| 대분류 | 소분류 | 요소기술 |
|---|---|---|
| Permeability | Drug absorption | Caco-2 cells Permeability Assay |
| 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 |
| S9 stability assay | ||
| Hepatocyte stability assay | ||
| Plasma stability | ||
| Species comparison (mouse, rat, dog, monkey, human) | ||
| Reaction phenotyping | Phase I (CYP1A2, 2B6, 2C8, 2C9, 2C19, 2D6, 3A4, 3A5 etc.) | |
| Phase II (UGT1A1, 1A3, 1A4, 1A6, 1A9, 2B7, 2B15) | ||
| Phase I (Non-CYPs, FMO, CES, MAO etc.) | ||
| Enzyme systems in the test (Recombinant enzymes, Microsomes, S9, Hepatocytes) | ||
| Kinetic studies (Km, Vmax, intrinsic clearance) | ||
| 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) |
| Efflux transport screening in overexpressing cells (P-gp, BCRP, MRP1, MRP2) | ||
| Cryopresesrved hepatocytes uptake | ||
| Kinetic studies (Km, Vmax, intrinsic clearance) | ||
| 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) |
| UGT inhibition assay (IC50) | ||
| Cytochrome P450 Inhibition Ki assay | ||
| Time-dependent inhibition | Cytochrome P450 (CYP) time dependent inhibition (single point) assay | |
| Cytochrome P450 time dependent inhibition (IC50 shift) assay | ||
| Cytochrome P450 time dependent inhibition (kinact/KI) assay | ||
| GSH conjugate (reactive metabolite) | ||
| Transporter inhibition | P-glycoprotein and BCRP Inhibition assay | |
| BSEP, MRP1, MRP2 Inhibition assay | ||
| Uptake transport inhibition in overexpressing cells or oocytes (OCTs, OATs, OATPs, NTCP) | ||
| Induction | mRNA expression level in human hepatocytes (CYPs, UGTs, Transporters) | |
| CYP activity in human hepatocytes | ||
| 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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