title: Degarelix for prostate cancer.
abstract: The growth of prostate cancer cells is hormone dependent in the majority of patients with the disease. Lowering testosterone either surgically or medically (usually with a gonadotropin releasing hormone (GnRH) agonist) is the standard of care in patients with metastatic prostate cancer. Degarelix is a new GnRH antagonist for the treatment of patients with prostate cancer. In contrast to GnRH agonists, the development of GnRH antagonists was hindered for a long time owing to histamine-releasing activity and lack of potency and water solubility. Recently, however, degarelix has been approved by the FDA for the treatment of advanced prostate cancer. This review summarizes the preclinical and clinical data available for degarelix and describes its potential role in the market of prostate cancer therapeutics.
authors.affiliation: Department of Urology, University of Lübeck Medical School, Ratzeburger Allee 160, Lübeck, Germany. doehn@medinf.mu-luebeck.de
authors.forename: Christian
authors.initials: C
authors.lastname: Doehn
authors.forename: Martin
authors.initials: M
authors.lastname: Sommerauer
authors.forename: Dieter
authors.initials: D
authors.lastname: Jocham
mesh_terms: D000818:Animals; D018931:Antineoplastic Agents, Hormonal / Q000627:therapeutic use*; D002986:Clinical Trials as Topic; D015507:Drugs, Investigational / Q000627:therapeutic use*; D006801:Humans; D008297:Male; D009842:Oligopeptides / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000627:therapeutic use*; D010330:Patents as Topic; D011471:Prostatic Neoplasms / Q000188:drug therapy*; D011966:Receptors, LHRH / Q000037:antagonists & inhibitors*
chemical_list: D018931:Antineoplastic Agents, Hormonal; D015507:Drugs, Investigational; D009842:Oligopeptides; D011966:Receptors, LHRH; C431566:acetyl-2-naphthylalanyl-3-chlorophenylalanyl-1-oxohexadecyl-seryl-4-aminophenylalanyl(hydroorotyl)-4-aminophenylalanyl(carbamoyl)-leucyl-ILys-prolyl-alaninamide