Comparative safety evaluation of selective androgen receptor modulators and anabolic androgenic steroids

Expert Opin Drug Saf. 2015;14(11):1773-85. doi: 10.1517/14740338.2015.1094052. Epub 2015 Sep 24.

Abstract

Introduction: Anabolic androgenic steroids (AASs) have been in use for decades for the treatment of short stature, severe burns, HIV wasting syndrome, osteoporosis, and anemia. However, their lack of selective effects on certain symptoms and unfavorable pharmacokinetic properties has limited their long-term usage in clinics.

Areas covered: Selective androgen receptor modulators (SARMs) have some advantages over AASs; they are highly specific for androgen receptors, are orally available, and, most importantly, act as strong receptor agonists in skeletal muscle and bone, and as weak agonists or antagonists in androgen-responsive tissues such as the prostate and sebaceous glands. The exact molecular mechanism, however, has not been fully elucidated. This article includes a toxicological review of major AASs, and a comparative safety analysis of major AASs and SARMs in clinical trials to evaluate the therapeutic potential of SARMs.

Expert opinion: Based on the robust tissue selectivity of SARMs over AASs, they are worth considering as a promising therapeutic option for the treatment of various muscle-wasting diseases.

Keywords: anabolic androgenic steroid; muscle wasting disease; safety; selective androgen receptor modulator.

Publication types

  • Comparative Study
  • Review

MeSH terms

  • Anabolic Agents / administration & dosage
  • Anabolic Agents / adverse effects*
  • Androgen Receptor Antagonists / administration & dosage
  • Androgen Receptor Antagonists / adverse effects*
  • Androgens / administration & dosage
  • Androgens / adverse effects*
  • Animals
  • Humans
  • Muscular Diseases / drug therapy
  • Muscular Diseases / pathology

Substances

  • Anabolic Agents
  • Androgen Receptor Antagonists
  • Androgens