Drug intelligence / Profile preview

E7107

Development stage
Phase 1
Lead developer
Eisai
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Intravenous
01

Overview

E7107 is a semisynthetic derivative of pladienolide B, a natural product originally isolated from Streptomyces platensis. It is the first-in-class small molecule inhibitor targeting the spliceosome, specifically binding to Splicing factor 3B subunit 1 (SF3B1). By inhibiting SF3B1, E7107 blocks normal pre-mRNA splicing in oncogenes, leading to antitumor effects. The drug was developed as an anticancer agent and underwent Phase I clinical trials for advanced solid tumors. However, its development was suspended due to unacceptable adverse events, including cases of vision loss and severe gastrointestinal toxicity[1][4][6][7].

02

Targets

SF3B1 (Splicing factor 3B subunit 1)

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