DMPK

Our In Vitro DMPK Capabilities

1. Metabolic Stability Studies

  • Evaluate the metabolic half-life of drug candidates in liver microsomes, S9 fractions, and hepatocytes from multiple species (human, rodent, non-human primates, etc.).
  • Measure intrinsic clearance and identify potential metabolic liabilities.
2. CYP450 Inhibition & Induction Assays
  • Assess the potential for drug-drug interactions (DDIs) by determining inhibition of major cytochrome P450 (CYP) enzymes (CYP1A2, 2C9, 2C19, 2D6, 3A4, etc.).
3. Plasma Protein Binding (PPB)
  • Determine the extent of drug binding to plasma proteins (e.g., albumin, α1-acid glycoprotein) using equilibrium dialysis, ultrafiltration, or ultracentrifugation methods.
  • Species-specific plasma binding studies for human, rat, dog, and non-human primates.
4. Blood-to-Plasma Partitioning
  • Evaluate drug distribution between red blood cells and plasma to assess compound pharmacokinetics and tissue exposure.
5. Metabolite Identification and Profiling
  • Identify and characterize drug metabolites using LC-MS/MS and high-resolution mass spectrometry (HRMS).
  • Assess metabolite formation pathways and potential active/inactive metabolites.
 
 

6. Drug Permeability & Transporter Studies

  • Caco-2 & MDCK Cell Permeability Assays: Evaluate passive and active transport across biological membranes.
  • P-glycoprotein (P-gp) & BCRP Efflux Assays: Determine interactions with efflux transporters using bidirectional permeability studies.
  • OATP, OAT, OCT Transporter Assays: Assess uptake and efflux of compounds via key transporters relevant for drug absorption and distribution.
7. Drug Stability & Solubility Assessment
  • Evaluate compound solubility in various media (PBS, simulated gastric/intestinal fluids).
  • Assess chemical and enzymatic stability in simulated gastric/intestinal fluids and biological matrices (plasma, microsomes).
8. Customized DMPK Study Designs
  • Tailored study designs to fit specific compound requirements.
  • Regulatory-compliant (GLP and non-GLP) workflows available for early drug development and IND-enabling studies.