Håkan P. Svensson

Activation of prodrugs by antibody-enzyme conjugates

Monoclonal antibodies (MAbs) against human tumor antigens have been the subject of extensive investigation as carriers of cytotoxic agents to tumor cells. Promising results, both in vitro and in vivo, have been obtained in studies involving immunoconjugates such as MAb-toxins (Vitetta et al., 1987; Blakey et al., 1988), MAb-drugs (Pietersz, 1990; Koppel, 1990), and radiolabeled MAbs (Goldenberg, 1990). Based on these findings, many such conjugates are currently being evaluated in the clinic.

A summary of monoclonal antibody-enzyme/prodrug

Abstract 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 antibodies are used to deliver enzymes to tumor cell surfaces. The enzymes are chosen for their abilities to convert relatively non-cytotoxic prodrugs into active anticancer agents. This review provides a summary of the in vitro and in vivo activities obtained from several promising monoclonal antibody-enzyme/prodrug combinations. Pharmacokinetic data is also presented that provides mechanistic insight into the antitumor activities obtained.