IATERRP9

Current menopausal hormone therapy (MHT) formulas are only recommended for 5 years, because long-term treatment increases the risk of breast cancer, strokes, blood clots and Alzheimer’s disease. MHT is no longer recommended for primary prevention of medical conditions that increase during menopause such as heart disease, osteoporosis and hip fractures.   Due to the side-effects of MHT only about 10% of menopausal women take MHT and most women stop taking them before 3 years of treatment.

IATERRP9 is a nuclear receptor reprogramming drug designed to make MHT safer for long-term to treat protracted menopausal symptoms and primary prevention of chronic diseases, such as heart disease, osteoporosis and diabetes.

IATERRP9 has a unique mode of action that distinguishes it from selective estrogen receptor modulators (SERMs). SERMs work by binding to the same site as estrogens on estrogen receptors. In contrast, IATERRP9 does not bind to the estrogen binding site. IATERRP9 is designed to be used in combination with estrogens that are currently approved in menopausal hormone therapy (MHT) to block the side-effects of estrogens so it can be used for long-term therapy. The most detrimental side-effect of estrogen is the increased risk of breast and endometrial cancer resulting from its proliferative action that leads to growth of breast and endometrial cells. 

Our studies found that IATERRP9 blocks estrogens from activating oncogenes, by a reprogramming mechanism. IATERRP9 also causes estrogens to regulate a new set of genes.

Currently there are no MHT formulations that are approved for long-term therapy. IATERRP9’s unique mechanism could make MHT safer for long-term therapy to prevent chronic diseases during and following menopause, such as heart disease and diabetes. IATERRP9 can block the genes that are involved in the development of fibroids and endometriosis, which are conditions that are driven by estrogens.