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Volume 42, Issue 9
Senomyx uses an approach, known as taste-blocking, to address the challenges of bitter APIs. Kenneth J. Simone, vice-president of Pharmaceutical Business Development, Senomyx, speaks with Pharmaceutical Technology about this technology.
It is well recognized that bitter APIs can have a negative effect on patient compliance. As a result, there is an increasing demand for taste-masking technologies that address this issue. Senomyx uses an alternative approach, known as taste-blocking, to address the challenges of bitter APIs. “The company was founded in 1998 based on the work of Charles Zuker from the University of California, San Diego, who is credited with the discovery of taste receptors in rodents,” Kenneth J. Simone, vice-president of Pharmaceutical Business Development, Senomyx, told Pharmaceutical Technology. “Since then, we have replicated this work in human taste receptors and determined the mechanism of action for sweet and bitter taste.”
Simone explains that in the human genome, there are 25 genes localized on three different chromosomes, which code for bitter taste receptors that are expressed in taste buds on the tongue. “Senomyx has developed proprietary assays for 22 of these receptors,” he says. “Using these assays with classical biotechnology approaches such as high throughput screening, chemical optimization, and taste tests, we have developed novel bitter taste blockers for food, beverages, over-the-counter (OTC), and pharmaceutical applications.” Pharmaceutical Technology spoke to Simone about Senomyx’s taste-blocking technology.
PharmTech: How does taste-blocking work, what is the mechanism of action or the principle behind the technology?
Simone: Our bitter taste blockers act as genuine receptor antagonists. They bind to the bitter receptor eliciting the bitterness of the active ingredient and keep the receptor inactive, resulting in a reduced level of bitter sensation being relayed from the receptor to the nerves, even in the presence of the bitter active ingredient. We also have the ability, through our proprietary assays, to screen compounds, such as APIs, to determine which bitter receptors the compound activates. This information allows us to focus on the dominant receptors and achieve maximum blocking effect.
PharmTech: How is it different than other taste-masking approaches?
Simone: The materials Senomyx has developed are blockers, not maskers. Our bitter taste blockers have no inherent taste on their own at usage levels and specifically block bitterness at the receptor level. Masking is typically approached by adding sweeteners or other flavoring agents, at high levels, to impart other taste characteristics in a formulation. The masking approach does not act specifically to attenuate bitterness, and as such, only limited success is achieved when trying to mitigate the bitterness of APIs. Many APIs are several hundred times more bitter than sources from food and beverages, like coffee.
PharmTech: Can you provide some examples of pharmaceutical applications of your taste-blocking technology?
Simone: Senomyx’s Bittermyx BB68 bitter blocker is already being used in API applications to attenuate bitterness. It is being evaluated for use in additional products. The work is focused on pediatric and geriatric solutions (i.e., liquid or dissolvable formats, and not encapsulated or coated tablets). In-vitro studies have demonstrated that BB68 can attenuate bitterness in cough and cold remedies using acetaminophen, guaifenesin, and dextromethorphan.
Vol. 42, No. 9
When referring to this article, please cite it as A. Siew, “Taste-Blocking-An Alternative to Tastemasking,” Pharmaceutical Technology 42 (9) 2018.