ADME-PK Profiling

DP

 

We have a broad portfolio of in-vitro ADME assays, pharmacokinetics and bioanalytical services.

These assays offer you a biological characterization of your compounds in terms absorption, distribution metabolism and elimination. All these parameters influence the performance and pharmacological activity of a drug.

Draconis Pharma offers tailor-made batteries of in-vitro and in-vivo assays adapted to your specific drug discovery & development programs.

(for further information or specific requirements, please contact us)

IN-VITRO ADME

Absorption/Distribution
  • Compound permeability in Caco-2 cells
  • Pgp Efflux
  • Protein-binding (ultracentrifugation and rapid equilibrium dialysis)
  • Blood partition coefficients
Metabolism
  • Metabolic stability in microsomes (rat, mouse, human, etc). Half life determination
  • Identification of metabolites
  • Biological stability in plasma, serum and blood
  • Reactive metabolite detection (glutathione adducts)
CYP450
  • In-vitro CYP450 inhibition (1A2, 2C9, 2C19, 2D6 and 3A4). Determination of IC50
  • Mechanism-based inhibition (or time-dependent CYP450 inhibition)
  • Reactive metabolite detection
Bioanalysis:
  • UV/Fluorescence/UPLC-MS/MS

 

IN-VIVO ADME (Pharmacokinetics)

In-vivo assays
  • Single and repeated dose in several species (rat, mouse and guinea pig) and different routes of administration (po, iv, ip, sc, topical, infusion)
  • Tissue distribution studies
  • Blood-brain barrier penetration studies
  • PK/PD studies
Bioanalysis:
  • Quantitative measurement of compounds in biological fluids and tissues
  • Metabolite identification in biological samples
  • Pharmacokinetic analysis from preclinical studies (WinNonlin)
 
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