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In vitro ADME
- Assay optimisation and validation based on sponsors’ needs
- Quality assurance norms to ensure data robustness
- Standardised assays available today –
- Solubility Assay: Kinetic, Equilibrium
- Chemical Stability: in PBS, in SGF, in SIF and T1/2 in PBS
- Partition Coefficient: Log P (Octanol/water or buffer),
Log D (Octanol/PBS),
Log D (Cyclohexane/PBS)
- Plasma Protein Binding and stability Assay: Plasma Binding,
Plasma Stability,
HSA Binding and
AGP Binding
- Metabolic stability Assay: Human Liver Microsome (HLM),
Rat Liver Homogenate (RLH) and
Rat Liver Microsome (RLM)
- Metabolic stability in Rec. Human CYPs: 1A1, 1A2, 2B6, 2C8, 2C18, 2C9, 2D6, 2E1, 3A4 and 3A5
- CYP Inhibition assay (fluorimetry): RLM, inhibitor and EFC/CEC/CMC/multiple
- Rec. Human CYP Inhibition Assay (fluorimetry): 1A1, 1A2, 2B6, 2C8, 2C18, 2C9, 2D6, 2E1, 3A4 and 3A5 with CEC/EFC/BFC substrate
- Permeability assays: PAMPA,
pH-PAMPA and
Caco-2
- Cytotoxicity Assay Panel: List of Cancer cell lines, Anti-proliferation – MTT,
DNA-synthesis inhibition – [3H]-Thymidine uptake,
Cytotoxicity – LDH release and
Protein synthesis inhibition – [14C]-Methionine uptake
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