Folate Receptor Targeted Cancer Chemotherapy

Abstract

The membrane-bound folate receptor (FR) is overexpressed on a wide range of human cancers. The vitamin folic acid is a high affinity ligand of the FR which retains its receptor binding and receptor-mediated endocytosis properties when conjugated to other molecules. Consequently, folate targeting technology has successfully been applied for the delivery of various chemotherapeutic agents to FR-positive cancers. Together with optimized spacers and self-immolative linkers, these folate-drug delivery systems have produced major enhancements in cancer cell-specific and selective potency over their nontargeted drug counterparts. Hence, it is hopeful that this targeting strategy will lead to improvements in the safety and efficacy of clinically-relevant anticancer therapeutic agents. The focus of this chapter will be to highlight the current status of folate-drug technology with particular emphasis on the recent advances in this field.