Toward a Cancer Drug of Fungal Origin

Med Res Rev. 2015 Sep;35(5):937-67. doi: 10.1002/med.21348. Epub 2015 Apr 8.


Although fungi produce highly structurally diverse metabolites, many of which have served as excellent sources of pharmaceuticals, no fungi-derived agent has been approved as a cancer drug so far. This is despite a tremendous amount of research being aimed at the identification of fungal metabolites with promising anticancer activities. This review discusses the results of clinical testing of fungal metabolites and their synthetic derivatives, with the goal to evaluate how far we are from an approved cancer drug of fungal origin. Also, because in vivo studies in animal models are predictive of the efficacy and toxicity of a given compound in a clinical situation, literature describing animal cancer testing of compounds of fungal origin is reviewed as well. Agents showing the potential to advance to clinical trials are also identified. Finally, the technological challenges involved in the exploitation of fungal biodiversity and procurement of sufficient quantities of clinical candidates are discussed, and potential solutions that could be pursued by researchers are highlighted.

Keywords: anguidine; aphidicolin; clinical trials; drug resistance; fumagillin; fungal metabolites; illudin S; phenylahistin; rhizoxin; wortmannin.

Publication types

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

MeSH terms

  • Androstadienes / therapeutic use
  • Animals
  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / therapeutic use
  • Aphidicolin / therapeutic use
  • Biological Products / chemistry
  • Clinical Trials as Topic
  • Cyclohexanes / therapeutic use
  • Diketopiperazines / therapeutic use
  • Disease Models, Animal
  • Drug Design
  • Drug Resistance, Neoplasm
  • Fatty Acids, Unsaturated / therapeutic use
  • Female
  • Fungi / chemistry*
  • Humans
  • Macrolides / therapeutic use
  • Male
  • Mice
  • Neoplasms / drug therapy*
  • Polycyclic Sesquiterpenes
  • Sesquiterpenes / therapeutic use
  • Trichothecenes / therapeutic use
  • Wortmannin


  • Androstadienes
  • Antineoplastic Agents
  • Biological Products
  • Cyclohexanes
  • Diketopiperazines
  • Fatty Acids, Unsaturated
  • Macrolides
  • Polycyclic Sesquiterpenes
  • Sesquiterpenes
  • Trichothecenes
  • phenylahistin
  • Aphidicolin
  • fumagillin
  • rhizoxin
  • illudin S
  • diacetoxyscirpenol
  • Wortmannin