title: Mass spectrometric characterization of urinary metabolites of the selective androgen receptor modulator andarine (S-4) for routine doping control purposes.
abstract: Selective androgen receptor modulators (SARMs) are potent anabolic agents with tissue-selective properties. Due to their potential misuse in elite sport, the World Anti-Doping Agency (WADA) has prohibited SARMs since 2008, and although no representative drug candidate has yet received full clinical approval, recent findings of SARMs illegally sold via the internet have further supported the need to efficiently test for these compounds in doping controls. In the present communication, the mass spectrometric characterization of urinary metabolites of the SARM Andarine (also referred to as S-4) compared with earlier in vitro and animal studies is reported. Liquid chromatography interfaced to high-resolution/high-accuracy (tandem) mass spectrometry was used to identify phase I and II metabolites, confirming the predicted target analytes for sports drug testing purposes including the glucuronic acid conjugates of the active drug, its monohydroxylated and/or deacetylated product, the hydrolysis product resulting from the removal of the compound's B-ring, as well as the sulfate of the monohydroxylated and the deacetylated phase I metabolite. The obtained data will support future efforts to effectively screen for and confirm the misuse of the non-approved drug candidate Andarine.
authors.affiliation: Institute of Biochemistry - Center for Preventive Doping Research, German Sport University Cologne, Am Sportpark Müngersdorf 6, 50933 Cologne, Germany. m.thevis@biochem.dshs-koeln.de
authors.forename: Mario
authors.initials: M
authors.lastname: Thevis
authors.forename: Andreas
authors.initials: A
authors.lastname: Thomas
authors.forename: Gregor
authors.initials: G
authors.lastname: Fusshöller
authors.forename: Simon
authors.initials: S
authors.lastname: Beuck
authors.forename: Hans
authors.initials: H
authors.lastname: Geyer
authors.forename: Wilhelm
authors.initials: W
authors.lastname: Schänzer
mesh_terms: D000081:Acetamides / Q000378:metabolism / Q000652:urine*; D000627:Aminophenols / Q000378:metabolism / Q000652:urine*; D045930:Anabolic Agents / Q000378:metabolism / Q000652:urine*; D000728:Androgens; D004300:Doping in Sports / Q000517:prevention & control; D006801:Humans; D008297:Male; D013058:Mass Spectrometry / Q000379:methods*; D008875:Middle Aged; D015813:Substance Abuse Detection / Q000379:methods*
chemical_list: D000081:Acetamides; D000627:Aminophenols; D045930:Anabolic Agents; D000728:Androgens; C492992:andarine