Equine in vivo metabolite profiling of the selective androgen receptor modulator LGD-3303 for doping control

LGD-3303 is a Selective Androgen Receptor Modulator (SARM) that is prohibited in both equine and human sports due to its anabolic properties. The aim of this study was to investigate the equine in vivo metabolite profile of LGD-3303 and identify drug metabolites that can be suitable as new and improved analytical targets for equine doping control. This was performed by an oral administration of 0.05 mg.kg(-1) LGD-3303 to horses, where blood and urine samples were collected up to 96 h after administration. The in vivo samples consisting of plasma, urine and hydrolyzed urine were analyzed utilizing ultra-high performance liquid chromatography hyphenated to a Q Exactive (TM) Orbitrap (TM) high resolution mass spectrometer with a heated electrospray ionization source. A total of eight metabolites of LGD-3303 were tentatively identified, including one carboxylated and several hydroxylated metabolites in combination with glucuronic acid conjugates. A monohydroxylated metabolite is suggested as an analytical target for doping control analysis of plasma and urine after hydrolysis with beta-glucuronidase, due to the high intensity and prolonged detection time in comparison to parent LGD-3303.

Knych, HeatherUniv Calif Davis, Sch Vet Med, Kenneth L Maddy Equine Analyt Pharmacol Lab, Davis, CA 95616 USA. (author)
Bondesson, UlfUppsala universitet,Analytisk farmaceutisk kemi(Swepub:uu)ulfbonde (author)
Pettersson, CurtUppsala universitet,Analytisk farmaceutisk kemi(Swepub:uu)curtps (author)
Tidstedt, BorjeNatl Vet Inst SVA, Dept Chem Environm & Feed Hyg, S-75189 Uppsala, Sweden. (author)
Stanley, ScottUniv Kentucky, Gluck Equine Res Ctr, Lexington, KY 40546 USA. (author)
Thevis, MarioGerman Sport Univ Cologne, Inst Biochem, Ctr Prevent Doping Res, D-50933 Cologne, Germany. (author)
Hedeland, MikaelUppsala universitet,Analytisk farmaceutisk kemi(Swepub:uu)mikahede (author)
Uppsala universitetAnalytisk farmaceutisk kemi (creator_code:org_t)

In:Journal of Pharmaceutical and Biomedical Analysis: Elsevier2330731-70851873-264X

By the author/editor: Nilsson Broberg, ...; Knych, Heather; Bondesson, Ulf; Pettersson, Curt; Tidstedt, Borje; Stanley, Scott; show more...; Thevis, Mario; Hedeland, Mikael; show less...

About the subject

NATURAL SCIENCES: NATURAL SCIENCES; and Chemical Science ...; and Analytical Chemi ...

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