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E3040 as dual 5-lipoxygenase and thromboxane A2 synthetase inhibitor


Contact Details

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

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
Name(s) of Infectious Organism(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 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
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
Non-GMP/GMP Animal Tox and DMPK Data Summary
Safety Summary

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)