Inactive

PROJECT DETAILS Opti-DDI: Regulatory compliant transporter inhibition screen for CNT1, CNT2, CNT3, ENT1, ENT2 and ENT4. Goal: Assess inhibition activity of test article (TA) for each human transporter... PROJECT DETAILS Opti-DDI: Regulatory compliant transporter inhibition screen for CNT1, CNT2, CNT3, ENT1, ENT2 and ENT4. Goal: Assess inhibition activity of test article (TA) for each human transporter individually, using study designs in compliance with FDA recommendations. Validated test systems: CNT1, CNT2, CNT3, ENT1, ENT2 and ENT4: Probe substrate uptake in MDCK cells expressing the transporter of interest and MDCK control cells. Test system controls: Transport control: transport of validated probe substrate of each transporter, tested at one concentration below its Km value Inhibition control: % of inhibition by validated reference inhibitor of each transporter, tested at a concentration >=10x of its Ki/IC50 value Identity of the probe substrates and reference inhibitors and corresponding acceptance criteria for positive controls for each transporter are specified in protocol. TA is tested for potential transporter inhibition at three concentrations. All conditions are performed in triplicate; triplicate data points are used to generate a single result.