Prodrugs therapeutic benefit

Several ADEPT systems that are beyond the scope of this chapter have been studied extensively and are the subject of many reviews.15,92-93 One of the most widely cited ADEPT systems employs a glucouronidase (GUS)-monoclonal antibody conjugate that activates a doxorubicin-glu-curonide prodrug. Studies have shown that there is a substantial therapeutic benefit, a higher level of drug in tumor tissue when compared... 

Many successes have been recorded in prodrug design, and a large variety of such compounds have proven their therapeutic value. Several complementary viewpoints can be adopted when addressing prodrugs, namely, their chemical classification, their mechanism of activation (i.e., enzymatic and/or non-enzymatic), their tissue selectivity, the possible production of toxic metabolites, and the gain in therapeutic benefit (Table 2). 

Gain in therapeutic benefit Prodrugs of marketed drugs (post hoc design) modest to marked benefit... 

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