Novel in vivo procedure for rapid pharmacokinetic screening of discovery compounds in rats

In therapeutic areas aimed at developing an orally administered drug, the pharmacokinetic profile of a drug candidate after oral administration in vivo is pivotal in evaluating its success. This can be done by monitoring the plasma concentration versus time after dosing and calculating the area unde...

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Bibliographic Details
Published in:Drug Discovery Today 1999-05, Vol.4 (5), p.232-237
Main Authors: Cox, Kathleen A., Dunn-Meynell, Kimberly, Korfmacher, Walter A., Broske, Lisa, Nomeir, Amin A., Lin, Chin-Chung, Cayen, Mitchell N., Barr, William H.
Format: Article
Language:English
Subjects:
AUC
Biological and medical sciences
drug metabolism
General pharmacology
LC-MS
mass spectrometry
Medical sciences
pharmacokinetics
Pharmacokinetics. Pharmacogenetics. Drug-receptor interactions
Pharmacology. Drug treatments
screening
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Summary:In therapeutic areas aimed at developing an orally administered drug, the pharmacokinetic profile of a drug candidate after oral administration in vivo is pivotal in evaluating its success. This can be done by monitoring the plasma concentration versus time after dosing and calculating the area under the curve (AUC). The authors describe a novel screening protocol in which an estimated AUC can be determined, allowing the rapid evaluation of large numbers of compounds and providing a rank order of estimated AUC values to prioritize compounds for further investigation.
ISSN:1359-6446
1878-5832
DOI:10.1016/S1359-6446(98)01299-9