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Details

Stereochemistry ACHIRAL
Molecular Formula C16H13F4NO2
Molecular Weight 327.2735
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of ROBENACOXIB

SMILES

CCC1=CC(CC(O)=O)=C(NC2=C(F)C(F)=CC(F)=C2F)C=C1

InChI

InChIKey=ZEXGDYFACFXQPF-UHFFFAOYSA-N
InChI=1S/C16H13F4NO2/c1-2-8-3-4-12(9(5-8)6-13(22)23)21-16-14(19)10(17)7-11(18)15(16)20/h3-5,7,21H,2,6H2,1H3,(H,22,23)

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Description

Robenacoxib (trade name Onsior) is a non-steroidal anti-inflammatory drug (NSAID) used in veterinary medicine for the relief of pain and inflammation in cats and dogs. In an inflammation model in cats, Robenacoxib had analgesic, anti-inflammatory and antipyretic actions with a rapid onset of action (0.5 h). In an in vitro whole blood assay in cats, Robenacoxib demonstrated selective COX-2 inhibition. After oral administration of robenacoxib tablets at 1 mg/kg without food, peak blood concentrations are attained rapidly with a median Tmax of 0.5 h, a mean Cmax of 1159 ng/ml and a mean AUC of 1337 ng*h/ml. Robenacoxib persists longer in the inflammatory exudate of a tissue cage model than in blood. The median Robenacoxib elimination half-life in exudate was about 27 hours versus 2.5 hours for blood. Robenacoxib is extensively metabolized by the liver in cats. The systemic exposure of lactam metabolite is about 25% of Robenacoxib exposure following oral administration to fed cats. Further, the systemic exposure to lactam appears to be two-fold greater in fed cats than fasted cats. Apart from one lactam metabolite, the identity of other metabolites is not known in cats.

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency
0.0429 µM [IC50]
7.888 µM [IC50]

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Onsior

PubMed

Sample Use Guides

In Vivo Use Guide
The dose of ONSIOR tablets is 0.45 mg/lb (1 mg/kg) orally once daily, for a maximum of three days. Body weight 5.5 to 13.2 lbs (2.5 to 6 kg) -- 1 whole tablet (6 mg robenacoxib) once daily Body weight 13.3 to 26.4 lbs (6.1 to 12 kg) 2 whole tablets (6+6 mg robenacoxib) once daily
Route of Administration: Oral
In Vitro Use Guide
26 canine tumour cell lines (CIPp, CIPm, CTBp, KMeCa, LMeCa, Mia, Pua, C1a, C2a, CMM7b, CMM8b, CMM9b, CMM10b, CMM11b, CMM12b, HOSa, OOSa, POSa, TCCUBa, Soraa, Lovea, 12041a, Peacea, 13008b, 13020b, Gena) were used for activity evaluation. Cells were treated with NSAIDs at final concentrations of 0, 4.1, 12, 37, 111, 333, and 1000 μM for 48 h. After incubation, cell viability was measured using a colourimetric cell counting assay kit (Cell Counting Kit-8, Dojindo Laboratories).