Novel BRCA1 Mimetics for Treatment of Er-α Positive Breast Cancers
Categories: “Cancer Therapeutics“
Reference #: 2008-033
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.
Potential treatment or prevention of breast cancers, endometrial cancers, and other cancers.
- 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.
Manuscript has been submitted
Patent application filed.