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Updated: Jun 21, 2026
06:13
Stepwise Dosing Protocol for Increased Throughput in Label-Free Impedance-Based GPCR Assays
Published on: February 21, 2020
High-throughput pharmacokinetics: cassette dosing.
1Biomet Division, Glaxo Wellcome R&D, Hertfordshire, SG12 0DP, UK. MKB2621@glaxowellcome.co.uk
Current Opinion in Drug Discovery & Development
|August 4, 2009
Summary
Drug discovery now yields many compounds, necessitating faster pharmacokinetic analysis. Cassette dosing in preclinical studies improves efficiency and reduces animal use for better drug candidate selection.
Area of Science:
- Pharmacokinetics and Drug Discovery
- Preclinical Drug Development
Background:
- Technological advances increase the number of lead compounds in drug discovery.
- Traditional preclinical drug selection is time-consuming and resource-intensive.
Purpose of the Study:
- To address the need for higher-throughput pharmacokinetic (PK) methods.
- To enable rational decision-making for a large number of drug compounds.
Main Methods:
- Utilized cassette dosing, administering mixtures of compounds to single animals.
- Administered up to ten compounds per dose via intravenous or oral routes.
- Analyzed samples using mass spectrometry.
Main Results:
- Successfully increased throughput for determining pharmacokinetic parameters.
- Reduced animal usage, addressing ethical considerations.
- Demonstrated a viable method for evaluating multiple compounds simultaneously.
Conclusions:
- Cassette dosing is an effective strategy for accelerating preclinical drug optimization.
- This approach supports efficient selection of drug candidates with optimal properties.
- Higher-throughput PK analysis is crucial for modern drug discovery pipelines.
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