| Posters (9)

Fasiglifam (TAK-875) is a GPR40 agonist which was developed for the treatment of type 2 diabetes. However, during Phase III clinical trials, it was withdrawn due to adverse liver effects.

In this poster, we focus on:

deciphering the mechanism of hepatotoxicity of fasiglifam (TAK-875)
understanding the impact of plasma protein binding and mitochondrial effects by fasiglifam using the Seahorse flux analyser platform

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Pharmacokinetic/pharmacodynamic (PK/PD) modelling plays an important role in drug development, especially in the case of antibiotics where the data generated is used for dose prediction up to Phase 2 clinical trials. This enables efficient study designs and identification of optimal dosing regimens that may suppress drug resistance.

In this poster, we focus on:

mathematical modelling of in vivo and in vitro data to generate a rational design with reduced animal requirements in order to determine the pharmacodynamic driver and magnitude of antibiotic efficacy
optimisation of the clinical dose regimen in Phase 2 clinical trials

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Vanoxerine is a multi-ion channel blocker. For this reason, it was developed as a therapy for atrial fibrillation. However, in Phase III trials, 11.5% of patients developed torsades de pointes. Using MEA and human iPSC-derived cardiomyocytes, it was possible to detect this cardiotoxic liability.

In this poster, we focus on:

the use of MEA and human iPSC-derived cardiomyocytes to detect vanoxerine arrhythmias
the time dependent effect of vanoxerine cardiotoxicity
the ADME properties of vanoxerine which may impact on its cardiotoxic effect

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Science Pool

Effects of Theophylline and Budesonide on Asthma Inflammation Model

Importance of Water Molecules in Protein-Ligand Complexes

Optimised Conditions for Measuring OX1 Receptor Occupancy

Discovery & Characterization of Neuroprotective Compounds Relevant to ALS

Characterisation of Novel P.aeruginosa QS Inhibitors

Tuning Covalent Reactivity: A Chemist’s Toolbox

Mechanism of Action Characterisation Using Cell Painting Techniques

Understanding the Hepatotoxicity of Fasiglifam (TAK-875)

PKPD Models for Antibiotic Efficacy

Detecting Vanoxerine Arrhythmia in Human iPSC-Derived Cardiomyocytes