Small molecule
PubChem CID 2662
Celecoxib
Celebrex
- Mechanism of action
- COX-2 selective inhibitor
- In plain language
- Eases pain and inflammation by mainly blocking one enzyme, COX-2, while leaving the other closely related enzyme, COX-1, largely alone — so unlike ibuprofen, naproxen, or aspirin, it doesn't thin the blood, though it still carries the same FDA warning about heart and stomach risks.
- How it works
- Celecoxib is a COX-2 selective NSAID. Unlike nonselective NSAIDs such as ibuprofen and naproxen, which inhibit both cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2), celecoxib's bulkier diaryl-pyrazole structure fits a side pocket present in the COX-2 active site but sterically excluded from COX-1, giving it much greater selectivity for COX-2 at therapeutic doses. Because it largely spares COX-1 in platelets, celecoxib does not reduce platelet aggregation or prolong bleeding time the way nonselective NSAIDs can, and per its FDA label it is not a substitute for aspirin in cardiovascular prophylaxis. Celecoxib still carries the same FDA boxed warning for cardiovascular thrombotic events and serious gastrointestinal bleeding, ulceration, and perforation that applies to NSAIDs generally; clinical trial data show it is non-inferior to nonselective NSAIDs on cardiovascular thrombotic risk and not statistically different on clinically relevant GI outcomes, despite a lower rate of endoscopic ulcers in one trial.
- Therapeutic applications
- Per FDA-approved labeling, CELEBREX is indicated for the management of the signs and symptoms of osteoarthritis, rheumatoid arthritis, and juvenile rheumatoid arthritis in patients 2 years and older; for ankylosing spondylitis; for acute pain in adults; and for primary dysmenorrhea.
- Class
- Small molecule
- Therapeutic area
- Analgesic / Anti-inflammatory
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