Detection and pharmacokinetics of grapiprant following oral administration to exercised Thoroughbred horses

Heather K Knych, Kelsey Seminoff, Dan S. McKemie

Research output: Contribution to journalArticle

1 Citation (Scopus)

Abstract

Traditional therapeutic options for the treatment of lameness associated with inflammation in performance horses include administration of cyclooxygenase enzyme inhibiting non-steroidal anti-inflammatory drugs (NSAID). As long-term use of these drugs can adversely impact the health of the horse, anti-inflammatories with a more favorable safety profile are warranted. Grapiprant is a newly approved non-cyclooxygenase inhibiting NSAID that has demonstrated efficacy and safety in other species and which may be a valuable alternative to traditional NSAIDs used in the horse. The objectives of the current study were to describe drug concentrations and the pharmacokinetics of grapiprant in exercised Thoroughbred horses and to develop an analytical method that could be used to regulate its use in performance horses. To that end, grapiprant, at a dose of 2 mg/kg was administered orally to 12 exercised Thoroughbred horses. Blood and urine samples were collected prior to and for up to 96 hours post drug administration. Drug concentrations were measured using liquid chromatography–tandem mass spectrometry. Grapiprant remained above the LOQ of the assay (0.005 ng/mL) in serum for 72 hours post administration and urine concentrations were above the LOQ until 96 hours. The Cmax, Tmax and elimination half-life were 31.9 ± 13.9 ng/mL, 1.5 ± 0.5 hours and 5.86 ± 2.46 hours, respectively. The drug was well tolerated in all horses at a dose of 2 mg/kg. Results support further study of this compound in horses. Furthermore, development of a highly sensitive analytical method demonstrate that this compound can be adequately regulated in performance horses.

Original languageEnglish (US)
Pages (from-to)1237-1243
Number of pages7
JournalDrug Testing and Analysis
Volume10
Issue number8
DOIs
StatePublished - Aug 1 2018

Fingerprint

Pharmacokinetics
horse
Horses
Oral Administration
drug
Pharmaceutical Preparations
Anti-Inflammatory Agents
urine
analytical method
Urine
Non-Steroidal Anti-Inflammatory Agents
safety
Prostaglandin-Endoperoxide Synthases
Safety
grapiprant
pharmacokinetics
detection
Mass spectrometry
Assays
Blood

Keywords

  • grapiprant
  • horse
  • horse racing
  • NSAID
  • pharmacokinetics

ASJC Scopus subject areas

  • Analytical Chemistry
  • Environmental Chemistry
  • Pharmaceutical Science
  • Spectroscopy

Cite this

Detection and pharmacokinetics of grapiprant following oral administration to exercised Thoroughbred horses. / Knych, Heather K; Seminoff, Kelsey; McKemie, Dan S.

In: Drug Testing and Analysis, Vol. 10, No. 8, 01.08.2018, p. 1237-1243.

Research output: Contribution to journalArticle

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