ANTIBODY-DIRECTED ENZYME PRODRUG THERAPY (ADEPT) WITH MUSTARD PRODRUGS

Antibody-directed enzyme prodrug therapy (ADEPT) is a two-step targeti ng procedure designed to improve the selectivity of anti-tumour agents . The approach is based on the activation of specially designed prodru gs by enzyme-antibody conjugates targeted to tumour-associated antigen s. This review concerns ADEPT using nitrogen mustard prodrugs and carb oxypeptidase G2 (CPG2) as the activating enzyme. The specific structur al features required of the nitrogen mustard prodrugs, their design, s yntheses, physicochemical properties, biological characteristics and a ctivation to the corresponding drugs are reviewed. The ADEPT clinical trial with a nitrogen mustard prodrug is also discussed.