Androgen Receptor Modulators: A Review of Recent Patents and Reports (2012-2018)

    Shinya Fujii, Hiroyuki Kagechika
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    TLDR New androgen receptor modulators show promise for treating diseases like prostate cancer and muscle wasting.
    The document from 2019 reviews patents and reports from 2012 to 2018 on androgen receptor (AR) modulators, highlighting the importance of AR in drug discovery for conditions like prostate cancer and muscle-wasting diseases. It discusses various AR modulators, including conventional antagonists, selective AR modulators (SARMs), degraders, and compounds targeting non-ligand-binding domains of AR. The review emphasizes the need for next-generation antiandrogens due to emerging AR mutations and suggests that targeting the N-terminal domain (NTD) and DNA-binding domain (DBD) could be promising strategies. It details the development of compounds with potent AR antagonistic or agonistic activities, some showing selective degradation of AR or dual inhibition of AR and other enzymes. The review also covers the structure-activity relationship of these modulators and their potential therapeutic benefits, including the treatment of osteoporosis, sarcopenia, frailty, and cancer cachexia. It concludes that noncompetitive AR transcription inhibitors and AR down-regulators are promising for treating androgen-related diseases and that further investigations into the clinical usefulness of NTD binders and novel compounds are expected to contribute to new therapeutic approaches. The document does not provide specific numbers of people involved in studies as it focuses on molecular structures and in vitro cell line experiments.
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