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Pharmacokinetics of masitinib in cats
François Bellamy1, Thomas Bader, Alain Moussy
1AB Science, 3 Avenue George V, 75008 Paris, France.
Abstract:
Masitinib is the first veterinary drug recently approved in Europe to treat mast cell tumours in dogs (Hahn et al. JVIM, Masivet). This inhibitor is selective and highly efficient in blocking c-Kit, PDGFR, and Lyn tyrosine kinase activities. It showed good efficacy and acceptable toxicity in several animal studies such as mice, rats, rabbits and dogs (Dubreuil P, et al. submitted, and Hahn et al. (J Vet Intern Med 22(6):8, 2008)). C-kit is a tyrosine kinase receptor that plays a critical role in the biology of mast cells including differentiation, survival, migration and cytokine/mediator release. Mast cells are involved in a number of allergy-and immune-related diseases in cats such as asthma (Reinero Carol et al. Vet Immunol Immunopathol 121(3-4):9, 2008), inflammatory bowel disease, (Janeczko et al. Vet Mic 128(1-2):15, 2008), and feline mast cell tumours (Rassnick et al. J Am Vet Med Assoc 232(8):1200-1205, 2008). Therefore, there might be a strong rationale to use masitinib in these indications. Here, we report the results of a preliminary pharmacokinetic study of masitinib in cats which showed a good bioavailability of ~60% in both sexes. We propose that an oral dose of 10-15 mg/kg masitinib is appropriate to achieve adequate plasma concentrations.
Insights
Masitinib, a tyrosine kinase inhibitor, shows promise for treating feline mast cell-related diseases. A preliminary pharmacokinetic study in cats suggests an oral dose of 10-15 mg/kg is appropriate for effective plasma concentrations.
Area of Science:
- Veterinary Pharmacology
- Oncology
- Immunology
Background:
- Masitinib is an approved veterinary drug for canine mast cell tumors, inhibiting key tyrosine kinases like c-Kit.
- C-Kit receptor tyrosine kinase is crucial for mast cell function and implicated in feline allergic and immune-related diseases.
- Feline mast cell tumors, asthma, and inflammatory bowel disease are conditions where mast cells play a significant role.
Purpose of the Study:
- To evaluate the pharmacokinetic profile of masitinib in cats.
- To determine a suitable oral dosage for masitinib in feline patients.
- To explore the potential therapeutic use of masitinib in feline mast cell-related conditions.
Main Methods:
- A preliminary pharmacokinetic study was conducted in cats.
- Masitinib bioavailability was assessed in both male and female cats.
- Plasma concentrations were measured to determine appropriate dosing.
Main Results:
- Masitinib demonstrated approximately 60% bioavailability in cats.
- An oral dose range of 10-15 mg/kg is proposed for achieving adequate plasma concentrations.
- The study provides initial data on masitinib pharmacokinetics in felines.
Conclusions:
- Masitinib exhibits favorable bioavailability in cats.
- The proposed oral dose of 10-15 mg/kg warrants further investigation for efficacy in feline mast cell-related diseases.
- Masitinib represents a potential therapeutic option for various feline conditions involving mast cell activity.
