GIBH has developed a new chemical class of COX-2 inhibitors

The international research team, composed of Dr. John J. Talley, Dr. Mark Obukowicz, Dr. Yanmei Zhang, Dr. Zhengchao Tu and Micky Tortorella have developed a new chemical entity as COX-2 inhibitors for the treatment of inflammation and inflammatory pain. This work was filed as Chinese patent (201210202059.x) and submitted for PCT application.

COX-2 selective inhibitors (coxibs) widely replaced traditional NSAIDs because they retained comparable efficacy, while limiting toxicity to the gastrointestinal tract. Coxibs fell into disfavor within clinical medicine because initial data linked them to cardiovascular risks of stroke and myocardial infarction compared with traditional NSAIDs.  However, compelling data from two recent clinical analyses (Trell et al., 2011; Olsen et al., 2011) have shown that similar and even short-term cardiovascular risks were associated with both coxibs and traditional NSAIDs and that the risks appeared to be drug-dependent rather than class-dependent.  These data are instilling renewed interest in coxibs, particularly with coxibs that have a unique pharmacological profile, which could thus fulfill an unmet medical need.

The new deuterium-containing compounds made at GIBH could fulfill an unmet medical need in inflammation and cancer.  As a class, they have been shown to confer potency, efficacy, and selectivity on par with the diaryl heterocyclic coxibs in the standard rat models of inflammation and pain.  They also have the potential to be renal-sparing and thereby mitigate coxib-induced hypertension due to their intrinsic and distinct structural, pharmacological, and physiochemical properties.