美沙拉嗪/透明质酸钠(Mesalazine/Sodium Hyaluronate) - 药物靶点：PP2A_在研适应症：溃疡性结肠炎_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Mesalamine-sodium hyalyronic

靶点

PP2A

作用机制

PP2A抑制剂(蛋白质磷酸酶2A抑制剂)

治疗领域

免疫系统疾病消化系统疾病

在研适应症

溃疡性结肠炎

非在研适应症-

原研机构

禾伸堂生技股份有限公司

在研机构

禾伸堂生技股份有限公司

Beijing Colin Likang Medical Research Co., Ltd

非在研机构-

最高研发阶段临床2期

首次获批日期-

最高研发阶段(中国)临床1期

特殊审评-

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结构

分子式C7H7NO3

InChIKeyKBOPZPXVLCULAV-UHFFFAOYSA-N

CAS号89-57-6

关联

3

项与美沙拉嗪/透明质酸钠相关的临床试验

CTR20241373 / Not yet recruiting临床1期

IBD98-M缓释胶囊在中国健康受试者中单次/多次给药、剂量递增、单中心、单臂、非随机的安全性、耐受性和药代动力学I期临床研究

？主要目的评估健康成年受试者单次和多次服用IBD98-M缓释胶囊的安全性和耐受性。？次要目的评估健康成年受试者单次和多次服用IBD98-M缓释胶囊的药代动力学（PK）特征。

开始日期-

申办/合作机构

禾伸堂生技股份有限公司

[+1]

EUCTR2015-001022-42-IT / Not yet recruiting临床2期

A Phase 2a, Multicenter, Randomized, Double-blind, Parallel-group, Placebo-controlled Trial of IBD98-M Delayed-release Capsules to Induce Remission in Patients with Active, Mild to Moderate Ulcerative Colitis

开始日期2015-12-01

申办/合作机构

禾伸堂生技股份有限公司

NCT02196662 / Completed临床1期

Pharmacokinetics of IBD98-M 400mg-57.5/Day in Healthy Volunteers

The primary objective of this study is to compare the rate and extent of absorption of mesalamine-sodium hyaluronate 200 mg-28.75 mg delayed-release capsule (IBD98-M, Test) versus Delzicol 400 mg delayed-release capsule (mesalamine Reference), administered as a single oral dose of 2 x 200 mg-28.75 mg delayed-release capsule (total dose of 400 mg-57.50 mg) or 1 x 400 mg delayed-release capsule under fasting conditions.

开始日期2014-07-01

申办/合作机构

禾伸堂生技股份有限公司

100 项与美沙拉嗪/透明质酸钠相关的临床结果

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100 项与美沙拉嗪/透明质酸钠相关的转化医学

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100 项与美沙拉嗪/透明质酸钠相关的专利（医药）

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3

项与美沙拉嗪/透明质酸钠相关的文献（医药）

2021-06-01·Bioorganic & Medicinal Chemistry Letters4区 · 医学

Design, synthesis and molecular modeling studies of novel mesalamine linked coumarin for treatment of inflammatory bowel disease

4区 · 医学

Article

作者: Mohapatra, Sujata ; Sharma, Tripti ; Abul Qais, Faizan ; Rath, Biswabhusan ; Patro, Randeep

Inflammatory bowel diseases (IBD) are continuous idiopathic inflammation of GIT. Ulcerative colitis, inflammation of the colonic or rectal mucosa has no known medical cure and its treatment is aimed at reducing the signs and symptoms associated with the disorders, induction and maintenance of remission. In this study, we have reported the synthesis of mesalamine and coumarin linked together by a diazo group. The compound was characterized by various spectroscopic methods. Therapeutic potential of the synthesized compound was investigated through acetic acid induced ulcerative rat model. Pharmacokinetic properties were predicted for the compounds by ADMET related descriptors. Molecular docking studies were conducted with four proteins (COX-2, MMP-9, TNF-α and MPO) to examine the interaction of mesalamine (MS) and mesalamine coumarin derivative (MS-CU). Moreover, molecular dynamic simulations were carried out to study the dynamics and stability of the complexes in solvent system. The binding energy of MS-CU with MPO, COX-2, MMP-9 and TNF-α was found to be -9.5, -10.4, -9.2 and -8.4 kcal/mol respectively. MS-CU exhibited higher binding affinity towards all tested proteins than MS. Molecular dynamic simulation reveals that both MS and MS-CU formed a stable complex with all test proteins in aqueous system. Overall binding energy of MS-CU was more than MS showing stronger affinity towards the test portions. In conclusion, Mesalamine-coumarin derivative reduces colonic damage in acetic acid induced ulcerative colitis in rat model, and therefore may prove to be effective in the management of IBD.

Molecules3区 · 化学

Combined Treatment with Hyaluronic Acid and Mesalamine Protects Rats from Inflammatory Bowel Disease Induced by Intracolonic Administration of Trinitrobenzenesulfonic Acid

3区 · 化学

ArticleOA

作者: Hung, Shao-Wen ; Yang, Cheng-Yao ; Chiu, Chih-Tung ; Kuo, Sheng-Nan

Drugs such as mesalamine (5-ASA) are currently recommended for the treatment of inflammatory bowel disease (IBD). To reduce the frequency of their administration and improve their therapeutic effect, this study investigated the adhesion efficacy, wound healing promotion, and decrease in inflammation in ulcers in the colonic tissue of rats with colitis after combined treatment with hyaluronic acid (HA) and 5-ASA (IBD98-M). HA-fluoresceinamine (FL) conjugates successfully adhered to the mucosal layer and were conjugated in the vascular tissue. In addition, macroscopic and microscopic observations indicated that colonic injuries reduced significantly after treatment with IBD98-M. Compared with PBS and 5-ASA treatment alone, treatment with IBD98-M more effectively reduced bowel inflammation and promoted colonic mucosal healing in TNBS-induced colitis. IBD98-M treatment also reduced myeloperoxidase activity and the expression levels of cyclooxygenase 2 and tumor necrosis factor-αin the colitis tissue. In conclusion, IBD98-M treatment strongly promoted wound healing in colonic injuries and significantly inhibited MPO activity in the inflamed colon tissue of rats. Combined treatment with HA and 5-ASA can accelerate wound healing and reduce inflammatory reaction in rat colitis.

Cells3区 · 生物学

A Phase 2a, Multicenter, Randomized, Double-Blind, Parallel-Group, Placebo-Controlled Trial of IBD98-M Delayed-Release Capsules to Induce Remission in Patients with Active and Mild to Moderate Ulcerative Colitis

3区 · 生物学

ArticleOA

作者: Fiorino, Gionata ; di Sabatino, Antonio ; Cassinotti, Andrea ; Sturniolo, Giacomo Carlo ; Bossa, Fabrizio ; Giuffrida, Paolo ; Danese, Silvio

IBD98-M is a delayed-release formulation of mesalamine (mesalazine) and SH with a potential therapeutic role in ulcerative colitis (UC). A total of 51 patients with a modified Ulcerative Colitis Disease Activity Index (UCDAI) score of ≥4 and ≤10, and a modified UCDAI endoscopy subscore ≥1 were randomized for 6 weeks of double-blind treatment with IBD98 0.8 g/day or IBD 1.2 g/day or placebo. The efficacy and safety of IBD98-M in mild to moderate active UC were primarily evaluated. At week 6, 1 (5.9%), 2 (12.5%), and 2 (11.1%) patients receiving IBD98-M 0.8 g, IBD98-M 1.2 g, and placebo, respectively, (p > 0.999) achieved clinical remission. Higher clinical response was seen in IBD98-M 1.2 g (31.3%) versus placebo (16.7%) and endoscopic improvement in IBD98-M 0.8 g (29.4%) versus placebo (22.2%) was seen. Fecal calprotectin levels were reduced in IBD98-M groups versus placebo (p > 0.05). IBD98-M patients achieved significant improvement in physical health summary score component of the SF-36 (p = 0.01 and p = 0.03 respectively) compared to placebo. IBD98-M did not meet the primary end point but had higher clinical response (1.2 g/day) and endoscopic improvement (0.8 g/day) compared to placebo. The safety result shown that IBD98-M treatment was safe and well tolerated in this patient population. No new safety signals or unexpected safety findings were observed during the study. Further trials with different stratification and longer follow-up may be needed to evaluate the efficacy.

100 项与美沙拉嗪/透明质酸钠相关的药物交易

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