Admescope, a preclinical ADME-Tox contract research organization (CRO), has announced that their N-in-one in vitro cytochrome P450 (CYP) enzyme inhibition assay is now also available with human hepatocytes.
The assay is designed to help drug development companies to determine if a new chemical acts as an inhibitor towards CYP-enzymes, which may potentially lead to a toxic drug-drug interactions.
“A CYP inhibition assay conducted with human hepatocytes may provide a better model for predicting clinical interactions than liver microsomes. This becomes very beneficial especially towards the end of the drug discovery process, when there are only few potential compounds left.” Says Ari Tolonen, CEO at Admescope.
The robust N-in-one assay has previously been available with liver microsomes but has now also been successfully validated with human hepatocytes to meet the rising customer need effectively. The assay reveals inhibition towards seven major CYP enzymes, 1A2, 2B6, 2C8, 2C9, 2C19, 2D6 and 3A4, as IC50 values in a single assay making it very cost efficient. All the IC50 values are well in line with literature data for each enzyme. The samples are analysed with LC/MS/MS and the service is also available as a high throughput screening version with 1-2 concentrations.
“We can also perform the assay by using human plasma as a suspension medium. This will result in IC50 values without the need to correct them by plasma bound/unbound calculations, as well as it enables the usage of higher test concentrations for poorly soluble compounds.” Continues Dr Sanna-Mari Aatsinki, Head of Drug Interactions at Admescope.