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E3040 as dual 5-lipoxygenase and thromboxane A2 synthetase inhibitor

SUBMISSION ID 425

Contact Details

Provider Eisai Co., Ltd. - Eisai
Partnership Hub Coordinator Name BIO Ventures for Global Health
401 Terry Avenue North
Seattle, WA 98109
USA
Tel: +1 206 732 2122
info@bvgh.org

Submission Summary

TitleE3040 as dual 5-lipoxygenase and thromboxane A2 synthetase inhibitor
Executive Summary/Abstract E3040 were found in the course of developing anti-inflammatory drug candidates for the treatment of inflammatory bowel diseases. E30340 inhibits both 5-lipoxygenase and TXA2 synthetase in cell-free in vitro assay. E3040 also showed therapeutic effect in TNB/ethanol-induced chronic colitis model by oral administration.
Keywords IBD; 5-lipoxygenase; thromboxane A2 synthetase

Disease Selection

Disease Unknown
Comment
Name(s) of Infectious Organism(s)
Vector(s)
Human Target Organ(s)
Mechanism of Action (MoA)
Molecular or Cellular Target Name(s)

Type of Data

Type of Data Pre-Clinical Candidate










PRE-CLINICAL CANDIDATE DATA SUBFIELDS

Pre-Clinical Candidate Description

 
Strategy for selecting Pre-Clinical Candidate
Origin of Pre-Clinical Lead and Lead Series
How many Pre-Clinical Candidates have been Selected?
How many Pre-Clinical Candidates Abandoned?
Reason for Abandoning
How many Pre-Clinical Candidates Untouched?
Reason for Not Pursuing

Pre-Clinical Chemistry Description

 
Chemistry approach(es) to Pre-Clinical Candidate
Chemical structure(s) of Pre-Clinical Candidate
C125_E3040.pdf
SAR analysis summary
Scale-up synthesis route

Pre-Clinical Candidate Profile

 
Potency IC50 for 5-lipoxygenase 0.23 microM RBL-1 ; IC50 for thromboxane A2 synyhetase 0.009 micro M ; Rat TNB/Ethanol-Induced Colitis Modela in vivo 61 percent inhibition at 100mg/kg/day
Off-target Activity
Animal Model/Data Description
In Vitro & In Vivo PK/PD
Solubility
Non-GMP/GMP Animal Tox and DMPK Data Summary
Safety Summary
Formulation
Other

Pre-Clinical Compound Availability

 
Quantity Produced in grams
Quantity Available in grams 0.01

Mechanism of Action (MoA)

 
Is the Mechanism of Action Known? No

Collaboration Status

 
In house only Yes

Publication/Patent Status

 
Proprietary Data Yes
Publicly Available Data (Reference) J. Med. Chem. 1994,37, 3062-3070.; British Journal of Pharmacology 2002 136, 383 -390.
Patented Data (Reference)