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E4010 as phosphodiesterase type V 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

TitleE4010 as phosphodiesterase type V inhibitor
Executive Summary/Abstract E4010 selectively and potently inhibited PDE5 isolated from porcine platelet. E4010 markedly reduced the increased pulmonary arterial pressure with a slight effect on systemic arterial pressure in the porcine model of heart failure. Thus,E4010 would be useful for the treatment of patients with pulmonary hypertension.
Keywords PDE5; phosphodiesterase; hypertension

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

Off-target Activity
Animal Model/Data Description 1 Long-term E4010 administration tomonocrotaline induced pulmonary hypertensive rats improved mortality. 2 E-4010, caused selective pulmonary vasodilation and attenuated the increase in pulmonary arterial pressure right ventricular hypertrophy, and pulmonary arterial remodeling induced by chronic hypoxia.
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) Jpn J Pharmacol. 77, 99-102, 1998.; Am. J. Physiol. 277 Lung Cell. Mol. Physiol. 21 : L225–L232, 1999.
Patented Data (Reference)