Folate-targeted therapeutic and imaging agents for cancer

Philip Low, Sumith Anurasiri Kularatne

Research output: Contribution to journalReview articlepeer-review

470 Scopus citations


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 ∼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.

Original languageEnglish (US)
Pages (from-to)256-262
Number of pages7
JournalCurrent Opinion in Chemical Biology
Issue number3
StatePublished - Jun 1 2009

ASJC Scopus subject areas

  • Analytical Chemistry
  • Biochemistry


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