Human in vivo metabolism study of LGD-4033

Human in vivo metabolism study of LGD-4033 / Argyro G. Fragkaki, Panagiotis Sakellariou, Polyxeni Kiousi, Nassia Kioukia-Fougia, Maria Tsivou, Michael Petrou, Yiannis Angelis. - (Drug Testing and Analysis 10 (2018) 11-12 (November-December); p. 1635-1645)

  • PMID: 30255601
  • DOI: 10.1002/dta.2512

Erratum in:

Human in vivo metabolism study of LGD-4033 / Argyro G. Fragkaki, Panagiotis Sakellariou, Polyxeni Kiousi, Nassia Kioukia-Fougia, Maria Tsivou, Michael Petrou, Yiannis Angelis. - (Drug Testing and Analysis 12 (2020) 1 (January); p. 164)

  • DOI: 10.1002/dta.2700. Epub 2019 Nov 17.
  • PMID: 31984662


Abstract

Selective androgen receptor modulators (SARMs) are an emerging class of therapeutics targeted to cachexia, sarcopenia, and hypogonadism treatment. LGD-4033 is a SARM which has been included on the Prohibited List annually released by the World Anti-Doping Agency (WADA). The aim of the present work was the investigation of the metabolism of LGD-4033 in a human excretion study after administration of an LGD-4033 supplement, the determination of the metabolites' excretion profiles with special interest in the determination of its long-term metabolites, and the comparison of the excretion time of the phase I and phase II metabolites. The results were also compared to those derived from previous LGD-4033 studies concerning both in vitro and in vivo experiments. Supplement containing LGD-4033 was administered to one human male volunteer and urine samples were collected up to almost 21 days. Analysis of the hydrolyzed (with β-glucuronidase) as well as of the non-hydrolyzed samples was performed using liquid chromatography-high resolution mass spectrometry (LC-HRMS) in negative ionization mode and revealed that, in both cases, the two isomers of the dihydroxylated metabolite (M5) were preferred target metabolites. The gluco-conjugated parent LGD-4033 and its gluco-conjugated metabolites M1 and M2 can be also considered as useful target analytes in non-hydrolyzed samples. The study also presents two trihydroxylated metabolites (M6) identified for the first time in human urine; one of them was recently reported in an LGD-4033 metabolism study in horse urine and plasma.

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Science
Study
Date
25 September 2018
People
Angelis, Yanis S.
Fragkaki, Argyro G.
Kioukia-Fougia, Nassia
Kiousi, Polyxeni
Petrou, Michael
Sakellariou, Panagiotis
Tsivou, Maria
Country
Greece
Language
English
Other organisations
Cyprus Anti-Doping Authority (CyADA)
Εθνικό και Καποδιστριακό Πανεπιστήμιο Αθηνών - National and Kapodistrian University of Athens (NKUA)
Laboratories
Athens, Greece: Doping Control Laboratory of Athens
Analytical aspects
Half-life / excretion time of substance
Mass spectrometry analysis
Metabolization
Testing method development
Doping classes
S1. Anabolic Agents
Substances
LGD-4033 (ligandrol)
Selective androgen receptor modulators (SARMs)
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22 October 2020
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24 October 2020
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