A patent has been filed and the research begun on what USF chemists say will enhance the capabilities of current drugs.
In the summer of 2000, Michael Zaworotko, chair of the USF department of chemistry, began developing what he calls “crystal engineering” while working with a team of four students.
“Basically we are modifying the structure of drug molecules in different ways than the conventional,” said Zaworotko.
A formulation of a drug is the tablet itself, Zaworotko said, comprised of both the active and inactive ingredients. The active pharmaceutical ingredient (API) gives the drug its unique identifiable characteristics. The rest of the formulation controls the drug’s release, solubility, stability and other properties, he said.
“When you patent a drug, you patent the active ingredient, not the formulation. So the active ingredient is kind of the key to everything,” he said.
Years ago, crystals were thought to be unalterable, but the theory has since been disproved. Through the science and technology of crystal engineering, the inactive ingredients can be altered by combining two substances into a crystalline form without changing the API, forming a “co-crystal.” Changing the API would create an entirely new drug, Zaworotko said. He emphasized that he and his students aren’t creating new drugs; they are improving the properties of current ones.
Besides improving current drugs, the process could help medicines that haven’t made it to the market because of poor stability or solubility, Zaworotko said.
Jennifer McMahon, a third-year graduate student working on the project, said she sees a great future in co-crystals.
“It is very exciting. We have an opportunity to make pharmaceuticals better,” she said.
The possibility of seeing co-crystal-form drugs soon is good, since FDA approval is not required.
“With FDA approved drugs, there are much higher standards and stringency to proving what you got,” he said. “If you make a new co-crystal, it is the same API as before, which has already been tested.”
With this discovery also comes USF’s new partnership with Transform Pharmaceuticals, Inc., a drug company based in Lexington, Mass. In many cases when a university develops something like co-crystals, Zaworotko said, a company simply purchases the technology in cash. Another option for the university is to open a pharmaceutical company to manufacture and market the drug, a risky but not unheard of undertaking, he said. The collaboration with Transform is unique in that both USF and the company “have a vested interest in the future,” he said.
According to a licensing agreement between USF and Transform, the company will have exclusive rights to new co-crystals developed by the university.
“Transform and USF have consolidated their early intellectual property and will combine intellectual property on their ongoing research,” a press release from the company said.
Zaworotko adds that the partnership is equal.
“We are partners,” Zaworotko said. “They didn’t buy the technology and go off on their own, they are working with us. Where our expertise ends, theirs begins.”
The company will also subsidize the development of the science and technology of crystal engineering, and see to the marketing and selling of co-crystal-form drugs.