Discovery Screening

QPS offers discovery screening as part of the drug candidate selection process. Discovery screen studies have rapid turnaround, require only small amounts of compound and provide timely feedback to the discovery chemist on structural activity relationships. A typical discovery screen may include:

 

  • Rodent pharmacokinetics in N-in-1 or discrete format

    • Single IV and PO dose to determine Cmax, Tmax, t½, and bioavailability

    • Allows chemical leads to be rank-ordered to optimize PK properties

  • Plasma protein binding in one rodent and one non-rodent species

    • Utilizing ultrafiltration or equilibrium dialysis

    • Determines the extent of binding to plasma proteins

  • In vitro cytochrome P540 (CYP450) inhibition in human liver microsomes

    • Utilizing CYP specific substrates to determine potential of lead structures to inhibit activity of human liver CYPs

    • Determines potential for metabolism-based drug-drug interactions

  • Preliminary assessment of formulations

    • Single oral dose of compound formulated in pharmaceutically acceptable vehicles

    • Helps eliminate chemical structures that may be difficult to formulate for oral dosage form