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Degarelix

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https://www.readbyqxmd.com/read/27793455/effects-of-long-acting-gnrh-antagonist-degarelix-acetate-on-plasma-insulin-like-peptide-3-testosterone-and-luteinizing-hormone-concentrations-and-scrotal-circumference-in-male-goats
#1
M A Hannan, N Kawate, Y Fukami, W W P N Weerakoon, E E Büllesbach, T Inaba, H Tamada
We recently reported that plasma insulin-like peptide 3 (INSL3) concentrations increased soon after endogenous and exogenous stimulations of LH in male goats and bulls. However, the effects of LH suppression on INSL3 secretion are unknown in domestic animals. Here, we examined the effects of a long-acting GnRH antagonist (degarelix acetate; 4 mg/kg) on the secretions of plasma INSL3 and testosterone in two phases, an immediate and a long-term phase in male goats (n = 6; aged, 13-16 months). During the immediate phase, blood was taken at 15-minute intervals for 8 hours on Days -5, 0, and 3...
January 15, 2017: Theriogenology
https://www.readbyqxmd.com/read/27768220/gnrh-agonist-or-antagonist-in-the-treatment-of-prostate-cancer-a-comparision-based-on-oncological-results
#2
Stefano Salciccia, Alessandro Gentilucci, Susanna Cattarino, Alessandro Sciarra
On the basis of the trials available, are we ready to consider GnRH antagonists better than agonists? Is there a population of patients who may benefit from antagonists more than agonists?We specifically focused our analysis on the significance of oncological results obtained in phase III trials directly comparing Degarelix with GnRH agonists. Oncological results were evaluated only in 1 trial (CS21) with some subanalysis and they were not the primary endpoints of the study. The follow-up duration was 364 days, and therefore, the number of events (all causes deaths and prostate cancer (PC), Prostate Specific Antigen (PSA), Hazard ratio (HR)-related deaths) was very low in both groups and this aspect strongly reduces the significance of overall survival evaluation...
November 18, 2016: Urologia
https://www.readbyqxmd.com/read/27756786/a-phase-ii-randomized-open-label-study-of-neoadjuvant-degarelix-versus-lhrh-agonist-in-prostate-cancer-patients-prior-to-radical-prostatectomy
#3
Rashid Sayyid, Andrew Evans, Karen Hersey, Ranjena Maloni, Antonio Hurtado-Coll, Girish Kulkarni, Antonio Finelli, Alexandre R Zlotta, Robert Hamilton, Martin Gleave, Neil Fleshner
PURPOSE: Degarelix, a new GnRH receptor antagonist with demonstrated efficacy as first-line treatment in the management of high-risk prostate cancer, possesses some theoretical advantages over LHRH analogues in terms of avoiding "testosterone flare" and lower FSH levels. We set out to determine if pre-operative degarelix influenced surrogates of disease control in a randomized phase II study. EXPERIMENTAL DESIGN: 39 patients were randomly assigned to one of 3 different neo-adjuvant arms: degarelix only, degarelix/bicalutmaide, or LHRH agonist/bicalutamide...
October 18, 2016: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
https://www.readbyqxmd.com/read/27586506/a-comparative-study-on-the-efficacies-of-gonadotropin-releasing-hormone-gnrh-agonist-and-gnrh-antagonist-in-neoadjuvant-androgen-deprivation-therapy-combined-with-transperineal-prostate-brachytherapy-for-localized-prostate-cancer
#4
Kenta Miki, Hiroshi Sasaki, Masahito Kido, Hiroyuki Takahashi, Manabu Aoki, Shin Egawa
BACKGROUND: Neoadjuvant androgen deprivation therapy (ADT) has been suggested to confer several clinical benefits in patients with prostate cancer (PCa) undergoing transperineal prostate brachytherapy (TPPB). Unlike gonadotropin-releasing hormone (GnRH) receptor agonists, a GnRH antagonist such as degarelix can achieve castrate levels of testosterone without testosterone flare. However, normalization of serum testosterone levels following completion of neoadjuvant ADT in either form of treatment has never been compared in clinical trials...
2016: BMC Cancer
https://www.readbyqxmd.com/read/27569357/-giant-prostate-carcinoma-a-case-report-and-long-term-outcomes-in-japanese-patients
#5
Jun Furumido, Takashige Abe, Hiroshi Kikuchi, Naoto Miyajima, Kunihiko Tsuchiya, Satoru Maruyama, Nobuo Shinohara
A 79-year-old male was referred to the Department of Gastroenterology in our hospital due to a large palpable abdominal mass, with the suspicion of a gastrointestinal stromal tumor. An abdominal computed tomographic (CT) scan revealed a huge mass of 270×208×144 mm which occupied the entire pelvic cavity. Since the specimens obtained by an endoscopic ultrasound-guided fine-needle aspiration via lower intestinal tract revealed a Gleason score 4+4 prostate adenocarcinoma, he was then referred to our department...
July 2016: Hinyokika Kiyo. Acta Urologica Japonica
https://www.readbyqxmd.com/read/27429605/response-of-degarelix-treatment-in-human-prostate-cancer-monitored-by-hr-mas-1-h-nmr-spectroscopy
#6
Basetti Madhu, Greg L Shaw, Anne Y Warren, David E Neal, John R Griffiths
INTRODUCTION: The androgen receptor (AR) is the master regulator of prostate cancer cell metabolism. Degarelix is a novel gonadotrophin-releasing hormone blocker, used to decrease serum androgen levels in order to treat advanced human prostate cancer. Little is known of the rapid metabolic response of the human prostate cancer tissue samples to the decreased androgen levels. OBJECTIVES: To investigate the metabolic responses in benign and cancerous tissue samples from patients after treatment with Degarelix by using HRMAS (1)H NMR spectroscopy...
2016: Metabolomics: Official Journal of the Metabolomic Society
https://www.readbyqxmd.com/read/27399062/a-meta-analysis-and-systematic-review-of-randomized-controlled-trials-with-degarelix-versus-gonadotropin-releasing-hormone-agonists-for-advanced-prostate-cancer
#7
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)
https://www.readbyqxmd.com/read/27390687/degarelix-for-the-treatment-of-advanced-prostate-cancer-compared-with-gnrh-agonists-a-systematic-review-and-meta-analysis
#8
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
https://www.readbyqxmd.com/read/27364704/questionable-oncologic-benefits-of-degarelix
#9
EDITORIAL
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
https://www.readbyqxmd.com/read/27306809/combination-of-gnrh-antagonist-degarelix-and-antiandrogen-is-effective-in-psa-reduction-and-bone-management-in-patients-with-prostate-cancer
#10
Junichi Hori, Naoki Wada, Gaku Tamaki, Makoto Azumi, Masafumi Kita, Tatsuya Iwata, Seiji Matsumoto, Hidehiro Kakizaki
OBJECTIVES: To investigate the efficacy of combination treatment of degarelix and antiandrogen in patients with prostate cancer. METHODS: We prospectively investigated the efficacy of combination treatment of degarelix and antiandrogen in 12 patients with treatment-naive prostate cancer. We surveyed PSA, LH, FSH and testosterone at day 3, 7, 14 and 28 during the initial month and thereafter once a month for 1 year. In cases with bone metastasis, we analyzed serum bone markers such as alkaline phosphatase(ALP), bone-type ALP and carboxyterminal telopeptide of type- I collagen once a month...
June 2016: Gan to Kagaku Ryoho. Cancer & Chemotherapy
https://www.readbyqxmd.com/read/27230983/elucidation-of-the-mechanism-of-suppressed-steroidogenesis-during-androgen-deprivation-therapy-of-prostate-cancer-patients-using-a-mouse-model
#11
H Taniguchi, T Katano, K Nishida, H Kinoshita, T Matsuda, S Ito
Androgen deprivation therapy (ADT) is the standard medical approach to the management of prostate cancer. Patients switched from a GnRH antagonist to a GnRH agonist, did not experience a testosterone surge in spite of the occurrence of luteinizing hormone (LH) surge in our protocol of clinical study. To clarify this observation, male mice pre-treated with two different doses of the GnRH antagonist degarelix for 28 days were further administered the GnRH agonist leuprolide or chorionic gonadotropin, and testosterone production of the mice was studied...
September 2016: Andrology
https://www.readbyqxmd.com/read/27189011/treatment-with-a-gnrh-receptor-agonist-but-not-the-gnrh-receptor-antagonist-degarelix-induces-atherosclerotic-plaque-instability-in-apoe-mice
#12
Anki Knutsson, Sabrina Hsiung, Selvi Celik, Sara Rattik, Ingrid Yao Mattisson, Maria Wigren, Howard I Scher, Jan Nilsson, Anna Hultgårdh-Nilsson
Androgen-deprivation therapy (ADT) for prostate cancer has been associated with increased risk for development of cardiovascular events and recent pooled analyses of randomized intervention trials suggest that this primarily is the case for patients with pre-existing cardiovascular disease treated with gonadotropin-releasing hormone receptor (GnRH-R) agonists. In the present study we investigated the effects of the GnRH-R agonist leuprolide and the GnRH-R antagonist degarelix on established atherosclerotic plaques in ApoE(-/-) mice...
May 18, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27034720/degarelix-monotherapy-compared-with-luteinizing-hormone-releasing-hormone-lhrh-agonists-plus-anti-androgen-flare-protection-in-advanced-prostate-cancer-an-analysis-of-two-randomized-controlled-trials
#13
Peter Iversen, Jan-Erik Damber, Anders Malmberg, Bo-Eric Persson, Laurence Klotz
OBJECTIVES: The objective of this study was to assess differences in efficacy outcomes between luteinizing hormone-releasing hormone (LHRH) agonist plus antiandrogen (AA) flare protection and monotherapy with the gonadotrophin-releasing hormone antagonist degarelix in patients with prostate cancer. METHODS: Data from 1455 patients were pooled from two prospective, phase III randomized 1-year clinical trials of degarelix versus LHRH agonist with or without AA. The AA bicalutamide was administered at the investigator's discretion...
April 2016: Therapeutic Advances in Urology
https://www.readbyqxmd.com/read/26989369/clinical-effect-of-switching-from-a-luteinizing-hormone-releasing-hormone-agonist-to-an-antagonist-in-patients-with-castration-resistant-prostate-cancer-and-serum-testosterone-level-%C3%A2-20-ng-dl
#14
Norihito Soga, Takumi Kageyama, Yuji Ogura, Tomomi Yamada, Norio Hayashi
INTRODUCTION: The efficacy of conversion from a luteinizing hormone-releasing hormone agonist to an antagonist was evaluated prospectively in patients with castration-resistant prostate cancer. MATERIALS AND METHODS: From October 2012 to December 2014, 8 cases with a serum testosterone level ≥ 20 ng/dl during following androgen deprivation therapy were enrolled and received degarelix monthly. The primary end-pointgoal was to determine the effective prostate-specific antigen response rate...
February 2016: Current Urology
https://www.readbyqxmd.com/read/26908406/differences-in-hypercholesterolemia-and-atherogenesis-induced-by-common-androgen-deprivation-therapies-in-male-mice
#15
Christian Bo Poulsen, Martin Bødtker Mortensen, Wolfgang Koechling, Charlotte Brandt Sørensen, Jacob Fog Bentzon
BACKGROUND: Treatment of prostate cancer often involves androgen deprivation therapy (ADT) by gonadotropin-releasing hormone (GnRH) receptor agonists, GnRH receptor antagonists, or orchiectomy. ADT may increase the rate of cardiovascular disease events, but recent clinical studies suggested that not all means of ADT carry the same risk, raising the possibility of non-testosterone-mediated effects of different forms of ADT on atherosclerosis. Here we compared effects of ADT on atherosclerosis in intact and orchiectomized Apoe-deficient mice...
February 2016: Journal of the American Heart Association
https://www.readbyqxmd.com/read/26892063/optimizing-subcutaneous-injection-of-the-gonadotropin-releasing-hormone-receptor-antagonist-degarelix
#16
Jack Barkin, Shelley Burton, Carole Lambert
The gonadotropin-releasing hormone (GnRH) receptor antagonist degarelix has several unique characteristics compared to luteinizing hormone-releasing hormone (LHRH) analogs used in the management of prostate cancer. Notable differences of GnRH receptor antagonists include no flare reaction, and a more rapid suppression of testosterone, luteinizing hormone (LH), follicle stimulating hormone (FSH) and prostate-specific antigen (PSA) compared to LHRH analogs. Despite emerging evidence supporting the use of GnRH receptor antagonists over the more widely used LHRH analogs in the management of prostate cancer, physicians may be reluctant to prescribe degarelix...
February 2016: Canadian Journal of Urology
https://www.readbyqxmd.com/read/26780073/-direct-and-indirect-costs-of-luteinising-hormone-releasing-hormone-analogues-in-the-treatment-of-locally-advanced-or-metastatic-prostate-cancer-in-italy
#17
Valeria Fadda, Dario Maratea
BACKGROUND: When analyzing the use of luteinizing hormone-releasing hormone (LHRH) analogues for different clinical indications, current available evidence does not support a presumed drug class effect among the various LHRH in the treatment of prostate cancer. METHODS: The following search key words were entered in the PubMed database and the NICE and FDA websites: “LHRH agonist AND prostatic cancer”, “androgen deprivation therapy”, “androgen suppression”, “buserelin”, “leuprorelin”, “goserelin”,“triptorelin”, “degarelix”...
December 2015: Recenti Progressi in Medicina
https://www.readbyqxmd.com/read/26674089/degarelix-therapy-for-prostate-cancer-in-a-real-world-setting-experience-from-the-german-iquo-association-for-uro-oncological-quality-assurance-firmagon%C3%A2-registry
#18
Götz Geiges, Thomas Harms, Gerald Rodemer, Ralf Eckert, Frank König, Rolf Eichenauer, Jörg Schroder
BACKGROUND: We investigated the use of the gonadotropin-releasing hormone (GnRH) antagonist degarelix in everyday clinical practice using registry data from uro-oncology practices in Germany. METHODS: Data were analysed retrospectively from the IQUO (Association for uro-oncological quality assurance) patient registry. Data were prospectively collected from all consecutive PCa patients treated with degarelix (n = 1010) in 138 uro-oncology practices in Germany between May 2009 and December 2013...
2015: BMC Urology
https://www.readbyqxmd.com/read/26657335/choline-kinase-alpha-as-an-androgen-receptor-chaperone-and-prostate-cancer-therapeutic-target
#19
Mohammad Asim, Charles E Massie, Folake Orafidiya, Nelma Pértega-Gomes, Anne Y Warren, Mohsen Esmaeili, Luke A Selth, Heather I Zecchini, Katarina Luko, Arham Qureshi, Ajoeb Baridi, Suraj Menon, Basetti Madhu, Carlos Escriu, Scott Lyons, Sarah L Vowler, Vincent R Zecchini, Greg Shaw, Wiebke Hessenkemper, Roslin Russell, Hisham Mohammed, Niki Stefanos, Andy G Lynch, Elena Grigorenko, Clive D'Santos, Chris Taylor, Alastair Lamb, Rouchelle Sriranjan, Jiali Yang, Rory Stark, Scott M Dehm, Paul S Rennie, Jason S Carroll, John R Griffiths, Simon Tavaré, Ian G Mills, Iain J McEwan, Aria Baniahmad, Wayne D Tilley, David E Neal
BACKGROUND: The androgen receptor (AR) is a major drug target in prostate cancer (PCa). We profiled the AR-regulated kinome to identify clinically relevant and druggable effectors of AR signaling. METHODS: Using genome-wide approaches, we interrogated all AR regulated kinases. Among these, choline kinase alpha (CHKA) expression was evaluated in benign (n = 195), prostatic intraepithelial neoplasia (PIN) (n = 153) and prostate cancer (PCa) lesions (n = 359). We interrogated how CHKA regulates AR signaling using biochemical assays and investigated androgen regulation of CHKA expression in men with PCa, both untreated (n = 20) and treated with an androgen biosynthesis inhibitor degarelix (n = 27)...
May 2016: Journal of the National Cancer Institute
https://www.readbyqxmd.com/read/26613055/prostate-cancer-associated-disseminated-intravascular-coagulation-with-excessive-fibrinolysis-treated-with-degarelix
#20
Shawn Y Ong, Josephine Taverna, Clint Jokerst, Thomas Enzler, Emad Hammode, Elisa Rogowitz, Myke R Green, Hani M Babiker
Disseminated intravascular coagulation (DIC) with excessive fibrinolysis (XFL) is a rare and acute life-threatening variant of DIC in patients with prostate cancer. Patients present with coagulopathy, hypofibrinogenemia, and systemic bleeding. We describe a case of DIC XFL caused by prostate cancer (PC) successfully treated with a single injection of degarelix, a gonadotropin-releasing hormone (GnRH) receptor antagonist. This led to prompt control of the patient's coagulopathy within ten days of treatment. Our case highlights features of this rare and devastating hemorrhagic complication of PC along with a fast-acting and effective therapeutic drug option...
2015: Case Reports in Oncological Medicine
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