MIZZOU NEWS

Healing Heartburn

In June, the Food and Drug Administration approved Rapinex, a fast-acting heartburn drug that was developed by University of Missouri-Columbia researcher Jeffrey Phillips and licensed to California-based pharmaceutical company Santarus, Inc. The FDA’s approval opens the door for the drug to go on the market this fall.

“This license agreement is one of the most important in the history of the University,” says Thomas Sharpe, executive director of the MU Office of Technology and Special Projects. “It allows Dr. Phillips’ innovation to reach a very large population of patients in need, and we expect it to generate revenues to the University that will allow us to make substantial improvements in our research and technology commercialization infrastructure.”

Rapinex is in a class of drugs called proton pump inhibitors, or PPIs. They are some of the best-selling drugs in the world, representing $13 billion in annual sales in the U.S. alone. The approved drug was an immediate-release, 20-milligram prescription form of omeprazole, used for treatment of heartburn and other symptoms of gastroesophageal reflux disease. In its approval, the FDA asked Santarus to change the drug’s name.

“The advantages of Rapinex is that it is absorbed faster, starts working immediately and lasts longer than drugs currently on the market,” says Phillips, a research associate professor and director of research in MU’s Department of Surgery in the School of Medicine. “Similar drugs require several doses before the full therapeutic effect occurs. Rapinex also is unique because it can be made in a liquid form, which is very useful for children and hospitalized patients.”

Santarus has applied for FDA approval for a 40-milligram version of Rapinex used to treat ulcers and prevent gastrointestinal bleeding in critically ill patients. A decision is expected by the end of the year. Phillips worked with Michael Metzler, former director of trauma services at MU Health Care, to test a precursor to Rapinex as a therapy for intensive-care patients with severe acid-related problems. Phillips says this was important because it allowed the identification of the best dosing strategy so that Santarus could design and perform the FDA study quickly.

Critically ill patients with stress ulcers often can’t swallow medication because of their underlying critical conditions. As a result, doctors trying to stem stress-related upper gastrointestinal bleeding must rely on liquid drugs administered by a feeding tube or intravenous medicines.

But this, too, presents problems, Phillips says. The I.V. form of the PPIs does not work rapidly. Oral liquid drugs work more quickly, but are not as potent at stopping acid production. The standard PPI drugs are available only as capsules containing enteric-coated granules or enteric-coated tablets that must be ground up. However, grinding destroys the enteric coating needed to protect the PPI from acid already built up in the stomach.

In his research, Phillips proposed a novel solution: Why not administer a single dose of sodium bicarbonate as an acid buffer, then wash crushed PPI granules down with an additional buffer? He reasoned that if even some of the drug were absorbed it would benefit the patient.

The result far surpassed these modest expectations. Not only did the buffer protect the drug in the stomach, but it substantially increased the speed at which the PPI entered a patient’s blood stream. Following publication of his discovery, Phillips turned to Sharpe for help in commercializing the discovery, and the two teamed up with Gerard Wood, a pharmaceutical industry consultant from Kansas City, to license the technology to Santarus. The company has worked aggressively to take a product based on Phillips’ work through human clinical trials and FDA approval, and it has worked with MU to maximize patent protection for the product.

“The role that Dr. Phillips’ work played in the development of Rapinex is a shining example of how research activities at MU can improve people’s lives,” says Vice Provost for Research Jim Coleman. “The spirit of MU’s faculty that drives them to conduct world-class research is a major reason that MU has outpaced the public members of the Association of American Universities in research growth, and why we think MU research can play a major role in defining Missouri’s economic future.”

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Last Update: November 15, 2007