CETRAXATE HYDROCHLORIDE

Possibly Marketed Outside US

Details

Stereochemistry	ACHIRAL
Molecular Formula	C17H23NO4.ClH
Molecular Weight	341.83
Optical Activity	UNSPECIFIED
Defined Stereocenters	2 / 2
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

Cl.NC[C@H]1CC[C@@H](CC1)C(=O)OC2=CC=C(CCC(O)=O)C=C2

InChI

InChIKey=USROQQUKEBHOFF-SKKCDYJJSA-N

InChI=1S/C17H23NO4.ClH/c18-11-13-1-6-14(7-2-13)17(21)22-15-8-3-12(4-9-15)5-10-16(19)20;/h3-4,8-9,13-14H,1-2,5-7,10-11,18H2,(H,19,20);1H/t13-,14-;

HIDE SMILES / InChI

Molecular Formula	C17H23NO4
Molecular Weight	305.3688
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	2 / 2
E/Z Centers	0
Optical Activity	UNSPECIFIED

Molecular Formula	ClH
Molecular Weight	36.461
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: http://www.rad-ar.or.jp/siori/english/kekka.cgi?n=1931
Curator's Comment: description was created based on several sources, including: http://www.229877.com/article/2016/0303/article_36173.html | https://www.ncbi.nlm.nih.gov/pubmed/4261023

Cetraxate is an oral gastrointestinal medication, mucosal protectant. Cetraxate might indirectly stimulate capsaicin-sensitive afferent nerves and increase mucosal blood flow, and that this may be a key mechanism underlying its gastroprotective action. Cetraxate prevents gastric mucosal blood flow decrease in H. pylori-infected patients. It is usually used to improve gastric mucosal lesion in acute gastritis or acute exacerbation of chronic gastritis and to treat gastric ulcer. The most commonly reported adverse reactions include constipation, rash, nausea, vomiting, dry mouth and diarrhea.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Trypsin 7 Target ID: CHEMBL2095204 Sources: https://www.ncbi.nlm.nih.gov/pubmed/4261023	Inhibitor 8504
UDP-galactosyltransferase (rat) 2 Target ID: UDP-galactosyltransferase (rat) Sources: https://www.ncbi.nlm.nih.gov/pubmed/9359921	Activator 1447
Prostaglandin Synthesis and Regulation 6 Target ID: WP1111 Sources: http://en.pharmacodia.com/web/drug/1_18820.html \| https://www.ncbi.nlm.nih.gov/pubmed/2305206	Modulator 846

Conditions

Condition	Modality	Targets	Highest Phase	Product
Gastritis 46 Sources: http://www.rad-ar.or.jp/siori/english/kekka.cgi?n=1931	Primary		Approved 8583	Neuer Approved Use It is usually used to improve gastric mucosal lesion in acute gastritis or acute exacerbation of chronic gastritis and to treat gastric ulcer.
Gastric ulcer 74 Sources: http://www.rad-ar.or.jp/siori/english/kekka.cgi?n=1931	Primary		Approved 8583	Neuer Approved Use It is usually used to improve gastric mucosal lesion in acute gastritis or acute exacerbation of chronic gastritis and to treat gastric ulcer.

C_max

Value	Dose	Co-administered	Analyte	Population
1.75 μg/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/4/530258_2329004C1129_4_002_1F.pdf#page=19	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:		TRANEXAMIC ACID plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status:

T_1/2

Value	Dose	Co-administered	Analyte	Population
1.73 h OTHER GOV'T https://www.info.pmda.go.jp/go/interview/4/530258_2329004C1129_4_002_1F.pdf#page=19	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:		TRANEXAMIC ACID plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status:

Doses

Dose	Population	Adverse events
200 mg 4 times / week multiple, oral Studied dose Dose: 200 mg, 4 times / week Route: oral Route: multiple Dose: 200 mg, 4 times / week Sources: https://pubmed.ncbi.nlm.nih.gov/7881024/	unhealthy Health Status: unhealthy Sex: M+F Food Status: FED Sources: https://pubmed.ncbi.nlm.nih.gov/7881024/	Other AEs: Facial flushing, Dizziness... Other AEs: Facial flushing (1 pt) Dizziness (1 pt) Sources: https://pubmed.ncbi.nlm.nih.gov/7881024/

AEs

AE	Significance	Dose	Population
Dizziness	1 pt	200 mg 4 times / week multiple, oral Studied dose Dose: 200 mg, 4 times / week Route: oral Route: multiple Dose: 200 mg, 4 times / week Sources: https://pubmed.ncbi.nlm.nih.gov/7881024/	unhealthy Health Status: unhealthy Sex: M+F Food Status: FED Sources: https://pubmed.ncbi.nlm.nih.gov/7881024/
Facial flushing	1 pt	200 mg 4 times / week multiple, oral Studied dose Dose: 200 mg, 4 times / week Route: oral Route: multiple Dose: 200 mg, 4 times / week Sources: https://pubmed.ncbi.nlm.nih.gov/7881024/	unhealthy Health Status: unhealthy Sex: M+F Food Status: FED Sources: https://pubmed.ncbi.nlm.nih.gov/7881024/

PubMed

Title	Date	PubMed
Gastroduodenal mucosal injury in patients taking low-dose aspirin and the role of gastric mucoprotective drugs: possible effect of rebamipide.	2010-07	20664727
Rebamipide: a gastrointestinal protective drug with pleiotropic activities.	2010-06	20528113
[Side effects of gastric muco-protective agents].	2007-10-28	18074538
Are gastroprotective drugs useful for gastric ulcer healing: re-evaluation using current ICH E9 guidelines.	2007-02	17323190
[Eradication therapy for the remnant stomach infected with Helicobacter pylori ].	2005-11	16363583
[Cetraxate hydrochloride (Neuer) induces the effectiveness of new triple therapy in H. pylori eradication].	2005-11	16363579
Comparison of the effects of cytoprotective drugs on human plasma adrenocorticotropic hormone and cortisol levels with continual stress exposure.	2005-11	16272707
15th anniversary of rebamipide: looking ahead to the new mechanisms and new applications.	2005-10	16184418
Efficacy of triple therapy plus cetraxate for the Helicobacter pylori eradication in partial gastrectomy patients.	2005-05	15906755
DA-9601 for erosive gastritis: results of a double-blind placebo-controlled phase III clinical trial.	2004-08-15	15285023
Comparison of cetraxate-based and pantoprazole-based triple therapies in the treatment of Helicobacter pylori infection.	2004-04	15244013
Cetraxate raises levels of calcitonin gene-related peptide and substance P in human plasma.	2004-04	15099451
Biocatalytic deprotection of a cetraxate ester by Microbacterium sp. strain 7-1W cells.	2003-01	12619695
Enzymatic preparation of D-beta-acetylthioisobutyric acid and cetraxate hydrochloride using a stereo- and/or regioselective hydrolase, 3,4-dihydrocoumarin hydrolase from Acinetobacter calcoaceticus.	2002-11	12436309
Purification and characterization of a novel esterase promising for the production of useful compounds from Microbacterium sp. 7-1W.	2002-01-10	11814667
Influence of Helicobacter pylori infection and cetraxate on gastric mucosal blood flow during healing of endoscopic mucosal resection-induced ulcers.	2001-11	11903737

Patents

Sample Use Guides

In Vivo Use Guide

200 mg 3-4 times per day

Route of Administration: Oral

In Vitro Use Guide

The amounts of Cetraxate to prolong the recalcification time of citrated plasma to 2 times were approximately 50 ug in the ordinary glass tube and 25 ug in the siliconized tube.

Substance Class	Chemical Created by `admin` on `Mon Mar 31 17:47:17 GMT 2025` Edited by `admin` on `Mon Mar 31 17:47:17 GMT 2025`
Record UNII	08IT6P8VHY
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

NEUER

Preferred Name

English

CETRAXATE HYDROCHLORIDE

Official Name

English

BENZENEPROPANOIC ACID, 4-(((4-(AMINOMETHYL)CYCLOHEXYL)CARBONYL)OXY)-, HYDROCHLORIDE, TRANS-

Common Name

English

DV-1006

Code

English

P-HYDROXYHYDROCINNAMIC ACID TRANS-4-(AMINOMETHYL)CYCLOHEXANECARBOXYLATE, HYDROCHLORIDE

Common Name

English

CETRAXATE HCL

Common Name

English

CETRAXATE HYDROCHLORIDE [USAN]

Common Name

English

CETRAXATE HYDROCHLORIDE [JAN]

Common Name

English

CETRAXATE HYDROCHLORIDE [MART.]

Common Name

English

CETRAXATE HYDROCHLORIDE [MI]

Common Name

English

Cetraxate hydrochloride [WHO-DD]

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C28197