The application of in vitro model systems to evaluate the toxicity of
xenobiotics has significantly enhanced our understanding of drug- and
chemical-induced target toxicity. From a scientific perspective, there
are several reasons for the popularity of in vitro model systems. Fro
m the public perspective, in vitro model systems enjoy increasing popu
larity because their application may allow a reduction in the number o
f live animals employed in toxicity testing. In this review, we presen
t an overview of the use of in vitro model systems to investigate targ
et organ toxicity of drugs and chemicals, and provide selective exampl
es of these model systems to better understand cutaneous and ocular to
xicity and the role of drug metabolism in the hepatotoxicity of select
ed agents. We conclude by examining the value and use of in vitro mode
l systems in industrial development of new pharmaceutical agents.