In-vitro metabolism of GW1516 and implementation of its major metabolites in routine doping controls

Ines Möller; Andreas Thomas; Simon Beuck; Grigory Rodchenkov; Wolfgang Bornatsch; Hans Geyer; Wilhelm Schänzer; Mario Thevis

In-vitro metabolism of GW1516 and implementation of its major metabolites in routine doping controls

Ines Möller, Andreas Thomas, Simon Beuck, Grigory Rodchenkov, Wolfgang Bornatsch, Hans Geyer, Wilhelm Schänzer, Mario Thevis

Publication: Chapter in Book/Report/Conference proceeding › Conference contribution - Article for conference › Research

Abstract

The PPARδ-agonist GW1516 is categorized as a gene doping substance by the World Anti-Doping Agency due to its upregulation of genes associated with oxidative metabolism and a modified substrate preference potentially resulting in an improved athletic performance. To enable the detection of abuse in sport via analysis of urine specimens, the phase-I and -II metabolism of GW1516 was simulated by an in-vitro assay. Two oxygenated metabolites (sulfoxide and sulfone) were identified as main phase-I metabolites as well as one hydroxylation and the respective monoglucuronides of GW1516 and the oxygenated metabolites as phase-II metabolites. As the sulfoxide and the sulfone were both excreted in urine, they were chosen as target analytes and successfully implemented in routine doping control procedures. Verf.-Referat

Original language	German
Title of host publication	Recent advances in doping analysis (18) : Proceedings of the Manfred-Donike-Workshop, 28th Cologne Workshop on Dope Analysis : 7th to 12th March 2010
Editors	Wilhelm Schänzer, Hans Geyer, A. Gotzmann, Ute Mareck
Number of pages	10
Publisher	Sportverlag Strauß
Publication date	2010
Pages	17-26
Publication status	Published - 2010
Event	Cologne Workshop on Dope Analysis - Köln, Germany Duration: 07.03.2010 → 12.03.2010 Conference number: 28

Citation

Möller, I., Thomas, A., Beuck, S., Rodchenkov, G., Bornatsch, W., Geyer, H., Schänzer, W., & Thevis, M. (2010). In-vitro metabolism of GW1516 and implementation of its major metabolites in routine doping controls. In W. Schänzer, H. Geyer, A. Gotzmann, & U. Mareck (Eds.), Recent advances in doping analysis (18) : Proceedings of the Manfred-Donike-Workshop, 28th Cologne Workshop on Dope Analysis : 7th to 12th March 2010 (pp. 17-26). (Recent advances in doping analysis; Vol. 18). Sportverlag Strauß.

Möller, Ines ; Thomas, Andreas ; Beuck, Simon et al. / In-vitro metabolism of GW1516 and implementation of its major metabolites in routine doping controls. Recent advances in doping analysis (18) : Proceedings of the Manfred-Donike-Workshop, 28th Cologne Workshop on Dope Analysis : 7th to 12th March 2010. editor / Wilhelm Schänzer ; Hans Geyer ; A. Gotzmann ; Ute Mareck. Sportverlag Strauß, 2010. pp. 17-26 (Recent advances in doping analysis).

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title = "In-vitro metabolism of GW1516 and implementation of its major metabolites in routine doping controls",

abstract = "The PPARδ-agonist GW1516 is categorized as a gene doping substance by the World Anti-Doping Agency due to its upregulation of genes associated with oxidative metabolism and a modified substrate preference potentially resulting in an improved athletic performance. To enable the detection of abuse in sport via analysis of urine specimens, the phase-I and -II metabolism of GW1516 was simulated by an in-vitro assay. Two oxygenated metabolites (sulfoxide and sulfone) were identified as main phase-I metabolites as well as one hydroxylation and the respective monoglucuronides of GW1516 and the oxygenated metabolites as phase-II metabolites. As the sulfoxide and the sulfone were both excreted in urine, they were chosen as target analytes and successfully implemented in routine doping control procedures. Verf.-Referat",

keywords = "Doping, Dopinganalyse, Dopingbek{\"a}mpfung, Dopingkontrolle, Dopingnachweis, Gendoping, Metabolit",

author = "Ines M{\"o}ller and Andreas Thomas and Simon Beuck and Grigory Rodchenkov and Wolfgang Bornatsch and Hans Geyer and Wilhelm Sch{\"a}nzer and Mario Thevis",

year = "2010",

language = "Deutsch",

series = "Recent advances in doping analysis",

publisher = "Sportverlag Strau{\ss}",

pages = "17--26",

editor = "Wilhelm Sch{\"a}nzer and Hans Geyer and A. Gotzmann and Ute Mareck",

booktitle = "Recent advances in doping analysis (18) : Proceedings of the Manfred-Donike-Workshop, 28th Cologne Workshop on Dope Analysis : 7th to 12th March 2010",

note = "Cologne Workshop on Dope Analysis ; Conference date: 07-03-2010 Through 12-03-2010",

}

Möller, I, Thomas, A, Beuck, S, Rodchenkov, G, Bornatsch, W, Geyer, H , Schänzer, W & Thevis, M 2010, In-vitro metabolism of GW1516 and implementation of its major metabolites in routine doping controls. in W Schänzer, H Geyer, A Gotzmann & U Mareck (eds), Recent advances in doping analysis (18) : Proceedings of the Manfred-Donike-Workshop, 28th Cologne Workshop on Dope Analysis : 7th to 12th March 2010. Recent advances in doping analysis, vol. 18, Sportverlag Strauß, pp. 17-26, Cologne Workshop on Dope Analysis, Köln, Germany, 07.03.10.

In-vitro metabolism of GW1516 and implementation of its major metabolites in routine doping controls. / Möller, Ines; Thomas, Andreas; Beuck, Simon et al.
Recent advances in doping analysis (18) : Proceedings of the Manfred-Donike-Workshop, 28th Cologne Workshop on Dope Analysis : 7th to 12th March 2010. ed. / Wilhelm Schänzer; Hans Geyer; A. Gotzmann; Ute Mareck. Sportverlag Strauß, 2010. p. 17-26 (Recent advances in doping analysis; Vol. 18).

Publication: Chapter in Book/Report/Conference proceeding › Conference contribution - Article for conference › Research

TY - CHAP

T1 - In-vitro metabolism of GW1516 and implementation of its major metabolites in routine doping controls

AU - Möller, Ines

AU - Thomas, Andreas

AU - Beuck, Simon

AU - Rodchenkov, Grigory

AU - Bornatsch, Wolfgang

AU - Geyer, Hans

AU - Schänzer, Wilhelm

AU - Thevis, Mario

N1 - Conference code: 28

PY - 2010

Y1 - 2010

N2 - The PPARδ-agonist GW1516 is categorized as a gene doping substance by the World Anti-Doping Agency due to its upregulation of genes associated with oxidative metabolism and a modified substrate preference potentially resulting in an improved athletic performance. To enable the detection of abuse in sport via analysis of urine specimens, the phase-I and -II metabolism of GW1516 was simulated by an in-vitro assay. Two oxygenated metabolites (sulfoxide and sulfone) were identified as main phase-I metabolites as well as one hydroxylation and the respective monoglucuronides of GW1516 and the oxygenated metabolites as phase-II metabolites. As the sulfoxide and the sulfone were both excreted in urine, they were chosen as target analytes and successfully implemented in routine doping control procedures. Verf.-Referat

AB - The PPARδ-agonist GW1516 is categorized as a gene doping substance by the World Anti-Doping Agency due to its upregulation of genes associated with oxidative metabolism and a modified substrate preference potentially resulting in an improved athletic performance. To enable the detection of abuse in sport via analysis of urine specimens, the phase-I and -II metabolism of GW1516 was simulated by an in-vitro assay. Two oxygenated metabolites (sulfoxide and sulfone) were identified as main phase-I metabolites as well as one hydroxylation and the respective monoglucuronides of GW1516 and the oxygenated metabolites as phase-II metabolites. As the sulfoxide and the sulfone were both excreted in urine, they were chosen as target analytes and successfully implemented in routine doping control procedures. Verf.-Referat

KW - Doping

KW - Dopinganalyse

KW - Dopingbekämpfung

KW - Dopingkontrolle

KW - Dopingnachweis

KW - Gendoping

KW - Metabolit

M3 - Konferenzbeitrag - Aufsatz in Konferenzband

T3 - Recent advances in doping analysis

SP - 17

EP - 26

BT - Recent advances in doping analysis (18) : Proceedings of the Manfred-Donike-Workshop, 28th Cologne Workshop on Dope Analysis : 7th to 12th March 2010

A2 - Schänzer, Wilhelm

A2 - Geyer, Hans

A2 - Gotzmann, A.

A2 - Mareck, Ute

PB - Sportverlag Strauß

T2 - Cologne Workshop on Dope Analysis

Y2 - 7 March 2010 through 12 March 2010

ER -

Möller I, Thomas A, Beuck S, Rodchenkov G, Bornatsch W, Geyer H et al. In-vitro metabolism of GW1516 and implementation of its major metabolites in routine doping controls. In Schänzer W, Geyer H, Gotzmann A, Mareck U, editors, Recent advances in doping analysis (18) : Proceedings of the Manfred-Donike-Workshop, 28th Cologne Workshop on Dope Analysis : 7th to 12th March 2010. Sportverlag Strauß. 2010. p. 17-26. (Recent advances in doping analysis).