Selected nonsteroidal antiinflammatory drugs (NSAIDs) and other analgesics: Selectivity for cyclooxygenase-2 and potency in inhibiting gastric COX activity

	COX-2 selectivity*	Gastric IC50 (µM)¶
NSAIDs
Ketoprofen	0.1	0.08
Ibuprofen	0.6	0.70
Indomethacin	0.7	0.85
Naproxen	1.0	0.52
Piroxicam	1.3	0.87
Ketoralac	1.5	0.33
Nabumetone	1.6	0.48
Etodolac	7.9	3.20
Celecoxib	9.2	11.14
Mefenamic acid	12.1	0.70
Nimesulide (not available in US)	58.3	1.49
Other analgesics
Aspirin (acetylsalicylic acid)	0.3	0.03
Salsalate (salicylsalicylic acid)	≥2.8	>100
Acetaminophen	4.0	>100

* In whole blood assays in man. A number ≅1 indicates COX non-selectivity while numbers much >1 indicate COX-2 selectivity. Values for nabumetone are for its active metabolite, 6-MNA.
¶ Concentration of drug that inhibits human gastric mucosal COX activity by 50 percent and thus gastric mucosal PG production by 50 percent. The lower the IC50, the more potent the inhibition of gastric COX activity for a given drug.

Adapted from: Cryer B, Feldman M. Cyclooxygenase-1 and cyclooxygenase-2 selectivity of widely used nonsteroidal anti-inflammatory drugs. Am J Med 1998; 104:413.

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Selected nonsteroidal antiinflammatory drugs (NSAIDs) and other analgesics: Selectivity for cyclooxygenase-2 and potency in inhibiting gastric COX activity