| Posters (10)

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 However, during Phase III clinical trials, it was withdrawn due to adverse liver effects.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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Tags: Posters, Toxicology & Safety

PKPD Models for Antibiotic Efficacy

Posted by Evotec on Feb 15, 2021 10:35:36 AM

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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Tags: Posters, In vivo Pharmacology

Detecting Vanoxerine Arrhythmia in Human iPSC-Derived Cardiomyocytes

Posted by Evotec on Feb 12, 2021 4:00:23 PM

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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Tags: Posters, Toxicology & Safety

Ultrafast LC-MS for HT-ADME Analysis in Drug Discovery

Posted by Evotec on Feb 12, 2021 3:57:17 PM

Reducing the sample cycle time for LC-MS analysis is critical in increasing throughput and improving efficiency.

In this poster, we focus on:

the development of a ultra-fast chromatography method with rapid cycle time
the analysis of the sensitivity, linearity, reproducibility, robustness and matrix effects for the method
applicability to intrinsic clearance determination

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Tags: Posters, ADME/DMPK

Unravelling the Mechanism of TAK875 DILI

Posted by Evotec on Feb 12, 2021 3:54:17 PM

TAK-875 (fasiglifam) is a GPR40 agonist which was developed for the treatment of type 2 diabetes. However, TAK-875 was withdrawn from phase III clinical trials due to drug-induced liver injury (DILI).

In this poster, we focus on:

investigating the mechanism behind the hepatotoxicity of TAK-875
an in-depth understanding of the effect of TAK-875 on mitochondrial toxicity
understanding the impact of plasma protein binding

Read our poster to learn more about our research!

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0 Comments Click here to read/write comments

Tags: Posters, Toxicology & Safety

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