Chemical Property of Rofecoxib
Chemical Property:
- Appearance/Colour:off-white (pale yellow) crystalline powder
- Vapor Pressure:2.42E-13mmHg at 25°C
- Melting Point:207 °C
- Refractive Index:1.619
- Boiling Point:577.6 °C at 760 mmHg
- Flash Point:303.1 °C
- PSA：68.82000
- Density:1.333 g/cm3
- LogP:3.63850
- Storage Temp.:Refrigerator
- Solubility.:DMSO: soluble5mg/mL, clear (warmed)
- Water Solubility.:9mg/L(25 oC)
- XLogP3:2.3
- Hydrogen Bond Donor Count:0
- Hydrogen Bond Acceptor Count:4
- Rotatable Bond Count:3
- Exact Mass:314.06128010
- Heavy Atom Count:22
- Complexity:556
- Purity/Quality:
-
98% *data from raw suppliers
Vioxx *data from reagent suppliers
Safty Information:
- Pictogram(s):
Xn
- Hazard Codes:Xn
- Statements:
22
- MSDS Files:
-
SDS file from LookChem
Useful:
- Drug Classes:Nonsteroidal Antiinflammatory Drugs
- Canonical SMILES:CS(=O)(=O)C1=CC=C(C=C1)C2=C(C(=O)OC2)C3=CC=CC=C3
- Recent ClinicalTrials:Study of Rofecoxib and Prolonged Constant Infusion of Gemcitabine in the Polychemotherapy Treatment of Advanced NSCLC
- Recent EU Clinical Trials:A Randomized, Double-Blind, Placebo-Controlled, Parallel Group, Phase III Study with a Long-Term, Open-label Extension to Evaluate the Efficacy and Safety of TRM-201 (Rofecoxib) in Patients with Hemophilic Arthropathy
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Description
Rofecoxib ts a non-steroidal anti-inflammatory drug (NSAID) launched
in Mexico, its first market, for the management of acute pain and the treatment
of osteoarthritis (OA) and primary dysmenorrhea. Rofecoxib can be obtained by
several different ways; one example is by arylation of a 4-bromofuranone with a
phenylboronic acid under Suzuki conditions. Rofecoxib is a highly selective
inhibitor of COX-2, the inducible isoform of cyclooxygenase and therefore
exhibits a potent antiinflammatory activity without concomitant gastric or renal
toxicities linked to the non-specific COX-1/2 inhibitors. In several clinical studies
in patients with knee or hip osteoarthritis, Rofecoxib was evaluated at 12.5-50
mg doses once daily: it demonstrated efficacy for all primary and secondary endpoints at doses considerably weaker than those for classical non-specific
NSAIDs, with good tolerance and less adverse effects. Selective COX-2
inhibitors potentially have a large spectrum of activity including new indications
such as Alzheimer's disease, colorectal cancer, irritable bowel disease or
urinary incontinence.
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Uses
A selective cyclooxygenase-2 (COX-2) inhibitor. Use as an anti-inflammatory, analgesic. antipsychotic Labeled Rizatriptan, intended for use as an internal standard for the quantification of Rizatriptan by GC- or LC-mass spectrometry. Rofecoxib has been used in high performance bioaffinity chromatography.
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Indications
Rofecoxib is approved for the treatment of osteoarthritis,
dysmenorrhea, and acute pain. The most
common adverse reactions to rofecoxib are mild to
moderate GI irritation (diarrhea, nausea, vomiting, dyspepsia,
abdominal pain). Lower extremity edema and
hypertension occur relatively frequently (about 3.5%).
It is not metabolized by CYP2C9, so rofecoxib should
not be subject to some of the interactions seen with
celecoxib. However, its metabolism is increased by the
coadministration of rifampin, which acts as a nonspecific
inducer of hepatic metabolism.
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Clinical Use
Rofecoxib was indicated for the relief of the signs and symptoms of osteoarthritis, for the management of acute pain
in adults, and for the treatment of primary
dysmenorrhea.
