Drug intelligence / Profile preview

eribulin liposomal (Eisai Co., Ltd.)

Development stage
Unknown
Lead developer
Eisai
Modality
Small Molecules, Nanoparticles → Drug Delivery Systems
Administration
Intravenous
01

Overview

Eribulin liposomal (E7389-LF) is a liposome-encapsulated formulation of eribulin, a non-taxane microtubule dynamics inhibitor originally derived from the marine sponge natural product halichondrin B. Developed by Eisai, this formulation utilizes a lipid bilayer to encapsulate eribulin, which enhances its concentration and retention in tumor tissues via the enhanced permeability and retention (EPR) effect. Eribulin liposomal exerts its antineoplastic effects by binding to the plus ends of microtubules, inhibiting their growth phase and sequestering tubulin into nonfunctional aggregates, which leads to G2/M phase cell cycle arrest and apoptosis. In addition to its direct cytotoxic effects, eribulin liposomal promotes tumor vascular remodeling and immunomodulatory activity, converting immune 'cold' tumors into 'hot' tumors by increasing the infiltration of CD8+ T cells and natural killer (NK) cells. It is being evaluated in clinical trials as a monotherapy and in combination with immune checkpoint inhibitors like nivolumab for various solid tumors, including gastric cancer, esophageal cancer, small cell lung cancer, and breast cancer.

Other names
eribulin liposomal formulationeribulin-LFliposomal eribulin
02

Targets

TUBB (Tubulin (alpha and beta subunits))

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