Marine sponge derived eribulin in preclinical and clinical studies for cancer

Eribulin mesylate is a completely synthetic, structurally simplified, macrocyclic ketone analogue of Halichondrin B. Halichondrin B is complex, natural, macrocyclic polyether derived from marine sponges. Eribulin has been approved by United States Food and Drug Administration in 2010 as a third line therapy for metastatic breast cancer patients, who have previously been treated with an anthracycline and a taxane. It has a microtubule dynamics inhibitory action. Preclinical studies have demonstrated a broad spectrum of anti-tumor activity in various cancer cell lines and synergistic action with multiple anticancer agents. It has also undergone clinical trials in non-small cell lung cancer, pancreatic, prostate, bladder, head and neck cancers, sarcomas and ovarian and other gynecological tumors. Various combination trials are currently ongoing. 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, pharmacokinetics, pharmacodynamics, mechanism of action, metabolism, preclinical studies and clinical trials.