ACS Honors Heroes Of Chemistry 2010

For their exceptional R&D work to develop a treatment for type 2 diabetes and a smoking-cessation product, five industrial scientists from two companies were named as this year’s Heroes of Chemistry. They were recognized on Aug. 22 at a formal dinner during the American Chemical Society’s national meeting in Boston.

The Heroes of Chemistry program, which began in 1996, honors chemical innovators for developing commercially successful products or technologies that benefit humankind. The honorees are meant to embody the ACS vision: improving people’s lives through the transforming power of chemistry.

Each year, an ACS panel selects the Heroes of Chemistry from a pool of chemical scientists nominated by their own companies. The Heroes of Chemistry innovations are the “result of the support and vision of corporate management, who invest in science, understand its application, and advocate for it within their organizations,” said ACS President Joseph S. Francisco at the awards event.

Among this year’s heroes is a team of Merck & Co. scientists who were responsible for the discovery and development of Januvia for the treatment of type 2 diabetes. Those honored were Joseph D. Armstrong III, senior director of the Discovery & Preclinical Sciences Integration Office at Merck; Nancy A. Thornberry, the company’s senior vice president and franchise head for diabetes and obesity; and Ann Weber, the company’s vice president of discovery and preclinical sciences and chemistry head.

Januvia inhibits the enzyme dipeptidyl peptidase 4, thereby increasing active incretin hormones and enhancing the body’s own mechanisms to lower glucose levels. In doing so, Januvia targets two key defects that cause poor glucose control in type 2 diabetes: decreased insulin release and uncontrolled glucose production by the liver.

“This amazing drug is not only highly effective but also efficient in that it was developed using an innovative synthesis that reduced waste during the manufacturing process,” Francisco said. Whereas the original production method involved eight steps, the new route involves only three and eliminates aqueous waste streams. It was recently recognized with a Presidential Green Chemistry Challenge Award, he noted (C&EN, June 28, page 9).

More than 21 million prescriptions have been written for Januvia in the U.S., and it has been approved for use in 89 countries and territories, Francisco said. It ranks second among branded oral type 2 diabetes agents in 2009 sales, which were $1.9 billion.

Two research fellows at Pfizer Global Research & Development—Jotham W. Coe and Brian T. O’Neill—were also recognized as Heroes of Chemistry for the discovery of varenicline, a breakthrough therapy for smoking cessation that is marketed as Chantix. O’Neill is laboratory head and research project leader in the neuroscience medicinal chemistry department at the company, and Coe is in Pfizer’s neuroscience department.

“Coe and O’Neill were major contributors to the conception of analogs and the design of enabling synthetic technology that made this program successful,” Francisco said. Varenicline is a partial antagonist of the α4β2 nicotinic receptor subtype. The product is unique in that it not only works to reduce cravings for nicotine, but it also simultaneously diminishes the positive reinforcement from nicotine.

Launched in 2006, Chantix generated worldwide sales of $700 million in 2009. It has been approved in 86 countries and prescribed to approximately 11 million people.

The products “discovered and developed by tonight’s honorees have saved or improved lives around the world,” Francisco said. “It is a source of great pride to us at ACS that, in each case, fundamental science has been brought to the marketplace to benefit all of us.”

Nominations for the 2011 Heroes of Chemistry program will be accepted starting in January 2011. Visit www.acs.org/awards for further information.