title: Eribulin mesylate.
abstract: Eribulin mesylate, a nontaxane, completely synthetic microtubule inhibitor, has recently been approved by the U.S. Food and Drug Administration as third-line treatment of metastatic breast cancer refractory to anthracyclines and taxanes. Eribulin is a synthetic analogue of halichondrin B, which inhibits microtubule polymerization by a mechanism distinct from other available antitubulin agents. Eribulin significantly increased overall survival (OS; median OS for the eribulin-treated group was 13.1 months versus 10.6 months for the group treated by investigator's choice) in a heavily pretreated metastatic breast cancer population. Eribulin has a manageable side-effect profile, notably neutropenia and fatigue, and a relatively low incidence of peripheral neuropathy. The mechanism of action, pharmacokinetics, preclinical antitumor activity, and clinical trials of eribulin in the metastatic breast cancer setting are reviewed here.
authors.affiliation: Department of Medicine, Division of Hematology and Oncology, Weill Cornell Medical College, New York, New York 10065, USA.
authors.forename: Sarika
authors.initials: S
authors.lastname: Jain
authors.forename: Linda T
authors.initials: LT
authors.lastname: Vahdat
mesh_terms: D000970:Antineoplastic Agents / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000627:therapeutic use; D001943:Breast Neoplasms / Q000188:drug therapy* / Q000378:metabolism; D002986:Clinical Trials as Topic; D005260:Female; D005663:Furans / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000627:therapeutic use; D006801:Humans; D007659:Ketones / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000627:therapeutic use; D008698:Mesylates / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000627:therapeutic use; D000095662:Polyether Polyketides
chemical_list: D000970:Antineoplastic Agents; D005663:Furans; D007659:Ketones; D008698:Mesylates; C490954:eribulin; D000095662:Polyether Polyketides