“We are delighted to have successfully leveraged our expertise in NNRs to bring forward a novel compound for smoking cessation, an area that is not only a major healthcare need but also where application of the NNR mechanism has been validated commercially,” said J. Donald deBethizy, President and CEO of Targacept.
“Emerging science has made the promise of NNR-targeted compounds as smoking cessation aids increasingly evident. It is important for a smoking cessation aid to specifically target the areas of the brain that serve as pathways for addiction, while addressing limitations of currently available products by minimizing unwanted side effects.”
Neuronal nicotinic receptors (NNRs) are a class of proteins in the nervous system that modulate the levels of key chemical messengers, such as dopamine. Nicotine’s addictive effects have been linked to over-stimulation of dopamine release in brain regions involved in feelings of reward and pleasure.
Various NNR subtypes modulate dopamine release in these pathways and represent optimal targets for therapeutic intervention. Compounds that can normalize the activity of these NNR subtypes have the potential to decrease the rewarding effects of nicotine and, as a result, the desire to smoke.
In July 2007, Targacept and GSK entered into a strategic alliance pursuant to which Targacept would utilize its proprietary Pentad™ drug discovery technology to discover novel small molecule product candidates that target specified NNR subtypes in five therapeutic areas -- pain, smoking cessation, addiction, obesity and Parkinson’s disease. GSK is participating in the alliance through its Center of Excellence for External Drug Discovery.
Statistics from the Centers for Disease Control and Prevention indicate that tobacco use remains the leading preventable cause of death in the United States, causing approximately 438,000 premature deaths each year. Datamonitor projects that the global prescription market for smoking cessation therapies will be as much as $4.6 billion by 2016.