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

Grapiprant: A snapshot of the current knowledge

Irene Sartini  1 , Mario Giorgi  2   3
Affiliations
Review

Grapiprant: A snapshot of the current knowledge

Irene Sartini et al. J Vet Pharmacol Ther. 2021 Sep.

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.

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Conflict of interest statement

Authors declare no conflict of interest.

Figures

FIGURE 1
FIGURE 1
Chemical structure of grapriprant (1‐[2‐[4‐(2‐ethyl‐4,6‐dimethylimidazo[4,5‐c]pyridin‐1‐yl) phenyl]ethyl]‐3‐(4‐methylphenyl) sulfonylurea)
FIGURE 2
FIGURE 2
Prostaglandins biosynthesis and related receptors. Grapiprant target is highlighted
FIGURE 3
FIGURE 3
Brief overview of the nociceptive system (top panel) and the role of PGE2 and the EP4 receptor in inflammatory nociception on the molecular level (bottom panel). AMPA, α‐amino‐3‐hydroxy‐5‐methyl‐4‐isoxazolepropionic acid receptor; CGRP, calcitonin gene‐related protein; CGRPr, calcitonin gene‐related protein receptor; CNS, central nervous system; DRG, dorsal root ganglia; Nav1.8, voltage‐gated sodium channel; NK, neurokinin receptor; NMDA, N‐methyl‐D‐aspartate receptor; PKA, protein kinase A; PKC, protein kinase C; Trk, Tropomyosin receptor kinase A (NGF receptor)
See this image and copyright information in PMC

References

    1. Anonymous (2016a). NADA 141‐455 GALLIPRANT. https://animaldrugsatfda.fda.gov/adafda/app/search/public/document/downl...
    1. Anonymous (2016b). Galliprant prescribing information. Aratana Therapeutics. https://files.brief.vet/2018‐07/Galliprant%20Prescribing%20Information_E...
    1. Baralla, E. , Vito, V. D. , Varoni, M. V. , Giorgi, M. , & Demontis, M. (2018). Novel LC‐MS/MS method for CJ‐023423 (grapiprant) determination in rabbit plasma. American Journal of Animal and Veterinary Sciences, 13, 45–50. 10.3844/ajavsp.2018.45.50 - DOI
    1. Basbaum, A. I. , Bautista, D. M. , Scherrer, G. , & Julius, D. (2009). Cellular and molecular mechanisms of pain. Cell, 139, 267–284. 10.1016/j.cell.2009.09.028 - DOI - PMC - PubMed
    1. Borer, L. R. , Seewald, W. , Peel, J. E. , & King, J. N. (2017). Evaluation of the dose‐response relationship of oral robenacoxib in urate crystal‐induced acute stifle synovitis in dogs. Journal of Veterinary Pharmacology and Therapeutics, 40, 148–157. 10.1111/jvp.12348 - DOI - PubMed

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