Inhibition of Bitter Taste from Oral Tenofovir Alafenamide

Children have difficulty swallowing capsules. Yet, when presented with liquid formulations, children often reject oral medications due to their intense bitterness. Presently, effective strategies identify methods, reagents, and tools block bitterness remain elusive. For a specific bitter-tasting drug, identification of the responsible bitter receptors discovery antagonists for those can provide method perceived We identified compound (6-methylflavone) that responses an intensely anti–human immunodeficiency virus (HIV) tenofovir alafenamide (TAF), using primary human taste bud epithelial cell culture as screening platform. Specifically, TAS2R39 TAS2R1 are main type 2 responding TAF observed via heterologously expressing TAS2R into HEK293 cells. In this assay, 6-methylflavone blocked TAF. sensory testing, 8 16 subjects showed reduction in after pretreating (or “prerinsing”) mixing Bitterness was completely reliably two these subjects. These data demonstrate combined approach culture–based screening, receptor-specific assays, psychophysical testing successfully discover molecules blocking pharmaceuticals, such HIV therapeutic Our hope is use blockers increase medical compliance vital medicines. SIGNIFICANCE STATEMENT Identification small molecule inhibits from may treating infections.