Pharmacokinetics of grapiprant, a selective EP4 prostaglandin PGE2 receptor antagonist, after 2 mg/kg oral and i.v. administrations in cats

• Published in: Journal of veterinary pharmacology and therapeutics 2017-12, Vol.40 (6), p.e11-e15
• Main Authors: Lebkowska‐Wieruszewska, B., De Vito, V., Owen, H., Poapholatep, A., Giorgi, M.
• Format: Article
• Language: English
• Subjects: bioavailability; cats; EP4 receptor antagonist; grapiprant; pharmacokinetics
• ISSN: 0140-7783; 1365-2885
• DOI: 10.1111/jvp.12414

Drugs that provide effective analgesia in cats are limited. The aim of the study was to assess the pharmacokinetics of grapiprant after 2 mg/kg administration via p.o. and i.v. routes in cats. Six healthy adult cats were used according to an open, single‐dose, two‐treatment, two‐period, randomized cross‐over design. Cats were assigned to two treatment groups and administered with 2 mg/kg of grapiprant (pure powder) through p.o. and i.v. administration. Blood samples were collected at preassigned times and analysed by a validated HPLC method. After both administrations, grapiprant concentrations were detectable in plasma for up to 24 hr in five of six animals. The critical parameters including clearance (173.2 ml hr−1 kg−1, range 120–326 ml hr−1 kg−1) and volume of distribution (918 ml/kg, range 611–1608 ml/kg) were calculated from the i.v. group. The mean oral F% was low (39.6% range 31.5%–45.2%). If the assumption that the minimal effective concentration in dogs (164 ng/ml) applies in cats too, grapiprant orally administered at 2 mg/kg might be effective for 10 hr. Further studies are necessary to establish the minimal effective concentration in this animal species.