title: Eribulin.
abstract: Eribulin (eribulin mesylate) is a non-taxane microtubule dynamics inhibitor with tubulin-based antimitotic activity and chemotherapeutic effects. Eribulin is used in the treatment of patients with locally advanced or metastatic breast cancer who have previously been treated with at least two chemotherapeutic regimens, including an anthracycline and a taxane. In in vitro studies, eribulin displayed antiproliferative activity against human breast cancer cell lines. Regression and elimination of breast tumours were observed in human tumour xenograft models. In the randomized, open-label, multinational, phase III EMBRACE trial in patients with locally recurrent or metastatic breast cancer, median overall survival was significantly longer in patients who received intravenous eribulin (n = 508) [13.1 months] compared with that in patients who received a treatment of physician's choice (n = 254) [10.6 months; hazard ratio 0.81; 95% CI 0.66, 0.99; p = 0.041]. Prior to enrolment, study participants had received between two and five chemotherapeutic regimens, including an anthracycline and a taxane. Consistent with the findings of earlier phase I and II trials, eribulin was reported to have a manageable tolerability profile in the EMBRACE trial. Peripheral neuropathy (incidence 5%) was the most common adverse event resulting in the discontinuation of eribulin treatment. The most common grade 3/4 adverse events in the eribulin group were neutropenia, leukopenia and asthenia or fatigue.
authors.affiliation: Adis, a Wolters Kluwer Business, Auckland, New Zealand. demail@adis.co.nz
authors.forename: Caroline M
authors.initials: CM
authors.lastname: Perry
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use*; D001943:Breast Neoplasms / Q000188:drug therapy* / Q000473:pathology; D005260:Female; D005663:Furans / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use*; D006801:Humans; D007659:Ketones / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use*; D008870:Microtubules / Q000187:drug effects / Q000378:metabolism; D014404:Tubulin / Q000378:metabolism; D000095662:Polyether Polyketides
chemical_list: D000970:Antineoplastic Agents; D005663:Furans; D007659:Ketones; D014404:Tubulin; C490954:eribulin; D000095662:Polyether Polyketides