Thiazolidinediones are Partially Effective Bitter Blockers

Area of Science:

• Pharmacology
• Sensory Science
• Drug Development

Background:

• Bitter taste of medications poses a significant barrier to patient compliance, particularly for essential drugs used by children and the elderly.
• Developing effective bitter blockers is crucial for improving therapeutic outcomes and public health.

Purpose of the Study:

• To evaluate the efficacy of a novel class of bitter blockers, thiazolidinediones (TZDs), in masking the bitter taste of specific medications.
• To compare the bitter-blocking effects of rosiglitazone (ROSI) and a simpler TZD against a known sweetener control.

Main Methods:

• Two thiazolidinediones (TZDs) and a positive control (neohesperidin dihydrochalcone, NHDC) were tested.
• Taste testing was conducted with two panels (general and genetically informative) using bitter drugs: tenofovir alafenamide fumarate (TAF) and praziquantel (PRAZ).
• Participants rated bitterness intensity on a 100-point visual analog scale.

Main Results:

• Significant person-to-person variability in perceived bitterness of TAF and PRAZ was observed.
• Both TAF and PRAZ were rated as less bitter when combined with NHDC compared to alone.
• Rosiglitazone (ROSI) partially suppressed bitterness, with differential effects on TAF and PRAZ between the two taste panels.

Conclusions:

• Thiazolidinediones (TZDs) demonstrate partial efficacy as bitter blockers, with effectiveness varying across different drugs, individuals, and populations.
• Further investigation into TZD bitter blockers is warranted, focusing on diverse populations and a wider range of drugs.
• The development of effective bitter receptor blockers holds promise for enhancing medication adherence.