CYP3A inhibition (HLM, testosterone substrate) - US
OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
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:
CYP3
Protein Name:
CYP3A4
Uniprot Number:
P08684
Gene Name:
CYP3A4
Gene ID:
1576
Organism:
Human
Construct Details:
Microsomes
Tissue:
Liver
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Enzymatic
Functional Mode:
Antagonist
Detection Method:
HPLC-MS/MS
Measured Response:
Peak Area Response
Testing Information
Substrate:
50 µM Testosterone
Incubation:
5 min pre-incubation and 10 min with NADPH at 37°C
Test Sample Requirements:
Minimum for 1) Screen: 100 μl of 10 mM stock -OR- 1 to 2 mg (pre-weighed). 2) Dose Response: 250 μl of 10 mM stock -OR- 1.5 to 2 mg (pre-weighed).
Turnaround Time
Standard:
10 Business Days
Additional Information
Brand:
Cerep
Testing Location:
USA - St Charles, MO
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