In vitro methods in the prediction of kinetics of drugs: focus on drug metabolism.
The absorption, distribution, metabolism, excretion and toxicity (ADMET) properties of a candidate drug influence its final clinical success. These properties have traditionally been evaluated by using various in vivo animal approaches, but recently, a number of in vitro and in silico methods have been introduced to determine key ADMET features. Basic events, such as absorption through the gut wall, binding to plasma proteins, active and passive transfer through the blood-brain barrier, and various metabolic parameters, can now be screened with rapid in vitro and computer modelling methods. The focus in this short review is on the basic in vitro and in silico methods that are used for studying the metabolism properties of new drug molecules.
Raunio
Hannu
H
Department of Pharmacology and Toxicology, University of Kuopio, Kuopio, Finland. hannu.raunio@uku.fi
Taavitsainen
Päivi
P
Honkakoski
Paavo
P
Juvonen
Risto
R
Pelkonen
Olavi
O
D000042:Absorption; D000826:Animal Testing Alternatives; D000818:Animals; D002460:Cell Line; D002478:Cells, Cultured; D003198:Computer Simulation; D003577:Cytochrome P-450 Enzyme System / Q000378:metabolism; D006801:Humans; D007408:Intestinal Absorption; D008099:Liver; D004364:Pharmaceutical Preparations / Q000378:metabolism*; D010599:Pharmacokinetics; D046509:Tissue Culture Techniques; D014018:Tissue Distribution; D018675:Toxicity Tests
D004364:Pharmaceutical Preparations; D003577:Cytochrome P-450 Enzyme System