40+ MILLION WOMEN ARE AFFECTED
The average age for the onset of menopause is about 50 years old, and there are more than 60 million menopausal women in the US alone. Approximately 75% of these women experience transient hot flashes, which cause sleep disruption and cause embarrassment during the daytime.
IT COSTS $3 BILLION PER YEAR TO MANAGE HOT FLASHES
The Study of Women Across the Nation found that median lifetime persistence for hot flashes is 7.4 years. Estimates place the total health expenditures for menopausal symptoms at $3 billion per year, not including the loss of productivity at work and increased energy use for air conditioning.
Estrogen-based products lead revenue in the global hormone therapy market. These estrogen therapies continue to be the fastest growing products to treat menopause symptoms but come with an increased risk of adverse effects such as stroke, cancer and heart disease later in life. The market for menopause-related hormone therapies is growing, partly due to the rapidly increasing population of menopausal women.
This expanding population creates a burgeoning demand in the market for more safe and effective treatments for the symptoms of menopause. Our technology aims to meet that demand. Our current lead compounds exhibit estrogen-like activity and structure but do not result in adverse effects commonly associated with current estrogen therapies. Because of the growing demand for menopausal symptom relief, there is heightened interest from pharmaceutical companies to partner with small drug development companies like Estrigenix Therapeutics, Inc. to integrate these products into their portfolios and drug development pipelines.
Long-term oral administration of a novel estrogen receptor beta agonist enhances memory and alleviates drug-induced vasodilation in young ovariectomized mice
The ovaries are the primary female organ for the production of the natural hormone estrogen. Ovariectomized mice are an established model for testing menopause treatments. We have demonstrated that long-term (9-weeks) oral treatment of ovariectomized mice with EGX358 moderated a chemically induced hot flash and improved memory to the same extent as estradiol without any adverse effects on anxiety, depression or weight gain.
Synthesis and evaluation of 4-cycloheptylphenols as selective estrogen receptor-b agonists (SERBAs)
EGX163, a seven-membered ring analog of EGX358, was prepared. This compound was found to be highly selective in activating estrogen receptor beta (~300 fold selectivity). A high level of selectivity for activating ERβ is crucial to providing the benefits of hormone replacement therapy while avoiding the deleterious risks of breast cancer.
A-C estrogens as potent and selective estrogen receptor-beta agonists (SERBAs) to enhance memory consolidation under low-estrogen conditions.
The synthesis of a highly selective estrogen receptor beta activator, EGX358 (ISP358), is reported. This compound was found to be effective in improving memory for a single dose in an ovariectomized mouse model for menopause by three methods of administration: direct infusion into the dorsal hippocampus, intraperitoneal injection or oral dosing. Of equal importance, we demonstrated that EGX358 does not cause growth/proliferation of ER+ breast cancer cells and does not inhibit the primary liver enzymes responsible for metabolism of other drugs at concentrations 1,250 times the effective concentration for activating ERβ.