A great deal of research has surrounded the use of monoclonal antibody
-enzyme conjugates for the activation of anticancer prodrugs. This is
a two-step approach to cancer chemotherapy in which monoclonal antibod
ies are used to deliver enzymes to tumor cell surfaces. The enzymes ar
e chosen for their abilities to convert relatively non-cytotoxic prodr
ugs into active anticancer agents. This review provides a summary of t
he in vitro and in vivo activities obtained from several promising mon
oclonal antibody-enzyme/prodrug combinations. Pharmacokinetic data is
also presented that provides mechanistic insight into the antitumor ac
tivities obtained.