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ADME & Toxicology 서비스

Absorption, Distribution, Metabolism, Excretion 분석을 통해 약물의 안정성을 평가할 수 있는 서비스

 

| Eurofins DiscoverX(Eurofins Discovery) 공식 대리점 

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

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