Celecoxib History

By Dr. Ananya Mandal, MDReviewed by Sally Robertson, B.Sc.

Celecoxib belongs to a class of drugs called the Coxibs, which work by inhibiting the enzyme cycloxygenase-2 (COX-2). This enzyme is key to the production of prostanglandin, an important mediator of pain and inflammation.

Some examples of interesting facts surrounding the discovery and use of celecoxib include:

• Celecoxib was developed by G. D Searle & Company and co-promoted under the name Cerebrex by Searle’s parent company (Monsanto Company) and Pfizer.
• Monsanto then merged with Pharmacia and Pfizer acquired Pharmacia’s medical research division, meaning Pfizer became the owner of the celecoxib molecule.
• In 1998, Celebrex received approval for use in rheumatoid arthritis and osteoarthritis. Although the US Food and Drugs Administration (FDA) approved the drug, it also added that Celebrex carried the risk of heart disease and blood vessel complications.
• In 1999, the FDA added a warning that Celebrex had the potential to interact with the blood thinner warfarin and cause serious side effects such as severe bleeding and even death.
• In 1999, the FDA also approved Celebrex for the treatment of familial adenomatous polyposis, which is a precursor for colon cancer. The drug had proved effective at reducing the growth of the intestinal polyps seen in the disease.
• Celebrex received FDA approval with cardiovascular risk warning for ankylosing spondylosis treatment in 2005 and for juvenile rheumatoid arthritis in 2006.
• In 2006, the results of the Adenoma Prevention with Celecoxib (APC trial) were presented which showed that daily use of celecoxib over three years significantly reduced the recurrence of adenoma and advanced adenoma when compared with placebo.
• In 2008, the lead investigator of APC reported that although the effects of the drug were diminished two years after the treatment was stopped, there was still a treatment benefit at five years. Overall, the risk of advanced adenoma developing was decreased by 41% in those who took 400 mg/day of celecoxib compared with those who took placebo. In patients who took 800 mg/day of celecoxib the risk was educed by 26%. The study, however, showed that use of celecoxib was associated with an increased risk of serious cardiovascular side effects. The safety studies suggested that the risk for serious adverse effects was highest in individuals who already had cardiovascular risk factors before taking the therapy.