DMPK

Removing road blocks to candidate selection

We are an experienced DMPK team taking projects from early stage to candidate selection and beyond using a wide range of in vitro ADME assays, Met ID and ex vivo bioanalysis. Tailored support is applied to every project to reflect current needs and we adapt to suit collaborator requirements. We work closely with other teams, sharing our skillset and furthering our combined knowledge.

In vitro

Kinetic solubility and phototoxicity screening by plate-based UV absorption
PAMPA
Cellular penetration by LCMS-MS
Plasma protein binding by equilibrium dialysis
Permeability assessments
- Caco-2 assays, bidirectional, plus and minus efflux inhibitors
- MDCK +/- MDR1
CYP inhibition by fluorescence and LCMS-MS, isoform profiling and time-dependent inhibition (TDI)
Microsomal clearance for CYP450 metabolism
- Microsomal UGT clearance assay also available
Microsomal binding
Glutathione conjugation
Hepatocyte clearance assay
Metabolite identification (Met ID)

In vivo

Design and management of outsourced studies
Bioanalysis of plasma and other biofluids
Tissue preparation and extraction for bioanalysis
Plasma and tissue biomarkers for PK/PD
- Including human samples
Pharmacokinetic evaluation and result reporting

Alternative applications - outside the box

Project X – compounds were highly bound to plasma, changed to using 10% plasma to differentiate between compounds and assist SAR
Project Y – chemical liability for direct glucuronidation so established microsomal UGT clearance assay to aid SAR
Project Z – compounds less potent in cell biology assays than predicted. A combination of cellular penetration studies and media stability analysis were used to explain the anomalous results

Meet our colleagues

Helen Cobb

Associate Principal Scientist, DMPK

Would you like to learn more?

For further information about partnering with Vernalis, or to find out more about our capabilities or career opportunities.

bd@vernalis.com hr@vernalis.com