Grapiprant
N-[[[2-[4-(2-Ethyl-4,6-dimethyl-1H-imidazo[4,5-c]pyridin-1-yl)phenyl]ethyl]amino]carbonyl]-4-methylbenzenesulfonamide
Also known as: Galliprant · CJ-023423 · RQ-00000007
Reviewed by the VetSheet Veterinary TeamUpdated Apr 5, 2026Evidence-based veterinary reference
Doses are a clinical reference for licensed veterinary professionals. Always confirm against the current label and the individual patient.
Dosing by species
🌎 NA — North America🌍 EU — Europe
Dogs
| Indication | Dose | Route | Frequency | Duration | Region |
|---|---|---|---|---|---|
| Management of mild to moderate pain caused by osteoarthritis | 2 mg/kg | PO | sid | As directed by veterinarian | 🌍 EU |
- Management of mild to moderate pain caused by osteoarthritis: For dogs >9 months of age and >3.6 kg.
Doses are a clinical reference for licensed veterinary professionals. Always confirm against the current label and the individual patient.
Overview
Grapiprant is a non-steroidal, non-cyclooxygenase (COX) inhibiting anti-inflammatory drug belonging to the piprant class. It specifically blocks the EP4 receptor, which is the primary mediator of prostaglandin E2 (PGE2) elicited pain and inflammation.
Clinical Pearl: Because it does not inhibit COX enzymes, grapiprant theoretically spares the production of beneficial prostaglandins involved in gastrointestinal, renal, and platelet homeostasis, potentially offering a safer profile for long-term osteoarthritis management.
Mechanism of action
Grapiprant is a highly selective EP4 receptor antagonist.
Arachidonic acid → COX enzymes → PGE2 → binds to EP4 receptors (mediating pain/inflammation).
By blocking the EP4 receptor, grapiprant inhibits PGE2-mediated vasodilation, vascular permeability, and sensory nerve sensitization without disrupting the synthesis of PGE2 or other prostanoids.
Safety & warnings
Contraindications
- Concurrent use with other NSAIDs or corticosteroids
- Breeding, pregnant, or lactating dogs
- Dogs under 9 months of age or weighing less than 3.6 kg
- Dogs weighing less than 3.6 kg
- Cats (not authorized for use)
- Known hypersensitivity to grapiprant
Adverse effects
- Vomiting
- Diarrhea
- Anorexia
- Lethargy
- Decreased serum albumin
- Soft-formed faeces
- Inappetence
- Mild decreases in serum albumin and total protein
- Haematemesis (very rare)
- Haemorrhagic diarrhoea (very rare)
Precautions
Use with caution in dogs with pre-existing hepatic or renal disease, or those with a history of gastrointestinal disease. Monitor liver enzymes, kidney values, and clinical signs of GI upset.
Clinical Pearl: Although COX-sparing, gastrointestinal adverse effects (vomiting, diarrhea) remain the most commonly reported side effects in clinical practice.
Drug interactions
Increased risk of gastrointestinal toxicity
Increased risk of gastrointestinal ulceration
Potential competition for protein binding sites
Increased risk of gastrointestinal toxicity and adverse effects. Concurrent use should be avoided.
Increased risk of gastrointestinal ulceration and adverse effects. Concurrent use should be avoided.
Monitoring
- Clinical response (pain scoring)
- Fecal consistency
- Appetite
- Baseline and periodic CBC, serum biochemistry (especially albumin, BUN, creatinine, liver enzymes)
- Clinical response to pain management
- Signs of gastrointestinal upset or ulceration (vomiting, diarrhoea, melaena)
- Serum albumin and total protein levels
- Baseline and periodic renal and hepatic panels, especially in older or compromised patients
Pharmacokinetics
Half-life
Absorption
Rapidly absorbed following oral administration. Peak plasma concentration (Tmax) is reached within 1-2 hours.
Distribution
Highly protein bound (>95%).
Metabolism
Hepatic metabolism.
Elimination
Excreted primarily in feces (via bile) and to a lesser extent in urine.
Overdose
Overdoses up to 15x the recommended dose for 9 months resulted in mild, transient GI signs (vomiting, soft feces) and mild decreases in total protein and albumin. No specific antidote exists; treat symptomatically with GI protectants and supportive care.
Available products
Formulations
- Oral tablets (20 mg, 60 mg, 100 mg)
- 20 mg oral tablet
- 60 mg oral tablet
- 100 mg oral tablet
Veterinary
- Galliprant 20 mg tablets
- Galliprant 60 mg tablets
- Galliprant 100 mg tablets
Regulatory status
Approved for control of pain and inflammation associated with osteoarthritis in dogs.
POM-V
POM-V
No regulatory data for: 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR
Storage & stability
Store at room temperature (below 30°C/86°F). Keep out of reach of children and animals.
Client information
Give this medication exactly as prescribed by your veterinarian. It can be given with or without food.
Watch for side effects such as vomiting, diarrhea, or loss of appetite. If these occur, stop the medication and contact your vet.
Do not give your dog any other pain medications (like aspirin, ibuprofen, or other veterinary NSAIDs) while they are taking grapiprant.
VetSheet drug reference is intended for licensed veterinary professionals as a clinical decision-support aid, not a substitute for professional judgement or the manufacturer’s current label.