The purpose of this work is to review the viability of the prodrug app
roach as a means of attaining targeted drug delivery. Through the use
of simple pharmacokinetic models, the initial discussion focuses on de
fining targeting and resolving the pharmacokinetic characteristics, of
both the drug and corresponding prodrug, necessary to achieve optimal
targeted delivery. Next, several examples of where the prodrug approa
ch has been used to achieve targeted delivery will be discussed. Lastl
y, due to the considerable attention it has received over the last 10
years, a brief section has been devoted to targeting by the use of pro
drugs in combination with monoclonal antibodies.