Our Cytochrome P450 (CYP) inhibition assay (IC50) services help to understand the properties of a New Chemical Entity's (NCE) drug-drug reaction. CYP P450 assay also aims to understand the drug's enzymatic conversion into one or more than one metabolite. The understanding of the metabolic pathway of the drug helps to assess the nature of the drug. CYP P450 inhibition data help medicinal chemists to enhance the properties of the drug and design strategies to investigate clinical DDI studies.
Our CYP Inhibition AssayP450 Services Include:
Cytochrome P450 (CYP) inhibition assay protocol (IC50)
| Test system | HLM probed with substrates specific for each isoform |
| Isoforms | 3A4, 2D6, 2C9, 1A2, 2C8, 2C19 and 2B6 |
| Test concentrations | 50 µM / IC50 concentrations |
| Incubation time | 10 min (3A4), 20 min (2D6, 2C9, 1A2, 2C8, 2C19, 2B6) |
| Test system | Human liver microsomes |
| Analysis | LC-MS/MS method |
| Deliverables | Percent inhibition and/or IC50 |
Cytochrome P450 time-dependent inhibition (kinact/KI)
| Design | Test compound pre-incubated in HLM probed with isoform-specific substrates to monitor the IC50 shift |
| Isoforms | 3A4, 2D6, 2C9, 2C19, 1A2 |
| Test concentrations | Compound dependent, six inactivator concentrations |
| Incubation time | 5 min with 6 pre-incubation time points |
| Test system | Human liver microsomes |
| Analysis | LC-MS/MS method |
| Deliverables | Percent inhibition, IC50, and IC50 shift |
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CYP Induction Study Protocol
| Test System | Cryopreserved inducible human hepatocytes |
| Method | mRNA estimation |
| Test concentrations | 50, 30 & 10µM |
| Incubation time | 72 hours with daily dosing |
| Test system | Plateable human hepatocytes |
| Deliverables | Fold Induction and/ or % induction with respect to positive control |
CYP Phenotyping Study
- Test System: Human recombinant CYPs
- Relative contribution of individual CYP isoforms to the metabolism of the parent compound estimated
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