Discovers a safe, effective drug for hypertension
A team of chemists led by Peter Buehlmayer of Basel, Switzerland, will be honored on August 20 by the world's largest scientific society for its role in discovering valsartan, a drug that controls high blood pressure without causing side effects. The team will be designated one of 12 Heroes of Chemistry by the American Chemical Society at its 220th national meeting in Washington, D.C.
High blood pressure, or hypertension, affects up to 20 percent of adults worldwide, said Buehlmayer, a research chemist with Novartis Pharma AG. People with hypertension often sense no symptoms, but the excess pressure can damage the heart, kidneys, brain and eyes. Various classes of drugs can improve the condition, but many patients experience side effects.
Such is not the case with valsartan, which Novartis markets as Diovan. The drug blocks a receptor for a hormone that raises blood pressure by causing arteries to constrict. "It's very effective and safe, with high tolerability," he said. "In clinical trials, there was virtually no difference among the control group and Diovan group with regard to side effects."
"We asked, how can we find a molecule that specifically and selectively blocks the AT1 receptor site of angiotensin II?" Buehlmayer said. "Then we generated ideas with computer-assisted modeling that tried to minimize the chemical structure and find out what parts are important."
By early 1990, the newly synthesized molecule they named valsartan looked promising in animal tests. Clinical trials began the next year, and Diovan arrived on the market in Germany in 1996.
Buehlmayer's team included Walter Fuhrer, Pascal Furet, Peter Herold, Bruno Kamber, Hans Kuehnis, Rene Lattmann, Thomas Leutert, Franz Ostermayer, Alfred Sallmann, Tibur Schmidlin and Paul Zbinden. All worked closely with Novartis biologists led by Marc de Gasparo, he noted.
The Heroes of Chemistry program, started in 1996, honors industrial chemists and chemical engineers who create commercially successful products that improve the quality of life.
A nonprofit organization with a membership of 161,000 chemists and chemical engineers, the American Chemical Society publishes scientific journals and databases, convenes major research conferences, and provides educational, science policy and career programs in chemistry. Its main offices are in Washington, D.C., and Columbus, Ohio.