Discovery and therapeutic promise of selective androgen receptor modulators.

Chen J; Kim J; Dalton JT

doi:10.1124/mi.5.3.7

Discovery and therapeutic promise of selective androgen receptor modulators.

Chen J, Kim J, Dalton JT

Molecular interventions · 2005 · doi:10.1124/mi.5.3.7 · PMID:15994457 · PMC2072877

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This review article examines the development and therapeutic potential of selective androgen receptor modulators, which are designed to provide tissue-specific androgenic effects while minimizing unwanted side effects. The author discusses the structural basis for ligand selectivity and highlights preclinical data demonstrating the efficacy of these compounds in treating conditions such as muscle wasting and prostate cancer. The paper outlines the mechanism by which these modulators differentially regulate gene transcription in various tissues compared to traditional androgens. The paper does not explicitly discuss endometriosis or adenomyosis; it was included in the corpus via a keyword match in the upstream search index.

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Abstract

Androgens are essential for male development and the maintenance of male secondary characteristics, such as bone mass, muscle mass, body composition, and spermatogenesis. The main disadvantages of steroidal androgens are their undesirable physicochemical and pharmacokinetic properties. The recent discovery of nonsteroidal selective androgen receptor modulators (SARMs) provides a promising alternative for testosterone replacement therapies with advantages including oral bioavailability, flexibility of structural modification, androgen receptor specificity, tissue selectivity, and the lack of steroid-related side effects.

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