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E2011: Monoamine Oxidase A selective inhibitor

SUBMISSION ID 442

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

TitleE2011: Monoamine Oxidase A selective inhibitor
Executive Summary/Abstract E2011, a MAO-A inhibitor which has been developed for treament of depression, inhibits MAO-A selectively 30,000 times more than MAO-B in rat brain homogenate. E2011 is effective in animal (mice) at a dose of 0.3mg/kg p.o..
Keywords MAO, depression; monoamine oxidase

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_E2011.pdf
SAR analysis summary
Scale-up synthesis route

Pre-Clinical Candidate Profile

 
Potency IC50=30nM for rat MAO-A and 920 microM for rat MAO-B. E2011 was active in mice from 0.3 mg/kg p.o.
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 of Pharmacol and Exp. Ther. 278, 243-251 1996
Patented Data (Reference)