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eribulin : ウィキペディア英語版
eribulin

Eribulin is an anticancer drug marketed by Eisai Co. under the trade name Halaven. The mesylate salt was approved by the U.S. Food and Drug Administration on November 15, 2010, to treat patients with metastatic breast cancer who have received at least two prior chemotherapy regimens for late-stage disease, including both anthracycline- and taxane-based chemotherapies. It was approved by Health Canada on December 14, 2011, for treatment of patients with metastatic breast cancer who have previously received at least two chemotherapeutic regimens for the treatment of metastatic disease.〔(Notice of Decision for HALAVEN )〕
Eribulin is also being investigated by Eisai Co. for use in a variety of other solid tumors, including non-small cell lung cancer, prostate cancer and sarcoma.〔http://www.clinicaltrials.gov/ct2/results?term=eribulin+OR+E7389〕
Eribulin is also known as E7389 and ER-086526, and also carries the US NCI designation NSC-707389.
==Structure and mechanism==
Eribulin is a fully synthetic macrocyclic analogue of the marine natural product halichondrin B, the parent molecule being a potent naturally occurring mitotic inhibitor with a unique mechanism of action found in the ''Halichondria'' genus of sponges. Eribulin is a mechanistically unique inhibitor of microtubule dynamics, binding predominantly to a small number of high affinity sites at the plus ends of existing microtubules. Eribulin exerts its anticancer effects by triggering apoptosis of cancer cells following prolonged and irreversible mitotic blockade.
A new synthetic route to the drug was published in 2009.

抄文引用元・出典: フリー百科事典『 ウィキペディア(Wikipedia)
ウィキペディアで「eribulin」の詳細全文を読む



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