According to the American Cancer Society, breast cancer is the most common cancer for women in the US, except for skin cancer. It comprised about 30% of all new female cancers each year. While breast cancer death rates have decreased over the last several decades, it remains the second leading cause of cancer death in women.

The Need

The estrogen receptor is a critical aspect of the diagnostic and treatment strategy for breast cancer. Discovery of the second estrogen receptor beta, Erβ, also plays a significant role in breast cancer. While selective ERβ agonists are used in breast cancer treatment, there remains a need to develop better and more effective therapeutic treatments for the disease. Moreover, these ERβ agonists have the potential to function as tumor suppressors in the treatment of additional cancers, such as colon and prostate cancer.

The Technology

Researchers at OSU have developed a library of seventeen newly designed ERβ agonists. These compounds have been synthesized and biologically evaluated in vitro for their Erβ selective agonist activity. Structural modifications have been leveraged in these new compounds for enhanced binding affinity.

Commercial Applications

Selective ERβ agonists are used for several estrogen-related diseases, including infertility, postmenopausal osteoporosis, and breast cancer, among other conditions. ERβ agonists are also being studied and developed for colon, prostate, and brain cancers.

Benefits/Advantages

Advantages of this technology include:

• Enhanced binding affinity and efficacy based on improved structural changes
• Expanded possibility for use in tumor suppression
• Comparable and improved performance of certain compounds compared to standard Erβ selective agonists
• Lead molecule is potent, orally bioavailable, and brain penetrant with favorable in vitro ADME and demonstrated in vivo efficacy in mouse models of ischemic heart failure, GBM, and NASH/liver fibrosis