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Detection of the growth hormone secretagogue MK-0677 in equine hair following oral administration.

Viljanto M, Cutler C, Taylor P, Habershon-Butcher J, Gray B.
Drug testing and analysis · December 19, 2022
Plain-language summary

This study investigated whether MK-0677 (ibutamoren), an orally active, non-peptide growth hormone secretagogue that activates the ghrelin receptor, could be detected in equine hair following oral administration to a single Thoroughbred racehorse. Researchers extracted MK-0677 and its O-dealkylated metabolite from mane and tail hair samples using an established method for prohibited substances, then analyzed them by liquid chromatography tandem mass spectrometry (LC-MS/MS). The study found that MK-0677 was detectable in all collected hair samples, with a detection window of up to 209 days in mane hair and 358 days in tail hair. A follow-up wash procedure confirmed true internal incorporation of the compound rather than mere surface contamination. Wash criteria analyses suggested that hair samples collected at later time points (≥52 days post-administration) reflected internal incorporation via the bloodstream, while the earliest sample (2 days) showed a combination of internal incorporation and external deposition via sweat and sebum. A key limitation is that the study involved only one horse, restricting generalizability. The findings are relevant to anti-doping efforts in equine sports, highlighting the long detection window MK-0677 may afford in hair matrices.

Why this grade: The study was conducted exclusively in a single Thoroughbred racehorse with no human subjects, providing pharmacokinetic and detection data relevant only to the equine context.

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Abstract

MK-0677 (ibutamoren) is an orally active non-peptide growth hormone secretagogue that binds to the ghrelin receptor stimulating the secretion of endogenous growth hormone. It is one of the most prevalent performance-enhancing compounds currently available online and is potentially subject to abuse both in human and equine sports. The aim of the current study was to investigate whether it could be detected in equine hair following oral administration of MK-0677 mesylate to a Thoroughbred racehorse. MK-0677 and its O-dealkylated metabolite were extracted using an existing method for prohibited substances in equine hair and analysed by liquid chromatography tandem mass spectrometry. This enabled the detection of MK-0677 in all hair samples collected, up to 209 days in mane and 358 days in tail. A follow-up methodology with an extensive wash procedure was carried out for selected hair samples, which unambiguously verified the presence of MK-0677. Wash criteria to differentiate between internal incorporation (via bloodstream) and external deposition (via sweat and sebum) was also assessed and indicated internal incorporation for the samples collected at later time points (≥52 days) and a combination of internal incorporation and external deposition for hair samples collected at the earlier time point (2 days).

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