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Prostate cancer (PCa) ranks the second most diagnosed cancers among men globally and the sixth leading cause of cancer-related deaths. Advanced prostate cancer can be defined as the recurrence after definitive therapies (radical prostatectomy or external beam radiotherapy) and de novo metastasis (metastasis without prior treatment). Advanced PCa can be categorized as metastatic hormone sensitive prostate cancer (mHSPC), non-metastatic castration resistant prostate cancer (nmCRPC), and metastatic castration resistant prostate cancer (mCRPC). Management of advanced PCa often involves castration to reduce testosterone levels, which can be achieved by gonadotropin releasing hormone antagonists such as degarelix and relugolix. Degarelix is injectable while relugolix is an orally administered form of GnRH antagonist. This review aims to explore the latest pharmacological aspects of these drugs to inform treatment decisions for advanced PCa.
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