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Promotional poster for Pharmaron's research on bitter taste blockers, featuring download info and scientific visuals on a molecular-themed background.

Poster Authors:

Michael Bestwick¹, Gillian Watt¹, Fran?ois Saint-Dizier¹, Amy Brown¹, Kevin Foote¹, Sebastien Campos¹, Jennifer Borthwick¹, O. Smith¹, Verity Kennett¹, John Pollard¹, John Maclean¹, R. Twidale¹, M. Tordoff², Carol Christensen², Peihua Jiang²

¹Pharmaron, West Hill Innovation Park, Hertford Road, Hoddesdon, Hertfordshire, EN11 9FH, United Kingdom

²Monell Chemical Senses Center, 3500 Market St, Philadelphia, PA 19104, United States

**PK/PD relationships, in vivo Evaluation, and Integrated Drug Discovery of Bitter Taste Blockers**

This poster was presented at the ELRIG Drug Discovery 2025.

The taste of medication is a critical factor in patient compliance, particularly for pediatric and geriatric populations. Bitter-tasting active pharmaceutical ingredients can significantly hinder adherence, thereby compromising treatment outcomes. To address this challenge, Pharmaron’s drug discovery services team worked with the Monell Chemical Senses Center to undertake an unconventional drug discovery project targeting bitter taste modulation.

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Integrated Drug Discovery

in vivo Pharmacology

DMPK Services

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Approach to Bitter Blocker Drug Discovery

To facilitate the discovery of bitter blockers, an integrated team from Pharmaron, the Monell Chemical Senses Center, and the Gates Foundation was assembled. An existing in vivo mouse model for bitter taste was optimized for drug discovery purposes, and PK/PD relationships were determined, enabling the model to be used for ranking and screening novel compounds.

Optimizing for Potency and ADME Properties

Lead optimization began with a tool compound and achieved improved potency (pIC₅₀ 8.1) compared to the initial compound (pIC₅₀ 7.3), while maintaining similar lipophilicity (Log D) and improving kinetic solubility. Optimization focused on key absorption properties relevant to the oral cavity, such as permeability and solubility.

Predictive Modeling for Efficient Screening

A predictive regression model was developed to correlate compound potency and concentration with observed in vivo efficacy. This model enabled more efficient lead selection and supported the development of optimized dosing strategies for future studies.

Download our poster to view our case study on the discovery of a novel bitter blocker performed in cooperation with the Monell Chemical Senses Center.