CYP2C8 inhibition IC50 (HLM, amodiaquine substrate) - ES

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.

Family:

CYP450

Sub Family:

CYP2

Protein Name:

CYP2C8

Uniprot Number:

P10632

Gene Name:

CYP2C8

Gene ID:

1558

Gene Aliases:

CPC8

Organism:

Human

Construct Details:

Microsomes