Global InformationIRGD information
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| Clinical data | |
|---|---|
| Routes of administration | Intravenous |
| Pharmacokinetic data | |
| Bioavailability | 100% |
| Metabolism | n/a |
| Elimination half-life | 1-3 hours |
| Duration of action | up to 24 hours |
| Excretion | Renal (100%) |
| Identifiers | |
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| Chemical and physical data | |
| Molar mass | (948.04 g/mol after conversion) |
iRGD is a 9-amino acid cyclic peptide (sequence: CRGDKGPDC) and a molecular mimicry agent that was originally identified in an in vivo screening of phage display libraries in tumor-bearing mice.[1] The peptide was able to home to tumor tissues, but in contrast to standard RGD (Arginylglycylaspartic acid) peptides, also spread much more extensively into extravascular tumor tissue. It was later identified that this extravasation and transport through extravascular tumor tissue was due to the bifunctional action of the molecule: after the initial RGD-mediated tumor homing, another pharmacological motif is able to manipulate tumor microenvironment, making it temporarily accessible to circulating drugs. This second step is mediated through specific secondary binding to neuropilin-1 receptor, and subsequent activation of a trans-tissue pathway, dubbed the C-end Rule, or CendR pathway.[2]
- ^ Sugahara KN, Teesalu T, Karmali PP, Kotamraju VR, Agemy L, Greenwald DR, Ruoslahti E (May 2010). "Coadministration of a tumor-penetrating peptide enhances the efficacy of cancer drugs". Science. 328 (5981): 1031–5. Bibcode:2010Sci...328.1031S. doi:10.1126/science.1183057. PMC 2881692. PMID 20378772.
- ^ Ruoslahti E (February 2017). "Tumor penetrating peptides for improved drug delivery". Advanced Drug Delivery Reviews. 110–111 (Supplement C): 3–12. doi:10.1016/j.addr.2016.03.008. PMC 5045823. PMID 27040947.