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Human In Vivo Metabolism and Elimination Behavior of Micro-Dosed Selective Androgen Receptor Modulator RAD140 for

Felicitas Wagener1, Luisa Euler1, Christian Görgens1

  • 1Institute of Biochemistry/Center for Preventive Doping Research, German Sports University Cologne, Am Sportpark Müngersdorf 6, 50933 Cologne, Germany.

Metabolites
|July 27, 2022
PubMed

Insights

RAD140, a prohibited substance in sports, has its human metabolism and excretion studied. This research identifies key metabolites in urine, aiding the World Anti-Doping Agency in distinguishing between intentional doping and supplement contamination.

Area of Science:

  • Pharmacology
  • Analytical Chemistry
  • Sports Science

Background:

  • RAD140 is a selective androgen receptor modulator banned by the World Anti-Doping Agency (WADA).
  • Distinguishing RAD140 doping from dietary supplement contamination is challenging due to limited human metabolism data.

Purpose of the Study:

  • To investigate the metabolism and excretion of RAD140 in humans.
  • To identify RAD140 metabolites in urine for improved doping control.

Main Methods:

  • Six micro-dose excretion studies were conducted with adult male volunteers.
  • Urine samples were analyzed using Liquid Chromatography-High Resolution Mass Spectrometry (LC-HRMS/MS).
  • Enzymatic hydrolysis was used for sample preparation to estimate RAD140 concentrations.

Main Results:

  • Multiple novel metabolites of RAD140 were detected in human urine.
  • Elimination profiles and detection times for six metabolites and intact RAD140 were established.
  • Metabolite ratios showed potential for estimating RAD140 dosage.

Conclusions:

  • The study provides crucial data on RAD140 metabolism and excretion in humans.
  • Identified metabolites and analytical methods will enhance doping control and case management.
  • This research supports WADA's efforts in combating illicit substance use in sports.
Keywords:
RAD140dopingelimination profilemetabolismselective androgen receptor modulators (SARMs)

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