Quintara Discovery

HT-ADME Assays

In vitro assays to assess ADME properties of potential drug candidates is an essential part of early drug discovery to reduce the attrition rate throughout downstream development. High throughput of these assays is particularly beneficial considering the large number of new chemical entities that need to be screened. LC/MS/MS with its sensitivity, reliability and robustness, is the current workhorse for ADME screens but is limited by throughput.

The RapidFire-MS Platform significantly decreases the processing time compared to conventional MS-based technologies while providing accurate results for data-driven decision thus helping to streamline drug discovery workflow. Producing label-free data at a rapid rate, the RapidFire MS/MS system can now use the high-throughput, mass spectrometry based method to analyze in vitro ADME assays in a fraction of the time required for conventional HPLC mass spectrometry techniques.

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At Quintara Discovery, RapidFire-MS/MS technology has been successfully adapted to the following high-throughput ADME assays.

  • CYP450 Inhibition assays: IC50 determination for test compounds against CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6 and CYP3A4 (other isoforms are available)
  • Permeability assays: Permeability for test compounds with MDCK, Caco-2, MDCK-MDR1 assay systems for measuring permeation and efflux by transporters