The continued importance of early ADME-Tox testing of lead compounds was the theme of the 16th North American Regional ISSX meeting. While much emphasis continued to be placed on testing for drug-drug interactions with cytochrome P450 enzymes, the most important family of primary metabolic enzymes, it was also pointed out that drug-drug interactions with transporter enzymes can also cause safety concerns with lead compounds. A large portion of a number of podium presentations concentrated on the importance of transporter enzymes in the distribution and elimination of compounds from the body. This was further emphasized by the FDA during their presentation on regulation of drug safety testing.
While LC/MS/MS is still an important readout for transporter enzyme assays, other detection methods suitable for microplate assays are coming to the fore which can use ubiquitous inexpensive detection instruments. An example of this is Solvo Biotechnology‘s P-gp PREDIVEZ Vesicular Transport Assay Kit, which uses fluorescent substrates to monitor activity and inhibition of this important efflux transporter enzyme.
BioTek plans to partner with reagent vendors such a Solvo, to demonstrate the automation and detection of these, and other ADME-Tox assay chemistries. This was demonstrated at the recent ISSX conference, where we presented two posters showing the automation and detection of luminescent primary and secondary metabolic enzyme assays.
What areas of ADME-Tox research do you feel will be important for drug safety testing? What throughput needs do you have to test the ADME-Tox properties of your lead compounds? How can BioTek help you to make this area of drug discovery easier, faster, and more reproducible?
By, BioTek Instruments