ADME-Tox screening in human models using TRAC

TRAC offers multiplex gene expression analysis with high sample throughput, making it ideal for screening applications in pre-clinical drug testing. We also have a range of pre-validated panels for ADME-Tox screening, making it fast and simple for you to start screening your drug compounds right away.

In the example below, TRAC was used to investigate cytochrome P450 expression in primary hepatocytes in response to drug treatments.

Human cytochrome P450 expression screening in primary hepatocytes

The cytochrome P450 superfamily (CYP) are the major enzymes involved in drug metabolism. Better understanding of CYP expression and activity helps to predict the toxicity and metabolism of drugs in the early stages of drug development. Therefore, CYP analysis in cultured primary hepatocytes is commonly used in preclinical pharmacological studies.

In this study, TRAC was used to analyze the expression of ten CYP genes from primary hepatocytes obtained from three donors. RT-qPCR was also performed to validate the assay. The cells were exposed to a range of treatments in DMSO, including the known CYP450 inducers rifampicin (RIF), phenobarbital (PB) and omeprazole (OME). The results for two of these genes and a subset of the treatments are shown below.

Human data

Conclusions

This experiment showed that TRAC can be used to analyze crude lysates of primary hepatocytes in 96-well plates. The results correlated strongly with RT-qPCR data, while offering lower error rates. The TRAC approach also saved significant time and reagent use compared to RT-qPCR.