Egualen Sodium Hydrate(Egualen Sodium Hydrate) - 药物靶点：TBXA2R_在研适应症：胃溃疡_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Azuletil、Egualen、Egualen sodium

+ [7]

靶点

TBXA2R

作用方式

拮抗剂

作用机制

TBXA2R拮抗剂(血栓素A2受体拮抗剂)

治疗领域

消化系统疾病

在研适应症

胃溃疡

非在研适应症-

原研机构

Kotobuki Pharmaceutical Co. Ltd.

在研机构

Kotobuki Pharmaceutical Co. Ltd.

非在研机构-

最高研发阶段批准上市

首次获批日期

日本 (1999-03-12),

胃溃疡

最高研发阶段(中国)-

特殊审评-

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结构/序列

分子式C15H18NaO3S

InChIKeyZIPRJZAWCYYGAV-UHFFFAOYSA-N

CAS号97683-31-3

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关联

2

项与 Egualen Sodium Hydrate 相关的临床试验

JPRN-UMIN000005599

/ CompletedN/AIIT

Investigation of the effect of the Egualen Sodium Hydrate mouthwash on the stomatitis induced by the gastroenterological cancer chemotherapy - Investigation of the effect of the Egualen Sodium Hydrate mouthwash on the stomatitis induced by the gastroenterological cancer chemotherapy

开始日期2011-06-01

申办/合作机构-

JPRN-UMIN000005429

/ RecruitingN/AIIT

Comparison of PPI with H2RA plus egualen sodium combination therapy for the artificial ulcer after ESD - Comparison of PPI with H2RA plus egualen sodium combination therapy for the artificial ulcer after ESD

开始日期2010-09-01

申办/合作机构

Kagawa University

100 项与 Egualen Sodium Hydrate 相关的临床结果

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100 项与 Egualen Sodium Hydrate 相关的转化医学

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100 项与 Egualen Sodium Hydrate 相关的专利（医药）

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50

项与 Egualen Sodium Hydrate 相关的文献（医药）

2022-07-01·European Journal of Medicinal Chemistry1区 · 医学

The azulene scaffold from a medicinal chemist's perspective: Physicochemical and in vitro parameters relevant for drug discovery

1区 · 医学

Article

作者: Yli-Kauhaluoma, Jari ; Kley, Jörg T ; Sieger, Peter ; Leino, Teppo O ; Wallén, Erik A A

Azulene is a bicyclic scaffold rarely applied in medicinal chemistry. Here we report physicochemical and in vitro parameters relevant for drug discovery for a series of diversely substituted azulenes. We synthesized and characterized several scaffold hopping series of analogously substituted azulenes, indoles and naphthalenes. This enabled a comparison of azulene with the more common scaffolds indole and naphthalene. Our data indicates that undesirably low photostability of azulenes is restricted to certain substitution patterns. Generally, we conclude that azulene is an underused lipophilic bicycle and should be considered as a valuable complement to the collection of medicinal chemistry scaffolds.

2018-01-01·Journal of Clinical Biochemistry and Nutrition4区 · 医学

Effect of egualen sodium hydrate on small-intestinal mucosal damage induced by low-dose aspirin: a prospective randomized clinical trial

4区 · 医学

Article

作者: Kawakami, Ken ; Kuramoto, Takanori ; Iguchi, Munetaka ; Kubota, Minori ; Nakazawa, Kei ; Nouda, Sadaharu ; Edogawa, Shoko ; Sakanaka, Taisuke ; Okada, Toshihiko ; Higuchi, Kazuhide ; Kakimoto, Kazuki ; Kojima, Yuichi ; Hirata, Yuki ; Inoue, Takuya ; Takeuchi, Toshihisa ; 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.

2015-06-26·Journal of Natural Products2区 · 生物学

Analysis of Physicochemical Properties for Drugs of Natural Origin

2区 · 生物学

Article

作者: Campitelli, Marc ; Camp, David ; Garavelas, Agatha

The impact of time, therapy area, and route of administration on 13 physicochemical properties calculated for 664 drugs developed from a natural prototype was investigated. The mean values for the majority of properties sampled over five periods from pre-1900 to 2013 were found to change in a statistically significant manner. In contrast, lipophilicity and aromatic ring count remained relatively constant, suggesting that these parameters are the most important for successful prosecution of a natural product drug discovery program if the route of administration is not focused exclusively on oral availability. An examination by therapy area revealed that anti-infective agents had the most differences in physicochemical property profiles compared with other areas, particularly with respect to lipophilicity. However, when this group was removed, the variation between the mean values for lipophilicity and aromatic ring count across the remaining therapy areas was again found not to change in a meaningful manner, further highlighting the importance of these two parameters. The vast majority of drugs with a natural progenitor were formulated for either oral and/or injectable administration. Injectables were, on average, larger and more polar than drugs developed for oral, topical, and inhalation routes.

100 项与 Egualen Sodium Hydrate 相关的药物交易

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