title: Eribulin -- a review of preclinical and clinical studies.
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.
authors.affiliation: Albert Einstein College of Medicine, Department of Medical Oncology, Montefiore Medical Center, 1695 Eastchester Road, Bronx, NY 10461, United States. umangtalking@gmail.com
authors.forename: Umang
authors.initials: U
authors.lastname: Swami
authors.forename: Imran
authors.initials: I
authors.lastname: Chaudhary
authors.forename: Mohammad H
authors.initials: MH
authors.lastname: Ghalib
authors.forename: Sanjay
authors.initials: S
authors.lastname: Goel
mesh_terms: D000818:Animals; D002986:Clinical Trials as Topic; D004353:Drug Evaluation, Preclinical; D064420:Drug-Related Side Effects and Adverse Reactions; D005663:Furans / Q000009:adverse effects / Q000378:metabolism / Q000494:pharmacology* / Q000627:therapeutic use*; D006801:Humans; D007659:Ketones / Q000009:adverse effects / Q000378:metabolism / Q000494:pharmacology* / Q000627:therapeutic use*; D009369:Neoplasms / Q000188:drug therapy*; D000095662:Polyether Polyketides
chemical_list: D005663:Furans; D007659:Ketones; C490954:eribulin; D000095662:Polyether Polyketides