분류 | 요소기술 |
---|---|
Physicochemical properties | Solubility (kinetic, thermodynamic) |
Chemical stability (Buffer, Biorelevant media) | |
Thermodynamic solubility | |
Permeability | PAMPA assay |
Caco-2 cells permeability | |
Protein binding | Plasma (Equilibrium dialysis, Ultrafiltration) |
Albumin, Alpha-glycoprotein (Equilibrium dialysis, Ultrafiltration) | |
Microsomal binding | |
Metabolism study | Plasma stability |
Microsomal stability | |
S9 stability | |
Hepatocyte stability | |
Metabolite profiling and Met ID (in vitro) | |
Metabolite profiling and Met ID (in vivo) | |
Reactive metabolite formation (GSH trapping) | |
CYP Phenotyping (CYP1A2, 2B6, 2C8, 2C9, 2C19, 2D6, 3A4/5) | |
UGT Phenotyping (UGT1A1, 1A3, 1A4, 1A6, 1A9, 2B7, 2B15) | |
Phenotyping_metabolite formation | |
Non-CYP (FMO, CES, NAT, SULT 외) | |
Transport study | ABC transport phenotyping (efflux transporters) |
SLC transport phenotyping (uptake transporters) | |
Peptide based uptake transport phenotyping (PEPT1/2, SMVT) | |
SLC transport phenotyping in Xenopus oocytes (OATPs, OATs, OCTs, MATEs) | |
Cryopreserved hepatocytes uptake | |
Hepatic excretion by Sandwich cultured hepatocytes | |
Enzyme Inhibition | CYP Inhibition (Screening, IC50 assay) |
CYP inhibition (Ki assay) | |
UGT Inhibition (Screening, IC50 assay) | |
UGT inhibition (Ki assay) | |
Time-Dependent Inhibition (IC50 shift assay) | |
Time-Dependent Inhibition (Ki and Kinact) | |
Transporter Inhibition | ABC transporter inhibition (efflux transporters_accumulation) |
ABC transporter inhibition (efflux transporters_bi-direction) | |
SLC transporter inhibition (uptake transporters) | |
Time-dependent inhibition of OATP, IC50 shift assay | |
Enzyme/Transporter Induction | Cell viability |
Transporter (CYPs, UGTs, Transporters) Induction | |
Enzyme activity in human hepatocytes | |
Enzyme Induction (EC50 assay) | |
BCS-Biowaiver | Solubility |
Chemical stability | |
Caco-2 cell permeability | |
Bioanalytical service | Method development |
Method validation | |
Sample analysis | |
PK analysis | |
- | Radiolabeled clinical ADME studies (Mass balance, Metabolite profiling & Identification) |
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