Grapiprant

China [CN]

Grapiprant Core Information

Generic Name: Grapiprant  Chinese Name: 格拉匹仑 (Grapiprant) CAS Number: 415903-37-6 Molecular Formula: C₂₆H₂₉N₅O₃S Molecular Weight: 491.61 g/mol Synonyms: CJ-023423, AT-001, AAT-007, RQ-00000007

Drug Type and Mechanism of Action

Drug Type: Selective EP4 prostaglandin receptor antagonist (PRA), non-COX inhibiting NSAID

Mechanism of Action:

Highly selective blockade of the PGE₂-EP4 signaling pathway (does not inhibit COX-1/COX-2)

Competitively binds to EP4 receptors, inhibiting downstream cAMP/PKA inflammation and pain sensitization pathways

Reduces joint inflammation, pain, and bone destruction, while preserving the physiological functions of other prostaglandins

Core Clinical Applications (2026)

Approved Indications:

Dogs: Control of pain and inflammation associated with osteoarthritis (OA) (Trade name: Galliprant®)

Humans: Clinical research phase (osteoarthritis, rheumatoid arthritis, pain management)

Dosage for Dogs: 2 mg/kg, once daily, orally on an empty stomach

Dosage Form: Chewable tablets (20 mg, 60 mg, 100 mg)

Physicochemical Properties (API)

Appearance: White to off-white crystalline powder

Solubility: Soluble in DMSO, methanol; poorly soluble in water

Stability: Powder stable for 3 years at -20℃; solution stable for 1 year at -80℃

Chirality: Contains a chiral center, single configuration

Foreign Trade / Supply Chain Highlights

Product Type: Active Pharmaceutical Ingredient (API), Intermediate, Reference Standard

Quality Standards: In-house standards, EP/USP (R&D stage)

Packaging: 1 kg/bag, 25 kg/drum (moisture-proof, light-proof)

HS Code: 2934999090

Compliance: FDA/EMA approved for veterinary use; human use in clinical phase II/III, patent protected