Drug intelligence / Profile preview

eribulin liposomal

Development stage
Phase 1
Lead developer
Eisai
Modality
Nanoparticles → Drug Delivery Systems, Small Molecules
Administration
Intravenous
01

Overview

Eribulin liposomal is a liposome-encapsulated formulation of the halichondrin-class microtubule dynamics inhibitor eribulin mesylate, engineered to enhance tumor delivery and exposure via the enhanced permeability and retention effect in solid tumors.[3][9][14] Like conventional eribulin, it binds to the vinca domain of tubulin to inhibit tubulin polymerization and microtubule assembly, leading to G2/M cell-cycle arrest and apoptosis, while also exerting non-mitotic effects such as vascular remodeling, reversal of epithelial–mesenchymal transition, and immunomodulation within the tumor microenvironment.[3][13] Liposomal encapsulation improves the pharmacokinetic profile and antitumor activity compared with standard eribulin in preclinical models, and early-phase clinical studies (e.g., E7389-LF) have shown manageable safety and encouraging activity in heavily pretreated patients with advanced solid tumors, including gastric and other cancers, supporting further development as an intravenous antineoplastic agent.[3][5][7][9][14]

Other names
eribulin liposomalliposomal eribulinliposomal eribulin mesylate
02

Targets

TUBB (Tubulin (alpha and beta subunits))

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