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Redpoint Bio Researchers Develop Method of Measuring and Classifying Bitterness in a Broad Range of Orally Aversive Pharmaceuticals

October 22, 2008

Scientists at Redpoint Bio Corporation (OTCBB: RPBC) have developed a quantitative method to measure and classify the bitter or bad taste of frequently used medicines. The work points to approaches that have the potential to reduce or eliminate the aversive flavor of many widely prescribed orally-dosed drugs. The findings appear in the October 2008 issue of the peer-reviewed journal Behavioural Pharmacology.

The research paper, entitled, “Quantitative Assessment of TRPM5-Dependent Oral Aversiveness Of Pharmaceuticals Using A Mouse Brief-Access Taste Aversion Assay,” was authored by members of Redpoint’s discovery research team, including Heather R. Devantier, Daniel J. Long, Francis X. Brennan, Stacy A. Carlucci, Cynthia Hendrix, Robert W. Bryant, F. Raymond Salemme and R. Kyle Palmer. An abstract is available online at http://www.behaviouralpharm.com/pt/re/bpharm/currenttoc.htm. (Behavioural Pharmacology 19:673-682).

Many of the 20 drugs tested by Redpoint in a non-invasive mouse based assay, called BATA, are for pediatric use and their aversive taste often compels children to refuse medication, despite parental pleas and doctors’ orders. In addition, oral liquid formulations are popular with the elderly and compliance may likewise suffer if the drug is bitter. Furthermore, bitter taste has impaired advancement of newer, more convenient fast dissolve or “melt in your mouth” drug forms. U.S. sales of liquid formulations and of oral-dissolve drugs are over $1 billion each.

This study is the first to examine the precise mechanism underlying the unpalatability of pharmaceutical drugs and has shown that many of these drugs conduct their bad taste response through a specific taste-cell protein known as the TRPM5 ion channel. These findings open the door to bitter taste reduction through the use of specific inhibitors of the TRPM5 ion channel, a research area Redpoint Bio is actively pursuing. The tested drugs represented a range of chemical structures and included antibiotics, antihistamines, antifungals, cough suppressants, analgesics, cycloheximide and quinine. The paper also describes the inclusion of a trained human taste panel in the study and noted a ‘striking correspondence in oral aversive potency between humans and mice.’

“We believe these findings have the potential to play a key role in reformulating existing oral drugs for better compliance, particularly in pediatric and geriatric care, and in enabling drug companies to reconsider drug candidates that were previously abandoned due to insurmountable bitterness,” said F. Raymond Salemme, Redpoint’s Chief Executive Officer.

“Studies of this nature lay the foundation for a deeper understanding of taste signaling and for engineering new modifiers to amplify or suppress a product’s native flavor,” he added. The authors noted that while it was expected that bitter tasting drugs would act at bitter receptors to create the bitter taste sensation, it wasn’t until recently that modern methods of pharmacology have been successfully applied to the problem.

About Redpoint Bio Corporation

Redpoint Bio is leveraging recent discoveries in the molecular biology of taste to discover and develop novel taste enhancers and aversive taste blockers for the food, beverage and pharmaceutical industries. Redpoint Bio’s food and beverage program is focused on identifying flavor enhancers that improve the taste of existing ingredients, reduce the need for excess sugar and salt, and contribute to the development of healthier, better-tasting foods and beverages. The pharmaceutical program uses a biochemical approach aimed at suppressing the bitterness of medicines, which has the potential to expand the range of formulation options and increase patient compliance. For more information, please visit the Company’s website at www.redpointbio.com.




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