CYP2A6 inhibition (HLM, coumarin substrate) - US

Background Information:

Cytochrome P450 (CYP) inhibition is one of the most common types of drug-drug interactions (DDI). When a drug inhibits a specific CYP isoform, it will reduce the metabolic activity toward a concomitant drug that is metabolized by this inhibited CYP isoform, resulting in the increase in the bioavailability of the victim drug, often to a point that toxicity is induced. Regulatory agencies have issued guidances recommending that all new molecular entity (NME) be screened for CYP inhibition liability, especially for CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, and CYP3A4. Eurofins can determine inhibition of the major CYP enzymes using drug substrates in human liver microsomes or with fluorescent substrates and recombinant human CYP enzymes.

Family:

CYP450

Sub Family:

CYP2

Protein Name:

CYP2A6

Uniprot Number:

P11509

Gene Name:

CYP2A6

Gene ID:

1548

Gene Aliases:

CPA6|CYP2A

Organism:

Human

Construct Details:

Microsomes

Tissue:

Liver