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. This panel tests for inhibition of 8 CYP's (CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, and CYP3A4 (midazolam and testosterone)) using a dose response of 8 concentrations for test compounds.
No. of Assays on Panel:
8
Assays on Panel:
Family
CYP450
Name
CYP3A inhibition IC50 (HLM, testosterone substrate) - ES
Item
5266
Protein
CYP3A4
Organism
Human
Assay Sub Type
Enzymatic
Family
CYP450
Name
CYP3A inhibition IC50 (HLM, midazolam substrate) - ES
Item
5267
Protein
CYP3A4
Organism
Human
Assay Sub Type
Enzymatic
Family
CYP450
Name
CYP2C19 inhibition IC50 (HLM, omeprazole substrate) - ES
Item
5268
Protein
CYP2C19
Organism
Human
Assay Sub Type
Enzymatic
Family
CYP450
Name
CYP2D6 inhibition IC50 (HLM, dextromethorphan substrate) - ES
Item
5269
Protein
CYP2D6
Organism
Human
Assay Sub Type
Enzymatic
Family
CYP450
Name
CYP1A inhibition IC50 (HLM, phenacetin substrate) - ES
Item
5270
Protein
Organism
Human
Assay Sub Type
Enzymatic
Family
CYP450
Name
CYP2B6 inhibition IC50 (HLM, bupropion substrate) - ES
Item
5271
Protein
CYP2B6
Organism
Human
Assay Sub Type
Enzymatic
Family
CYP450
Name
CYP2C9 inhibition IC50 (HLM, diclofenac substrate) - ES
Item
5272
Protein
CYP2C9
Organism
Human
Assay Sub Type
Enzymatic
Family
CYP450
Name
CYP2C8 inhibition IC50 (HLM, amodiaquine substrate) - ES
Item
5273
Protein
CYP2C8
Organism
Human
Assay Sub Type
Enzymatic
Family:
CYP450
Organism:
Human
Construct Details:
Microsomes
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Enzymatic
Functional Mode:
Antagonist
Detection Method:
HPLC-MS/MS
Measured Response:
Peak Area Response
Testing Information
Test Concentration / Dose:
Assay is performed with multiple concentrations (0.03, 0.1, 0.3, 1, 3, 10, 30, and 100 µM) using 2 replicates
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:
Spain - Murcia
RELATED SOLUTIONS
CYP inhibition panel (HLM, package of 8 assays) - ES
Item: G393
Time-dependent CYP inhibition (HLM, package of 10 assays) - ES
Item: G397
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