The Efficacy and Safety of Degarelix, a GnRH Antagonist: A 12-month, Multicentre, Randomized, Maintenance Dose-finding Phase II Study in Japanese Patients with Prostate Cancer

Abstract

Both monthly degarelix dosing regimens were found to be effective in testosterone suppression without a testosterone surge, prostate-specific antigen reductions and anti-tumour effect in Japanese patients with prostate cancer, as was shown in the overseas Phase III study. Degarelix was also well tolerated.

Androgen receptor antagonists for prostate cancer therapy

“…To circumvent the flares, LHRH antagonists have been developed, resulting in an equally effective, but more rapid chemical castration as LHRH agonists (Van Poppel et al 2008, Crawford et al 2011, Garnick & Mottet 2012, Ozono et al 2012. Moreover, the LHRH antagonists do not have increased risk for cardiovascular diseases as is the case for LHRH agonists (Levine et al 2010).…”

Bench-to-bedside development of agonists and antagonists of luteinizing hormone–releasing hormone for treatment of advanced prostate cancer

“…The efficacy and safety of degarelix were evaluated in 3 open-label, randomized, parallel-group, 1-year dose-finding phase II clinical trials in Europe/South Africa [38], North America [39], and Japan [40], including adult men with histologically confirmed PCa (all stages) for whom hormonal treatment was indicated. These studies determined that the most effective doses of degarelix were 240-mg loading dose and 80-or 160-mg maintenance dose.…”

The current abilities of third-generation luteinizing hormone-releasing hormone antagonists in the treatment of hormone-responsive prostate cancer

“…Препарат высвобожда-ется в кровоток в два этапа: короткая, начальная, фаза быстрого высвобождения, затем фаза медленного высвобождения, при ко-торой период полураспада препарата составляет несколько не-дель. Удлиненный полураспад после подкожной инъекции дега-реликса считается следствием очень медленного высвобождения лекарственного вещества из комплекса, который образуется в месте инъекции [19,[31][32][33][34][35][36][37].…”

“…Пациенты (средний возраст 74 го-да) имели средний исходный уровень тестостерона и ПСА 4,41 и 22,4 нг/мл соответственно. Степень распространенности заболе-вания: локализованная форма -у 46% пациентов, местно-рас-пространенная -у 30%, метастатическая -у 23% и неклассифи-цированная -меньше 1% пациентов [35].…”