22
Views
29
CrossRef citations to date
0
Altmetric
Miscellaneous

Recently reported inhibitors of cyclooxygenase-2

Pages 21-29 | Published online: 25 Feb 2005
 

Abstract

Cyclooxygenase inhibitors exert their effect by preventing the conversion of arachidonic acid (AA) to prostaglandins (PGs), a primary class of mediators of inflammation. Recently, a second isoform of cyclooxygenase, now known as cyclooxygenase-2 (COX-2), has been discovered which is produced in response to inflammatory stimuli. Selective COX-2 inhibitors have been demonstrated to be anti-inflammatory and analgesic without causing the gastrointestinal damage associated with current non-selective cyclooxygenase inhibitors. Mechanistically, selective COX-2 inhibitors decrease inflammation by preventing ‘overproduction’ of PGs while allowing COX-1 to produce the basal levels of PGs necessary for the health of certain tissues (e.g., the gastrointestinal tract). The realisation that the serious side-effect profile can be markedly reduced has led the pharmaceutical industry to expend much effort to discover novel selective COX-2 inhibitors for the worldwide market (estimated to be about US$5 bn). Many chemical classes of compounds have been developed, some of which are currently in clinical trials. This review will cover the patent literature over the past 15 months.

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.