Darolutamide
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Darolutamide is an androgen receptor antagonist used for castration-resistant, non-metastatic prostate cancer and metastatic hormone-sensitive prostate cancer.
Darolutamide is an androgen receptor antagonist used for castration-resistant, non-metastatic prostate cancer and metastatic hormone-sensitive prostate cancer.
The actions of androgens on androgen receptors (AR) potentiate the growth and survival of prostate cancer cells. Darolutamide competitively inhibits androgens from binding to their receptors, inhibiting AR nuclear translocation, as well as AR-mediated transcription. The end result of these processes is a decrease in prostate cancer cell proliferation and tumor size. Its main metabolite, keto-darolutamide, shows similar pharmacological activity to the parent drug, darolutamide. Darolutamide has been found to bind more tightly to the AR receptor than apalutamide and enzalutamide, which are other androgen receptor antagonists. Darolutamide can act as a progesterone receptor (PR) antagonist in the laboratory setting with approximately 1% activity when compared to its actions at the androgen receptor. The clinical relevance is not known at this time.
Darolutamide is indicated for the treatment of adults with non-metastatic castration-resistant prostate cancer (nmCRPC) and metastatic hormone-sensitive prostate cancer (mHSPC) in combination with docetaxel.
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