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E5700 as squalene synthase 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

TitleE5700 as squalene synthase inhibitor
Executive Summary/Abstract Through the exploratory research for treatment of hypolipidemia, E5700 was found to be a novel squalene synthase inhibitor, E5700 possesses potent squalene synthase inhibitory activity and shows inhibitory activity to hepatic cholesterol biosynthesis in rats. It is also reported that E5700 possesses some activities against Leishmania amazonensis, Toxoplasma gondii tachyzoites, and Trypanosoma cruzi.
Keywords Toxoplasma; squalene; Trypanosoma; Leishmania; synthase

Disease Selection

Disease Chagas disease (American trypanosomiasis);Leishmaniasis
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 IC50 for squalene synthase in liver microsomes isolated from human=0.332 nM 2 ED50 for hepatic cholesterol biosynthesis in rats inhibited=0.52 mg/kg. 3 Low nanomolar IC50 range for antiproliferative effects against promastigotes and intracellular amastigotes of Leishmania amazonensis Josefaa 4 IC50 for anti-Toxoplasma gondii arresting parasite growth =0.23 micro M 5 Dose dependent effect on parasitemia and survival in murine model of acute Chagas disease.
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
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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) Antimicrobial Agent Chemotherapy. 2004, p. 2379–2387.; J. Antimicrobial Chemotherapy. 2006, 58, 59–65.; Antimicrobial Agent Chemotherapy. 2008, 4098–4114.
Patented Data (Reference)