ADME

ADME (Absorption, Distribution, Metabolism, and Excretion) studies are conducted during the early discovery, lead optimisation, and preclinical development phases. These testing results are to provide information for characterisation and ranking of the compounds based on their properties, and to predict their fate after administration into the human body. At clinical development, the same information related to pharmacokinetics (PK) and pharmacodynamics (PD), is collected to enable and confirm effective use of the candidate drugs.

In the lead optimization or ADME predication stage of a drug-discovery program, comprehensive in vitro ADME profiling needs to be complimented with animal experiments to provide deeper insights into drug metabolism and pharmacokinetics (DMPK). All of the ADME screening and properties validation services in our experimental platform include metabolic profiling, stability, metabolite identification, bioavailability screens, CYP450 inhibition and induction assays, drug-drug-interactions, quantitative bioanalysis, drug transporters, etc.

In vitro ADME and DMPK Services
in vitro metabolism
  • Cytochrome P450 and UGT Reaction Phenotyping
  • Cytochrome P450 Induction
  • Cytochrome P450 Inhibition
  • Cytochrome P450 Ki
  • Hepatocyte Stability
  • Low Clearance HµREL Co-culture Assay
  • Low Clearance Hepatocyte Stability
  • Hepatic Uptake
  • Metabolite Profiling and Identification
  • Microsomal Binding
  • Microsomal Stability
  • Plasma Stability
  • PXR and AhR Nuclear Receptor Activation
  • S9 Stability
  • Time Dependent Inhibition (IC50 Shift)
  • Time Dependent Inhibition (kinact/KI )
  • Time Dependent Inhibition (single point)
  • UGT Inhibition
  • Monoamine Oxidase Inhibition
  • Monoamine Oxidase Reaction Phenotyping
  • Carboxylesterase Inhibition
  • Carboxylesterase Reaction Phenotyping
  • Aldehyde Oxidase Reaction Phenotyping
In vitro ADME and DMPK Services
in vitro permeability and transporters
  • PAMPA
  • Caco-2 Permeability
  • MDCK-MDR1 Permeability
  • P-gp Substrate Identification
  • BCRP Substrate Identification
  • Human SLC Transporter Substrate Identification
  • Human MRP Transporter Substrate Identification
  • Preclinical Hepatic Oatp Uptake Transporter Substrate Identification
  • P-gp Inhibition
  • BCRP Inhibition
  • Human SLC Transporter Inhibition
  • BSEP and MRP Inhibition
  • Preclinical Hepatic Oatp Uptake Transporter Inhibition
  • Other transporter assays
physico-chemical property measurements
  • pH/Solubility Profiling
  • Compound Stability
  • Log D
in vitro protein binding
  • Brain Tissue Binding
  • Plasma Protein Binding
  • Whole Blood Binding
  • Blood to Plasma Ratio

Our instrument and detective systems include SFC, HPLC, RP LC, UPC^2, UPLC, GC, ELSD, MS, CAD Detection, PDA/UV, NMR, Accurate Mass MS, etc. ADME services provided by MedAI maintain and comply with regulatory guidelines, providing constant confidence in the data. We are focusing on offering cost-effective, high-quality, reproducible data and flexible solutions with fast turnaround times. Be our partner to advance your drug discovery and development projects.

Online Inquiry

Please submit a detailed description of your project. We will provide you with a customized project plan to meet your research requests. You can also send emails directly to inquiry@protheragen.com for inquiries.

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