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Physiologically Based Pharmacokinetic Models of Tyrosine Kinase Inhibitors: A Systems Pharmacological Approach to Drug Disposition
Author(s) -
Gallo J M
Publication year - 2013
Publication title -
clinical pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.941
H-Index - 188
eISSN - 1532-6535
pISSN - 0009-9236
DOI - 10.1038/clpt.2012.244
Subject(s) - clinical pharmacology , physiologically based pharmacokinetic modelling , pharmacokinetics , pharmacology , bioavailability , disposition , drug , tyrosine kinase , tyrosine kinase inhibitor , medicine , psychology , cancer , receptor , social psychology
The emergence of low‐molecular‐weight tyrosine kinase inhibitors (TKIs) has revolutionized anticancer drug therapy. It is not unexpected that lead TKIs are sought with favorable macropharmacokinetic characteristics, such as high oral bioavailability; however, surprisingly little emphasis has been given to the tissue disposition of TKIs, the site of drug action. This article discusses how physiologically based pharmacokinetic (PBPK) models can address this deficiency and help improve our understanding of the determinants of TKI efficacy. Clinical Pharmacology & Therapeutics (2013); 93 3, 236–238. doi: 10.1038/clpt.2012.244