Universität zu Köln

Wagener, Felicitas, Guddat, Sven, Gorgens, Christian, Angelis, Yiannis S., Petrou, Michael, Lagojda, Andreas, Kuehne, Dirk and Thevis, Mario (2022). Investigations into the elimination profiles and metabolite ratios of micro-dosed selective androgen receptor modulator LGD-4033 for doping control purposes. Anal. Bioanal. Chem., 414 (2). S. 1151 - 1163. HEIDELBERG: SPRINGER HEIDELBERG. ISSN 1618-2650

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Abstract

LGD-4033 (ligandrol) is a selective androgen receptor modulator (SARM), which is prohibited in sports by the World Anti-Doping Agency (WADA) and led to 62 adverse analytical findings (AAFs) in 2019. But not only deliberate doping with LGD-4033 constitutes a problem. In the past years, some AAFs that concerned SARMs can be attributed to contaminated dietary supplements (DS). Thus, the urgency to develop methods to differentiate between inadvertent doping and abuse of SARMs to benefit from the performance-enhancing effect of the compound in sports is growing. To gain a better understanding of the metabolism and excretion patterns of LGD-4033, human micro-dose excretion studies at 1, 10, and 50 mu g LGD-4033 were conducted. Collected urine samples were prepared for analysis using enzymatic hydrolysis followed by solid-phase extraction and analyzed via LC-HRMS/MS. Including isomers, a total of 15 phase I metabolites were detected in the urine samples. The LC-HRMS/MS method was validated for qualitative detection of LGD-4033, allowing for a limit of detection (LOD) of 8 pg/mL. The metabolite M1, representing the epimer of LGD-4033, was synthesized and the structure elucidated by NMR spectroscopy. As the M1/LGD-4033 ratio changes over time, the ratio and the approximate LGD-4033 concentration can contribute to estimating the time point of drug intake and dose of LGD-4033 in doping control urine samples, which is particularly relevant in anti-doping result management.

Item Type:	Journal Article
Creators:	Creators Email ORCID ORCID Put Code Wagener, Felicitas UNSPECIFIED UNSPECIFIED UNSPECIFIED Guddat, Sven UNSPECIFIED UNSPECIFIED UNSPECIFIED Gorgens, Christian UNSPECIFIED UNSPECIFIED UNSPECIFIED Angelis, Yiannis S. UNSPECIFIED UNSPECIFIED UNSPECIFIED Petrou, Michael UNSPECIFIED UNSPECIFIED UNSPECIFIED Lagojda, Andreas UNSPECIFIED UNSPECIFIED UNSPECIFIED Kuehne, Dirk UNSPECIFIED UNSPECIFIED UNSPECIFIED Thevis, Mario UNSPECIFIED UNSPECIFIED UNSPECIFIED
URN:	urn:nbn:de:hbz:38-589560
DOI:	10.1007/s00216-021-03740-7
Journal or Publication Title:	Anal. Bioanal. Chem.
Volume:	414
Number:	2
Page Range:	S. 1151 - 1163
Date:	2022
Publisher:	SPRINGER HEIDELBERG
Place of Publication:	HEIDELBERG
ISSN:	1618-2650
Language:	English
Faculty:	Unspecified
Divisions:	Unspecified
Subjects:	no entry
Uncontrolled Keywords:	Keywords Language SARMS Multiple languages Biochemical Research Methods; Chemistry, Analytical Multiple languages
URI:	http://kups.ub.uni-koeln.de/id/eprint/58956