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Selective Androgen Receptor Modulators in Drug Discovery: Medicinal Chemistry and Therapeutic Potential

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Modulation of the androgen receptor has the potential to be an effective treatment for hypogonadism, andropause, and associated conditions such as sarcopenia, osteoporosis, benign prostatic hyperplasia, and sexual dysfunction. Side effects associated with classical anabolic steroid treatments have driven the quest for drugs that demonstrate improved therapeutic profiles. Novel, non-steroidal compounds that show tissue selective activity and improved pharmacokinetic properties have been developed. This review provides an overview of current advances in the development of selective androgen receptor modulators (SARMs).
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Keywords: AR; SARMs; dihydrotestosterone; estradiol; hypogonadism; modulation; testosterone; tissue selectivity

Document Type: Research Article

Affiliations: GlaxoSmithKline Inc, Metabolic and Viral Diseases Drug Discovery, Research Triangle Park, PO Box 13398, NC 27705, USA.

Publication date: February 1, 2006

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