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Kamisu, Japan

Chiba H.,API Research | Tagami K.,API Research
Yuki Gosei Kagaku Kyokaishi/Journal of Synthetic Organic Chemistry | Year: 2011

HALAVEN™ (eribulin mesylate, E7389) is a novel anticancer agent discovered and developed by Eisai, which was approved by the United States Food and Drug Administration (FDA) for the treatment of patients with metastatic breast cancer who have previously received at least two chemotherapeutic regimens for the treatment of metastatic disease. HALAVEN™ is a non-taxane, microtubule dynamics inhibitor and a synthetic analog of halichondrin B, a natural product isolated from the marine sponge Halichondria okadai. Although the structure of HALAVEN™ is substantially simplified relative to halichondrin B, the development of this complex molecule only by chemical synthesis represents a significant challenge in terms of pharmaceutical development In this article, a developmental history of HALAVEN from its discovery to process development aiming at commercial production is described.

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