Mass spectrometry of selective androgen receptor modulators

J Mass Spectrom. 2008 Jul;43(7):865-76. doi: 10.1002/jms.1438.


Nonsteroidal selective androgen receptor modulators (SARMs) are an emerging class of drugs for treatment of various diseases including osteoporosis and muscle wasting as well as the correction of age-related functional decline such as muscle strength and power. Several SARMs, which have advanced to preclinical and clinical trials, are composed of diverse chemical structures including arylpropionamide-, bicyclic hydantoin-, quinoline-, and tetrahydroquinoline-derived nuclei. Since January 2008, SARMs have been categorized as anabolic agents and prohibited by the World Anti-Doping Agency (WADA). Suitable detection methods for these low-molecular weight drugs were based on mass spectrometric approaches, which necessitated the elucidation of dissociation pathways in order to characterize and identify the target analytes in doping control samples as well as potential metabolic products and synthetic analogs. Fragmentation patterns of representatives of each category of SARMs after electrospray ionization (ESI) and collision-induced dissociation (CID) as well as electron ionization (EI) are summarized. The complexity and structural heterogeneity of these drugs is a daunting challenge for detection methods.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Anabolic Agents / urine*
  • Androgen Antagonists / urine*
  • Androgen Receptor Antagonists*
  • Doping in Sports*
  • Humans
  • Male
  • Receptors, Androgen
  • Spectrometry, Mass, Electrospray Ionization / methods*
  • Sports
  • Substance Abuse Detection / methods*


  • AR protein, human
  • Anabolic Agents
  • Androgen Antagonists
  • Androgen Receptor Antagonists
  • Receptors, Androgen