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Update on COX-2 inhibitor patents with a focus on optimised formulation and therapeutic scope of drug combinations making use of COX-2 inhibitors

: Puhlmann, U.; Schäfer, D.; Ziemann, C.


Expert Opinion on Therapeutic Patents 16 (2006), Nr. 4, S.403-430
ISSN: 0962-2594
ISSN: 1354-3776
Fraunhofer ITEM ()
COX-2; drug combination; rheumatic disease; Cancer; Inflammation; Pain

Selective cyclooxygenase-2 (COX-2) inhibitors, like coxibs, demonstrate efficacy in the treatment of pain and inflammation, comparable to unselective non-steroidal anti-inflammatory drugs (NSAIDs). COX-2 expression was, for a long time, linked only to pathophysiology, but ongoing research has also demonstrated constitutive COX-2 expression within normal tissues such as brain, kidney, pancreas, intestine and blood vessels. Irrespective of their tendency to reduce severe gastrointestinal (GI) events, strong debates have been ignited regarding new adverse effects of specific COX-2 inhibitors, most notably those of a cardiovascular (CV) nature, such as blood pressure elevation, myocardial infarction and stroke. This review evaluates the recent patent literature concerning new therapeutic options offered by selective COX-2 inhibitors, with emphasis on technological improvements and COX-2 inhibitors as components of drug combinations.