Blockage of gonadrotropin-releasing hormone (GnRH) receptor (GnRHR) leads to a decrease in both luteinizing hormone (LH) and follicle-stimulating hormone (FSH) release from the pituitary, and subsequently testosterone production from testes is suppressed. Degarelix is a GnRHR antagonist used in patients with prostate cancer (PCa) who need androgen deprivation therapy (ADT). In vitro, cell viability of different prostate cells was decreased after 24, 48, or 72h of treatment with 10 μM degarelix. Furthermore, degarelix treatment induced a significant increase on caspase 3/7 activation compared to control in normal, hyperplasia, and cancer cells indicating that cells were undergoing apoptosis using the caspase cascade[3]. In vivo, at single subcutaneous injections of 0.3 to 10 μg/kg in rats, degarelix produced a dose-dependent suppression of the pituitary-gonadal axis as revealed by the decrease in plasma LH and testosterone levels[4].
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