Toll-like receptor agonists in cancer therapy

Immunotherapy. 2009 Nov;1(6):949-64. doi: 10.2217/imt.09.70.


Toll-like receptors (TLRs) are pattern-recognition receptors related to the Drosophila Toll protein. TLR activation alerts the immune system to microbial products and initiates innate and adaptive immune responses. The naturally powerful immunostimulatory property of TLR agonists can be exploited for active immunotherapy against cancer. Antitumor activity has been demonstrated in several cancers, and TLR agonists are now undergoing extensive clinical investigation. This review discusses recent advances in the field and highlights potential opportunities for the clinical development of TLR agonists as single agent immunomodulators, vaccine adjuvants and in combination with conventional cancer therapies.

Keywords: CpG; Toll-like receptor; Toll-like receptor agonist; bacillus Calmette–Guerin; imiquimod; immunotherapy; monophosphoryl lipid A; polyriboinosinic-polyribocytidylic acid; resiquimod; vaccine adjuvant.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Adjuvants, Pharmaceutic / therapeutic use*
  • Animals
  • Antineoplastic Agents / pharmacology
  • Antineoplastic Agents / therapeutic use*
  • Drug Therapy, Combination
  • Humans
  • Immunomodulation*
  • Neoplasms / drug therapy*
  • Neoplasms / immunology
  • Toll-Like Receptors / agonists*
  • Toll-Like Receptors / immunology


  • Adjuvants, Pharmaceutic
  • Antineoplastic Agents
  • Toll-Like Receptors