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

Categories: "Cancer Therapeutics"

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.