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Degarelix review

Alessandro Sciarra, Andrea Fasulo, Antonio Ciardi, Elisa Petrangeli, Alessandro Gentilucci, Martina Maggi, Michele Innocenzi, Federico Pierella, Vincenzo Gentile, Stefano Salciccia, Susanna Cattarino
Our aim was to systematically evaluate the benefits of degarelix as antagonist versus agonists of gonadotropin-releasing hormones (GnRH) for the treatment of advanced prostate cancer (PC). This comparison was performed either in terms of biochemical or oncological or safety profiles. To this end we, carried out a systematic review and meta-analysis of the literature.We selected only studies directly and prospectively analyzing the two treatments in the same population (randomized phase III studies). We followed the Preferred Reporting Items for Systematic Reviews and meta-analyses process for reporting studies...
July 2016: Medicine (Baltimore)
Seyed Alireza Hosseini, Fatemeh Rajabi, Ali Akbari Sari, Mohsen Ayati, Saeed Heidari, Fawzieh Ghamary
BACKGROUND: Hormone therapy is currently the mainstay in the management of locally advanced and metastatic prostate cancer. We performed a systematic review to compare safety, efficacy and effectiveness of degarelix, a new gonadotropin-releasing hormone (GnRH) antagonist (blocker), versus gonadotropin-releasing hormone (GnRH) agonists. METHODS: MEDLINE, Web of Science and the Cochrane library were searched to identify all of the published Randomized Controlled Trials (RCTs) that used degarelix versus gonadotropin-releasing hormone agonists with or without anti-androgen therapy for the treatment of prostate cancer...
2016: Medical Journal of the Islamic Republic of Iran
Fernando P Secin
INTRODUCTION: Luteinizing hormone releasing hormone (LhRh) antagonist degarelix has been approved by the Food and Drug Administration (FDA) for the treatment of advanced prostate cancer in 2008. However, the studies that followed such initial approval have several limitations. OBJECTIVE: To make a critical review of those publications. METHODS: Literature search on degarelix. RESULTS: The studies supporting the use of degarelix are criticized on the basis of selection bias in regards to the heterogeneous populations described, ad hoc analyses with low statistical merit, and the presentation of selected data that would appear to be favorable to the evaluated medication...
October 2016: Urologic Oncology
Laurence Klotz
INTRODUCTION: Luteinizing hormone-releasing hormone (LHRH) agonists have been the mainstay of androgen deprivation therapy (ADT) for advanced prostate cancer for over two decades. However, their limitations include a transient initial rise in testosterone, failure to reduce testosterone to castrate levels in some patients, incomplete suppression of follicle-stimulating hormone (FSH), and an increased risk of cardiovascular (CV) events in those with pre-existing CV disease. This article considers whether the LHRH antagonist degarelix offers significant advantages over LHRH agonists...
2015: Expert Opinion on Drug Metabolism & Toxicology
Takahiro Kimura, Hiroshi Sasaki, Kouhei Akazawa, Shin Egawa
Degarelix is a gonadotropin-releasing hormone (GnRH) antagonist that is approved for the treatment of prostate cancer. GnRH antagonists bind directly to and block GnRH receptors, without causing the initial testosterone surge associated with GnRH agonists. A pivotal phase III study indicated that degarelix induced significantly faster reduction of testosterone and prostate-specific antigen level than GnRH agonist does. In addition, its 5-year extension trial suggested that patients could be safely switched from GnRH agonist to degarelix treatment with sustained efficacy, as measured by biochemical markers...
July 2015: Urologic Oncology
Marilena Manea, Marina Montagnani Marelli, Roberta M Moretti, Roberto Maggi, Monica Marzagalli, Patrizia Limonta
It is now well established that hormonal pathways are involved in the development of prostate cancer towards the castration resistant (CRPC) stage and can be effective molecular targets for novel treatment strategies. Most CRPC are sensitive to androgens and this can be due to the intratumoral production of androgens, androgen receptor (AR) amplification/ mutations and epigenetic modifications of AR expression/signaling. Based on these observations, potent agents targeting the AR axis were developed: 1) inhibitors of CYP17 (a key enzyme in the production of androgens), such as abiraterone and orteronel; 2) AR antagonists that bind to AR and impair AR activation, such as enzalutamide and ARN-509...
2014: Recent Patents on Anti-cancer Drug Discovery
Judd W Moul
INTRODUCTION: Androgen deprivation therapy (ADT) is the lynchpin of treatment for advanced prostate cancer. Prescribing physicians and patients have a choice between orchiectomy, luteinizing hormone releasing hormone (LHRH) agonists, combined androgen deprivation (CAD) or LHRH antagonists. MATERIALS AND METHODS: Literature relating to the use of LHRH antagonists in the management of prostate cancer was reviewed. RESULTS: Abarelix was the first-in-class LHRH pure antagonist that was Food and Drug Administration (FDA) approved in 2003...
April 2014: Canadian Journal of Urology
Natalie J Carter, Susan J Keam
Degarelix (Firmagon(®); Gonax(®)) is a gonadotropin-releasing hormone receptor antagonist that is approved for the treatment of advanced (hormone-dependent) prostate cancer in the US and EU and the treatment of prostate cancer in Japan. In a pivotal randomized, controlled, 12-month phase III study, degarelix (initial subcutaneous dose of 240 mg followed by monthly dosages of 80 mg) was noninferior to leuprolide (monthly intramuscular dosages of 7.5 mg) in patients with prostate cancer of any stage for which endocrine treatment was indicated (except neoadjuvant hormonal therapy) with regard to suppression of testosterone to castration levels (i...
April 2014: Drugs
Yuanshan Cui, Huantao Zong, Huilei Yan, Nan Li, Yong Zhang
OBJECTIVE: We performed a systematic review and meta-analysis to assess the efficacy and tolerability of degarelix for lower urinary tract symptom relief, prostate volume reduction and quality of life improvement in men with prostate cancer (PCa). MATERIALS AND METHODS: A literature review was performed to identify all of the published randomized controlled trials (RCTs) that used degarelix versus gonadotropin-releasing hormone agonists plus antiandrogens therapy for the treatment of PCa...
2014: Urologia Internationalis
Ferenc G Rick, Norman L Block, Andrew V Schally
INTRODUCTION: Androgen deprivation therapy (ADT) has been the first-line standard of care for treating patients with hormone-sensitive advanced prostate cancer (PCa) for many decades. The agonists of luteinizing hormone-releasing hormone (LHRH), also called gonadotropin-releasing hormone, are still the most frequently used form of medical ADT. AREAS COVERED: This article reviews the available data and most recent information concerning the use of LHRH agonists in advanced PCa...
November 2013: Expert Opinion on Pharmacotherapy
(no author information available yet)
Prostate cancer sometimes metastasizes, especially to bone, which may cause pain, fractures and spinal cord compression. What are the best first-line treatment options for patients with metastatic prostate cancer? To answer this question, we conducted a review of the literature, using the standard Prescrire methodology. Suppressing androgen secretion by surgically removing the testicles (orchiectomy) or by administering a gonadorelin agonist relieves the pain associated with bone metastases in about 80% of patients...
February 2013: Prescrire International
Stéphane Oudard
The landscape of prostate cancer treatment is rapidly changing as extensive research into potential therapies yields new options. In this article, the literature is reviewed to identify emerging therapies for advanced prostate cancer. Emphasis is placed on agents that have been approved in the United States of America (USA) and the European Union, or that have reached phase III clinical studies. Several new therapies have been approved in recent years across different stages of the natural history of the disease...
May 2013: Cancer Treatment Reviews
N D Shore, P-A Abrahamsson, J Anderson, E D Crawford, P Lange
Androgen deprivation therapy (ADT) is first-line treatment for metastatic prostate cancer (PCa). Gonadotrophin-releasing hormone (GnRH) agonists are the most commonly used ADT but have several theoretical physiologic disadvantages (e.g. initial testosterone surge, potential microsurges upon repeat administration). Testosterone surge delays the intended serologic endpoint of testosterone suppression and may exacerbate clinical symptoms. GnRH antagonists were developed with a view toward overcoming these potential adverse physiologic events...
March 2013: Prostate Cancer and Prostatic Diseases
Alexandra Masson-Lecomte, Laurent Guy, Philippe Pedron, Franck Bruyere, Morgan Rouprêt, Bonaventure Nsabimbona, Mickael Dahan, Patrice Hoffman, Laurent Salomon, Dimitri Vordos, Andras Hoznek, Philippe Le Corvoisier, Pierrick Morel, Claude Abbou, Alexandre de la Taille
PURPOSE: At the time of castration resistance, it is recommended to realize hormonal manipulations before chemotherapy. We evaluated the impact of a switch from GnRH agonist to antagonist in patients with castration-resistant prostate cancer on PSA and testosterone levels at 3 months. METHODS: Retrospectively, 17 patients from 5 different centers undergoing androgen deprivation therapy and presenting rising PSA confirmed on 3 blood samples 2 weeks apart and despite a castrate testosterone level (<0...
April 2013: World Journal of Urology
Hein Van Poppel, Laurence Klotz
Gonadotropin-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...
July 2012: International Journal of Urology: Official Journal of the Japanese Urological Association
Laurent Boccon-Gibod, Egbert van der Meulen, Bo-Eric Persson
Androgen deprivation therapy (ADT) is the main treatment approach in advanced prostate cancer and in recent years has primarily involved the use of gonadotropin-releasing hormone (GnRH) agonists. However, despite their efficacy, GnRH agonists have several drawbacks associated with their mode of action. These include an initial testosterone surge and testosterone microsurges on repeat administration. GnRH antagonists provide an alternative approach to ADT with a more direct mode of action that involves immediate blockade of GnRH receptors...
June 2011: Therapeutic Advances in Urology
Lanting Lu, Jaime Peters, Chris Roome, Ken Stein
OBJECTIVE: To evaluate the cost-effectiveness of degarelix vs luteinizing hormone-releasing hormone analogue (triptorelin) plus short-term antiandrogen treatment for advanced prostate cancer. METHODS: We developed a decision analytic model based on a clinical trial and literature review. The two interventions evaluated were: (i) monthly injection of degarelix and (ii) 3-monthly triptorelin therapy plus short-term flutamide, cyproterone or bicalutamide treatment...
April 2012: BJU International
Orkun Tan, Orhan Bukulmez
PURPOSE OF REVIEW: Gonadotropin-releasing hormone (GnRH) receptors are not only detected in the central nervous system but also in tissues such as ovary, endometrium, breast, gastrointestinal system, placenta and malignant tumors of ovary and breast. The direct role of GnRH-antagonists in ovarian function, implantation, cancer pathogenesis and treatment is under extensive investigation. This study reviews the biochemistry and molecular and cellular biology of GnRH-antagonists as well as GnRH types and their receptors...
August 2011: Current Opinion in Obstetrics & Gynecology
Hendrik Van Poppel
Medical castration using gonadotropin-releasing hormone (GnRH) receptor agonists currently provides the mainstay of androgen deprivation therapy for prostate cancer. Although effective, these agents only reduce testosterone levels after a delay of 14 to 21 days; they also cause an initial surge in testosterone that can stimulate the cancer and lead to exacerbation of symptoms ("clinical flare") in patients with advanced disease. Phase III trial data for the recently approved GnRH receptor blocker, degarelix, demonstrated that it is as effective and well tolerated as GnRH agonists...
2010: Cancer Management and Research
Philip Savage
Over the past decade, 23 new cancer treatment drugs have been introduced, many have brought major benefits to patient care, whilst others have maintained clinical benefits with reduced toxicity. In this article, the historical trends in drug numbers, therapeutic classification, and treatment costs have been reviewed. Drugs are classified by years of introduction, therapeutic classification, and an assessment of relative treatment cost using a contemporary 'standard' treatment compared with the relevant UK GDP per capita...
March 2012: Journal of Oncology Pharmacy Practice
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