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Pharmacokinetics in drug discovery.
Ana Ruiz-Garcia1, Marival Bermejo, Aaron Moss
1Pharmacokinetics and Drug Metabolism, Amgen, Inc, 1201 Amgen Court West, Seattle, Washington 98119, USA. anruiz@amgen.com
Journal of Pharmaceutical Sciences
|July 17, 2007
Summary
This review covers pharmacokinetics (PK) in drug discovery, detailing LADMET properties and assessment methods. Early application of preclinical assays is crucial for discovering safe, effective therapeutics efficiently.
Area of Science:
- Pharmacology
- Drug Discovery
- Toxicology
Background:
- Pharmacokinetics (PK) is essential for drug discovery, encompassing Liberation, Absorption, Distribution, Metabolism, Excretion, and Toxicity (LADMET).
- Understanding PK profiles early is critical for successful drug development.
- This review synthesizes current knowledge on PK in the drug discovery pipeline.
Purpose of the Study:
- To provide a comprehensive overview of pharmacokinetics in drug discovery.
- To review computational (in silico), in vitro, and in vivo methodologies for PK assessment.
- To discuss mathematical approaches for establishing pharmacokinetic profiles.
Main Methods:
- Literature review of pharmacokinetics in drug discovery.
- Overview of LADMET properties and their significance.
- Discussion of computational, in vitro, and in vivo methods for PK evaluation.
- Analysis of mathematical models for PK profiling.
Main Results:
- Pharmacokinetics involves LADMET processes crucial for drug efficacy and safety.
- In silico and in vitro methods offer early predictions of PK properties.
- Various in vivo assays and mathematical models are used for comprehensive PK assessment.
- Appropriate preclinical assays are vital for efficient drug discovery.
Conclusions:
- Effective pharmacokinetic assessment using preclinical assays is key to drug discovery success.
- Early integration of PK evaluation enhances the identification of safe and effective therapeutics.
- Strategic application of PK tools accelerates the delivery of novel medicines to patients.
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