Eribulin mesilate - Antimitotic drug tubulin polymerization inhibitor oncolytic

The natural compound halichondrin B demonstrated promising anticancer activity in vitro and in vivo, but insufficient natural sources of halichondrin B limited its therapeutic application. Eribulin mesilate (E-7389), a structurally optimized synthetic analogue of halichondrin 13, retained the natural compound's subnanomolar anticancer activity in vitro. The agent also induced marked tumor regression in a variety of human tumor xenograft models in vivo. Preclinical studies demonstrated that eribulin exerted its anticancer activity via a tubulin-based mechanism leading to disruption of the mitotic spindle, mitotic arrest and cancer cell apoptosis. Eribulin exhibits rapid and extensive tissue distribution and a long terminal half-life in animals (rats and dogs) and in patients with refractory or advanced solid tumors. Eribulin showed promising anticancer efficacy in patients with refractory or advanced tumors who had previously received chemotherapy. It has also demonstrated synergistic effects when combined with gemcitabine, cisplatin, epirubicin, trastuzumab, docetaxel and vinorelbine.