Grapiprant

Products

Grapiprant is commercially available in some countries as a veterinary medicine in tablet form for dogs (Galliprant).

Structure and properties

Grapiprant (C26H29N5O3S, Mr = 491.6 g/mol)

Effects

Grapiprant (ATCvet QM01AX92) has analgesic and anti-inflammatory properties. The effects are due to selective antagonism at the EP4 receptor and displacement of the natural ligand prostaglandin E2 (PGE2). The EP4 receptor is mainly responsible for triggering pain and inflammation. Grapiprant can also be classified as an NSAID (non-steroidal anti-inflammatory drug), but it does not inhibit the cyclooxygenases COX-1 and COX-2, unlike the classical agents. Because it does not abrogate the physiologic effects of PGE2 and other prostanoids, it tends to cause fewer side effects than the COX inhibitors and should be better tolerated. Grapiprant also binds to the human EP4 receptor, but no drugs are yet available for humans.

Indications

For the treatment of pain and inflammation associated with osteoarthritis in dogs.

Dosage

According to the product information leaflet. The tablets are administered once daily.

Contraindications

Grapiprant is contraindicated in case of hypersensitivity. Full precautions can be found in the drug label.

Adverse Effects

The most common possible adverse effects include vomiting, soft stools, diarrhea, and poor appetite.