Scientists at UB and Therex Technologies Inc. have developed a remarkably versatile, antibacterial compound with anti-inflammatory properties that they are investigating as a potential topical treatment for acne and gingivitis, and as a preventive agent for skin cancer.

Trifluorosal, which comes from the same class of compounds as aspirin, will be evaluated in a clinical trial as an acne treatment beginning early next year under a $750,000 SBIR (Small Business Innovation Research) grant from the National Institute of Arthritis and Musculoskeletal and Skin Diseases to Therex.

Under a $100,000 grant from the National Cancer Institute, Trifluorosal also will undergo Phase I studies to examine the feasibility of developing it as a preventive agent for skin cancer.

Therex is a graduate of the UB Technology Incubator and a subsidiary of OmniPharm Inc., another graduate of the incubator.

It previously was awarded grants totaling $650,000 from the National Institute of Dental and Craniofacial Research to investigate the same compound's potential for treating gingivitis.

"If it turns out to be useful for several of these indications, the market potential for Trifluorosal is at the billion-dollar level," said Joseph Dunn, president of Therex, and research associate professor in the Department of Oral Biology in the School of Dental Medicine. "If it turns out only to be useful in the application with the smallest market, then its potential is still in the hundreds of millions."

Developed and patented by UB researchers in the School of Pharmacy and Pharmaceutical Sciences and the School of Dental Medicine, Trifluorosal was licensed to Therex.

In exchange for exclusive rights to the compound, UB has retained 5 percent ownership of Therex, and will receive royalties from sales of any products that result.

Dunn cautioned that there is a long way to go if the compound is deemed marketable. He noted that the road from a New Drug Application to the marketplace takes three to five years per drug per indication for a drug. It also takes anywhere from $25 million to $400 million in funding, a cost that makes partnering with a major company a necessity.

Two major U.S. pharmaceutical companies already have expressed interest in Trifluorosal.

UB researchers identified the chemical precursor to Trifluorosal while conducting federally funded research in which they were searching for antibacterial compounds in products already on the market that adhered well to skin or mucous membranes.

The idea was that if such compounds became the basis for new treatments, they likely would be safe, explained Robert J. Genco, SUNY Distinguished Professor and chair of the Department of Oral Biology, since they already were on the market and were designed to be active only at the surface and not absorbed into the body.

Genco and colleagues found the precursor in shampoos and soaps, then modified it and developed Trifluorosal. Further work by UB and Therex researchers has resulted in a second generation of active compounds.

"Trifluorosal is an antibacterial agent, but since it is not an antibiotic, it has a very low potential for producing bacterial resistance," said Genco. "At the same time, it is an anti-inflammatory agent and has a molecular structure similar to aspirin and its toxicity is extremely low. It is a member of the salicylanilide-type of agents, which bind strongly to skin and mucous membranes."

Genco and his co-researchers, Robert Coburn, professor of chemistry, and Richard Todd Evans, professor of oral biology—and both principals with Therex—initially were interested in the compound as a dental plaque inhibitor.

"Trifluorosal is as effective in inhibiting plaque and gingivitis as chlorhexidine, the most effective compound now on the market," said Genco. "However, Trifluorosal does not have the bad taste and tendency to stain teeth that characterizes chlorhexidine."

The researchers later found that it also kills the bacteria that cause acne.

After Therex licensed the compound from UB, the company's researchers found it also absorbed ultraviolet light and enhanced the repair of skin damage caused by sunlight, and therefore may be an important ingredient in lotions that prevent sunburn and skin cancer.

"The beauty of this agent is that it's very effective when applied topically, so we looked for diseases that could be treated or prevented this way," Dunn explained. "It is the inflammatory component that connects these diseases and what may turn sunburn into skin cancer."

The company simultaneously is investigating the applications for acne, skin cancer and gingivitis.

"We're investigating several therapeutic tracks in parallel since there is a lot of overlap in this research," said Genco. "So that makes it a very efficient research program.

"UB has been very supportive by working to patent these developments, by taking an equity position in Therex and by fostering development of this local company," said Genco.

Therex also has licensed two chemical libraries for drug screening from UB and to date has developed and filed patents for a drug candidate from one of them that shows significant promise for treating multi-drug-resistant breast cancer.