Abstract
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™ Orbitrap™ 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 β-glucuronidase, due to the high intensity and prolonged detection time in comparison to parent LGD-3303.
Document Type
Article
Publication Date
9-2023
Digital Object Identifier (DOI)
https://doi.org/10.1016/j.jpba.2023.115468
Funding Information
This research did not receive any specific grant from funding agencies in the public, commercial, or not-for-profit sectors.
Repository Citation
Broberg, Malin Nilsson; Knych, Heather; Bondesson, Ulf; Pettersson, Curt; Tidstedt, Börje; Stanley, Scott; Thevis, Mario; and Hedeland, Mikael, "Equine in vivo metabolite profiling of the selective androgen receptor modulator LGD-3303 for doping control" (2023). UK CARES Faculty Publications. 89.
https://uknowledge.uky.edu/ukcares_facpub/89
Included in
Analytical Chemistry Commons, Medical Biochemistry Commons, Pharmaceutics and Drug Design Commons
Notes/Citation Information
0731-7085/© 2023 The Authors. Published by Elsevier B.V. This is an open access article under the CC BY license (http://creativecommons.org/licenses/by/4.0/).