Pharmacology and DMPK

ADME-PK and preformulation

Design, make, test and analyze cycle support

The DMPK team has extensive pharma and biotech experience delivering high-quality data, helping medicinal chemists design better compounds, and supporting better decisions throughout drug discovery. From the hit-to-lead through lead optimization, DMPK parameters help direct resources to the most promising chemical series and ensure the selection of the drug candidate.

Our comprehensive portfolio includes in vitro, and in vivo tests coupled with analytical techniques. We tailor flexible DMPK screening cascades specifically designed to boost medicinal chemistry programs, including the development of customized methods.

Absorption

  • Chrom LogD
  • LogD / LogP
  • pKa
  • Solubility (kinetic) (by LC-UV)
  • Solubility (thermodynamic)
  • Chemical stability
  • Caco2

Distribution

  • Plasma protein binding
  • Blood plasma partitioning
  • Tissue binding

Metabolism

  • Microsomes
  • Hepatocytes
  • Long Term plated Hepatocytes
  • Metabolite ID (microsomes/hepatocytes)

Drug drug interaction

  • CYP inhibition
  • CYP3A Time Dependent Inhibition (development ongoing)

Excretion

  • Determination of excretion route (rat PK -urine, faeces, bile)

in vivo pharmacokinetics

  • Administration routes: intravenous, per os (PO), intra-peritoneal, subcutaneous
  • Matrices: blood, plasma, bile, urine, faeces, tissues and tumor

Preformulation

Developing an appropriate formulation is key to maximize in vivo exposure of therapeutics, the dedicated formulation team can perform the following studies:

  • Design of a stable non-precipitating solution
  • Early formulation development
  • Advanced formulation for poorly soluble compounds
  • Batch analysis and control
  • Physicochemical properties of compounds

The data generated can help to better understand SAR as well as ADME and PK properties.

Our teams can work on small quantities to support early discovery projects.