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Grapiprant information


Grapiprant
Clinical data
Trade namesGalliprant
Routes of
administration
By mouth
ATCvet code
  • QM01AX92 (WHO)
Legal status
Legal status
  • CA: ℞-only[1]
  • US: ℞-only[2]
Pharmacokinetic data
Bioavailability6.6 L/kg, high volume of distribution
Elimination half-life5.86 hours in horses
ExcretionKidney
Identifiers
IUPAC name
  • 3-[2-(4-{2-Ethyl-4,6-dimethyl-1H-imidazo[4,5-c]pyridin-1-yl}phenyl)ethyl]-1-(4-methylbenzenesulfonyl)urea
CAS Number
  • 415903-37-6
PubChem CID
  • 11677589
DrugBank
  • DB12836 checkY
ChemSpider
  • 9852318
UNII
  • J9F5ZPH7NB
CompTox Dashboard (EPA)
  • DTXSID60194419 Edit this at Wikidata
Chemical and physical data
FormulaC26H29N5O3S
Molar mass491.61 g·mol−1
3D model (JSmol)
  • Interactive image
SMILES
  • CCC1=NC2=C(C)N=C(C)C=C2N1C1=CC=C(CCNC(=O)NS(=O)(=O)C2=CC=C(C)C=C2)C=C1
InChI
  • InChI=1S/C19H22N2OS/c1-14(22)15-9-10-19-17(13-15)21(12-6-11-20(2)3)16-7-4-5-8-18(16)23-19/h4-5,7-10,13H,6,11-12H2,1-3H3
  • Key:HZVLFTCYCLXTGV-UHFFFAOYSA-N

Grapiprant, sold under the brand name Galliprant, is a small molecule drug that belongs in the piprant class. This analgesic and anti-inflammatory drug is primarily used as a pain relief for mild to moderate inflammation related to osteoarthritis in dogs. Grapiprant has been approved by the FDA's Center for Veterinary Medicine and was categorized as a non-cyclooxygenase inhibiting non-steroidal anti-inflammatory drug (NSAID) in March 2016.[3]

Preclinical studies also indicate that grapiprant is not only efficacious as a reliever of acute pain but also in chronic pain relief and inflammation. The effect of the drug is directly proportional to the dosage and its effects are comparable to human medications such as rofecoxib and piroxicam.[4]

Grapiprant has also been tested in humans,[5] and was researched to be used as pain control for inflammation associated with osteoarthritis.

Grapiprant is widely accepted in veterinary medicine due to its specific and targeted approach to pain management in dogs. The serum concentration of grapiprant is increased when used in conjunction with other drugs such as acetaminophen, albendazole, and alitretinoin.[citation needed]

Common side effects are intestinal related effects such as mild diarrhea, appetite loss, and vomiting.[6] It is theorised that it might lead to reduced tear production due to it being a sulfa-based medication,[citation needed] as well as decreased albumin levels.[7]

  1. ^ "Approved in 2020: Drugs for human use". Health Canada. 26 July 2021. Retrieved 27 March 2024.
  2. ^ "Galliprant- grapiprant tablet". DailyMed. 28 November 2023. Retrieved 28 March 2024.
  3. ^ "Grapiprant". DrugBank. Retrieved 15 May 2019.
  4. ^ "Grapiprant". PubChem. U.S. National Library of Medicine.
  5. ^ Nagahisa A, Okumura T (June 2017). "Pharmacology of grapiprant, a novel EP4 antagonist: receptor binding, efficacy in a rodent postoperative pain model, and a dose estimation for controlling pain in dogs". Journal of Veterinary Pharmacology and Therapeutics. 40 (3): 285–292. doi:10.1111/jvp.12349. PMID 27597397.
  6. ^ "Galliprant". Center for Veterinary Medicine. U.S. Food and Drug Administration. 20 December 2019.
  7. ^ "Galliprant®". dailymed.nlm.nih.gov. Retrieved 1 February 2021.

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Resveratrol

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Phenacetin

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Diclofenac

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Ketorolac

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Naproxen

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Cyclooxygenase

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