Grapiprant: A snapshot of the current knowledge

J Vet Pharmacol Ther. 2021 Sep;44(5):679-688. doi: 10.1111/jvp.12983. Epub 2021 May 31.

Abstract

Grapiprant is the pioneer member of the novel piprant class, a potent and specific antagonist of the prostaglandin E2 receptor 4. It has been approved in veterinary medicine for the control of pain and inflammation associated with osteoarthritis in dogs at the dose regimen of 2 mg/kg once a day by the FDA and EMA (for pain only) in 2016 and 2018, respectively. The aim of this narrative review was to report the analytical methods, pharmacokinetics, pharmacodynamics and safety of grapiprant in several animal species using the best available published scientific evidence. In conclusion, most of the analytical methods proposed for grapiprant detection are simple, reliable, sensitive and validated. The pharmacokinetics show discrepancies between animal species. The therapeutic efficacy seems more suited to chronic rather than acute pain.

Keywords: analytical method; grapiprant; pharmacodynamics; pharmacokinetics; review; safety.

Publication types

  • Review

MeSH terms

  • Animals
  • Dinoprostone
  • Dog Diseases* / drug therapy
  • Dogs
  • Osteoarthritis* / drug therapy
  • Osteoarthritis* / veterinary
  • Pain / veterinary
  • Sulfonylurea Compounds

Substances

  • Sulfonylurea Compounds
  • grapiprant
  • Dinoprostone