Cytochrome P450s (CYPs) and other enzymes metabolize the majority of therapeutic drugs. Changes in the disposition of these enzymes can alter the ADME (absorption, distribution, metabolism, and excretion) properties of drugs. In addition, co-administered drugs can lead to ineffective therapies if the drug-drug interactions (DDI) increase the rate of metabolic clearance of either drug. In order to assess the potential for loss of drug efficacy, ADME/DMPK (Drug Metabolism and Pharmacokinetics) researchers measure induction of genes for drug metabolizing enzymes such as CYPs to support drug discovery programs. A common methodology used is to determine CYP induction via mRNA expression and CYP enzyme activity using cryopreserved human hepatocytes.
QuantiGene Assays enable ADME/DMPK/Toxicology researchers to:
- Use hepatocytes more efficiently to measure gene expression for multiple drug metabolizing or transporting enzymes in the same well
- Obtain data on targets when a substrate assay is not available
- Follow the 2017 FDA draft guidance on in vitro Metabolism- and Transporter-Mediated Drug-Drug Interaction Studies by using mRNA level as an endpoint[1]
Figure 1. Omeprazole concentration response curves and EC50 values for various ADME genes.
Multiplex ADME/Tox gene expression panel
The QuantiGene Plex ADME Panel targets 50 genes for various phase I and II metabolizing enzymes and phase III transporters, and includes 8 Reference genes. This panel is compatible with all Luminex instruments.
| Accession | Gene Name | Symbol |
|---|---|---|
| NM_019093 | UDP glycosyltransferase 1 family, polypeptide A3 | UGT1A3 |
| NM_000341 | solute carrier family 3 (cystine, dibasic and neutral amino acid transporters, activator of cystine, dibasic and neutral amino acid transport), member 1 | SLC3A1 |
| NM_006446 | solute carrier organic anion transporter family, member 1B1 | SLCO1B1 |
| NM_000106 | cytochrome P450, family 2, subfamily D, polypeptide 6 | CYP2D6 |
| NM_001461 | flavin containing monooxygenase 5 | FMO5 |
| NM_003167 | sulfotransferase family, cytosolic, 2A, dehydroepiandrosterone (DHEA) -preferring, member 1 | SULT2A1 |
| NM_002046 | glyceraldehyde-3-phosphate dehydrogenase | GAPDH |
| NM_001101 | actin, beta | ACTB |
| NM_000379 | xanthine dehydrogenase | XDH |
| NM_017460 | cytochrome P450, family 3, subfamily A, polypeptide 4 | CYP3A4 |
| NM_000463 | UDP glycosyltransferase 1 family, polypeptide A1 | UGT1A1 |
| NM_000181 | Glucuronidase, beta | GUSB |
| NM_001159 | aldehyde oxidase 1 | AOX1 |
| NM_000773 | cytochrome P450, family 2, subfamily E, polypeptide 1 | CYP2E1 |
| NM_003742 | ATP-binding cassette, sub-family B (MDR/TAP), member 11 | ABCB11 |
| NM_000291 | phosphoglycerate kinase 1 | PGK1 |
| NM_000767 | cytochrome P450, family 2, subfamily B, polypeptide 6 | CYP2B6 |
| NM_003057 | solute carrier family 22 (organic cation transporter), member 1 | SLC22A1 |
| NM_003194 | TATA box binding protein | TBP |
| NM_002021 | flavin containing monooxygenase 1 | FMO1 |
| NM_007120 | UDP glycosyltransferase 1 family, polypeptide A4 | UGT1A4 |
| NM_004827 | ATP-binding cassette, sub-family G (WHITE), member 2 | ABCG2 |
| NM_000770 | cytochrome P450, family 2, subfamily C, polypeptide 8 | CYP2C8 |
| NM_000762 | cytochrome P450, family 2, subfamily A, polypeptide 6 | CYP2A6 |
| NM_000937 | polymerase (RNA) II (DNA directed) polypeptide A, 220kDa | POLR2A |
| NM_000761 | cytochrome P450, family 1, subfamily A, polypeptide 2 | CYP1A2 |
| NM_001074 | UDP glycosyltransferase 2 family, polypeptide B7 | UGT2B7 |
| NM_000769 | cytochrome P450, family 2, subfamily C, polypeptide 19 | CYP2C19 |
| NM_001076 | UDP glycosyltransferase 2 family, polypeptide B15 | UGT2B15 |
| NM_021027 | UDP glycosyltransferase 1 family, polypeptide A9 | UGT1A9 |
| NM_005502 | ATP-binding cassette, sub-family A (ABC1), member 1 | ABCA1 |
| NM_000775 | cytochrome P450, family 2, subfamily J, polypeptide 2 | CYP2J2 |
| NM_004605 | sulfotransferase family, cytosolic, 2B, member 1 | SULT2B1 |
| NM_007256 | solute carrier organic anion transporter family, member 2B1 | SLCO2B1 |
| NM_000194 | Hypoxanthine phosphoribosyltransferase 1 | HPRT1 |
| NM_004996 | ATP-binding cassette, sub-family C (CFTR/MRP), member 1 | ABCC1 |
| NM_000898 | monoamine oxidase B | MAOB |
| NM_000777 | cytochrome P450, family 3, subfamily A, polypeptide 5 | CYP3A5 |
| NM_001055 | sulfotransferase family, cytosolic, 1A, phenol-preferring, member 1 | SULT1A1 |
| NM_000771 | cytochrome P450, family 2, subfamily C, polypeptide 9 | CYP2C9 |
| NM_006894 | flavin containing monooxygenase 3 | FMO3 |
| NM_001072 | UDP glycosyltransferase 1 family, polypeptide A6 | UGT1A6 |
| NM_000499 | cytochrome P450, family 1, subfamily A, polypeptide 1 | CYP1A1 |
| NM_019844 | solute carrier organic anion transporter family, member 1B3 | SLCO1B3 |
| NM_000240 | monoamine oxidase A | MAOA |
| NM_000942 | peptidylprolyl isomerase B (cyclophilin B) | PPIB |
| NM_000392 | ATP-binding cassette, sub-family C (CFTR/MRP), member 2 | ABCC2 |
| NM_006516 | solute carrier family 2 (facilitated glucose transporter), member 1 | SLC2A1 |
| NM_003049 | solute carrier family 10 (sodium/bile acid cotransporter family), member 1 | SLC10A1 |
| NM_000927 | ATP-binding cassette, sub-family B (MDR/TAP), member 1 | ABCB1 |
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For Research Use Only. Not for use in diagnostic procedures.