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
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)
DescriptionSources: https://dailymed.nlm.nih.gov/dailymed/fda/fdaDrugXsl.cfm?setid=5d2b37c6-0744-492b-8004-1364676cf29bCurator's Comment: description was created based on several sources, including
http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Summary_for_the_public/veterinary/000127/WC500067754.pdf | https://www.ncbi.nlm.nih.gov/pubmed/28408514 | https://www.ncbi.nlm.nih.gov/pubmed/28283079
Sources: https://dailymed.nlm.nih.gov/dailymed/fda/fdaDrugXsl.cfm?setid=5d2b37c6-0744-492b-8004-1364676cf29b
Curator's Comment: description was created based on several sources, including
http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Summary_for_the_public/veterinary/000127/WC500067754.pdf | https://www.ncbi.nlm.nih.gov/pubmed/28408514 | https://www.ncbi.nlm.nih.gov/pubmed/28283079
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
Sources: https://www.google.com/patents/WO1999011605A8
Curator's Comment: # Novartis Ag, Novartis Erfind Verwalt Gmbh
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL4033 Sources: https://www.ncbi.nlm.nih.gov/pubmed/20004922 |
0.0429 µM [IC50] | ||
Target ID: CHEMBL4133 Sources: https://www.ncbi.nlm.nih.gov/pubmed/20004922 |
7.888 µM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Onsior Approved UseIndication: ONSIOR tablets are indicated for the control of postoperative pain and
inflammation associated with orthopedic surgery, ovariohysterectomy and
castration, in cats ≥ 5.5 lbs (2.5 kg) and ≥ 4 months of age; for up to a
maximum of 3 days. |
Sample Use Guides
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
Sources: https://www.ncbi.nlm.nih.gov/pubmed/28283079
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).
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WHO-VATC |
QM01AH91
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EMA VETERINARY ASSESSMENT REPORTS |
ONSIOR [AUTHORIZED]
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EMA VETERINARY ASSESSMENT REPORTS |
ONSIOR [AUTHORIZED]
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NCI_THESAURUS |
C257
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CFR |
21 CFR 520.2075
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C80565
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Z588009C7C
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76269
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220991-32-2
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CHEMBL2107774
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ROBENACOXIB
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C551524
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DTXSID90176607
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Z588009C7C
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1250203
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300000023733
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ACTIVE MOIETY