Title:Desirable Properties for 3rd Generation Cyclooxygenase-2 Inhibitors
Volume: 16
Issue: 16
Author(s): Micky D. Tortorella, Yanmei Zhang and John Talley
Affiliation:
Keywords:
COX-2, Inflammation, PGE2, Cancer, Pain.
Abstract: Coxibs are a class of powerful drugs used by millions of people
worldwide to treat a wide variety of ailments such as muscular skeletal pain and
inflammation. The primary mechanism of action of coxibs is the potent inhibition of
the COX-2 enzyme. Unfortunately, their use is limited to patients due to a variety of
factors including poor solubility, negative effects on renal clearance and increased
risk of cardiovascular pathology. However, because of their effectiveness in
blocking PGE2 mediated inflammation, a key pathway that drives many diseases,
there is a clear unmet medical need to develop new COX-2 inhibitors that are free of
the aforementioned problems. The purpose of this prospectus is to define the
specific properties that are desired in 3rd generation coxibs as a starting point for the
development of new and better drugs.