Drug intelligence / Profile preview

grapiprant

Development stage
Phase 2
Lead developer
Aratana Therapeutics
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Grapiprant is a small molecule drug in the piprant class, primarily used as an analgesic and anti-inflammatory agent for the control of pain and inflammation associated with osteoarthritis in dogs. Unlike traditional NSAIDs, grapiprant does not inhibit cyclooxygenase enzymes but instead acts as a highly selective antagonist of the prostaglandin E2 (PGE2) EP4 receptor. The EP4 receptor is a key mediator of PGE2-driven pain and inflammation, particularly through sensitization of sensory neurons and promotion of inflammatory processes. By selectively blocking this receptor, grapiprant provides targeted relief from arthritic pain while minimizing interference with other prostaglandin pathways that are important for normal physiological functions such as gastrointestinal protection and renal function. Grapiprant was developed specifically for veterinary use but has also been researched in humans for osteoarthritis-related pain[1][2][5][6].

Brand names
Galliprant
Other names
N-((4-(2-ethyl-4,6-dimethyl-1H-imidazo[4,5-c]pyridin-1-yl)phenethyl)carbamoyl)-4-methylbenzenesulfonamide
02

Targets

PTGER4 (Prostaglandin E2 receptor EP4 subtype)

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