CSF-1/CSF-1R targeting agents in clinical development for cancer therapy

Curr Opin Pharmacol. 2015 Aug;23:45-51. doi: 10.1016/j.coph.2015.05.008. Epub 2015 Jun 4.


Macrophage infiltration has been identified as an independent poor prognostic factor for several cancer entities. In mouse tumor models macrophages orchestrate various tumor-promoting processes. This observation sparked an interest to therapeutically target these plastic innate immune cells. To date, blockade of colony stimulating factor-1 or its receptor represents the only truly selective approach to manipulate macrophages in cancer patients. Here, we discuss the currently available information on efficacy and safety of various CSF-1/CSF-1R inhibitors in cancer patients and highlight potential combination partners emerging from preclinical studies while considering the differences between mouse and human macrophage biology.

Publication types

  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / administration & dosage
  • Antineoplastic Agents / immunology*
  • Drug Delivery Systems / trends*
  • Drug Discovery / trends
  • Humans
  • Macrophage Colony-Stimulating Factor / immunology*
  • Macrophages / drug effects
  • Macrophages / immunology*
  • Neoplasms / drug therapy
  • Neoplasms / immunology*
  • Receptor, Macrophage Colony-Stimulating Factor / immunology*
  • Signal Transduction / drug effects
  • Signal Transduction / immunology


  • Antineoplastic Agents
  • Macrophage Colony-Stimulating Factor
  • Receptor, Macrophage Colony-Stimulating Factor