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Review
. 2012 Feb;81(2):163-84.
doi: 10.1016/j.critrevonc.2011.03.002. Epub 2011 Apr 14.

Eribulin -- a review of preclinical and clinical studies

Umang Swami  1 , Imran Chaudhary, Mohammad H Ghalib, Sanjay Goel
Affiliations
Review

Eribulin -- a review of preclinical and clinical studies

Umang Swami et al. Crit Rev Oncol Hematol. 2012 Feb.

Abstract

Eribulin mesylate is a non-taxane, structurally simplified, completely synthetic, halichondrin B derivative with an end poisoning, microtubule inhibitory action. Preclinical studies have demonstrated activity in various cancer cell lines and synergistic action with gemcitabine, epirubicin, trastuzumab, cisplatin, docetaxel and vinorelbine. Eribulin has recently been approved by United States Food and Drug Administration as a third line therapy for metastatic breast cancer patients, who have previously been treated with an anthracycline and a taxane. It has also advanced to phase II trials in non-small cell lung cancer, pancreatic, prostate, bladder, head and neck cancers, sarcomas and ovarian and other gynecological tumors. Combination trials with carboplatin, gemcitabine, pemetrexed, cisplatin, and erlotinib are currently ongoing. Eribulin potentially has a low incidence of peripheral neuropathy. The predominant side effects are neutropenia and fatigue, which are manageable. This article reviews the available information on eribulin with respect to its clinical pharmacology, mechanism of action, pharmacokinetics, pharmacodynamics, metabolism, preclinical studies and clinical trials.

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Figures

Fig. 1
Fig. 1
Chemical structure of halichondrin B.
Fig. 2
Fig. 2
Chemical structure of eribulin mesylate.
Fig. 3
Fig. 3
Mechanism of action of eribulin (courtesy EISAI).
Fig. 4
Fig. 4
Plasma Cmax versus dose following a 1-h infusion of eribulin on day 1. (B) Plasma area under the concentration–time curve (AUC0-8) versus dose following a 1-h infusion of eribulin on day 1. (C) Plasma concentration versus time profile for the 1.0 mg/m2 treatment group (n = 9). From: Ref. [10].
Fig. 5
Fig. 5
Eribulin related adverse events of interest or ≥10% incidence as seen in 394 patients with MBC [55,56].
See this image and copyright information in PMC

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