Science Pool

Importance of Metabolism, PK and Toxicity in Drug Design

Posted by Evotec on Mar 6, 2021 2:26:12 PM

Tags: Articles & Whitepapers, ADME/DMPK, Toxicology & Safety

Adding Value to your Company with Lean SixSigma

Posted by Evotec on Mar 6, 2021 2:24:41 PM

Tags: Articles & Whitepapers, ADME/DMPK

PK and Metabolism of Lumiracoxib in Chimeric Humanized and Murinized FRG Mice

Posted by Evotec on Mar 4, 2021 10:11:43 PM

Tags: Articles & Whitepapers, ADME/DMPK, Age-Related Diseases

Drug-Drug Interaction (DDI) Regulatory Guide

Posted by Evotec on Feb 16, 2021 10:13:56 AM

Our popular, easy-to-follow guide: 'DDI Regulatory Guidance' is now on its 3rd edition.

Read about:

  • an easy to follow summary and comparison of the latest DDI guidance from the FDA and the EMA
  • a focus on reaction phenotyping, cytochrome P450 inhibition, cytochrome P450 induction, drug transporter substrate studies and drug transporter inhibition
  • an overview of the regulatory methods and interpretation of data

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Tags: Guides, ADME/DMPK, IND Enabling Studies/Preclinical Development

Methods to Investigate In Vitro Skin Metabolism

Posted by Evotec on Feb 15, 2021 12:59:28 PM

The skin is the largest organ in the human body. It contains enzymes capable of drug metabolism.

In this presentation, we focus on:

  • the physiology of the skin and an overview of skin enzymology
  • the role of skin metabolism in absorption, efficacy, homeostasis, drug delivery and toxicity
  • adverse reactions in the skin including the mechanism behind skin sensitisation
  • in vitro methods for investigating skin metabolism

View the presentation to learn more!

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Tags: Presentations, ADME/DMPK

Are TripleTOFs the Future for HT-ADME/Toxicity Screening?

Posted by Evotec on Feb 12, 2021 8:34:02 PM

LC-MS provides the analytical endpoint for most discovery ADME assays. There is a constant drive to reduce LC-MS run times whilst maintaining quality. 

In this presentation, we focus on:

  • a comparison of triple quadrupole MS/MS vs TripleTOF MS
  • validation data for performance of the TripleTOF MS 
  • use of the TripleTOF in high throughput ADME screening including intrinsic clearance assays and soft spot analysis.

View the presentation to learn more!

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Tags: Presentations, ADME/DMPK

Transporter DDI - An Evaluation of Approaches and Methodology

Posted by Evotec on Feb 12, 2021 5:31:58 PM

Due to an aging population, polypharmacy is increasing. Drug-drug interactions account for 5% of UK hospital admissions, and are a particular concern for common co-meds such as statins.

In this presentation, we focus on:

  • a background to drug-drug interactions (DDI)
  • the use of the mechanistic static models in the prediction of transporter-mediated DDI
  • a comparison of the different published models and their performance 

View the presentation to learn more!

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Tags: Presentations, ADME/DMPK

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

Read our poster to learn more about our research!

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Tags: Posters, ADME/DMPK

Application of a Low Intrinsic Clearance Assay in Drug Discovery

Posted by Evotec on Feb 12, 2021 3:50:55 PM

In order to accurately predict human pharmacokinetics and efficacious dose, a robust measurements of clearance is essential.

In this poster, we focus on:

  • a novel primary human hepatocyte media supplement (HepExtendTM)
  • a comparison of HepExtendTM with the widely used CM4000 with and without a Geltrex overlay
  • a correlation of scaled in vitro human intrinsic clearance with in vivo human intrinsic clearance

Read our poster to learn more about our research!

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Tags: Posters, ADME/DMPK

Mass Defect Filtering for Metabolite Soft Spot ID

Posted by Evotec on Feb 12, 2021 2:33:07 PM

Real time mass defect filtering (MDF) on independent acquisition (IDA) scans enable the generation of simultaneous selective MS and MSMS data in one injection.

In this poster, we focus on:

  • the use of high resolution mass spectrometry and mass defect filtering combined with rapid chromatographic run times and semi-automated commercial software for soft-spot identification of metabolites
  • demonstration of the metabolite soft-spot method using verapamil and dextromethorphan

Read our poster to learn more about our research!

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Tags: Posters, ADME/DMPK