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LGD\u20104033 is a SARM which has been included on the Prohibited List annually released by the World Anti\u2010Doping Agency (WADA). The aim of the present work was the investigation of the metabolism of LGD\u20104033 in a human excretion study after administration of an LGD\u20104033 supplement, the determination of the metabolites' excretion profiles with special interest in the determination of its long\u2010term 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\u20104033 studies concerning both in vitro and in vivo experiments.<\/jats:p><jats:p>Supplement containing LGD\u20104033 was administered to one human male volunteer and urine samples were collected up to almost 21\u00a0days. Analysis of the hydrolyzed (with \u03b2\u2010glucuronidase) as well as of the non\u2010hydrolyzed samples was performed using liquid chromatography\u2013high resolution mass spectrometry (LC\u2013HRMS) in negative ionization mode and revealed that, in both cases, the two isomers of the dihydroxylated metabolite (M5) were preferred target metabolites. The gluco\u2010conjugated parent LGD\u20104033 and its gluco\u2010conjugated metabolites M1 and M2 can be also considered as useful target analytes in non\u2010hydrolyzed 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\u20104033 metabolism study in horse urine and plasma.<\/jats:p>","DOI":"10.1002\/dta.2512","type":"journal-article","created":{"date-parts":[[2018,9,25]],"date-time":"2018-09-25T21:59:07Z","timestamp":1537912747000},"page":"1635-1645","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":39,"title":["Human in vivo metabolism study of LGD\u20104033"],"prefix":"10.1002","volume":"10","author":[{"ORCID":"https:\/\/orcid.org\/0000-0002-9422-670X","authenticated-orcid":false,"given":"Argyro G.","family":"Fragkaki","sequence":"first","affiliation":[{"name":"Doping Control Laboratory of Athens Olympic Athletic Center of Athens \u201cSpyros Louis\u201d  37 Kifisias Avenue 15123 Maroussi 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