Exploring the Role of ADME for Anticancer Prodrugs

Anticancer drug administration is currently associated with high toxicity and a lack of tumor specificity. Prodrugs are being developed to improve the therapeutic index of these drugs by lowering toxicity and increasing efficacy. Alkylating drugs, particularly nitrogen-containing alkylating agents, are often used to treat hematological along with malignancies; they act as anticancer agents at all stages of the cell cycle, preventing tumor cells from replicating. Certain alkylating drugs have been made more lipophilic, allowing them to permeate cells and increase their alkylating action against malignancies. Various novel antimetabolites are showing impressive development at clinical level, either due to a novel mode of action, smart combination, or innovative prodrug design, as summarized in this chapter. The advancement of prodrugs, such as 5-fluorouracil (5-FU), paclitaxel, as well as other cytotoxic medicines routinely utilized in cancer treatments, will be discussed. Although most of these medicines are still in the initial phases of development, those that have already had a clinical impact will be discussed in this chapter.