Eribulin

Information about Eribulin

Eribulin mesylate is an inhibitor of microtubule function and is used as an antineoplastic agent for refractory, metastatic breast cancer and liposarcoma. 

Liver safety of Eribulin

Despite its cytotoxic activity against cancer cells, eribulin has rarely been implicated in causing clinically apparent acute liver injury. 

Mechanism of action of Eribulin

Eribulin (er' i bue' lin) is a synthetic macrocyclic analogue of halichondrin B, a naturally occurring inhibitor of mitotic division found in a species of marine sponges (Halichondria okadai).  Eribulin binds to the growing ends of microtubules preventing cell division (mitotic arrest) which leads to tubulin sequestration in aggregates and apoptotic cell death. 

FDA approval information for Eribulin

Eribulin was approved for use in cancer chemotherapy in 2010 and current indications are for metastatic breast cancer after failure of chemotherapy with an anthracycline and taxane.  It is also approved for use in metastatic, refractory liposarcoma.  Eribulin is given intravenously in doses of 1.4 mg/m2, typically on days 1 and 8 of 21 day cycles.  Eribulin is available in single use vials of 1 mg per 2 mL under the trade name Halaven. 

Side effects of Eribulin

Side effects are common and include nausea, vomiting, fatigue, headache, dizziness, peripheral neuropathy, hoarseness, ataxia, dysphagia, urinary retention, constipation, diarrhea, bone marrow suppression, alopecia and phlebitis at the infusion site.  Rare, but potentially severe adverse events include severe neutropenia, peripheral neuropathy, prolongation of the QTc interval and embryo-fetal toxicity.

 

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