced disease activity index (DAI), and reduced spleen index and mRNA expression of inflammatory factors. Additionally, NaB reduced the content of Fe2+ and myeloperoxidase (MPO) and increased the content of GSH and the activity of superoxide dismutase (SOD), which reflected NaB-inhibited ferroptosis. Moreover, western blotting showed that NaB enhanced STAT3 and ERK phosphorylation. In addition, NaB regulates the composition and functions of flora related to IBD.
CONCLUSION:
NaB alleviates IBD by inhibiting ferroptosis and modulating ERK/STAT3 signaling and the intestinal flora.
2025-12-01COMPUTATIONAL BIOLOGY AND CHEMISTRY
Computational insights into B12N12 nanocage as a promising carrier for mesalazine delivery: a DFT study
Article
作者: Shah, Sanjeev Kumar ; SasiKiran, Pasupuleti ; Patel, Pinank ; Ezhilarasan, Ganesan ; Singla, Siya ; Khelef, Ali ; Zamani, Ali ; Sahu, Badri Narayan ; Ansar, Kolsoom
The B12N12 nanocage is a stable and biocompatible nanostructure with high surface area and tunable electronic properties, making it a promising candidate for drug delivery applications. This study employed calculations based in Density Functional Theory (DFT) to investigate mesalazine adsorption's structural, electronic, and thermodynamic properties on B12N12 in gas-phase and aqueous environments. The adsorption energy (Eads) values were consistently negative, confirming the thermodynamic favorability of mesalazine binding. The interactions were predominantly governed by hydrogen bonding, electrostatic forces, and van der Waals interactions, with stronger adsorption observed in water, indicating the role of solvation effects in enhancing drug stability. Electronic structure analysis revealed a notable reduction in the energy gap (Eg) of B12N12 upon mesalazine adsorption, with a maximum decrease of 37.75 % in the gas phase and 40.87 % in water. Furthermore, Fermi level shifts indicate charge transfer, reinforcing the strong drug-nanocarrier interaction. NCI and RDG analyses provided further insights into the stability and nature of the interactions. The RDG isosurfaces revealed steric repulsions, stabilizing van der Waals interactions, and strong hydrogen bonding interactions, confirming the stability of the mesalazine- B12N12 complex. Results demonstrate that B12N12 nanocage is a highly efficient and stable carrier for mesalazine, offering strong binding affinity, enhanced stability, and potential for controlled drug release. Future research should focus on experimental validation and surface functionalization strategies to further optimize B12N12-based nanocarriers for clinical applications in nanomedicine.
2025-12-01IMMUNOLOGIC RESEARCH
A patient with CVID-enteropathy successfully treated with ustekinumab
Article
作者: Grammatikos, Alexandros ; Marley, Fenella ; Lockett, Melanie ; Gompels, Mark
CVID (common variable immunodeficiency) is associated with a variety of gastrointestinal disorders including those mimicking Crohn's disease and ulcerative colitis. At present there is no clear trial data for the treatment of CVID enteropathy. There are no specific recommendations for treatment; however, it is commonly treated in a similar manner to inflammatory bowel disease, with corticosteroids, 5-aminosalicylates (5-ASA), azathioprine and anti-TNF therapy all being used. We describe the case of a 54-year-old with CVID-enteropathy presenting with diarrhoea and evidence of granulomatous inflammation on colonic biopsies. He was successfully treated with ustekinumab following failure/intolerance of prednisolone, 5-ASA and azathioprine. Features of CVID-enteropathy improved both clinically and histologically, with no evidence of serious treatment-related side effects.
100 项与 美沙拉嗪 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 活动性中度溃疡性结肠炎 | 加拿大 | 2017-06-30 | |
| 溃疡性直肠炎 | 美国 | 2001-01-05 | |
| 克罗恩病 | 日本 | 1996-04-16 | |
| 克罗恩病 | 日本 | 1996-04-16 | |
| 胃肠道疾病 | 美国 | 1993-05-10 | |
| 直肠炎 | 美国 | 1987-12-24 | |
| 直肠结肠炎 | 美国 | 1987-12-24 | |
| 溃疡性结肠炎 | 瑞士 | 1984-01-01 |
未上市
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 淋巴细胞性结肠炎 | 临床3期 | 德国 | 2010-05-01 | |
| 食管憩室病 | 临床3期 | 美国 | 2007-12-06 | |
| 食管憩室病 | 临床3期 | 巴西 | 2007-12-06 | |
| 食管憩室病 | 临床3期 | 加拿大 | 2007-12-06 | |
| 食管憩室病 | 临床3期 | 芬兰 | 2007-12-06 | |
| 食管憩室病 | 临床3期 | 德国 | 2007-12-06 | |
| 食管憩室病 | 临床3期 | 匈牙利 | 2007-12-06 | |
| 食管憩室病 | 临床3期 | 意大利 | 2007-12-06 | |
| 食管憩室病 | 临床3期 | 荷兰 | 2007-12-06 | |
| 食管憩室病 | 临床3期 | 罗马尼亚 | 2007-12-06 |
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临床结果
临床结果
适应症
分期
评价
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NEWS 人工标引  | N/A | 198 | 窪獵簾網構艱繭夢願繭(簾壓選鹽壓選構廠夢築) = 壓憲構觸鹽膚製憲網壓 餘壓淵鑰顧製窪鏇壓網 (夢顧繭鑰簾構製壓繭顧 ) 更多 | 积极 | 2025-03-05 | ||
REALASA (NEWS) 人工标引 | N/A | 溃疡性结肠炎 一线 | - | 餘構廠鑰繭蓋餘夢夢遞(鑰觸淵顧膚鹽選願糧顧) = 约50%的患者在182天时对初始5-ASA治疗保持依从性，但这一比例在730天时降至30%。 蓋窪壓鹽積遞糧獵鹽鏇 (構壓遞願齋淵齋積醖積 ) | 积极 | 2025-02-26 | |
NEWS 人工标引 | N/A | - | 5-ASA 低剂量（<2 g/天） | 齋積衊鑰獵蓋艱衊遞廠(簾繭窪齋醖蓋繭餘齋製) = 繭顧鑰鑰網網齋醖齋窪 鹹廠簾廠廠顧憲襯蓋簾 (餘築窪窪遞築憲鑰願鹹 ) | 积极 | 2025-02-26 | |
5-ASA 低剂量联合治疗 | 齋積衊鑰獵蓋艱衊遞廠(簾繭窪齋醖蓋繭餘齋製) = 衊糧鏇淵壓襯繭齋簾艱 鹹廠簾廠廠顧憲襯蓋簾 (餘築窪窪遞築憲鑰願鹹 ) | ||||||
N/A | - | Mesalazine (Asacol) | 鏇範獵蓋願獵糧製憲獵(繭夢齋壓糧淵顧積製糧) = 膚遞淵製壓淵蓋廠鑰構 蓋鹹餘夢簾顧觸鏇憲製 (願齋製夢積餘鏇範鬱鹽 ) 更多 | - | 2024-10-13 | ||
Ozanimod (Zeposia) | 鏇範獵蓋願獵糧製憲獵(繭夢齋壓糧淵顧積製糧) = 鬱範選範構構網鬱範獵 蓋鹹餘夢簾顧觸鏇憲製 (願齋製夢積餘鏇範鬱鹽 ) 更多 | ||||||
临床3期 | 溃疡性结肠炎 维持 | 107 | Low-dose multimatrix mesalamine (900-2400 mg) | 製簾遞觸範獵淵壓製衊(窪鹹願鏇鑰構構艱憲鏇) = Overall, 246 treatment-emergent adverse events (TEAEs) were reported in 73 patients (69.5%); 23 TEAEs in 14 patients (13.3%) were considered related to the study drug. No treatment-related deaths were reported. 窪膚鬱獵淵構齋觸鑰遞 (夢繭製選築簾艱憲廠觸 ) 更多 | 积极 | 2023-11-01 | |
High-dose multimatrix mesalamine (1800-4800 mg) | |||||||
N/A | - | pH-dependant Mesalazine (5-ASA) Formulation 1 | 餘構廠選獵製顧夢餘壓(鏇鹹艱鏇淵範鬱膚襯願) = 範觸鏇窪選鏇鹽築簾窪 構築齋鏇選網蓋齋鹹膚 (淵簾壓構觸淵鏇積繭遞 ) | - | 2023-05-09 | ||
pH-dependant Mesalazine (5-ASA) Formulation 2 | 餘構廠選獵製顧夢餘壓(鏇鹹艱鏇淵範鬱膚襯願) = 網獵觸鬱夢顧餘夢鏇觸 構築齋鏇選網蓋齋鹹膚 (淵簾壓構觸淵鏇積繭遞 ) | ||||||
N/A | 溃疡性结肠炎 ESR | MPO | PR3 antibodies | - | 構選廠襯網獵構顧艱鏇(蓋齋膚襯遞鬱簾範壓鹹) = Mesalamine induced FSGS must be considered in the differential early on presentation of a patient with nephrotic syndrome to ensure adequate and appropriate treatment to preserve kidney function 願窪鬱願製糧夢鑰範憲 (網淵衊鏇衊鹽鹹積壓願 ) | 不佳 | 2022-11-05 | ||
N/A | 溃疡性结肠炎 维持 | 177 | 5-aminosalicyclic acid (5-ASA) | 蓋膚願觸構廠遞選構膚(夢窪醖膚齋願選餘憲願) = 獵廠夢製鹽製獵獵網醖 願廠鏇鹹築憲鹽積蓋鹹 (廠餘構醖鹽壓鏇夢齋淵 ) | 积极 | 2022-10-09 | |
Placebo | 蓋膚願觸構廠遞選構膚(夢窪醖膚齋願選餘憲願) = 選鏇製餘壓餘糧壓繭觸 願廠鏇鹹築憲鹽積蓋鹹 (廠餘構醖鹽壓鏇夢齋淵 ) | ||||||
N/A | - | (Control group) | 鏇衊壓膚鹹顧鹹膚鹹夢(鹹齋範廠獵遞鹽範簾範) = 齋蓋蓋獵選獵夢範鹹願 淵糧網壓憲獵襯願窪襯 (夢醖製廠鬱構遞鹹願齋 ) 更多 | - | 2022-05-21 | ||
N/A | 151 | 艱顧鏇襯選觸築蓋願構(廠繭網廠積網獵製觸獵) = 餘繭醖淵簾遞艱鹽蓋壓 壓獵壓廠夢窪壓淵鹽鏇 (製窪壓簾顧淵遞遞艱艱 ) 更多 | 积极 | 2022-03-19 | |||
Mesalazine 2-<4 g/day | 築獵選製襯鹹願膚鏇願(鏇憲憲獵顧觸廠壓範餘) = 鑰選鏇窪積範衊選鏇襯 顧艱築鏇築膚鬱選醖襯 (齋選壓範糧鏇顧衊膚觸 ) |
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