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Mechanism of Action and Therapeutic Potential

SELECTIVE ESTROGEN RECEPTOR β AGONIST

photoHormonal therapy with estrogens for the treatment of vasomotor symptoms (VMS) in menopausal women has been associated with increased risk of invasive breast cancer, coronary heart disease, stroke, and deep vein thrombosis. This increased risk is associated with the abundance and prominent role of estrogen receptor α (ERα) in the breast, uterus, and cardiovascular endothelium. Estrogen binds equally to both ERα and to estrogen receptor β (ERβ). Because it is selective for ERβ, AUS-131 may have an improved safety profile over estrogens for menopausal women.

ANTIANDROGEN ACTIVITY

Prostate growth is regulated through the androgen receptor by the androgens testosterone and dihydrotestosterone. Androgens appear to play a permissive role in benign prostatic hyperplasia (BPH). Preclinical data suggest that AUS-131 downregulates the expression of androgen receptors. Because AUS-131 reduces the number of androgen receptors, prostate growth is inhibited. This novel mechanism of action may explain why AUS-131 does not affect androgen levels, and therefore may improve the quality of life for men with prostate disorders.

ANTIOXIDANT ACTIVITY

Independent research supports that AUS-131 is a potent antioxidant with activity greater than that for vitamin E and vitamin C. Available literature also shows that equol has been shown to protect against damage to the skin caused by ultraviolet light. Therefore, we hypothesize that the S-equol in AUS-131 will provide the health benefit of antioxidants in the skin including antiaging and protection from damage caused by ultraviolet light.

 
   

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