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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 related to 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 expected to be 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.

 
   

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