期刊
CRITICAL REVIEWS IN ONCOLOGY HEMATOLOGY
卷 81, 期 2, 页码 163-184出版社
ELSEVIER SCIENCE INC
DOI: 10.1016/j.critrevonc.2011.03.002
关键词
Breast cancer; EMBRACE; Eribulin; E7389; Halichondrin B; Halaven (TM); Microtubule inhibitor; NSC 707389
资金
- NCI NIH HHS [K12 CA132783] Funding Source: Medline
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. (C) 2011 Elsevier Ireland Ltd. All rights reserved.
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