Humans detect bitter and poisonous substances with 25 different bitter taste receptors expressed in taste receptor cells located in taste buds on the surface of the tongue. These receptors belong to the vast family of Class A G protein-coupled receptors and, using cell based assays, at least 22 of these receptors have now been functionalized. Surprisingly a single bitter taste receptor can be activated by several chemically diverse ligands and, conversely, a specific bitter ligand can activate several bitter receptors. Senomyx followed a classical discovery paradigm for the identification and development of potent bitter receptor antagonists that could potentially serve as FMPs for the food, beverage, OTC and pharmaceutical industries. High throughput screening was performed on 13 different receptors using a library of diverse structures. Hits were then analyzed for potency, specificity and selectivity. Several lead series were then evaluated for attenuation of bitterness of representative tastants. Based on its potency, positive effects in sensory studies and physical properties, BB68 (3-(1-((3,5-dimethylisoxazol-4-yl)methyl)-1H-pyrazol-4-yl)-1-(3-hydroxybenzyl)imidazolidine-2,4-dione(S6821, CAS 1119831-25-2) was promoted as a development candidate. Following a battery of safety and toxicological studies, BB68 received FEMA GRAS status in 2010 followed by additional regulatory approvals by JECFA, China, Japan, Korea, Mexico & Indonesia. BB68 now being commercialized in several countries to effectively attenuate the bitterness of pharmaceutical and consumer products.

Discovery and function of flavors with modifying properties (FMPs) for attenuation of bitterness in consumer products, pharmaceuticals and OTCs

256th National Meeting (2018)

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