Gonadotropin‐releasing hormone: An update review of the antagonists versus agonists

International Journal of Urology - Tập 19 Số 7 - Trang 594-601 - 2012
Hendrik Van Poppel1, Laurence Klotz2
1Dept of Urology, University Hospitals Leuven, Belgium
2Division of Urology, University of Toronto, Toronto, Ontario, Canada

Tóm tắt

AbstractGonadotropin‐releasing hormone agonists and antagonists provide androgen‐deprivation therapy for prostate cancer. Unlike agonists, gonadotropin‐releasing hormone antagonists have a direct mode of action to block pituitary gonadotropin‐releasing hormone receptors. There are two licensed gonadotropin‐releasing hormone antagonists, degarelix and abarelix. Of these, degarelix is the more extensively studied and has been documented to be more effective than the well‐established, first‐line agonist, leuprolide, in terms of substantially faster onset of castration, faster suppression of prostate‐specific antigen, no risk for testosterone surge or clinical flare, and improved prostate‐specific antigen progression‐free survival, suggesting a delay in castration resistance. Other than minor injection‐site reactions, degarelix is generally well tolerated, without systemic allergic reactions and with most adverse events consistent with androgen suppression or the underlying condition. In conclusion, degarelix provides a rational, first‐line androgen‐deprivation therapy suitable for the treatment of prostate cancer, with faster onset of castration than with agonists, and no testosterone surge. Furthermore, data suggest that degarelix improves disease control compared with leuprolide, and might delay the onset of castration‐resistant disease. In view of these clinical benefits and the lack of need for concomitant anti‐androgen treatment, gonadotropin‐releasing hormone antagonists might replace gonadotropin‐releasing hormone agonists as first‐line androgen‐deprivation therapy in the future.

Từ khóa


Tài liệu tham khảo

10.1016/j.urology.2007.12.070

Thompson IM, 2001, Flare associated with LHRH‐agonist therapy, Rev. Urol., 3, S10

10.1016/j.eursup.2005.08.004

10.1016/j.juro.2007.05.129

Hotte SJ, 2010, Current management of castrate‐resistant prostate cancer, Curr. Oncol., 17, S72, 10.3747/co.v17i0.718

10.1016/j.eururo.2009.06.027

HeidenreichA BollaM JoniauSet al.2011.Guidelines on prostate cancer. [Cited 8 August 2011.] Available from URL:http://www.uroweb.org/gls/pdf/08_Prostate_Cancer.pdf

10.1111/j.1464-410X.2005.05798.x

10.1111/j.1464-410X.2005.05946.x

10.4065/82.2.243

10.1530/ERC-10-0343

Guyton AC, 1991, Textbook of Medical Physiology, 885

10.1007/BF00922743

10.1124/jpet.106.112326

10.1517/14656566.5.10.2171

10.1016/j.eururo.2008.04.065

10.1016/j.juro.2008.07.033

10.1111/j.1464-410X.2008.08183.x

10.1016/j.juro.2011.04.083

10.1016/S0090-4295(01)01342-5

Selvaggi F, 2001, Comparison of abarelix depot (A‐D) and goserelin (G) plus bicalutamide (B) in advanced prostate cancer: results of a multicentre, open‐label, randomised, phase III study, Eur. Urol., 39, 78

10.1016/S0022-5347(05)66353-7

10.1097/00005392-200204000-00021

Plenaxis Drug Information.2011. [Cited 8 August 2011]. Available from URL:http://www.rxlist.com/plenaxis‐drug.htm#

10.1016/j.ijrobp.2004.04.048

10.1200/JCO.2006.06.4246

10.1200/JCO.2008.19.9810

10.1016/j.eururo.2009.11.029

10.1016/S1569-9056(10)60144-3

10.1097/01.cad.0000231476.84782.55

10.1097/01.ju.0000059584.47272.9d

10.1177/1756287211414457

10.5489/cuaj.1145

10.1038/aja.2008.36

US Food and Drug Administration.2010.GnRH agonists: label change – increased risk of diabetes and cardiovascular disease (update). [Cited 8 August 2011]. Available from URL:http://www.fda.gov/Safety/MedWatch/SafetyInformation/SafetyAlertsforHumanMedicalProducts/ucm230359.htm

10.1016/j.juro.2010.08.012

10.1016/j.juro.2011.07.035

10.2217/14796694.2.6.677

10.1016/j.tem.2008.09.003

WaknineY.2005.International approvals: plenaxis tostrex troxatyl. [Cited 8 August 2011]. Available from URL:http://www.medscape.com/viewarticle/513892

Specialty European Pharma.2011.Your partner in urology. [Cited 8 August 2011]. Available from URL:http://www.specialityeuropeanpharma.com

10.1124/jpet.301.1.95

10.1111/j.1365-2125.2010.03730.x

10.1111/j.1464-410X.2009.08981.x

AndersonJ Al‐AliG WirthMet al.Improved relief of lower urinary tract symptoms (LUTS) with a gonadotrophin‐releasing hormone (GnRH) blocker compared with an agonist + antiandrogen (AA) in an open‐label randomised study (CS28). Abstract presented at the European Multidisciplinary Meeting on Urological Cancers Barcelona Spain 2011.

Thông tin
Thông tin xuất bản

International Journal of Urology

Tập 19 Số 7

594-601

Thông tin tác giả