New Drug Paradigm: Liquid Crystal Pharmaceuticals

Kent State University, Summa Health System and IC-MedTech Inc. have taken steps toward that goal. Their collaborative efforts have yielded an innovative liquid crystal technology that offers the promise of new drugs which may more effectively manage cancer and other diseases.

Dr. Chun-che Tsai, Kent State professor of chemistry; Dr. Jim Jamison, manager of Urology, Obstetrics and Gynecology Core Basic Research Laboratory for Summa Health System; and Mr. Tom Miller, president of IC-MedTech Inc., a California-based biotechnology company, have developed a new paradigm in drug discovery based on the pharmacologic properties of liquid crystals called Liquid Crystal Pharmaceuticals™ or LCPs.

Recently, the team gathered at Kent State University’s Office of Technology Transfer to file applications for two new patents: one for a new LCP-based anti-tumor drug called Tolecine™ and another for a formulation that combines Tolecine™ and another LCP, Apatone®.

“The path-breaking discoveries of Dr. Tsai and his colleagues offer compelling proof of the value of university research and the enormous good that can come from collaborations between universities and the private sector,” says Kent State President Lester A. Lefton.  “As Kent State researchers tackle cancer and a host of other real-world ills and issues, they are bringing their leading-edge knowledge and creativity to our students and playing a significant role in economic development.” 

Though best known for their use in laptops, televisions and cell phones, liquid crystals also include families of organic substances that are essential for all life called lyotropic liquid crystals. Examples of lyotropic liquid crystals include DNA, proteins and cholesterol. LCPs are a unique class of lyotropic liquid crystals that represent novel drug candidates for the treatment of a wide range of diseases.

“Mother nature is the ultimate chemist,” says Tsai. “Although we use creative and sophisticated computer modeling techniques to screen for our candidate compounds, I’m always amazed at how nature puts it all together.” 

The most recent research involving LCPs has yielded a new investigational anti-tumor drug called Tolecine™, a compound that also has antiviral and antibacterial applications. Created by Tsai, it has been shown to be even more effective than the current standard of care for herpes.

The team’s second patent application involves a formulation that combines Tolecine™ and another LCP, Apatone®, which attacks cancer cells via multiple pathways to offer improved efficacy. Apatone® has been successfully tested in more than 30 human tumor cell lines at Summa and in a Phase I/IIa clinical trial, which demonstrated a delaying effect in the progression of end-stage cancer patients. In addition, the FDA granted Apatone® orphan-drug status for the treatment of metastatic, or locally advanced, inoperable bladder cancer in August 2007.

Unlike other chemotherapy drugs, TolecineTM and Apatone®have low toxicity and do not target dividing cells. Instead, they are activated by inflammation that occurs in and around tumor cells, sparing healthy cells. “We want to kill cancer cells specifically without killing surrounding tissues,” says Jamison.

Innovative, low-toxicity drugs such as Tolecine™ and Apatone®provide new hope in the battle against cancer and other diseases in the next few years. “Research on LCPs provides a solid scientific foundation for generations of new drugs,” says Miller. Adds Tsai: “LCPs are an untapped frontier from which many new, exciting treatments are now emerging.”