Clinical Medicine Reviews in Oncology

Manipulation of the hypothalamic-pituitary-gonadal axis via androgen deprivation therapy has been in use since the 1940’s for the treatment of advanced prostate cancer. Androgen deprivation may be achieved via surgical castration or pharmacological castration. Pharmacological castration is preferred by patients due to its decreased psychological impact on body image and potential reversibility. Gonadotropin releasing hormone (GnRH) agonists have been a mainstay in androgen suppression. Recently degarelix, a GnRH antagonist, has been proven to be as effective and not inferior to GnRH analogues, such as leuprolide, in a phase III trial. Degarelix was found to have no initial testosterone surge, reach castrate levels of testosterone by day three, have no testosterone microsurges, have the ability to keep follicle stimulating hormone suppressed and have lower histaminogenic potency compared to its predecessor abarelix. A review of the pharmacokinetics, clinical trial findings, safety and ongoing debates as to the best application of degarelix is presented.