Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
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.

PubMed Disclaimer

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

Similar articles

See all similar articles

Cited by

See all "Cited by" articles

References

    1. Uemura D, Takahashi K, Yamamoto T, et al. Norhalichondrin A: an antitumor polyether macrolide from a marine sponge. J Am Chem Soc. 1985;107(16):4796–8.
    1. Hirata Y, Uemura D. Halichondrins—antitumor polyether macrolides from a marine sponge. Pure Appl Chem. 1986;58(5):701–10.
    1. Pettit GR, Herald CL, Boyd MR, et al. Isolation and structure of the cell growth inhibitory constituents from the western Pacific marine sponge Axinella sp. J Med Chem. 1991;34(11):3339–40. - PubMed
    1. Pettit GR, Tan R, Gao F, et al. Isolation and structure of halistatin 1 from the eastern Indian Ocean marine sponge Phakellia carteri. J Org Chem. 1993;58(9):2538–43.
    1. Gravelos DG, Lake R, Blunt JW, Munro MHG, Litaudon MSP. Halichondrins: cytotoxic polyether macrolides. European Patent Office; Munich, Switzerland: 1993. Publication number EP 0 572 109 A1.