Discovery and Therapeutic Promise of Selective Androgen Receptor Modulators

  1. Jiyun Chen1,
  2. Juhyun Kim1 and
  3. James T. Dalton1,2
  1. 1Division of Pharmaceutics, College of Pharmacy, The Ohio State University, Columbus, Ohio 43210, and
  2. 2GTx, Inc., Memphis, TN 38163


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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