Gestrinone

Endometriosis is common disease characterized by the presence of endometrial tissue outside the uterus which affects approximately 10% of premenopausal women. Gestrinone is a synthetic steroid used occasionally to treat endometriosis.{12994} It acts centrally on the hypothalamic-pituitary system to suppress release of lutenizing hormone (LH) and follicle-stimulating hormone (FSH), thus reducing estrogen synthesis.{12994} It also binds to androgen (AR), progesterone (PR), and estrogen (ER) receptors in the human endometrial tissue but not to steroid hormone binding globulin or corticord-binding globulin.{13002} Gestrinone binds to AR and PR with EC50 values of approximately 20 and 30 nM, respectively.{12992} These values reflect approximately 5-6 fold lower affinity than testosterone and progesterone, the natural AR and PR ligands, for these receptors.{12992}