Prodrugs of anthracyclines in cancer chemotherapy

Current Medicinal Chemistry
Felix KratzM Gitzel

Abstract

Designing and developing truly tumor-specific prodrugs remains a challenge in the field of cancer chemotherapy. Active targeting strategies, on the one hand, aim at exploiting membrane-associated receptors or antigens for drug delivery; on the other hand, the enhanced vascular permeability and retention of macromolecules in tumor tissue substantiates the concept of passive targeting. Consequently, research efforts have concentrated on conjugating anticancer agents with a wide spectrum of carriers including antibodies, peptides, serum proteins, and synthetic polymers. Conversely, low-molecular weight prodrugs of anticancer agents have been developed that do not bear an active or passive targeting moiety, but are activated by tumor-associated enzymes at the tumor site. Anthracyclines probably represent the class of anticancer agents that has been most widely used for the development of prodrugs. This overview gives an update of the various low- and high-molecular weight prodrugs of anthracyclines, e.g. with antibodies, peptides, carbohydrates, serum proteins or synthetic polymers, that have been developed over the past 20 years and that exemplify the salient features of a respective drug delivery system. A detailed description wi...Continue Reading

Citations

Jun 17, 2008·Applied Microbiology and Biotechnology·Andriy LuzhetskyyAndreas Bechthold
Feb 21, 2009·Cancer Chemotherapy and Pharmacology·Khalid Abu AjajFelix Kratz
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Feb 10, 2009·Bioconjugate Chemistry·Khalid Abu AjajFelix Kratz
Jan 1, 2021·Journal of Medicinal Chemistry·Mona AlasKamaljit Kaur

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