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Degarelix

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https://www.readbyqxmd.com/read/29624800/efficacy-and-safety-of-3-month-dosing-regimen-of-degarelix-in-japanese-subjects-with-prostate-cancer-a-phase-iii-study
#1
Seiichiro Ozono, Taiji Tsukamoto, Seiji Naito, Shigeo Horie, Yasuo Ohashi, Hiroji Uemura, Yumiko Yokomizo, Satoshi Fukasawa, Hidehito Kusuoka, Rio Akazawa, Masako Saito, Hideyuki Akaza
Non-inferiority in the cumulative castration rate of the 3-month formulation of degarelix compared with the 3-month formulation of goserelin was evaluated in subjects with prostate cancer. A phase III, open-label, parallel-arm study was conducted. An initial dose of 240 mg of degarelix or 3.6 mg of goserelin was subcutaneously administered; after day 28, a maintenance dose of 480 mg of degarelix or 10.8 mg of goserelin was administered once every 84 days. Non-inferiority in castration rate and safety of degarelix to goserelin were evaluated...
April 6, 2018: Cancer Science
https://www.readbyqxmd.com/read/29606109/neoadjuvant-degarelix-with-or-without-apalutamide-followed-by-radical-prostatectomy-for-intermediate-and-high-risk-prostate-cancer-arneo-a-randomized-double-blind-placebo-controlled-trial
#2
Lorenzo Tosco, Annouschka Laenen, Thomas Gevaert, Isabelle Salmon, Christine Decaestecker, Elai Davicioni, Christine Buerki, Frank Claessens, Johan Swinnen, Karolien Goffin, Raymond Oyen, Wouter Everaerts, Lisa Moris, Gert De Meerleer, Karin Haustermans, Steven Joniau
BACKGROUND: Recent retrospective data suggest that neoadjuvant androgen deprivation therapy can improve the prognosis of high-risk prostate cancer (PCa) patients. Novel androgen receptor pathway inhibitors are nowadays available for treatment of metastatic PCa and these compounds are promising for early stage disease. Apalutamide is a pure androgen antagonist with a very high affinity with the androgen receptor. The combination of apalutamide with degarelix, an LHRH antagonist, could increase the efficacy compared to degarelix alone...
April 2, 2018: BMC Cancer
https://www.readbyqxmd.com/read/29556048/combining-immune-check-point-blockade-and-cryoablation-in-an-immunocompetent-hormone-sensitive-murine-model-of-prostate-cancer
#3
Benjamin Benzon, Stephanie A Glavaris, Brian W Simons, Robert M Hughes, Kamyar Ghabili, Patrick Mullane, Rebecca Miller, Katriana Nugent, Brian Shinder, Jeffrey Tosoian, Ephraim J Fuchs, Phuoc T Tran, Paula J Hurley, Milena Vuica-Ross, Edward M Schaeffer, Charles G Drake, Ashley E Ross
BACKGROUND: Prostate cancer remains the second leading cause of cancer related death in men. Immune check point blocking antibodies have revolutionized treatment of multiple solid tumors, but results in prostate cancer remain marginal. Previous reports have suggested that local therapies, in particular cryoablation might increase tumor immunogenicity. In this work, we examine potential synergism between tumor cryoabalation and check point blocking antibodies. METHODS: FVB/NJ mice were injected subcutaneously into each flank with either 1 × 106 or 0...
March 20, 2018: Prostate Cancer and Prostatic Diseases
https://www.readbyqxmd.com/read/29552115/usefulness-of-endoscopic-ultrasound-guided-fine-needle-aspiration-for-lymphadenopathy
#4
Yuki Tanisaka, Shomei Ryozawa, Masanori Kobayashi, Maiko Harada, Tsutomu Kobatake, Kumiko Omiya, Hirotoshi Iwano, Shin Arai, Kouichi Nonaka, Yumi Mashimo
Lymphadenopathy may be difficult to diagnose using imaging results alone. Endoscopic ultrasound-guided fine needle aspiration (EUS-FNA) may help to diagnose and determine the appropriate management of lymphadenopathy. EUS-FNA has been used as a safe and less invasive method for obtaining pathologic specimens from extraluminal lesions using endoscopic ultrasound. The present study evaluated the usefulness of EUS-FNA for lymphadenopathy. Between July 2013 and December 2016, 72 patients undergoing EUS-FNA for lymphadenopathy that could not be diagnosed solely using imaging were included...
April 2018: Oncology Letters
https://www.readbyqxmd.com/read/29545772/a-proof-of-concept-clinical-trial-of-a-single-luteal-use-of-long-acting-gonadotropin-releasing-hormone-antagonist-degarelix-in-controlled-ovarian-stimulation-for-in-vitro-fertilization-long-antagonist-protocol
#5
Evangelos G Papanikolaou, Hakan Yarali, Evi Timotheou, Michael Grynberg, Odysseas Zafeiratis, Herman Tournaye, Robert Najdecki
Introduction: A drawback of gonadotropin-releasing hormone (GnRH) antagonist protocols in in vitro fertilization (IVF) is that they have limited flexibility in cycle programming. This proof of concept study explored the efficacy of a single-dose, long-acting GnRH antagonist IVF protocol. Trial registration number is NCT03240159, retrospectively registered on March 08, 2017. Materials and methods: The efficacy of a single-dose long-acting antagonist, degarelix, was explored initially in healthy donors and subsequently in infertile patients...
2018: Frontiers in Endocrinology
https://www.readbyqxmd.com/read/29534997/a-phase-ii-randomized-multicentre-study-comparing-10-months-versus-4-months-of-degarelix-firmagon%C3%A2-therapy-in-prolonging-the-off-treatment-interval-in-men-with-localized-prostate-cancer-receiving-intermittent-androgen-deprivation-therapy-for-biochemical-recurrence
#6
L Klotz, A Loblaw, R Siemens, P Ouellette, A Kapoor, M Kebabdjian, L Zhang, F Saad
BACKGROUND: In men initiating intermittent androgen deprivation therapy (IADT), a range of induction durations, between 3 and 12 months, have been employed. OBJECTIVE: To determine if the duration of induction ADT influences the duration of the off treatment interval and the recovery of serum testosterone (T). MANEUVER: This was a prospective, randomized, open label study. Men with biochemical recurrence after local therapy for prostate cancer, with a negative bone scan, were randomized between 4 and 10 months of monthly Degarelix...
March 10, 2018: Journal of Urology
https://www.readbyqxmd.com/read/29463549/androgen-deprivation-therapy-potentiates-the-efficacy-of-vascular-targeted-photodynamic-therapy-of-prostate-cancer-xenografts
#7
Kwanghee Kim, Philip A Watson, Souhil Lebdai, Sylvia Jebiwott, Alexander Somma, Stephen P La Rosa, Dipti Mehta, Katie S Murray, Hans G Lilja, David Ulmert, Sebastien Monette, Avigdor J Scherz, Jonathan Coleman
PURPOSE: WST11 vascular targeted photodynamic therapy (VTP) is a local ablation approach relying upon rapid, free radical-mediated destruction of tumor vasculature. A phase III trial showed that VTP significantly reduced disease progression when compared to active surveillance in patients with low-risk prostate cancer (PCa). The aim of this study was to identify a druggable pathway that could be combined with VTP to improve its efficacy and applicability to higher risk PCa tumors. EXPERIMENTAL DESIGN: Transcriptome analysis of VTP treated tumors (LNCaP-AR xenografts) was used to identify a candidate pathway for combination therapy...
February 20, 2018: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
https://www.readbyqxmd.com/read/29446744/delivery-of-peptidic-gonadotropin-releasing-hormone-antagonists
#8
Rawda Yaseen AlSheyyab, Bashar Mohammad Al-Taani, Rana Mohammad Obeidat, Motasem Mohammad Alsmadi, Rafeef Khalid Masaedeh, Raghda Nasry Sabat
GnRH antagonists have several clinical applications in prostate cancer, regulation of ovulation induction in females, breast cancer, male contraception and others. Antagonists differ from natural GnRH decapeptide in having five or more amino acid substitutions. Whereas most of antagonists are available as subcutaneous (SC) formula for injection, some are formulated as a depot formulation for sustained release (e.g. Cetrarelix, Degarelix). Systemic delivery of cetrorelix acetate by intratracheal route can be achieved using dry powder for inhalation of adhesive mixture when the powder deposition reaches stage four...
February 14, 2018: Current Drug Delivery
https://www.readbyqxmd.com/read/29398594/a-phase-ii-trial-of-8-weeks-of-degarelix-for-prostate-volume-reduction-efficacy-and-hormonal-recovery
#9
M A Korzeniowski, J M Crook, D Bowes, M Gaztañaga, A Ots, J Jazwal, J Rose, A Tétreault-Laflamme, L Pilote, R Halperin, D Kim, D Petrik, C Araujo, F Bachand
PURPOSE: The purpose of this study was to determine the efficacy of 8 weeks of degarelix for prostate downsizing before interstitial brachytherapy. We also report associated toxicity and the time course of endocrine recovery over the following 12 months. METHODS AND MATERIALS: Fifty patients were accrued to an open-label Phase II clinical trial (www.clinicaltrials.gov ID NCT01446991). Baseline prostate transrectal ultrasound (TRUS) was performed on all patients followed by degarelix administration and a repeat TRUS at Week 8...
February 2, 2018: Brachytherapy
https://www.readbyqxmd.com/read/29378196/additive-effect-of-simultaneous-continuous-administration-of-degarelix-and-tak-448-on-lh-suppression-in-a-castrated-rat-model
#10
Jacek Stalewski, Diane M Hargrove, Monica Wolfe, Trudy A Kohout, Adeela Kamal
Gonadotropin releasing hormone (GnRH) analogs have long been used in androgen deprivation therapy (ADT) in the treatment of prostate cancer. Chronic administration of either GnRH agonists or antagonists leads to suppression of testosterone production in the testes via either downregulation or direct blockade of the GnRH receptor in the pituitary, respectively. Chronic administration of kisspeptin analogs has more recently been shown to lead to testosterone suppression via desensitization of GnRH neurons in the hypothalamus and an optimized kisspeptin analog, TAK-448, was proven effective in a small phase 1 trial...
January 25, 2018: European Journal of Pharmacology
https://www.readbyqxmd.com/read/29051056/recovery-of-serum-testosterone-levels-and-sexual-function-in-patients-treated-with-short-term-luteinizing-hormone-releasing-hormone-antagonist-as-a-neoadjuvant-therapy-before-external-radiotherapy-for-intermediate-risk-prostate-cancer-preliminary-prospective
#11
Takahiro Inoue, Takashi Mizowaki, Daijiro Kabata, Ayumi Shintani, Naoki Terada, Toshinari Yamasaki, Hiromitsu Negoro, Takashi Kobayashi, Kiyonao Nakamura, Haruo Inokuchi, Osamu Ogawa
INTRODUCTION: External beam radiation therapy (EBRT) with short-term androgen deprivation therapy is the standard of care for intermediate-risk prostate cancer patients. However, no study to date has evaluated the hormonal kinetics or sexual and hormonal function recovery after cessation of short-term luteinizing hormone (LH)-releasing hormone (LHRH) antagonist treatment. PATIENTS AND METHODS: Ten intermediate-risk prostate cancer patients (mean age, 69.9 years) were included...
September 23, 2017: Clinical Genitourinary Cancer
https://www.readbyqxmd.com/read/28960413/an-efficient-synthesis-of-deuterium-labeled-degarelix-acetate-a-third-generation-gonadotropin-releasing-hormone-receptor-antagonist
#12
Yu Huang, Jingshun Chen, Baomin Liu, Hua Wang, Lu Zhang, Zhengbang Chen, Yinsheng Zhang
Degarelix acetate, a third-generation gonadotropin-releasing hormone (GnRH) receptor antagonist, shows great potential in the treatment of many androgen-related diseases. To support clinical studies of degarelix acetate, deuterium-labeled degarelix is highly desired for use as an internal standard. Using D2 O/D3 PO4 as a deuterium source, 2-amino-3-(naphthalen-2-yl)propanoic acid was converted to deuterated degarelix acetate in 13 steps and in 14% overall yield.
September 29, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/28870102/therapeutic-outcomes-of-the-lhrh-antagonists
#13
REVIEW
Athanasios Dellis, Athanasios Papatsoris
Recently, LHRH antagonists have been established in the management of advanced prostate cancer, although the vast majority of Medical Oncologists and Urologists still prefer the LHRH agonists. Areas Covered: In this article we assess the therapeutic outcomes and the safety of the LHRH antagonists (mainly degarelix) compared to the LHRH agonists. Expert Commentary: Relevant studies demonstrated that LHRH antagonists are at least non-inferior to the LHRH agonists regarding therapeutic efficacy and safety, while there is potential benefit over the LHRH agonists in terms of cardiovascular morbidity and disease control...
October 2017: Expert Review of Pharmacoeconomics & Outcomes Research
https://www.readbyqxmd.com/read/28851333/a-gonadotropin-releasing-hormone-antagonist-reduces-serum-adrenal-androgen-levels-in-prostate-cancer-patients
#14
Yoshiyuki Miyazawa, Yoshitaka Sekine, Takahiro Syuto, Masashi Nomura, Hidekazu Koike, Hiroshi Matsui, Yasuhiro Shibata, Kazuto Ito, Kazuhiro Suzuki
BACKGROUND: Adrenal androgens play an important role in the development of castration-resistant prostate cancer therapeutics. The effect of gonadotropin-releasing hormone (GnRH) antagonists on adrenal androgens has not been studied sufficiently. We measured testicular and adrenal androgen levels in patients treated with a GnRH antagonist. METHODS: This study included 47 patients with histologically proven prostate cancer. All of the patients were treated with the GnRH antagonist degarelix...
August 29, 2017: BMC Urology
https://www.readbyqxmd.com/read/28680962/switching-from-an-lhrh-antagonist-to-an-lhrh-agonist-a-case-report-of-10-finnish-patients-with-advanced-prostate-cancer
#15
Harri Visapää
INTRODUCTION: Luteinizing hormone-releasing hormone (LHRH) analogues are widely used for the treatment of advanced hormone-dependent prostate cancer. However, there are currently no clinical guidelines for switching between LHRH analogues. It has been reported that there may be clinical benefits for patients switching between different formulations of LHRH agonists, as well as from an LHRH agonist to LHRH antagonist, but there are no published data on switching from an LHRH antagonist to an LHRH agonist...
2017: Oncology and Therapy
https://www.readbyqxmd.com/read/28660498/effect-of-degarelix-a-gonadotropin-releasing-hormone-receptor-antagonist-for-the-treatment-of-prostate-cancer-on-cardiac-repolarisation-in-a-randomised-placebo-and-active-comparator-controlled-thorough-qt-qtc-trial-in-healthy-men
#16
Håkan Olsson, Niclas Petri, Lars Erichsen, Anders Malmberg, Lars Grundemar
BACKGROUND AND OBJECTIVES: Degarelix is a gonadotropin-releasing hormone antagonist registered for the treatment of advanced hormone-dependent prostate cancer. Treatment causing androgen deprivation is associated with QT prolongation and this study investigated whether degarelix at supratherapeutic concentrations has an intrinsic effect per se on cardiac repolarisation and the QT interval. METHODS: This was a single-centre, randomised, crossover study comparing the effect of degarelix, placebo, and the positive control moxifloxacin on the QT interval...
September 2017: Clinical Drug Investigation
https://www.readbyqxmd.com/read/28480768/degarelix-versus-luteinizing-hormone-releasing-hormone-agonists-for-the-treatment-of-prostate-cancer
#17
REVIEW
Timothy N Clinton, Solomon L Woldu, Ganesh V Raj
Androgen deprivation therapy (ADT) is the mainstay for advanced, hormone-sensitive prostate cancer, and options include surgical castration, luteinizing hormone-releasing hormone (LHRH) agonist, and more recently, gonadotropin releasing hormone (GnRH) antagonist therapy. Our understanding of the mechanisms and adverse effects of ADT has increased substantially, including the class-specific adverse effects of ADT. Areas covered: This review will summarize the pharmacodynamic and pharmacokinetic properties of the GnRH antagonist degarelix and its role in the management of advanced prostate cancer, the clinical evidence supporting its regulatory approval, as well as potential benefits and disadvantages over traditional LHRH agonist therapy...
June 2017: Expert Opinion on Pharmacotherapy
https://www.readbyqxmd.com/read/28405705/-cost-effectiveness-of-gnrh-antagonists-in-patients-with-prostate-cancer-and-cardiovascular-risk-comparative-analysis-against-leuprorelin-by-the-number-needed-to-treat
#18
D Anderson, J Lehmann, T Ecker, S Vosgerau, V Donatz
BACKGROUND: Recent studies suggest that androgen deprivation therapy (ADT) is associated with increased cardiovascular (CV) risk for patients with hormone-sensitive prostate cancer (PCa) and pre-existing CV disease. This risk seems to be different for the gonadotropin-releasing hormone (GnRH) agonists leuprolide and goserelin and GnRH antagonists, whereas the slightly more expensive GnRH antagonist shows a beneficial risk profile. The present study assesses the cost effectiveness of degarelix compared to leuprolide for PCa patients with increased CV risk...
July 2017: Der Urologe. Ausg. A
https://www.readbyqxmd.com/read/28394542/-effectiveness-and-safety-of-degarelix-in-treating-hormone-sensitive-prostate-cancer-review-of-the-recent-literature
#19
A V Govorov, A O Vasil'ev, D Yu Pushkar
Since their first clinical use in 1990 and up to the present time, the luteinizing hormone-releasing hormone (LHRH) analogues have formed the mainstay of androgen deprivation therapy of patients with hormone-sensitive prostate cancer. The transient testosterone surge inherent in this group of hormonal therapy medications might contribute to cardiovascular complications, limiting to some extent their use. Conversely, LHRH antagonists have a minimal adverse effect profile and their use in clinical practice is seen as more promising...
December 2016: Urologii︠a︡
https://www.readbyqxmd.com/read/28394498/degarelix-versus-goserelin-plus-bicalutamide-in-the-short-term-relief-of-lower-urinary-tract-symptoms-in-prostate-cancer-patients-results-of-a-pooled-analysis
#20
RANDOMIZED CONTROLLED TRIAL
Malcolm Mason, Pierre Richaud, Zsolt Bosnyak, Anders Malmberg, Anders Neijber
OBJECTIVE: In patients with prostate cancer (PCa), prostate enlargement may give rise to lower urinary tract symptoms (LUTS); many patients suffer from moderate-to-severe symptoms. We compare the efficacy of degarelix and goserelin plus bicalutamide in improving LUTS in PCa patients. METHODS: Data were pooled from three Phase 3, randomized clinical trials of once-monthly treatment for 12 weeks with degarelix (240/80 mg; n = 289) or goserelin (3.6 mg) plus bicalutamide (50 mg; n = 174) for initial flare protection...
May 2017: Lower Urinary Tract Symptoms
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