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QuickView for Rofecoxib (compound)

Name: rofecoxib
PubChem Compound ID: 11681277
Molecular formula: C17H14O4S
Molecular weight: 319.387 g/mol
Name: rofecoxib
Name (isomeric): DB00533
Drug Type: small molecule
MK 996; MK 966
Brand: Vioxx
Category: Cyclooxygenase Inhibitors, Cyclooxygenase 2 Inhibitors
CAS number: 162011-90-7
Indication: For the treatment of osteoarthritis, rheumatoid arthritis, acute pain in adults, and primary dysmenorrhea, as well as acute treatment of migraine attacks with or without auras.
Rofecoxib, a selective cyclooxygenase-2 (COX-2) inhibitor, is classified as a nonsteroidal anti-inflammatory drug (NSAID). Unlike celecoxib, rofecoxib lacks a sulfonamide chain and does not require CYP450 enzymes for metabolism. Like other NSAIDs, rofecoxib exhibits anti-inflammatory, analgesic, and antipyretic activity. NSAIDs appear to inhibit pr...
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Mechanism of Action:
The anti-inflammatory, analgesic, and antipyretic effects of NSAIDs appear to result from the inhibition of prostaglandin synthesis. Although the exact mechanism of action has not been determined, these effects appear to be mediated through the inhibition of the COX-2 isoenzyme at the sites of inflammation with subsequent reduction in the synthesis...
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Absorption: The mean oral bioavailability of rofecoxib at therapeutically recommended doses of 12.5, 25, and 50 mg is approximately 93%.
Protein binding: 87%
Biotransformation: Hepatic. Metabolism of rofecoxib is primarily mediated through reduction by cytosolic enzymes. The principal metabolic products are the cis-dihydro and trans-dihydro derivatives of rofecoxib, which account for nearly 56% of recovered radioactivity in the urine. An additional 8.8% of the dose was recovered as the glucuronide of the hydroxy derivative, a product of oxidative metabolism. The biotransformation of rofecoxib and this metabolite is reversible in humans to a limited extent (< 5%). These metabolites are inactive as COX-1 or COX-2 inhibitors. Cytochrome P450 plays a minor role in metabolism of rofecoxib.
Half Life: 17 hours
Toxicity: No overdoses of rofecoxib were reported during clinical trials. Administration of single doses of rofecoxib 1000 mg to 6 healthy volunteers and multiple doses of 250 mg/day for 14 days to 75 healthy volunteers did not result in serious toxicity.
Affected organisms: Humans and other mammals
Drug interaction:
AminophyllineRofecoxib increases the effect and toxicity of theophylline
MethotrexateRofecoxib increases the levels of methotrexate
TheophyllineRofecoxib increases the effect and toxicity of theophylline
OxtriphyllineRofecoxib increases the effect and toxicity of theophylline
LithiumThe COX-2 inhibitor increases serum levels of lithium