Multiple modes of action of eribulin mesylate: Emerging data and clinical implications

Cancer Treatment Reviews
Javier CortésBruce A Littlefield

Abstract

Eribulin mesylate (eribulin) is a synthetic analogue of the marine-sponge natural product halichondrin B. Eribulin exhibits potent antiproliferative activities against a variety of human cancer cell types in vitro and in vivo, and is used for the treatment of certain patients with advanced breast cancer or liposarcoma who are refractory to other treatments. The antiproliferative effects of eribulin have long been attributed to its antimitotic activities. Unlike other microtubule-targeting agents, eribulin inhibits microtubule polymerization through specific plus end binding, thus interfering with microtubule dynamic instability. Non-mitotic effects of eribulin on tumor biology have also been established in laboratory settings including: tumor vasculature remodeling, increased vascular perfusion, reduced hypoxia, and phenotypic changes involving reversal of epithelial-to-mesenchymal transition (EMT), resulting in reduced capacities for migration, invasion, and seeding lung metastases in experimental models. Preclinical data suggest that increased perfusion following eribulin treatment improves delivery of subsequent drugs. Supporting evidence for eribulin's non-mitotic effects in the clinical setting include increased tumor oxyg...Continue Reading

Citations

Dec 21, 2019·Future Oncology·Anna PaioliAlessandra Longhi
Nov 30, 2019·International Journal of Molecular Sciences·Olga MéndezJosep Villanueva
May 21, 2019·Expert Opinion on Drug Safety·Jose Manuel Perez-Garcia, Javier Cortes
Jul 3, 2019·Cancers·Sara El-SahliSheng Liu
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