Grapiprant: A snapshot of the current knowledge

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.

Pharmacokinetics of grapiprant and effects on TNF‐alpha concentrations following oral administration to horses

“…Grapiprant (Galliprant®), is a novel ‘non‐traditional NSAID’, approved for the use in dogs (Sartini & Giorgi, 2021). In contrast to traditional NSAIDs that inhibit production of eicosanoids through COX inhibition, grapiprant blocks the binding of these mediators to receptors, specifically binding of Prostaglandin E 2 (PGE 2 ) to the EP 4 receptor (Sartini & Giorgi, 2021).…”

“…Grapiprant (Galliprant®), is a novel ‘non‐traditional NSAID’, approved for the use in dogs (Sartini & Giorgi, 2021). In contrast to traditional NSAIDs that inhibit production of eicosanoids through COX inhibition, grapiprant blocks the binding of these mediators to receptors, specifically binding of Prostaglandin E 2 (PGE 2 ) to the EP 4 receptor (Sartini & Giorgi, 2021). In addition to playing a role in certain homeostatic processes, PGE 2 can also elicit inflammation, sensitize sensory neurons and increase vasodilation and vascular permeability (Boyd et al, 2011; Chen et al, 2010; Lin et al, 2006; Nagahisa & Okumura, 2017; Nakao et al, 2007).…”

“…While there are several effective NSAIDs approved by the Food and Drug Administration for use in horses, many are associated with unwanted side effects such as gastric ulceration, inhibition of intestinal healing following ischemic injury, right dorsal colitis, renal toxicity and inhibition of bone and wound healing (Knych, 2017). These untoward effects are often attributed to inhibition of cyclooxygenase enzymes (COX), namely COX-1.Grapiprant (Galliprant®), is a novel 'non-traditional NSAID', approved for the use in dogs (Sartini & Giorgi, 2021). In contrast to traditional NSAIDs that inhibit production of eicosanoids through COX inhibition, grapiprant blocks the binding of these mediators to receptors, specifically binding of Prostaglandin E 2 (PGE 2 ) to the EP 4 receptor (Sartini & Giorgi, 2021).…”

“…These untoward effects are often attributed to inhibition of cyclooxygenase enzymes (COX), namely COX-1.Grapiprant (Galliprant®), is a novel 'non-traditional NSAID', approved for the use in dogs (Sartini & Giorgi, 2021). In contrast to traditional NSAIDs that inhibit production of eicosanoids through COX inhibition, grapiprant blocks the binding of these mediators to receptors, specifically binding of Prostaglandin E 2 (PGE 2 ) to the EP 4 receptor (Sartini & Giorgi, 2021). In addition to playing a role in certain homeostatic processes, PGE 2 can also elicit inflammation,…”

“…sensitize sensory neurons and increase vasodilation and vascular permeability (Boyd et al, 2011;Chen et al, 2010;Lin et al, 2006;Nagahisa & Okumura, 2017;Nakao et al, 2007). The EP 4 receptor serves as the primary mediator of the PGE 2 mediated proinflammatory pathway responsible for these effects (Sartini & Giorgi, 2021).…”