Grapiprant (Synonyms: CJ-023423; RQ-00000007; AAT-007)


Grapiprant is a selective EP4 receptor antagonist whose physiological ligand is prostaglandin E2 (PGE2). Target: prostaglandin receptor in vitro: Grapiprant is a novel pharmacologically active ingredient, acts as a selective EP4 receptor antagonist whose physiological ligand is prostaglandin E2 (PGE2). [1] in vivo: Grapiprant is currently under development for use in humans and dogs for the control of pain and inflammation associated with osteoarthritis. [1] Results suggested the safety of long-term oral administration of grapiprant to dogs. Efficacy of grapiprant in the treatment of dogs with osteoarthritis needs to be evaluated in other studies. [2]

CJ-023,423 is also effective in models of acute and chronic inflammatory pain. CJ-023,423 significantly reduces mechanical hyperalgesia in the carrageenan model. Furthermore, CJ-023,423 significantly reverses complete Freund's adjuvant-induced chronic inflammatory pain response. Taken together, the present data indicate that CJ-023,423, a highly potent and selective antagonist of both human and rat EP(4) receptors, produces antihyperalgesic effects in animal models of inflammatory pain. Thus, specific blockade of the EP(4) receptor signaling may represent a novel therapeutic approach for the treatment of inflammatory pain.