Novel BRCA1 Mimetics for Treatment of Er-α Positive Breast Cancers

Reference #: 2008-033

OTC Contact: Ruchika Nijhara, Ph.D., MBA, CLP, Director (Directory Information | Send a Message)

Description

Resistance to anti-estrogenic therapies remains as a very significant problem in the treatment of breast cancer. Georgetown researchers have developed novel class of compounds and methods for the treatment of estrogen receptor (ER)-α positive breast cancers. This new class of ER-α antagonists inhibits ER-α by a mechanism distinct from conventional anti-estrogenic agents, and interacts with an ER-α site distinct from the ligand binding pocket. These BRCA1 mimetics are effective against Tamoxifen resistant cells. The compounds are pure ER-α antagonists, rather than a partial antagonist, partial agonist like Tamoxifen.

Applications

Potential treatment or prevention of breast cancers, endometrial cancers, and other cancers.

Advantages

Potential therapeutic for tumors that have become resistant to Tamoxifen and other anti-estrogens
Potential therapeutic for tumors with de novo resistance to Tamoxifen
Can be used in place of or with Tamoxifen in any ER-α positive breast cancer

Stage of Development

Researchers have identified and synthesized compounds that inhibit ER-α activity in multiple cell lines. Mechanism of action studies have been completed.

Relevant Publications

Manuscript has been submitted

Patent Status

Patent application filed.