Science Pool

Learn more about pKa and LogP determination including:

• Background information
• Assay details and protocol summary
• Data generated for pKa and LogP

In this fact sheet you will learn more about our phototoxicity assay including:

• Background information
• Assay details and protocol summary
• Data generated in the phototoxicity assay

Learn more about our reactive metabolite glutathione trapping assay including:

• Background information
• Assay details and protocol summary
• Data generated in the glutathione trapping assay

Learn more about the S9 stability assay including:

• Background information
• Assay details and protocol summary
• Data generated in the S9 stability assay

Learn more about our 3D structural cardiotoxicity assay including:

• Background information 
• Assay details and protocol summary
• Data generated in the 3D structural cardiotoxicity assay

The ‘core’ metabolome of the Bacteroidetes genus Chitinophaga was recently discovered to consist of only seven metabolites. A structural relationship in terms of shared lipid moieties among four of them was postulated. Here, structure elucidation and characterization via ultra-high resolution mass spectrometry (UHR-MS) and nuclear magnetic resonance (NMR) spectroscopy of those four lipids (two lipoamino acids (LAAs), two lysophosphatidylethanolamines (LPEs)), as well as several other undescribed LAAs and N-acyl amino acids (NAAAs), identified during isolation were carried out. 

LEARN MORE

Earlier this year, Evotec hosted a complimentary webinar, ‘INDiGO-Select: profiling and selecting your optimal clinical development candidate’.

INDiGO-Select focuses on better understanding (or increasing the knowledge) of the lead molecule chemistry, its physical-chemistry properties and preclinical DMPK and safety profile, helping to minimise the risk of failure during transition into the subsequent development stages. Evotec’s Manager, Integrated Development Programmes, Sabrina Pagliarusco and Senior Scientific Project Leader, Federico Tosini, take the audience on a journey starting with the war on attrition and a deeper dive into the importance of having a well-designed approach to de-risking. A relatively small investment at the candidate selection stage allows early identification of potential developability liabilities and challenges which consequently allow for a quicker reaction, at a lower cost.

Evotec’s approach to integrated solutions in drug development – INDiGO-Select and INDiGO – are then highlighted. The INDiGO-Select package is never the same for the candidate as it depends on the data that is generated during the discovery phase. To identify any gaps and technical risks, the key areas of focus are the chemistry and pharmaceutical properties, DMPK, the PK/PD relationship and preliminary safety assessment. The next stage – INDiGO - then accelerates early drug candidates into the clinic by reducing time from nomination to regulatory submission. The advantage is that this program can be customised based on data generated during the select and be conducted at a unique site while integrated, so all actions can be performed under the same roof.

Two case studies that used the INDiGO-Select package are then highlighted. The first focuses on low bioavailability, where the client – a small Biotech – has a therapeutic target in neurodegenerative diseases. The activities performed and data presented highlight the impact that an INDiGO-Select model can have on the progress of IND-enabling activities. A second example looks at chemistry and preclinical PK variability. For this particular case study, the objective was to increase the knowledge on the candidate profile and its developability, reducing the risks of later failure in the full development phase. In this instance, the compound was characterised further and, thanks to the data generated, some potential issues were identified to be considered and monitored during the customised development phase.

Choosing the INDiGO-Select model has a number of benefits including enhanced quality of selected drug candidates, increased probability of success later in development and an overall reduction of development costs and project timelines.

Discover more about INDiGO-Select by streaming this insightful webinar from our experts now!

Date: 04th - 08th October 2021

Location: Virtual

Speaker: Chris Strock 

Talk Title: Enhancing Seizure Prediction:  Rat and Human MEA models offer complementary results

Learn more about SPS Annual Meeting & Exhibition

Reactive metabolites play a role in drug-induced toxicity. Early stage in vitro screening for electrophilic reactive metabolite formation involves the use of trapping agents such as glutathione (GSH) in the presence of a drug metabolising system.

In this poster, we focus on:

• the use of an alternative GSH trapping method using combined stable labelled GSH (GSH-¹³C₂,¹⁵N) with unlabelled GSH
• the advantages of the stable labelled GSH method over common approaches for the detection of GSH conjugation such as GSH neutral loss post acquisition
• analytical conditions including the HPLC and mass spectrometric methods 
• validation data for a set of literature compounds

Read our poster to learn more about our research!

LEARN MORE