CYP INHIBITION

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Detailed CYP inhibition profiles are now required for the registration of novel molecular entities. 

Inhibition of individual CYPs by your discovery compounds can be assessed either by liver microsomes or recombinant CYP preparations, in combination with specific probe substrates. 

As a reliable and cost-effective initial screening we recommend to assess inhibition potencies against the 7 most relevant CYP isoforms, i.e. CYP1A2, 2B6, 2C8, 2C9, 2C19, 2D6 and 3A4.

CYP Inhibition Assay Protocol:

Test article concentration: 30,10, 3.3, 1.1, 0.37, 0.12, 0.041 and 0 µM (other upon request) 

Incubation time: 5 to 45 minutes as per the isoform 

Incubation temperature: 37 C 

Number of Replicates: n = 2  

Assay condition: Phosphate buffer 

Assay matrix: CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6 and CYP3A4   (other isoforms are available) 

Controls: Known isoform specific inhibitors 

Analysis Method: LC/MS/MS 

Data Delivery: IC50