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High throughput physicochemical profiling for drug discovery.

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

Journal of Pharmaceutical Sciences

|December 18, 2001

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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.