Dual COXIB/TP antagonists : a possible new twist in NSAID pharmacology and cardiovascular risk
Articolo
Data di Pubblicazione:
2010
Citazione:
Dual COXIB/TP antagonists : a possible new twist in NSAID pharmacology and cardiovascular risk / G. E. Rovati, A. Sala, V. Capra, S. E. Dahlén, G. Folco. - In: TRENDS IN PHARMACOLOGICAL SCIENCES. - ISSN 0165-6147. - 31:3(2010), pp. 102-107. [10.1016/j.tips.2009.11.007]
Abstract:
In the 1990s, after identification of two cyclo-oxygenase (COX) isoforms catalyzing the synthesis of prostaglandins and thromboxane A(2) (TXA(2)), a new class of non-steroidal anti-inflammatory drug (NSAID) became available (COX-2 inhibitors, or COXIBs). COXIBs have become among the best-selling drugs because of their gastrointestinal safety compared with NSAIDs. Concomitantly, increasing evidence for a potential cardiovascular hazard associated with COXIBs emerged. This suggested that selective inhibition of the synthesis of COX-2-derived prostanoids could lead to undesired disruption of the intricate inter-eicosanoid network. Further improvement of COXIBs is therefore necessary, and a potential strategy might involve targeting the TXA(2) receptor to balance the undesired cardiovascular effects of COXIBs. It has recently been demonstrated that a traditional NSAID and a selective COXIB possess an additional activity: weak competitive antagonism at the TXA(2) receptor. Full exploitation of dual-targeted compounds may represent a 'new twist in NSAID pharmacology'.
Tipologia IRIS:
01 - Articolo su periodico
Keywords:
FANS ; coxib ; inflammation ; cardiovascular
Elenco autori:
G.E. Rovati, A. Sala, V. Capra, S.E. Dahlén, G. Folco
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