Prostaglandin E2 (PGE2; ) is the major PG synthesized at sites of inflammation and plays an important role in different inflammatory diseases. It acts as a mediator of pain and inflammation and promotes bone destruction. The increased synthesis of PGE2 during inflammation can be accounted for by increased expression of both COX-2 and microsomal PGE synthase-1 (mPGES-1). CAY10700 is an orally bioavailable inhibitor of mPGES-1 (IC50 = 0.24 μM in an in vitro human whole blood assay). It is inactive against COX-1 and COX-2 (9% inhibition at 100 μM and 16% at 30 μM, respectively).
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