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Jun 24, 2002
 |  BioCentury  |  Tools & Techniques

The COX-2 difficulties

The molecular rationale for cyclo-oxygenase 2 inhibitors is simple: avoid gastrointestinal complications associated with traditional non-steroidal anti-inflammatory drugs by focusing on the specific COX-2 enzyme primarily found in inflamed tissues, not on the COX-1 enzymes found in a variety of tissues including those in the stomach.

But this rationale has yet to pan out fully in the real world. In part, the theory hasn't been fully tested, because some of the clinical trials had flaws - such as allowing concomitant use of aspirin, which can cause GI effects.

At the same time, inhibition of COX-2 might cause its own problems, as cardiovascular side effects have been seen in some patients. While this may be because the enzyme also is found in cardiovascular endothelial cells, it's not yet known if COX-2 itself is the cause of the side effects.

Recent attempts to improve the labels regarding adverse GI events for Celebrex celecoxib from Pfizer Inc. and Pharmacia Corp. and Vioxx rofecoxib from Merck & Co. Inc. have fallen short of their goals.

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