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Targeted drug delivery and penetration into solid tumors

Angelo Corti1, Fabio Pastorino, Flavio Curnis

  • 1Division of Molecular Oncology and IIT Network Research Unit of Molecular Neuroscience, San Raffaele Scientific Institute, via Olgettina 58, 20132 Milan, Italy. corti.angelo@hsr.it

Medicinal Research Reviews
|February 3, 2011
PubMed

Insights

Targeting tumor vasculature with peptide-drug conjugates, like Asn-Gly-Arg (NGR) peptides, enhances chemotherapy delivery. NGR-tumor necrosis factor-α fusion proteins also improve drug penetration in neoplastic tissues.

Area of Science:

  • Oncology
  • Biotechnology
  • Pharmacology

Background:

  • Chemotherapeutic drug delivery and penetration into tumors are significantly hindered by abnormal tumor vasculature and altered stromal composition.
  • Neoplastic tissues present unique barriers to effective drug distribution, impacting treatment efficacy.

Purpose of the Study:

  • To explore strategies for improving chemotherapeutic drug delivery and penetration into tumor cells.
  • To investigate the potential of tumor vasculature-homing peptides and biological agents in enhancing drug delivery.
  • To evaluate the efficacy of Asn-Gly-Arg (NGR)-containing peptides and NGR-tumor necrosis factor-α (NGR-TNF) in overcoming drug delivery barriers.

Main Methods:

  • Coupling chemotherapeutic drugs with tumor vasculature-homing peptides, specifically those containing the Asn-Gly-Arg (NGR) motif.
  • Administering drugs in combination with biological agents that modulate the integrity of tumor endothelial lining.
  • Utilizing NGR-TNF, a fusion protein designed to selectively alter drug penetration barriers, and testing it in a Phase III clinical trial for malignant pleural mesothelioma.

Main Results:

  • Asn-Gly-Arg (NGR)-containing peptides show promise as ligands for targeted drug delivery to tumor vasculature.
  • NGR-TNF demonstrates the ability to selectively alter drug penetration barriers within tumors.
  • The NGR-TNF approach is currently under evaluation in a randomized Phase III trial for malignant pleural mesothelioma, indicating significant clinical interest.

Conclusions:

  • Targeting tumor vasculature with specific peptides like NGR offers a viable strategy to enhance drug delivery to cancer cells.
  • NGR-TNF represents a promising therapeutic agent for improving drug penetration in neoplastic tissues.
  • These peptide-based strategies hold potential for improving the effectiveness of chemotherapy in various cancers, including malignant pleural mesothelioma.

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