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Related Experiment Videos

High throughput physicochemical profiling for drug discovery.

E H Kerns1

  • 1Wyeth-Ayerst Research, Princeton, New Jersey 08543-8000, USA. kernse@war.wyeth.com

Journal of Pharmaceutical Sciences
|December 18, 2001
PubMed
Summary
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Drug candidate profiling using physicochemical and physiological properties accelerates selection and optimization. High-throughput methods for solubility, permeability, and stability assessment are discussed to reduce drug development time and attrition.

Area of Science:

  • Drug Discovery and Development
  • Pharmaceutical Sciences
  • Medicinal Chemistry

Background:

  • Drug development faces significant attrition and lengthy timelines.
  • Early assessment of drug candidate properties is crucial for success.
  • Integrating property profiling with activity screening streamlines the process.

Purpose of the Study:

  • To address drug development bottlenecks by profiling physicochemical and physiological properties early.
  • To present and compare high-throughput methods for essential drug property assessment.
  • To discuss the strategic application of these methods in drug discovery.

Main Methods:

  • High-throughput screening assays for solubility.
  • Permeability assays (e.g., Caco-2, PAMPA).

Related Experiment Videos

  • Lipophilicity (logP/logD) determination.
  • pKa measurement techniques.
  • Stability and integrity testing (chemical and metabolic).

    • Main Results:

    • Detailed comparison of various high-throughput methods for key drug properties.
    • Demonstration of how property profiling aids in candidate selection and optimization.
    • Insights into the application strategies for integrating property data into discovery workflows.

    Conclusions:

    • Early and efficient measurement of drug properties is vital for successful drug development.
    • High-throughput methods enable parallel assessment of activity and pharmaceutical properties.
    • Strategic implementation of property profiling reduces attrition and development time.