Quantification of osilodrostat in horse urine using LC/ESI-HRMS to establish an elimination profile for doping control.
Abstract: The use of osilodrostat, developed as a medication for Cushing's disease but categorized as an anabolic agent, is banned in horses by both the International Federation of Horseracing Authorities and the Fédération Equestre Internationale. For doping control purposes, elimination profiles of hydrolyzed osilodrostat in horse urine were established and the detectability of free forms of osilodrostat and its major metabolite, mono-hydroxylated osilodrostat (M1c), was investigated. Post-administration urine samples obtained from a gelding and three mares were analyzed to establish the elimination profiles of osilodrostat using a validated method involving efficient enzymatic hydrolysis followed by LC/ESI-HRMS analysis. Applying the validated quantification method with an LLOQ of 0.05 ng/ml, hydrolyzed osilodrostat could be quantified in post-administration urine samples from 48 to 72 h post-administration; by contrast, both hydrolyzed osilodrostat and M1c were detected up to 2 weeks. In addition, confirmatory analysis identified the presence of hydrolyzed osilodrostat for up to 72 h post-administration. For doping control purposes, we recommend monitoring both hydrolyzed M1c and osilodrostat because of the greater detectability of M1c and the availability of a reference material of osilodrostat, which is essential for confirmatory analysis. [Box: see text].
Publication Date: 2024-09-05 PubMed ID: 39235065DOI: 10.1080/17576180.2024.2385848Google Scholar: Lookup
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- Journal Article
Summary
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This research paper investigates the detection of the drug Osilodrostat in horse urine, aiming to establish an elimination profile that could help in anti-doping efforts.
Introduction
- Osilodrostat is a medication initially developed for Cushing’s disease but is classified as an anabolic agent that boosts performance in horses.
- The drug is considered illegal in horse racing and other equestrian sports and is banned by both the International Federation of Horseracing Authorities and the Fédération Equestre Internationale.
Objective and Methodology
- The primary aim of this research was to establish elimination profiles of hydrolyzed osilodrostat in horse urine, in order to detect the presence of the drug for doping control purposes.
- The secondary objective was to investigate the detectability of free forms of osilodrostat and its major metabolite, mono-hydroxylated osilodrostat (M1c).
- The researchers used post-administration urine samples obtained from a gelding and three mares.
- The elimination profiles of Osilodrostat were analyzed using a validated method involving efficient enzymatic hydrolysis followed by Liquid chromatography-electrospray ionization-high resolution mass spectrometry (LC/ESI-HRMS) analysis.
Results and Findings
- The validated quantification method allowed the researchers to quantify hydrolyzed osilodrostat in post-administration urine samples from 48 to 72 hours post-administration.
- Both hydrolyzed osilodrostat and its metabolite, M1c, were detectable up to two weeks post-administration.
- A confirmatory analysis also identified the presence of hydrolyzed osilodrostat for up to 72 hours post-administration.
Conclusion
- For doping control purposes, the researchers recommend monitoring both hydrolyzed M1c and osilodrostat.
- Emphasis is placed on M1c due to its greater detectability and the availability of a reference material of osilodrostat, which is crucial for confirmatory analysis.
Cite This Article
APA
Ishii H, Shigematsu R, Takemoto S, Ishikawa Y, Mizobe F, Nomura M, Arima D, Kunii H, Yuasa R, Yamanaka T, Tanabe S, Nagata SI, Yamada M, Leung GN.
(2024).
Quantification of osilodrostat in horse urine using LC/ESI-HRMS to establish an elimination profile for doping control.
Bioanalysis, 1-12.
https://doi.org/10.1080/17576180.2024.2385848 Publication
Researcher Affiliations
- Drug Analysis Department, Laboratory of Racing Chemistry, 1731-2 Tsuruta-machi, Utsunomiya, Tochigi, 320-0851, Japan.
- Department of Pharmaceutical Sciences, Tohoku University Hospital, 1-1 Seiryo-machi, Aoba-ku, Sendai, Miyagi, 980-8574, Japan.
- Drug Analysis Department, Laboratory of Racing Chemistry, 1731-2 Tsuruta-machi, Utsunomiya, Tochigi, 320-0851, Japan.
- Drug Analysis Department, Laboratory of Racing Chemistry, 1731-2 Tsuruta-machi, Utsunomiya, Tochigi, 320-0851, Japan.
- Anti-Doping Section, Equine Department, Japan Racing Association, 1-1-1 Nishishimbashi, Minato-ku, Tokyo, 105-0003, Japan.
- Anti-Doping Section, Equine Department, Japan Racing Association, 1-1-1 Nishishimbashi, Minato-ku, Tokyo, 105-0003, Japan.
- Anti-Doping Section, Equine Department, Japan Racing Association, 1-1-1 Nishishimbashi, Minato-ku, Tokyo, 105-0003, Japan.
- Equine Veterinary Clinic, Horse Racing School, Japan Racing Association, 835-1 Ne Shiroi city, Chiba, Japan, 270-1431, Japan.
- Equine Veterinary Clinic, Horse Racing School, Japan Racing Association, 835-1 Ne Shiroi city, Chiba, Japan, 270-1431, Japan.
- Equine Veterinary Clinic, Horse Racing School, Japan Racing Association, 835-1 Ne Shiroi city, Chiba, Japan, 270-1431, Japan.
- Research Planning & Coordination Division, Equine Research Institute, Japan Racing Association, 1400-4 Shiba, Shimotsuke, Tochigi, 329-0412, Japan.
- Research Planning & Coordination Division, Equine Research Institute, Japan Racing Association, 1400-4 Shiba, Shimotsuke, Tochigi, 329-0412, Japan.
- Drug Analysis Department, Laboratory of Racing Chemistry, 1731-2 Tsuruta-machi, Utsunomiya, Tochigi, 320-0851, Japan.
- Drug Analysis Department, Laboratory of Racing Chemistry, 1731-2 Tsuruta-machi, Utsunomiya, Tochigi, 320-0851, Japan.
- Drug Analysis Department, Laboratory of Racing Chemistry, 1731-2 Tsuruta-machi, Utsunomiya, Tochigi, 320-0851, Japan.
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