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Drug Discov Today. 2007 Mar;12(5-6):241-8. Epub 2007 Feb 7.

Expanding the therapeutic use of androgens via selective androgen receptor modulators (SARMs).

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  • 1Division of Pharmaceutics, College of Pharmacy, The Ohio State University, 500 W 12th Avenue, Columbus, OH 43210, USA.


Selective androgen receptor modulators (SARMs) are a novel class of androgen receptor (AR) ligands that might change the future of androgen therapy dramatically. With improved pharmacokinetic characteristics and tissue-selective pharmacological activities, SARMs are expected to greatly extend the clinical applications of androgens to osteoporosis, muscle wasting, male contraception and diseases of the prostate. Mechanistic studies with currently available SARMs will help to define the contributions of differential tissue distribution, tissue-specific expression of 5alpha-reductase, ligand-specific regulation of gene expression and AR interactions with tissue-specific coactivators to their observed tissue selectivity, and lead to even greater expansion of selective anabolic therapies.

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