Dr. Harry Jacobson addresses the crowd at the P&G announcement as Mayor Bill Purcell listens. (photo by Dana Johnson)
Procter & Gamble patents
to spark new drug discovery
A new “super aspirin” that heals ulcers while it relieves pain could be among a collection of chemical compounds given last week by Procter & Gamble to Vanderbilt University.
Procter & Gamble donated its proprietary “COX-2 Inhibitor Technology” – 196 patents and all associated intellectual property for compounds that block the action of the enzyme cyclooxygenase-2.
Two prescription COX-2 inhibitors, Celebrex and Vioxx, have already generated excitement as stomach-friendly treatments for arthritis. And the promise of these drugs doesn’t end with pain and inflammation relief. COX-2 inhibitors may also find use in the prevention and treatment of cancer and Alzheimer’s disease.
“I feel a little bit like a kid on Christmas morning, waiting to open up what may be one of the biggest gifts one could have a chance to open,” Dr. Harry Jacobson, vice chancellor for Health Affairs, told the crowd gathered for the donation announcement.
“Celebrex and Vioxx are already household names,” Jacobson said. “We hope to add a third COX-2 inhibitor to this list.”
The global market for Celebrex and Vioxx is approximately $3 billion annually. If Vanderbilt succeeds in developing and commercializing a new “super aspirin” drug, future royalties could reach $1 billion annually.
The gift of patent rights to the COX-2 inhibitors is the sixth in a series of Procter & Gamble technology donations to leading universities and research institutions.
“We are now creating more technology than we can possibly develop,” said Nancy Eddy, Ph.D., director of Procter & Gamble Pharmaceuticals. “So we are opening our doors and donating some of those technologies so that their potential can be realized.”
Procter & Gamble’s external consultants identified Vanderbilt – a longtime leader in research areas that include the cyclooxygenase enzymes – as the university most uniquely qualified to further develop the COX-2 inhibitor technology.
“This gift is an enormously important affirmation of the fact that we do world class work here,” said Chancellor E. Gordon Gee, after accepting a stack of patent folders adorned with a large ribbon bow.
COX-2 inhibitors sidestep the gastrointestinal side effects of aspirin and related non-steroidal anti-inflammatory drugs (NSAIDs) by blocking COX-2 – an enzyme that contributes to inflammation – but not interfering with the related enzyme COX-1 that protects the stomach lining. Because NSAIDs like aspirin, ibuprofen, and acetaminophen block both COX-2 and COX-1, they relieve pain and inflammation, but at the same time, they expose the stomach to damage.
Of the nearly 200 compounds being donated to Vanderbilt, one has been tested more extensively and holds promise for commercialization. In animal studies, this lead compound appears to be as effective an anti-inflammatory as Celebrex and Vioxx, with an added edge – an ulcer healing effect.
Although Celebrex and Vioxx do not appear to cause the gastric side effects that other NSAIDs do, they slow the healing of ulcers that are already present. The Procter & Gamble lead compound, on the other hand, seems to promote ulcer healing and may even prevent the development of NSAID-induced ulcers.
“We have no idea how this compound is working to promote ulcer healing,” said Dr. L. Jackson Roberts II, professor of Pharmacology and Medicine. “This is something we will try to understand. Who knows, we may uncover some new mechanism of ulcer healing.”
Beyond pain relief, COX-2 inhibitors may find applications as cancer drugs.
“There is great excitement about the potential of COX-2 inhibitors for both cancer prevention and cancer treatment,” said Dr. Mace L. Rothenberg, Ingram Professor of Cancer Research and director of Phase I Drug Development for the Vanderbilt-Ingram Cancer Center.
Dr. Raymond N. DuBois Jr., Mina Cobb Wallace Professor of Cancer Prevention and associate director for Cancer Prevention for Vanderbilt-Ingram, and others are testing Celebrex in patients to see if it can prevent colon cancer by blocking the growth of pre-cancerous polyps in the colon.
Used in combination with chemotherapy, COX-2 inhibitors appear to improve the tumor killing activity of the chemotherapy, Rothenberg said. He will screen a number of drug combinations, including the Procter & Gamble compounds, to identify leads for cancer treatment.
The framework for commercializing the COX-2 inhibitor technology, in place in the Office of Enterprise Development directed by George M. Stadler, was an important factor in Procter & Gamble’s decision to donate the technology to Vanderbilt.
To develop the Procter & Gamble lead compound as a therapeutic drug, Vanderbilt has established a new company called PharmaVU, Inc. through the Office of Enterprise Development with an investment from the University’s Chancellor Fund. PharmaVU plans to contract the remaining animal toxicology studies to an outside company and then conduct Phase I clinical trials.
“Carrying the drug through Phase I trials will greatly enhance its value,” Roberts said. “At that point, it should be very attractive for a company to license and further develop it through Phase II and Phase III trials and eventually marketing.”
Procter & Gamble is an industry leader in donating technologies to universities and research institutions, Roberts said. If the technology is further developed and marketed, the value of the donation becomes tax deductible. In addition to donating the patents to Vanderbilt, Procter & Gamble will provide funds to maintain the patents for three years and to assist in drug development.
“This is the highest form of great corporate citizenship,” Gee said at the donation announcement. Mayor Bill Purcell also thanked Procter & Gamble, noting that the technology donation will stimulate economic development and enhance people’s lives in the Nashville area and beyond.
“After hearing what these drugs could do,” Purcell said, “I feel better already.”
The Procter & Gamble donation is the second gift of patent technology to Vanderbilt. In December 1999, the DuPont Company donated a patented chemical manufacturing process. The process provides a low cost method for producing the chemical building blocks for a class of COX-2 inhibitors developed by Lawrence J. Marnett, Ph.D., Mary Geddes Stahlman Professor of Cancer Research and associate director for Basic Science Programs for Vanderbilt-Ingram.