Delving into the Latest Updates on Ecabet Sodium Hydrate with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Ecabet, Ecabet Sodium, Ecabet Sodium Granules

+ [7]

Target-

Mechanism

Urease inhibitors

Therapeutic Areas

Digestive System Disorders

Active Indication

Acute gastritisChronic gastritisStomach Ulcer

Inactive Indication

Colitis, UlcerativeDry Eye Syndromes

Originator Organization

Mitsubishi Tanabe Pharma Corp.

Active Organization

Mitsubishi Tanabe Pharma Corp.BCWORLD PHARM. Co., Ltd.

Inactive Organization

Senju Pharmaceutical Co., Ltd.

ISTA Pharmaceuticals, Inc.

Drug Highest PhaseApproved

First Approval Date

JP (01 Oct 1993),

Stomach Ulcer

Regulation-

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Structure

Molecular FormulaC20H28NaO5S

InChIKeyJNTMHWBQZJIWMT-YGJXXQMASA-N

CAS Registry86408-72-2

View All Structures (2)

SummarySelaginella 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.

01 May 2020·European Journal of PharmacologyQ3 · MEDICINE

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

Q3 · MEDICINE

Article

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

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.

01 Dec 2019·BMC GastroenterologyQ3 · MEDICINE

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

Q3 · MEDICINE

ArticleOA

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

BACKGROUNDWe aimed to investigate how high-dose ecabet sodium affects low-dose aspirin-induced small intestinal mucosal injury in healthy volunteers.METHODSHealthy 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.RESULTSA 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).CONCLUSIONSEcabet sodium had a preventive effect on low-dose aspirin-induced small intestinal mucosal injury in the upper part of the small intestine.TRIAL REGISTRATIONISRCTN 99322160 , 01/10/2018.

100 Deals associated with Ecabet Sodium Hydrate

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External Link

KEGG	Wiki	ATC	Drug Bank
D01991	-	A02B	DB05265

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Acute gastritis	JP	Mitsubishi Tanabe Pharma Corp.	22 Nov 1995
Chronic gastritis	JP	Mitsubishi Tanabe Pharma Corp.	22 Nov 1995
Stomach Ulcer	JP	Mitsubishi Tanabe Pharma Corp.	01 Oct 1993

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Colitis, Ulcerative	Phase 2	JP	Mitsubishi Tanabe Pharma Corp.	-
Dry Eye Syndromes	Phase 2	US	ISTA Pharmaceuticals, Inc.	-
Dry Eye Syndromes	Phase 2	JP	Senju Pharmaceutical Co., Ltd.	-

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT00667004 (CTgov)	Phase 2	Dry Eye Syndromes	183	Ecabet (Ecabet Ophthalmic Solution)	lpfvpykayu(cpubnpjond) = flwixcdypb kmqdqwbjik (lauesaqpdg, napnctagce - bnolbrurmj) View more	-	03 Sep 2020
				placebo (Vehicle)	lpfvpykayu(cpubnpjond) = zntbdbwphz kmqdqwbjik (lauesaqpdg, hjvskrtsss - qbjlaodjky) View more