Bisphosphonates' antitumor activity: an unravelled side of a multifaceted drug class

Bone. 2011 Jan;48(1):71-9. doi: 10.1016/j.bone.2010.07.016. Epub 2010 Jul 22.


Bisphosphonates, especially nitrogen-containing bisphosphonates (N-BPs), are widely used to preserve and improve bone health in patients with cancer because they inhibit osteoclast-mediated bone resorption. In addition to their effects on bone, preclinical evidence strongly suggests that N-BPs exert anticancer activity without the involvement of osteoclasts by interacting with macrophages, endothelial cells and tumor cells, and by stimulating the cytotoxicity of γδ T cells, a subset of human T cells. This review examines the current insights and fronts of ongoing preclinical research on N-BPs' antitumor activity.

Publication types

  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / immunology
  • Antineoplastic Agents / pharmacology*
  • Bone Resorption / drug therapy
  • Cell Line, Tumor
  • Cytotoxicity, Immunologic / drug effects
  • Cytotoxicity, Immunologic / immunology
  • Diphosphonates / immunology
  • Diphosphonates / pharmacology*
  • Disease Models, Animal
  • Drug Evaluation, Preclinical
  • Forecasting
  • Humans
  • Macrophages / drug effects
  • Mice
  • Mice, SCID
  • Neoplasms / drug therapy*
  • Neoplasms / prevention & control*
  • Osteoclasts / drug effects
  • T-Lymphocytes / immunology
  • T-Lymphocytes / metabolism


  • Antineoplastic Agents
  • Diphosphonates