Contraceptive Potential of GnRH Antagonists

Following elucidation of the structure of gonadotropin-releasing hormones (GnRH) by the laboratories of Schally [1] and Guilleman [2] in 1971, hundreds of analogs, both agonists and antagonists of GnRH, were synthesized and tested. Early success in increasing the potency of agonists and recognition of the ability of GnRH agonists paradoxically to inhibit the pituitary-gonadal axis quickly brought GnRH agonists to the forefront of investigation. It is now known that chronic administration of GnRH agonists effectively inhibits the reproductive/ endocrine systems and is useful in the treatment of conditions such as precocious puberty, prostatic carcinoma and uterine fibroids.