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The Story of Celebrex
Peter Isakson, Ph.D.
Jaime Masferrer, Ph.D.
Karen Seibert, Ph.D.
John Talley, Ph.D.
Honorees Peter Isakson, Ph.D., Jamie Masferrer, Ph.D., Karen Seibert, Ph.D., and John Talley, Ph.D. of Pharmacia created the molecule celecoxib, the basis for the medicine Celebrex®, which blocks the inflammation-triggering action of the COX-2 enzyme, bringing relief to millions of people around the world who suffer from osteoarthritis, rheumatoid arthritis, and pain.
Until the 1980s, the conventional wisdom held that there was only one COX, or cyclooxygenase enzyme, which both protected the stomach lining and caused inflammation. For that reason, most medicines for arthritis also caused gastrointestinal problems in many patients. But these scientists and their colleagues hypothesized that there were two COX enzymes, and set out to block the enzyme involved in inflammation without affecting the enzyme that protects stomach lining. In 1991, after the gene sequence for the COX-2 enzyme was published, the scientists looked for a molecule that would selectively block the COX-2 enzyme.
Dr. John Talley and his team of medicinal chemists manipulated molecules and made thousands of different analogs. Promising compounds were given to the biologists who set up a system to evaluate compounds quickly for their pharmacological profiles. They finally found a compound that was a strong selective inhibitor of COX-2, but it had a long half-life - it lingered in the body too long. The molecule was sent back to the laboratory and modified, and the scientists synthesized the compound that eventually became Celebrex.
Clinical trials of Celebrex began in 1995. In all, some 13,000 volunteers in countries all over the world took part in the trials. In June 1998, the company submitted an application to the Food and Drug Administration (FDA) to market the drug. The FDA gave the application an accelerated review, and on December 30, 1998, Celebrex was approved for the treatment of osteoarthritis and rheumatoid arthritis. It has also been approved for familial adenomatous polyposis, a rare and devastating disease that often leads to colon cancer.
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