ABSTRACT
The concept of prodrugs is not new in the field of medicine, yet it has emerged as one of the most prominent approaches in the last few decades to increase the selectivity and efficiency of antineoplastic agents. Prodrugs are chemically modified, inactive, bioreversible derivatives of pharmacologically active agents which should get transformed in vivo, either enzymatically or chemically, to release the pharmacologically active agents. The most conventional prodrug approach aims at improving the pharmacokinetic, physicochemical and biopharmaceutical characteristics of therapeutically active compounds. Chapter 10 includes the basis for the application of prodrug approach and elementary functional moieties capable for prodrug modification, and discuss the important characteristics and applications of prodrugs in cancer therapy. It further accentuates on different targeted prodrug designs, along with nanotechnology-enabled prodrugs developed to augment the specificity of chemotherapeutic drugs. A brief discussion on the potential hitches that can arise from insufficient activation of such prodrugs is also presented.
