Peptides against cancer (L-11627, 11964)

Highlights

Angiogenesis is essential for the growth and progression of malignant tumours, and is used as an indicator of the degree of malignancy. Restricting the supply of blood to tumours by inhibiting angiogenesis has emerged as an innovative strategy to control both tumour growth and metastasis. Current anti-angiogenic drugs have targeted single stimulators involved in this multifactorial process, but are not sufficient to significantly reduce tumour burden and prolong life.

NRC has developed peptides with novel anti-angiogenic properties that are effective against many different stimulators of angiogenesis. The NRC peptides exhibit direct anti-tumorogenic properties against different types of tumours and have been validated in vivo. The anti-angiogenic activity against multiple stimulators, combined with the direct inhibition of tumour growth, position these peptides as promising treatments against malignant tumours.

Technology transfer

  • Commercial exploitation licence
  • R&D agreement for development

Market applications

  • Treatment of malignant tumours in a variety of cancers

How it works

Figure 1: Line graph with tumour volume in mm3 on the Y axis and days post treatment on the X axis. Growth of a control tumour is shown by a blue line and growth of a tumour treated with NRC's peptides (CIBP-4) is shown by a red line. Control tumour has reached a size of approximately 2500 mm3 at 25 days post treatment, while tumour treated with NRC's peptide has reached a size of approximately 1250 mm3 at 25 days post treatment.

Anti-angiogenic agents have some advantages over conventional anti-cancer therapies: direct accessibility from the circulation and low rate of drug resistance due to the genetic stability of endothelial cells. While preclinical trials of angiogenic inhibitors have been promising, showing partial or complete tumour regression without any drug resistance, clinical studies have only shown the stabilization of tumour growth with little to no regression. This is because advanced-stage tumours have already activated various signalling pathways that allow them to easily override the angiogenic restrictions of one inhibitor.

NRC's peptides inhibit the angiogenic responses induced by a number of growth factors including IGF-1, VEGF, PlGF, bFGF and S100A4. In addition, the peptides exhibit direct anti-tumorogenic properties against different types of tumors. NRC has demonstrated that the anti-angiogenic and anti-tumorigenic activity is predominantly located in the C-terminal sequence of the protein and is in part mediated by inhibition of intracellular cathepsin B and L activities in endothelial/tumoral cells. The anti-tumorigenic efficacy of the peptides has been validated in vivo using a subcutaneous xenograft glioblastoma mouse model.

Benefits

  • Potent pleiotropic inhibitory action against diverse stimulators of angiogenesis, as opposed to just one
  • Potent, angiogenesis-independent, anti-tumorigenic action
  • Novel mechanism of action on an enzymatic pathway involved in both angiogenesis and tumorigenesis
  • Proof of concept validated in vivo

Patents

  • NRC file 11627: Patents pending in the US, Canada, and Europe.
  • NRC file 11964: Patents granted in Europe, pending in the US and Canada.

Contact

Guy Le Houillier, Client Relationship Leader
Telephone: 514-496-6374
Email: Guy.LeHouillier@cnrc-nrc.gc.ca

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