A major focus of current drug research is to improve drug targeting to inte
rnal target sites such as to solid tumors or specific organs. The objective
of drug targeting, especially for cancer chemotherapy and radioimmunothera
py, is to enhance the effectiveness of the drug by concentrating it at the
target site and minimizing its effects in nontarget sites. Although tumor t
argeting has been obtained with large long-circulating radiolabeled antibod
y molecules, normal organ activity, especially in the blood kidneys, liver,
and bone marrow is a significant problem. Over the last 20 years, studies
to improve the therapeutic use of antibodies have included the use of antib
ody fragments, chase molecules, metabolizable linkers, antibody-directed en
zyme prodrugs (ADEPT), local delivery, and pretargeting. Here, we will revi
ew the most interesting recent advances in pretargeting biotechnology. (C)
2001 Elsevier Science Inc. All rights reserved.