Definition

An orally bioavailable gonadotropin-releasing hormone (GnRH) receptor antagonist, with potential hormone production inhibitory activity. Upon oral administration, GnRH antagonist SHR7280 competes with GnRH for receptor binding and inhibits GnRH receptor signaling in the anterior pituitary gland, thereby inhibiting the secretion and release of luteinizing hormone (LH) and follicle stimulating hormone (FSH). In males, the inhibition of LH secretion prevents the release of testosterone. Since testosterone is required to sustain prostate growth, reducing testosterone levels may inhibit hormone-dependent prostate cancer cell proliferation. In females, this prevents the production of estrogen by the ovaries and may relieve symptoms from sex-hormone dependent diseases. Since SHR7280 reduces the occurrence of premature LH surge in females, premature ovulation is also prevented.