SEPIMOSTAT

Details

Stereochemistry	ACHIRAL
Molecular Formula	C21H19N5O2
Molecular Weight	373.4079
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

NC(=N)C1=CC2=C(C=C1)C=C(OC(=O)C3=CC=C(NC4=NCCN4)C=C3)C=C2

InChI

InChIKey=QMRJOIUGPCVZPH-UHFFFAOYSA-N

InChI=1S/C21H19N5O2/c22-19(23)16-2-1-15-12-18(8-5-14(15)11-16)28-20(27)13-3-6-17(7-4-13)26-21-24-9-10-25-21/h1-8,11-12H,9-10H2,(H3,22,23)(H2,24,25,26)

HIDE SMILES / InChI

Molecular Formula	C21H19N5O2
Molecular Weight	373.4079
Charge	0
Count

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

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/1689782 | https://www.ncbi.nlm.nih.gov/pubmed/8185343 | https://www.ncbi.nlm.nih.gov/pubmed/10467964 | https://adisinsight.springer.com/drugs/800002018

Sepimostat (also known as FUT-187) was developed as a serine protease inhibitor including Clr, Cls, kallikrein, trypsin, plasmin, and thrombin. Sepimostat participated in early phase II clinical study on patients with reflux esophagitis. As a result, sepimostat could be used for postgastrectomy reflux esophagitis at the dose level of 300 mg/day or less. Experiments on rodents have shown that the drug could be also useful in the therapy of alcohol-induced pancreatitis. However, all these studies were discontinued.

Originator

Approval Year

PubMed

Title	Date	PubMed
Effect of sepimostat mesilate on experimental venous thrombosis in rats.	2001-02-01	11228342
Oral administration of sepimostat mesilate prevents acute alcohol pancreatic injury in rats.	1999-07	10467964
[Early phase II study of FUT-187 (sepimostat mesilate) on reflux esophagitis--mainly on postgastrectomy reflux esophagitis].	1994-05	8185343
[Reproductive and developmental toxicity studies of FUT-187. (V)--Perinatal and postnatal study in rats with oral administration of FUT-187].	1992-12	1296026
[Reproductive and developmental toxicity studies of FUT-187. (III)--Postnatal study in rat F1 offspring from dams treated orally with FUT-187 during the period of fetal organogenesis].	1992-12	1296025
Pharmacological studies on 6-amidino-2-naphthyl[4-(4,5-dihydro-1H-imidazol-2-yl)amino] benzoate dimethane sulfonate (FUT-187). I: Inhibitory activities on various kinds of enzymes in vitro and anticomplement activity in vivo.	1990-01	1689782

Sample Use Guides

In Vivo Use Guide

FUT-187 (SEPIMOSTAT) was administered orally at the dose of 300 mg/day or 400 mg/day four times daily, after meals and at bedtime, for 4 consecutive weeks

Route of Administration: Oral

Substance Class	Chemical Created by `admin` on `Mon Mar 31 18:28:50 GMT 2025` Edited by `admin` on `Mon Mar 31 18:28:50 GMT 2025`
Record UNII	5ZFR16F4QQ
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

SEPIMOSTAT [MI]

Preferred Name

English

SEPIMOSTAT

Official Name

English

sepimostat [INN]

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C783