Overview
iRGD is a cyclic peptide with the amino acid sequence Cys-Arg-Gly-Asp-Lys-Gly-Pro-Asp-Cys. Extensively researched for oncology applications, it enhances the targeting and permeability of cancer treatments. By binding to integrins on tumor endothelial cells, iRGD undergoes protease cleavage that activates binding to neuropilin-1, a receptor that regulates cellular transport. This unique pathway improves drug delivery into tumor tissue, making therapies more effective and less toxic.
iRGD is a cyclic peptide with the amino acid sequence Cys-Arg-Gly-Asp-Lys-Gly-Pro-Asp-Cys. Extensively researched for oncology applications, it enhances the targeting and permeability of cancer treatments. By binding to integrins on tumor endothelial cells, iRGD undergoes protease cleavage that activates binding to neuropilin-1, a receptor that regulates cellular transport. This unique pathway improves drug delivery into tumor tissue, making therapies more effective and less toxic.
Key Benefits of iRGD
- Enhanced Drug Accumulation: Increases tumor permeability, enabling deeper penetration and higher local concentrations.
- Greater Treatment Efficacy: Demonstrated up to a 40-fold increase in tumor drug levels, significantly reducing growth and improving outcomes.
- Reduced Toxicity: Allows lower drug dosages with equivalent or greater therapeutic effects, minimizing systemic side effects.
- Versatile Application: Effective with small molecules (e.g., doxorubicin), nanoparticles (e.g., liposomal doxorubicin, nab-paclitaxel), and monoclonal antibodies (e.g., trastuzumab).
Mechanism of Action
- Binds selectively to integrins on tumor blood vessels.
- Proteolytic cleavage exposes a binding site for neuropilin-1.
- Neuropilin-1 activation opens a transport pathway that increases vascular and tissue permeability specifically in tumors.
- Enhances uptake of co-administered cancer drugs without requiring chemical conjugation.
Clinical Research
- Tumor Penetration: Mouse tumor models show that iRGD improves vascular and tissue permeability, enabling drugs to reach extravascular tumor tissue more effectively.
- Drug Efficacy:
- Co-administration with doxorubicin, nab-paclitaxel, liposomal doxorubicin, or trastuzumab increased tumor drug accumulation up to 40×.
- Equivalent tumor suppression achieved at one-third of the standard drug dose, indicating safer and more efficient treatment potential.
Product Information
- Product Name: iRGD (Cancer Targeting Peptide)
- Applications:
- Enhance permeability and efficacy of anti-cancer drugs
- Reduce systemic toxicity of cancer treatments
- Mode of Action: Integrin binding → protease cleavage → neuropilin-1 activation → increased tumor permeability and drug penetration
- Compatibility: Effective with small molecules, nanoparticles, and monoclonal antibodies
