Ferroquine, the next generation antimalarial drug, has antitumor activity

Sci Rep. 2017 Nov 21;7(1):15896. doi: 10.1038/s41598-017-16154-2.


Despite the tremendous progress in medicine, cancer remains one of the most serious global health problems awaiting new effective therapies. Here we present ferroquine (FQ), the next generation antimalarial drug, as a promising candidate for repositioning as cancer therapeutics. We report that FQ potently inhibits autophagy, perturbs lysosomal function and impairs prostate tumor growth in vivo. We demonstrate that FQ negatively regulates Akt kinase and hypoxia-inducible factor-1α (HIF-1α) and is particularly effective in starved and hypoxic conditions frequently observed in advanced solid cancers. FQ enhances the anticancer activity of several chemotherapeutics suggesting its potential application as an adjuvant to existing anticancer therapy. Alike its parent compound chloroquine (CQ), FQ accumulates within and deacidifies lysosomes. Further, FQ induces lysosomal membrane permeabilization, mitochondrial depolarization and caspase-independent cancer cell death. Overall, our work identifies ferroquine as a promising new drug with a potent anticancer activity.

MeSH terms

  • Aminoquinolines / chemistry
  • Aminoquinolines / pharmacology*
  • Animals
  • Antimalarials / chemistry
  • Antimalarials / pharmacology*
  • Antineoplastic Agents / pharmacology*
  • Autophagy / drug effects
  • Caspases / metabolism
  • Cell Cycle Checkpoints / drug effects
  • Cell Death / drug effects
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Chloroquine / chemistry
  • Chloroquine / pharmacology
  • Female
  • Ferrous Compounds / chemistry
  • Ferrous Compounds / pharmacology*
  • Hydrogen-Ion Concentration
  • Intracellular Membranes / drug effects
  • Intracellular Membranes / metabolism
  • Lysosomes / drug effects
  • Lysosomes / metabolism
  • Metallocenes
  • Mice, Nude
  • Neoplasms / pathology
  • Permeability
  • Stress, Physiological
  • Xenograft Model Antitumor Assays


  • Aminoquinolines
  • Antimalarials
  • Antineoplastic Agents
  • Ferrous Compounds
  • Metallocenes
  • Chloroquine
  • ferroquine
  • Caspases