Delving into the Latest Updates on Egualen Sodium Hydrate with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Azuletil, Egualen, Egualen sodium

+ [7]

Target

TBXA2R

Mechanism

TBXA2R antagonists(Thromboxane A2 receptor antagonists)

Therapeutic Areas

Digestive System Disorders

Active Indication

Stomach Ulcer

Inactive Indication-

Originator Organization

Kotobuki Pharmaceutical Co. Ltd.

Active Organization

Kotobuki Pharmaceutical Co. Ltd.

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date

JP (12 Mar 1999),

Stomach Ulcer

Regulation-

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Structure

Molecular FormulaC15H18NaO3S

InChIKeyZIPRJZAWCYYGAV-UHFFFAOYSA-N

CAS Registry97683-31-3

View All Structures (3)

Author: Kawakami, Ken ; Kuramoto, Takanori ; Iguchi, Munetaka ; Kubota, Minori ; Edogawa, Shoko ; Nouda, Sadaharu ; Nakazawa, Kei ; Sakanaka, Taisuke ; Okada, Toshihiko ; Higuchi, Kazuhide ; Kakimoto, Kazuki ; Kojima, Yuichi ; Hirata, Yuki ; Takeuchi, Toshihisa ; Inoue, Takuya ; Harada, Satoshi ; Ota, Kazuhiro ; Fujiwara, Kaori

Low-dose aspirin, which is widely used to reduce the risk of cardio- and cerebrovascular thrombosis, often induces gastroenteropathy by increasing the permeability of the mucosa. However, therapeutic strategies for patients with low-dose aspirin-induced small intestinal injury have not been determined. We evaluated the preventative effect of egualen sodium hydrate, a gastro-protective agent that suppresses indomethacin-induced small-intestinal damage in rats, against small-intestinal mucosal damage induced by low-dose aspirin in healthy adult male volunteers. Participants were randomly allocated to receive aspirin 100 mg/kg daily (control group, n = 10) or aspirin 100 mg/kg plus egualen sodium 30 mg daily (egualen sodium group, n = 10). Small intestinal mucosal injury was evaluated by capsule endoscopy two weeks after initiation of drug administration. Fecal analyses (occult blood test, immunochemical test, transferrin measurement and calprotectin measurement) were carried out before and after treatment. Egualen sodium significantly suppressed the total number of small intestinal injuries detected by capsule endoscopy and the positive ratio for the fecal occult blood test. Daily use of 30 mg of egualen sodium showed a preventative effect on low-dose aspirin-induced small intestinal injury. Since acid suppression therapy was reported to exacerbate NSAIDs-induced enteropathy via dysbiosis, egualen sodium may be useful for patients treated with low-dose aspirin.

01 Feb 2013·Journal of physiology and pharmacology : an official journal of the Polish Physiological Society

Prophylactic effect of egualen sodium, a stable azulene derivative, on gastrointestinal damage induced by ischemia/reperfusion, double antiplatelet therapy and loxoprofen in rats.

Article

Author: Takeuchi, K ; Hara, D ; Murakami, T ; Amagase, K ; Yoshida, Y

We examined the effect of egualen, a stable azulene derivative, against gastric damage induced by ischemia/reperfusion (I/R), gastric bleeding induced by double antiplatelet therapy with aspirin (ASA) plus clopidogrel, and small intestinal damage generated by loxoprofen, and investigated the possible mechanisms involved in its protective action. Male C57BL/6 mice or SD rats were used under urethane anesthesia (gastric lesions) or in a conscious (intestinal lesions) state. I/R-induced gastric injury was produced in mice by clamping the celiac artery for 30 min, followed by reperfusion for 60 min. Gastric bleeding was induced in rats by luminal perfusion with 25 mM ASA+50 mM HCl for 2 hours in the presence of clopidogrel (30 mg/kg). To produce small intestinal lesions the rats were given loxoprofen (60 mg/kg) p.o. and killed 24 hours later. Egualen was given i.d. 60 min before I/R or ASA perfusion, while given p.o. twice 30 min before and 6 hours after loxoprofen. Egualen significantly prevented the I/R-induced gastric damage, and the effect was equivalent to that of seratrodast (TXA2 antagonist). This agent also significantly suppressed gastric bleeding induced by ASA plus clopidogrel, similar to PGE2. Likewise, egualen significantly prevented loxoprofen-induced damage in the small intestine, accompanied by an increase in the secretion of mucus and suppression of bacterial invasion as well as iNOS expression. These results suggest that egualen has a prophylactic effect against various lesions in the gastrointestinal mucosa, probably through its characteristic pharmacological properties, such as TXA2 antagonistic action, local mucosal protection, and stimulation of mucus secretion.

01 Jan 2001·PharmacologyQ4 · MEDICINE

Inhibitory Effect of Egualen Sodium: A New Stable Derivative of Azulene on Histamine Release from Mast Cell-Like Cells in the Stomach

Q4 · MEDICINE

Article

Author: Akagi, Masaaki ; Mochizuki, Seiichiro ; Tasaka, Kenji ; Matsui, Nobuaki

We studied the inhibitory effect of egualen sodium (ES) (sodium 3-ethyl-7-isopropyl-1-azulenesulfonate 1/3 hydrate, KT1–32), a new derivative and more stable compound than azulene, on histamine release from the mucosal histaminocytes and elucidated the mechanism for this action. ES prevented the histamine release from isolated mast cell-like cells of the guinea pig stomach induced by A23187 in a dose-dependent fashion. ES dose-dependently inhibited the histamine release from lung pieces of sensitized guinea pigs induced by an antigen-antibody reaction. ES also inhibited histamine release from rat peritoneal mast cells induced by compound 48/80 or antigen-antibody reaction. ES exhibited the membrane stabilizing activity on DPPC liposomes. These findings suggest that ES may prevent histamine release from histaminocytes induced by various stimuli and the stabilizing action of the cell membrane may be responsible for the inhibition of histamine release.

100 Deals associated with Egualen Sodium Hydrate

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