Targeted drug delivery and penetration into solid tumors

Med Res Rev. 2012 Sep;32(5):1078-91. doi: 10.1002/med.20238. Epub 2011 Feb 1.


Delivery and penetration of chemotherapeutic drugs into tumors are limited by a number of factors related to abnormal vasculature and altered stroma composition in neoplastic tissues. Coupling of chemotherapeutic drugs with tumor vasculature-homing peptides or administration of drugs in combination with biological agents that affect the integrity of the endothelial lining of tumor vasculature is an appealing strategy to improve drug delivery to tumor cells. Promising approaches to achieve this goal are based on the use of Asn-Gly-Arg (NGR)-containing peptides as ligands for drug delivery and of NGR-TNF, a peptide-tumor necrosis factor-α fusion protein that selectively alters drug penetration barriers and that is currently tested in a randomized Phase III trial in patients with malignant pleural mesothelioma.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Clinical Trials as Topic
  • Drug Delivery Systems / methods*
  • Humans
  • Ligands
  • Neoplasms / blood supply
  • Neoplasms / drug therapy*
  • Recombinant Fusion Proteins / immunology
  • Recombinant Fusion Proteins / therapeutic use
  • Tumor Necrosis Factor-alpha / immunology
  • Tumor Necrosis Factor-alpha / therapeutic use


  • Ligands
  • Recombinant Fusion Proteins
  • Tumor Necrosis Factor-alpha
  • tumor necrosis factor-alpha, CNGRC fusion protein, human