Enzalutamide binds to androgen receptors and thereby inhibits them (antiandrogen). In addition, translocation in the cell nuclei is inhibited and the binding to the DNA is weakened, as well as the recruitment of cofactors for transcription. This leads to the inhibition of gene expression, which are regulated by the androgen receptors. Due to the triple mechanism of action, Enzalutamide differs from the usual anti-androgenic substances. Due to its anti-androgenic properties, the active ingredient also has an antineoplastic effect in androgen-sensitive tumors (e.g. metastatic prostate cancer).
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