In vitro metabolic studies of novel selective androgen receptor modulators and their use for doping control analysis

Drug Test Anal. 2022 Jan;14(1):122-136. doi: 10.1002/dta.3151. Epub 2021 Sep 7.

Abstract

Selective androgen receptor modulators were developed as a treatment of choice for diseases that are currently treated or symtomatically treated with steroidal androgens. The present study aimed to explore the metabolic pathways of four structurally unrelated SARMs, namely, PF-06260414, TFM-4AS-1, BMS-564929, and GSK 2881078, in terms of their potential toxicology or doping control analysis. Detected metabolism, mainly resulting from a single or multiple hydroxylations, methoxylation, demethylation, dehydrogenation, and glucuronidation, was considered as potential markers of intake of examined SARMs.

Keywords: BMS-564929; GSK 2881078; PF-0620414; TFM-4AS-1; metabolites.

MeSH terms

  • Anabolic Agents / analysis*
  • Anabolic Agents / metabolism
  • Androgen Receptor Antagonists / analysis
  • Androgen Receptor Antagonists / metabolism
  • Androgens / analysis
  • Androgens / metabolism
  • Doping in Sports / prevention & control*
  • Female
  • Humans
  • Male
  • Microsomes, Liver / metabolism
  • Substance Abuse Detection / methods*

Substances

  • Anabolic Agents
  • Androgen Receptor Antagonists
  • Androgens