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Research Reveals Cancer Drug Effectiveness Substantially Advanced
Date:4/8/2010

ng to unique receptors in the vasculature of cancers. The RGD peptide’s ability to home to tumors has been used to design new compounds for cancer diagnosis and treatment.

The new variant of RGD (iRGD—internalizing RGD) combines the RGD motif with a tissue penetration element called CendR. Like the earlier RGD peptides, iRGD homes to tumors, but exposure of the CendR motif when the iRGD is enzymatically cleaved acti-vates a transport system through tumor blood vessel walls into the tumor core. In a paper published in Cancer Cell late last year, the research team showed that coupling iRGD to anti-cancer drugs allowed them to penetrate deep into tumors, effectively increasing the activity of the drugs.

The research reported in this latest Science paper adds a new and important twist to the story: The researchers made the unanticipated discovery that anti-cancer drugs do not need to be chemically attached to the iRGD peptide for iRGD to boost their efficacy. Simply co-administering iRGD with a drug enhances the drug’s anti-cancer properties. Co-administration could be even more effective at delivering therapeutic agents inside tumors than conjugating the agents with the peptide. This new paradigm means that iRGD has the potential to enhance the efficacy of already approved drugs without creat-ing new chemical entities, which would complicate the path to approval for clinical use.

In addition to being effective against human breast, prostate and pancreatic cancers grown in mice, iRGD can penetrate other tumor types
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