TOMOXIPROLE SELECTIVELY INHIBITS CYCLOOXYGENASE-2

Tomoxiprole is a nonsteroidal anti-inflammatory compound that was repo rted to have low ulcerogenic potential, a quality that would be expect ed of a cyclooxygenase-2-selective inhibitor, and, in fact, we find it is selective JOY this isozyme. In stably transfected COS cells, the c ompound inhibits recombinant human cyclooxygenase-2 (IC50 = 7 nM) more potently than recombinant cyclooxygenase-2 (IC50 = 240 nM), and simil ar results are obtained with partially pure ovine enzyme preparations. The compound is thus a very potent as well as selective inhibitor of cyclooxygenase-2. As is true of some other cyclooxygenase-2-selective inhibitors, tomoxiprole inhibition of cyclooxygenase-2 but not cycloox ygenase-1 is time-dependent.