In Vitro Pharmacokinetic Assays

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Services

• Determination of plasma protein binding rate Plasma stability tests Liver microsomal metabolism tests CYP450 inhibition tests CYP450 induction tests Metabolite speculation Metabolite identification Estimation of metabolic pathway Identification of metabolic pathway Transmembrane transport test Drug-drug interaction Metabolic phenotype research Hepatocyte metabolic stability tests

Evaluation performance

• Medicilon Preclinical Pharmacokinetics Department can complete nearly thousands of single pharmacokinetic researches in vitro every year.The research categories involve micromolecule drugs, bio-tech-based drugs and natural product drugs.

Software

• WinNolin and WastonLim are used for calculation and processing of pharmacokinetic research data and management of analytical laboratory.

FAQ

• What is in vitro ADME Study?

  • PPB(plasma protein-binding):3 concentrations (including effective concentrations),N=3, focusing on concentration dependence and species differences.

  • Metabolic stability/MetID (in vitro metabolism): Metabolic stability/ METID (in vitro metabolism): Focuses on species differences to provide a reference for PK/PD/Tox species selection in vivo

  • CYP inhibition (P450 inhibition): IC50 or Ki, 1A2,2B6,2C8,2C9,2C19, 2D6,3A4

  • CYP induction (P450 induction): human hepatocytes from 3 donors, mRNA expression and/or enzyme activity changes:1A2, 2B6, 3A4 (refer to FDA Guidances: DD2006 Draft and 2020 In vitro DDI for data analysis)

  • Reaction phenotyping: Identification of CYP/Non-CYP metabolic pathways

  • Caco-2: In vitro absorption model

  • Transporter substrate assessment & inhibition (Transporter study):

    (1) P-gp, BCRP

    (2) Liver transporters (OATP1B1, OATP1B3)

    (3) Kidney transporters (OAT1, POAT3, OCT2, MATE1, MATE2-K)

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