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Clinical experience with cyclooxygenase-2 inhibitors
1Department of Pulmonary Research, Boehringer Ingelheim Pharma KG, Biberach an der Riss, Germany. joanne.vanryn@bc.boehringer-ingelheim.com
Summary
Selective cyclooxygenase-2 (COX-2) inhibition offers anti-inflammatory benefits, while COX-1 inhibition increases side effects. This review covers COX-2 regulation, assays for new selective inhibitors, and clinical data for drugs like celecoxib.
Area of Science:
- Biochemistry
- Pharmacology
- Immunology
Background:
- Cyclooxygenase-2 (COX-2) inhibition is key in anti-inflammatory processes.
- Cyclooxygenase-1 (COX-1) inhibition is linked to increased side effect frequency.
- Existing nonsteroidal anti-inflammatory drug (NSAID) classifications do not fully address the COX-2 concept.
Purpose of the Study:
- To review the regulation of COX-2 in inflammatory processes.
- To summarize in vitro assays for classifying new selective COX-2 inhibitors.
- To discuss clinical data for novel selective and highly selective COX-2 inhibitors.
Main Methods:
- Review of in vitro and in vivo experimental data on COX-2 regulation.
- Analysis of various in vitro assays for inhibitor classification.
- Compilation and discussion of published clinical trial data.
Main Results:
- Experimental data support the role of selective COX-2 inhibition in anti-inflammation.
- Newer selective and highly selective COX-2 inhibitors require distinct classification methods.
- Clinical data for meloxicam, nimesulide, etodolac, celecoxib, and MK966 are presented.
Conclusions:
- Selective COX-2 inhibition is a promising therapeutic strategy for inflammation.
- Development of specific assays is crucial for characterizing novel COX-2 inhibitors.
- Emerging selective COX-2 inhibitors show potential with discussed clinical outcomes.