Current understanding of prostate cancer has identified the androgen receptor (AR) signalling pathway as a logical target for the treatment of CRPC. AR is the biological target of androgens, like testosterone and dihydrotestosterone (DHT). Available therapies that inhibit the AR signalling pathway include AR blockers, androgen biosynthesis inhibitors, and AR signalling inhibitors. Enzalutamide is a competitive and selective silent antagonist of AR and effects multiple stages of the signalling pathway. It has been described as an AR signaling inhibitor in addition to antagonist. As a result of its use, proliferation of prostate cancer cells decreases which ultimately leads to apoptosis and decreased tumour volume.
Furthermore, Enzalutamide, the first approved AR signalling inhibitor, has a novel mode of action targeting AR signalling at three key stages. The direct mode of action of enzalutamide has been shown to translate into clinical responses in patients with mCRPC. In conclusion, the targeting of the AR signalling pathway in patients with mCRPC results in numerous clinical benefits.
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