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In Vitro Study for CYP450 Enzyme Induction

In Vitro Study for CYP450 Enzyme Induction

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021-50800743

Enzyme induction test was conducted to evaluate whether the tested product had a potential induction effect on liver drug metabolism of CYP450 subenzyme or UGT enzyme from the level of enzyme activity or mRNA expression, to understand its potential DDI risk, and to provide parameters for PBPK modeling and reference for subsequent clinical drug combination.

Incubation system 

Attached primary liver cells                                                                                                                   

Species

Man

Tested enzymes

CYP450 enzymes: CYP1A2, 2B6, 2C8, 2C9, 2C19 and 3A, etc

Test concentration of the sample

1-6, which is designed according to the drug efficacy and toxicity data of the customer

Cell density

0.7×106 cells/mL

Incubation time

2-4 days (can be adjusted according to different requirements)

Analytical method

LC-MS/MS

microcoder

RT-PCR instrument

Evaluation index

enzyme activity

mRNA

Data presentation

Relative activity (% of VC)

Relative positive control activity (%)

Proportion of mRNA increase relative to positive control group (% of PC)

The concentration of EC50 for half of the maximum induction effect in vitro

Maximum induction effect Emax in vitro


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