Investigation of in vitro generated metabolites of GLPG0492 using equine liver microsomes for doping control

Tajudheen K. Karatt, M. Anwar Sathiq, Saraswathy Laya, Moses Philip, Abdul Khader Karakka Kal, Michael Benedict Subhahar

Research output: Contribution to journalArticlepeer-review

5 Citations (Scopus)

Abstract

An effective alternative to testosterone therapy is selective androgen receptor modulators, a class of compounds that has a tissue-specific effect on muscle and bone. These drugs, which enhance performance, pose a severe abuse risk in competitive sports. GLPG0492 is one of the selective androgen receptor modulators discovered in recent decades. This compound has a unique tissue-specific action for muscle and bone against steroid receptors and acts as a partial agonist for androgen receptors. This study examined GLPG0492 and its metabolites in vitro using equine liver microsomes. Liquid chromatography–high-resolution mass spectrometry was utilized to determine the probable structures of detected metabolites. This study identified 39 metabolites of GLPG0492 (21 phase I and 18 phase II). The hydroxylation of GLPG0492 results in monohydroxylated and dihydroxylated metabolites. Additionally, the study detected dissociated side chains (3-methyl and 4-(hydroxymethyl)) and corresponding hydroxylated metabolites. A series of glucuronic acid- and sulfonic acid-conjugated analogs of GLPG0492 were detected during phase II of the study. The findings might help in the detection of GLPG0492 and the elucidation of its illegal use in equestrian sports.

Original languageEnglish
Pages (from-to)605-628
Number of pages24
JournalDrug Testing and Analysis
Volume15
Issue number6
DOIs
Publication statusPublished - Jun 2023

Keywords

  • GLPG0492
  • SARMs
  • doping control
  • in vitro
  • selective androgen receptor modulators

ASJC Scopus subject areas

  • Analytical Chemistry
  • Environmental Chemistry
  • Pharmaceutical Science
  • Spectroscopy

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