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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 |