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Ketodarolutamide is a nonsteroidal antiandrogen (NSAA) and the major active metabolite of darolutamide. Like its parent compound, it acts as a highly selective and high-affinity competitive silent antagonist of the androgen receptor (AR). Ketodarolutamide demonstrates potent inhibition of AR signaling with higher affinity than other NSAAs such as enzalutamide and apalutamide. It exhibits limited central nervous system distribution, indicating peripheral selectivity. The drug shows little or no inhibition or induction of cytochrome P450 enzymes like CYP3A4. Ketodarolutamide is not marketed independently but is relevant pharmacologically due to its activity as the main metabolite responsible for much of darolutamide’s clinical effect in prostate cancer therapy[1][4][6].
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