INTRODUCTION
Absorption, Distribution, Metabolism, Excretion 분석을 통해 약물의 안정성을 평가할 수 있는 서비스입니다.
Assay 종류 및 평가항목
A. Bioavailability: 약물이 체내 순환에 들어가는 속도와 그 정도를 측정
- Compound Solubility
- Protein binding
- Absorption and Permeability
- Partition Coefficient
- Blood Partitioning
- Bioavailability Panel: in vivo oral absorption을 예측할 수 있는 key in vitro assay
B. Drug Metabolism: 약물의 효능과 안정성 평가
- Metabolic Stability (Intrinsic Clearance): Liver S9, Liver Microsomes, Hepatocyte, Intestine (S9 and Microsomes)
- Compound Stability in Blood and Plasma
- CYP450 Inhibition & Time-Dependent Inhibition (TDI)
- CYP450 Phenotyping
- CYP450 Induction: mRNA levels and Enzyme activity
- PXR, CAR, and AhR, Nuclear Receptor Activation Assays
- UGT Inhibition & Phenotyping
- Glutathione and Glucuronide Conjugation
- Bioanalytical Services: Linearity, Quantitative Bioanalysis
- Metabolite Identification and Profiling
C. Transporter: ABC transporters & SLS transporter와 약물의 상호작용 측정
- Drug Substrate Assessment
- Drug Inhibition Assessment
D. Toxicology: 낮은 ADME/PK 활성과 관련된 약물독성 관찰
- Genotoxicity: Ames test and Fluctuation Assays
- Hepatoxicity
- Cardiotoxicity
- Cytotoxicity
- Nephrotoxicity
- Custom and Specialty Toxicity
Tier 1 ADME Panel Assay
신약 개발에서 올바른 PK profile을 보이는 후보 약물을 선별하는데 필수적인 요소 (solubility, permeability, protein binding, intrinsic clearance, lipophilicity) 들로 구성되어 화합물의 특성을 빠르게 확인할 수 있는 Panel assay입니다.
NAME | ITEM # |
Aqueous solubility (simulated gastric fluid) | 2061 |
Aqueous solubility (simulated intestinal fluid) | 2062 |
Protein binding (plasma, human) | 2194 |
A-B permeability (Caco-2, pH 6.5/7.4) | 3318 |
B-A permeability (Caco-2, pH 6.5/7.4) | 3320 |
Partition coefficient (log D, n-octanol/PBS, pH 7.4) | 417 |
Aqueous solubility (PBS, pH 7.4) | 435 |
Intrinsic clearance (liver microsomes- human) | 607 |
Tier 2 ADME Panel Assay
Tier 2 ADME Panel은 IND-enabling assay로서 lead compound을 임상적으로 사용하는데 필요한 데이터 (CYP inhibition, CYP phenotyping, CYP induction, transporter substrate/inhibition assay)를 생성하는 Assay로 구성되어 있습니다.
NAME | ITEM # |
CYP Inhibition (HLM:package of 8 CYP assays) | G232 |
Time Dependent CYP Inhibition Panel (HLM; package of 10 assays) | G234 |
CYP Phenotyping Panel | G230 |
CYP Induction Panel (human hepatocytes, mRNA level, 3 donors) | G345 |
P-gp substrate assessment (Caco-2) | G206 |
BCRP substrate assessment (Caco-2) | G330 |
Transporter Inhibition Panel | G346 |
서비스 절차
서비스 문의