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KI0127Firocoxib1 mg$324

Chemical Characteristic

Product NameFirocoxib
SynonymsEquioxx, Previcox, ML-1785713
CAS No.189954-96-9
Molecular Weight 336.4
FormulaC17H20O5S
Chemical Name3-(Cyclopropylmethoxy)-5,5-dimethyl-4-[4-(methylsulfonyl)phenyl]-2(5H)-furanone
SmilesO1C(=O)C(=C(C1(C)C)c1ccc(cc1)S(=O)(=O)C)OCC1CC1
Chemical Structure

Biological activities

Firocoxib is a non-steroidal anti-inflammatory drug of the cyclooxygenase(COX)-2 inhibitor. In vitro canine whole blood assays, 50% inhibition of firocoxib for COX-1 and COX-2 activity are 119.1 and 0.31 mM, respectively, and selectivity ratio for inhibiting COX-2 relative to COX-1 is 384. In female mixed-breed dogs, firocoxib has high oral bioavailability, low systemic clearance (77 mL/min/kg), and an elimination half-life of 5.9 hours. Furthermore, firocoxib is efficacious when administered prophylactically and therapeutically to dogs with urate crystal-induced synovitis.[1] In vitro feline whole blood assays, 50% inhibition of ?rocoxib for COX-1 and COX-2 activity are 75 and 0.13 mM, respectively, and selectivity ratio for inhibiting COX-2 relative to COX-1 is 58. In male cats, firocoxib (i.v. 2 mg/kg and oral 3 mg/kg administration) has moderate to high oral bioavailability (54% to 70%), low plasma clearance (4.7 to 5.8 mL/min/kg), and an elimination half-life of 8.7 to 12.2 hours. Furthermore, firocoxib at doses from 0.75 to 3 mg/kg is efficacious in attenuating fever when administered to cats 1 or 14 hours before lipopolysaccharide (LPS) challenge.[2] In horses administered either a single oral or intravenous dose of ?rocoxib at 0.1 mg/kg, oral firocoxib is well absorbed with an average bioavailability (absolute) of 79% and a Cmax of 75 ng/mL at 3.9 hour. The average elimination half-life is 30 hour. Following intravenous administration the average Cmax is 210 ng/mL and the elimination half-life is 34 hours. Besides, urinary excretion is the major route of elimination, and the clearance rate was 37 mL/h/kg.[3] In a sodium urate crystal induced synovitis model of arthritis in dogs, peak vertical force as a percentage of baseline is 72.0%, 79.0% and 52.7% for firocoxib, vedaprofen and carprofen, respectively, at 3 hours. However, At 7 hours, firocoxib with a peak vertical force of 99.3% of baseline differs significantly from carprofen (peak vertical force of 84.6%) and placebo (peak vertical force of 69.6%), but is not statistically different from vedaprofen (peak vertical force of 90.9%).[4]

Protocols

Firocoxib is eluted with 2 mL of acetonitrile. [3]

References

[1] McCann ME, et al. In vitro effects and in vivo efficacy of a novel cyclooxygenase-2 inhibitor in dogs with experimentally induced synovitis. Am J Vet Res. 2004, 65(4): 503-512.
[2] McCann ME, et al. In vitro effects and in vivo efficacy of a novel cyclooxygenase-2 inhibitor in cats with lipopolysaccharide-induced pyrexia. Am J Vet Res. 2005, 66(7): 1278-1284.
[3] Kvaternick V, et al. Pharmacokinetics and metabolism of orally administered firocoxib, a novel second generation coxib, in horses. J Vet Pharmacol Ther. 2007, 30(3): 208-217.
[4] Hazewinkel HA, et al. Comparison of the effects of firocoxib, carprofen and vedaprofen in a sodium urate crystal induced synovitis model of arthritis in dogs. Res Vet Sci. 2008, 84(1): 74-79.

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