Permeability | Drug absorption | |
Caco-2 cells Permeability Assay |
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Parallel artificial membrane permeability assay (PAMPA) |
Hepatic excretion | |
Sandwich cultured hepatocytes |
Plasma protein binding | Protein binding | |
Plasma protein binding assay (Equilibrium dialysis) |
Drug metabollism | Metabolic stabililty | |
Microsomal stability assay |
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S9 stability assay |
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Hepatocyte stability assay |
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Plasma stability |
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Species comparison (mouse, rat, dog, monkey, human) |
Reaction phenotyping | |
Phase I (CYP1A2, 2B6, 2C8, 2C9, 2C19, 2D6, 3A4, 3A5 etc.) |
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Phase II (UGT1A1, 1A3, 1A4, 1A6, 1A9, 2B7, 2B15) |
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Phase I (Non-CYPs, FMO, CES, MAO etc.) |
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Enzyme systems in the test (Recombinant enzymes, Microsomes, S9, Hepatocytes) |
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Kinetic studies (Km, Vmax, intrinsic clearance) |
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Pharmocogenetics study (CYP2C19*10, 2D6*10B, 4F2*3) |
Met ID | |
Metabolites profiling and Met ID |
Drug transporters | Transporter substrate identification | |
Uptake transport screening in overexpressing cells or oocytes (OCTs, OATs, OATPs, MATEs) |
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Efflux transport screening in overexpressing cells (P-gp, BCRP, MRP1, MRP2) |
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Cryopresesrved hepatocytes uptake |
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Kinetic studies (Km, Vmax, intrinsic clearance) |
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Pharmacogenetics study (OCT2 A270S, OATP1B1*15, NTCP*2, MDR1 G2677T/A, BCRP Q141K) |
Drug-Drug interaction | Metabolizing enzyme inhibition | |
Cytochrome P450 (CYP) inhibition assay (IC50) |
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UGT inhibition assay (IC50) |
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Cytochrome P450 Inhibition Ki assay |
Time-dependent inhibition | |
Cytochrome P450 (CYP) time dependent inhibition (single point) assay |
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Cytochrome P450 time dependent inhibition (IC50 shift) assay |
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Cytochrome P450 time dependent inhibition (kinact/KI) assay |
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GSH conjugate (reactive metabolite) |
Transporter inhibition | |
P-glycoprotein and BCRP Inhibition assay |
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BSEP, MRP1, MRP2 Inhibition assay |
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Uptake transport inhibition in overexpressing cells or oocytes (OCTs, OATs, OATPs, NTCP) |
Induction | |
mRNA expression level in human hepatocytes (CYPs, UGTs, Transporters) |
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CYP activity in human hepatocytes |
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Reporter assay (PXR) |
In vitro to in vivo Extrapolation | |
IVIVE prediction |
Preclinical study | Linearity / Bioavailability | |
IV/Oral administration PK |
Mass balance | |
Radio-labeled compound PK |
Distribution | |
Tissue distribution (brain, liver, kidney...) |
Met ID | |
Metabolites profiling and Met ID |
Billiary /Renal excretion | |
Bile cannulation |
Bioanalytical services |
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