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Abstract
Cancer therapies that exploit targeting ligands to deliver attached cytotoxic drugs
selectively to malignant cells are currently receiving significant attention. While
antibody-targeted drugs have been the first to enter the clinic, recent studies demonstrate
that the vitamin folic acid can also be used to deliver attached imaging and therapeutic
agents selectively to malignant cells in both animal tumor models and human cancer
patients. Thus, folate conjugates bind to folate receptors that are overexpressed
on approximately 40% of human cancers and mediate internalization of their attached
drugs by receptor-mediated endocytosis. With the use of proper linkers, folate-targeted
drugs can be released inside their target cells where they can perform their desired
cytotoxic functions. Based on this strategy, six folate-targeted drugs are currently
in human clinical trials.