Comparison of an Ecabet Sodium and PPI in the treatment of endoscopic submucosal dissection (ESD)-induced ulcers in early gastric cancer: prospective randomized study - The prospective randomized study of ESD-induce ulcer

开始日期2013-07-29

申办/合作机构

Kinki University

JPRN-UMIN000007735 / RecruitingN/AIIT

Randomised comparison study: eradication therapy for Helicobacter pylori with or without ecabet sodium after endoscopic submucosal dissection (ESD) of early gastric cancer - Quadruple eradication therapy with ecabet sodium of early gastric cancer after ESD.

开始日期2012-02-01

申办/合作机构-

JPRN-UMIN000033984 / Completed

Preventive effect of ecabet sodium on low-dose aspirin-induced small intestinal mucosal injury: A randomized, double-blind, pilot study - Preventive effect of ecabet sodium on low-dose aspirin-induced small intestinal mucosal injury

开始日期2011-10-04

申办/合作机构

Osaka Medical College

100 项与依卡倍特钠相关的临床结果

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100 项与依卡倍特钠相关的转化医学

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100 项与依卡倍特钠相关的专利（医药）

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项与依卡倍特钠相关的文献（医药）

2023-01-01·Plant biotechnology journal

Structural and mechanistic insights into the precise product synthesis by a bifunctional miltiradiene synthase

Article

作者: Su, Ping ; Gao, Wei ; Tong, Yuru ; Jiang, Tao ; Huang, Luqi ; Ma, Xiaoli ; Xu, Haifeng ; Chen, Kang ; Hu, Tianyuan ; Cui, Guanghong

Summary:

Selaginella moellendorffii miltiradiene synthase (SmMDS) is a unique bifunctional diterpene synthase (diTPS) that catalyses the successive cyclization of (E,E,E)‐geranylgeranyl diphosphate (GGPP) via (+)‐copalyl diphosphate (CPP) to miltiradiene, which is a crucial precursor of important medicinal compounds, such as triptolide, ecabet sodium and carnosol. Miltiradiene synthetic processes have been studied in monofunctional diTPSs, while the precise mechanism by which active site amino acids determine product simplicity and the experimental evidence for reaction intermediates remain elusive. In addition, how bifunctional diTPSs work compared to monofunctional enzymes is attractive for detailed research. Here, by mutagenesis studies of SmMDS, we confirmed that pimar‐15‐en‐8‐yl+ is an intermediate in miltiradiene synthesis. Moreover, we determined the apo‐state and the GGPP‐bound state crystal structures of SmMDS. By structure analysis and mutagenesis experiments, possible contributions of key residues both in class I and II active sites were suggested. Based on the structural and functional analyses, we confirmed the copal‐15‐yl+ intermediate and unveiled more details of the catalysis process in the SmMDS class I active site. Moreover, the structural and experimental results suggest an internal channel for (+)‐CPP produced in the class II active site moving towards the class I active site. Our research is a good example for intermediate identification of diTPSs and provides new insights into the product specificity determinants and intermediate transport, which should greatly facilitate the precise controlled synthesis of various diterpenes.

2020-05-01·European journal of pharmacology3区 · 医学

Evaluating the mucoprotective effect of polydeoxyribonucleotide against indomethacin-induced gastropathy via the MAPK/NF-κB signaling pathway in rats

3区 · 医学

Article

作者: Jin, Jun-Jang ; Kwak, Min Seop ; Kim, Chang-Ju ; Hwang, Lakkyong ; Han, Jin Hee ; Kim, Sang-Hoon ; Yoon, Jin Young ; Jeon, Jung Won ; Ko, Il-Gyu

Non-steroidal anti-inflammatory drugs (NSAIDs) cause gastric mucosal damage and gastric ulceration. Among the most commonly used NSAIDs, indomethacin upregulates mucosal tumor necrosis factor-α, which activates nuclear factor-kappa B (NF-κB), and mitogen-activated protein kinases (MAPK) to induce various pro-inflammatory mediators. Polydeoxyribonucleotide (PDRN) is an adenosine A_2A receptor agonist that exerts anti-inflammatory effects. In this study, we evaluated the efficacy of PDRN in the initial treatment of gastropathy against that of ecabet sodium and irsoglandin maleate, which are commonly used medications. The rats were administrated indomethacin once a day for 7 days after 24 h of fasting to induce gastropathy. Rats in the drug-treated groups were orally administrated 500 μl of distilled water containing the drug once daily for 7 days 1 h after indomethacin administration. Indomethacin administration caused mucosal damage and increased pro-inflammatory cytokine release. Both NF-κB and MAPK cascade factors were increased by indomethacin administration. PDRN therapy more potently suppressed the expressions of NF-κB and MAPK cascade factors compared to other drugs. The expression of cyclic adenosine-3',5'-monophosphate was also increased by PDRN treatment in the indomethacin-induced gastropathy rats. These changes led to a reduction in pro-inflammatory cytokines and apoptotic factors, which ultimately promote recovery of damaged gastric tissue. Therefore, PDRN may serve as a new therapeutic option in the initial treatment of NSAIDs-induced gastropathy.

2019-12-01·BMC gastroenterology3区 · 医学

Preventive effect of ecabet sodium on low-dose aspirin-induced small intestinal mucosal injury: a randomized, double-blind, pilot study

3区 · 医学

ArticleOA

作者: Nouda, Sadaharu ; Kojima, Yuichi ; Sugawara, Noriaki ; Higuchi, Kazuhide ; Kuramoto, Takanori ; Ota, Kazuhiro ; Takeuchi, Toshihisa ; Hirata, Yuki ; Kakimoto, Kazuki ; Harada, Satoshi

BACKGROUND:

We aimed to investigate how high-dose ecabet sodium affects low-dose aspirin-induced small intestinal mucosal injury in healthy volunteers.

METHODS:

Healthy volunteers were enrolled randomly into one of two groups with the following drug regimens for 2 weeks: group A, low-dose aspirin once per day and group B, low-dose aspirin and 4.0 g of ecabet sodium. Small bowel capsule endoscopy was performed before and 2 weeks after low-dose aspirin administration.

RESULTS:

A significant difference was found in the median number [range] of small intestinal lesions between baseline and two weeks after low-dose aspirin administration in group A (baseline: 1 [0-5], after: 5 [1-11]; p = 0.0059) but not in group B (baseline: 0.5 [0-9], after: 3 [0-23]; p = 0.0586). In group B, although the median number [range] of lesions in the first tertile of the small intestine did not increase two weeks after low-dose aspirin administration (baseline: 0 [0-4], after: 1.5 [0-8]; p = 0.2969), the number of lesions in the second and third tertiles of the small intestine increased significantly (baseline: 0 [0-5], after: 2 [0-15]; p = 0.0469).

CONCLUSIONS:

Ecabet sodium had a preventive effect on low-dose aspirin-induced small intestinal mucosal injury in the upper part of the small intestine.

TRIAL REGISTRATION:

ISRCTN 99322160 , 01/10/2018.

项与依卡倍特钠相关的新闻（医药）

2023-11-27

·赛柏蓝

消化系统用药，7图渠道格局分析

随着人们生活方式的改变和人口老龄化进程的加快，消化系统疾病的发病率逐年上升，且呈现年轻化趋势，由此也为消化系统药物带来持续稳定的市场需求。根据法伯全渠道数据，在2022年中国医疗机构*市场中，消化系统用药的销售占比为6.0%，市场规模达719.2亿，消化性溃疡、肝胆疾病、功能性胃肠道疾病和肠道疾病等不同类别用药的头部品种渠道分布特征各异。01整体市场萎缩乡镇卫生院渠道逆势而上数据显示，在新冠疫情、带量采购（VBP）、分级诊疗等政策的影响下，2022年我国全部医疗机构消化系统用药市场规模同比下降9.4%。可以看到除了乡镇卫生院外，2022年其他三个渠道均同比明显降低。2019-2022年乡镇卫生院一路逆势而上，获得了6.0%的年复合增长，到2022年占比达7.9%（图1）。图1-消化系统用药市场渠道格局变化趋势消化系统用药市场规模的萎缩主要受到VBP的影响。作为该领域占比最高的类别，消化性溃疡用药中的质子泵抑制剂（PPI）类药物如奥美拉唑、泮托拉唑、艾司奥美拉唑等品种近年来依次被纳入第3-5批VBP，到2022年消化性溃疡用药在总体医疗机构份额已降低到40%以下（图2）。图2-消化系统用药分类及总体医疗机构销售额分布变化2022年总体医疗机构消化系统用药市场中共有360多个品种。数据显示，消化性溃疡、肝胆疾病、功能性胃肠道疾病和肠道疾病等类别用药的头部品种渠道分布特征各异。02消化性溃疡用药多个品种广阔市场成绩亮眼在消化性溃疡用药销售额排名前十的品种中，法莫替丁注射剂、盐酸雷尼替丁注射剂、以及第3批VBP品种奥美拉唑胶囊在广阔市场（除城市医院渠道外）成绩亮眼，尤其在乡镇卫生院渠道贡献度远高于细分市场平均水平。口服剂型销售额较高的是雷贝拉唑钠肠溶片和雷贝拉唑钠肠溶胶囊，在社区卫生中心渠道销售贡献度较高（图3）。图3-2022年消化性溃疡用药头部品种渠道销售额分布03肝胆疾病用药普遍城市医院占比较高肝胆疾病用药的头部品种中，绝大部分在城市医院规模占比超过70%。县域医院贡献高于细分市场平均水平（18.6%）的是熊去氧胆酸片、水飞蓟宾胶囊和甘草酸二铵胶囊。另外值得关注的是，甘草酸单铵半胱氨酸注射剂在乡镇卫生院的占比较高（图4）。图4-2022年肝胆疾病用药头部品种渠道销售额分布04功能性胃肠道用药3个品种由广阔市场主导功能性胃肠道疾病用药头部品种中，枸橼酸莫沙必利片、多潘立酮片、甲氧氯普胺注射剂在广阔市场的规模占比高于核心市场。尤其是多潘立酮片，在城市医院份额只占11.3%（图5）。图5-2022年功能性胃肠道疾病用药头部品种渠道销售额分布05肠道疾病用药TOP3品种广阔市场贡献度高肠道疾病用药销售额排名前三位的品种都有较高的广阔市场贡献度。位于榜首的双歧杆菌三联活菌胶囊在社区卫生中心的占比达到23.3%，地衣芽孢杆菌活菌胶囊的乡镇卫生院渠道销售贡献占比为19.1%。县域医院渠道贡献较高的包括双歧杆菌四联活菌片和口服补液盐散剂等（图6）。图6-2022年肠道疾病用药头部品种渠道销售额分布06创新药：城市医院渠道依旧占绝对优势与老牌品种呈现的多样化渠道分布不同，新上市的创新品种主要还是在城市及县域医院放量。据不完全统计，2018-2022年药监局NMPA批准上市的消化系统创新品种主要有：止吐药和止恶心药市场的福沙匹坦双葡甲胺注射剂（2019年获批，目前市场中有江苏豪森、正大天晴、齐鲁制药和罗欣集团四家企业的产品）；消化性溃疡用药市场的依卡倍特钠颗粒剂（江苏亚邦集团2018年获批）；富马酸伏诺拉生片（武田2019年底获批）；功能性胃肠道疾病用药利那洛肽胶囊（阿斯利康2019年获批）；肠道疾病用药市场的维得利珠单抗注射剂（武田2020年获批）。以上新品种中，除江苏亚邦集团的独家仿制产品依卡倍特钠颗粒外，其余均已纳入国家医保目录。数据显示，从全部新品种的销售额渠道分布看，乡镇卫生院和社区卫生中心对大部分新产品的销售贡献仍然较小，城市医院在新产品销售贡献上占绝对优势，2022年占比仍然在90%以上。关注具体创新产品的渠道分布，获批较早的江苏亚邦的依卡倍特钠颗粒剂在县域医院获得了较高的销量占比，阿斯利康的利那洛肽胶囊在社区卫生中心取得了一部分销量（图7）。图7-2022年消化系统用药新上市品种（产品）销售额渠道分布在研产品中，目前处于临床III期，预计未来五年会上市的消化系统药物主要有治疗活动性溃疡性结肠炎的Etrasimod片（云屹药业）和Mirikizumab注射液（礼来）、适用于原发性胆汁性胆管炎的两个药品奥贝胆酸片（泰州复旦张江药业）和Linerixibat片（GSK）、治疗中重度克罗恩病的Risankizumab注射液（艾伯维）、以及适用于功能性便秘的普卡那肽片（美国synergy制药公司）。随着这些消化系统新药的上市，整体市场发展和渠道格局将持续发生变化。END来源 | 法伯科技Pharbers赛柏蓝药械交流群扫描下方二维码加入医药代理商转型交流群扫描下方二维码加入

100 项与依卡倍特钠相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D01991	-	A02B	DB05265

研发状态

批准上市

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
急性胃炎	日本	Mitsubishi Tanabe Pharma Corp.	1995-11-22
慢性胃炎	日本	Mitsubishi Tanabe Pharma Corp.	1995-11-22
胃溃疡	日本	Mitsubishi Tanabe Pharma Corp.	1993-10-01

未上市

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适应症	最高研发状态	国家/地区	公司	日期
溃疡性结肠炎	临床3期	日本	Mitsubishi Tanabe Pharma Corp.	-
干眼综合征	临床2期	美国	ISTA Pharmaceuticals, Inc.	-
干眼综合征	临床2期	日本	Senju Pharmaceutical Co., Ltd.	-

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适应症

分期

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT00667004 (CTgov)	临床2期	干眼综合征	183	Ecabet (Ecabet Ophthalmic Solution)	衊餘餘膚繭鹹簾廠鹹蓋(淵憲鹹顧遞鑰淵艱積糧) = 顧觸鬱範鹽構鑰憲積艱網糧膚製膚製構衊膚餘 (網糧製襯膚壓願築艱夢, 齋淵襯淵觸鏇艱蓋糧獵 ~ 餘構鬱壓壓鹽餘獵範觸) 更多	-	2020-09-03
				placebo (Vehicle)	衊餘餘膚繭鹹簾廠鹹蓋(淵憲鹹顧遞鑰淵艱積糧) = 願願齋鬱築糧築鏇衊積網糧膚製膚製構衊膚餘 (網糧製襯膚壓願築艱夢, 壓憲網製餘築網膚糧襯 ~ 網艱廠鏇廠遞鏇糧醖夢) 更多