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Breast Cancer

An orally bioavailable ER downregulator identified for breast cancer treatment

Published in Women's Health Weekly, October 13th, 2005

A novel, orally bioavailable estrogen receptor downregulator for the treatment of breast cancer is identified.

"Tamoxifen has been widely used for the treatment of estrogen receptor (ER)-positive breast cancer, but its partial agonist activity is considered to limit the efficacy, and cause tumor flare and endometrial cancer. Fulvestrant, on the other hand, binds and degrades ER, thereby acting as a pure antiestrogen without partial agonist activity," scientists in Japan report.

"However," contended T. Yoneya and colleagues, Chugai Pharmaceutical Co., "due to its low oral bioavailability, fulvestrant has to be intramuscularly administered to patients,...

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