GHRP‐2 (pralmorelin, D‐Ala‐D‐(β‐naphthyl)‐Ala‐Ala‐Trp‐D‐Phe‐Lys‐NH2), which belongs to a class of growth hormone secretagogue (GHS), is intravenously used to diagnose growth hormone (GH) deficiency. Because it may be misused in expectation of a growth‐promoting effect by athletes, the illicit use of GHS by athletes has been prohibited by the World Anti‐Doping Agency (WADA). Therefore, the mass spectrometric identification of urinary GHRP‐2 and its metabolite D‐Ala‐D‐(β‐naphthyl)‐Ala‐Ala‐OH (AA‐3) was studied using liquid chromatography/electrospray ionization tandem mass spectrometry for doping control purposes. The method consists of solid‐phase extraction using stable‐isotope‐labeled GHRP‐2 as an internal standard and subsequent ultra‐performance liquid chromatography/tandem mass spectrometry, and the two target peptides were determined at urinary concentrations of 0.5–10 ng/mL. The recoveries ranged from 84 to 101%, and the assay precisions were calculated as 1.6–3.8% (intra‐day) and 1.9–4.3% (inter‐day). Intravenous administration of GHRP‐2 in ten male volunteers was studied to demonstrate the applicability of the method. In all ten cases, unchanged GHRP‐2 and its specific metabolite AA‐3 were detected in urine. Copyright © 2010 John Wiley & Sons, Ltd.