Disclaimer: This is for the purpose of education only. Don’t try to self supplement or self medicate.
What is i-RGD?
RGD is actually the amino acid sequence. The “i” applies to its conformation. It is one of the many cell permeability affecting peptides.
Thymosin alpha is made in the thymus gland.
PNC27 is one of the gene suppressing peptides.
Mechanisms of Action
In addition to its broad augmentation of every step of the immune cascade, thymosin alpha specifically increases the viral antigen expression on tumor cells, making them more susceptible to the body’s own cancer fighting immune mechanisms. Tumor antigen is presented to (CD8+) T cells by MHC class I molecules. Thus, thymosin alpha up regulates MHC class I expression, and thus improves CD8+ T cell activation.
i-RGD specifically binds to neuropilin-1 and integrins – receptors primarily on cancer cells – causing a confirmational change that opens up the cell membrane. This leads to a dramatically increased delivery of chemotherapy to cancer cells. The cancers that produce angiogenesis are the ones that have a great deal of integrins. So this peptide works particularly well against cancers that erode in a particularly vascular way.
Thus, the i-RGD hones in on the cancer cells specifically opening those cells to chemotherapeutic destruction preferentially. So, lower doses of chemotherapy can be used, providing less damage to non-cancer tissues. But tumor lysis syndrome still occurs unfortunately, albeit more selectively of cancer cells than non-malignant tissues.
Segue to the third peptide for treating cancer which only causes programmed tumor cell apoptosis with something like 100% specificity and killing, a process that produces much less tumor lysis syndrome dumping then chemotherapy induced cell necrosis… PNC27.
PNC27. It is drawn to tumor cells and then activates tumor suppression genes; not tumor cell necrosis – but, rather tumor cell programmed death, apoptosis.
This is the mechanism of action, briefly. The main tumor suppression gene is P-53. It controls tumor suppression at almost every transcription site. PNC27 activates P-53.
P-53 is a gene that is only activated in cells under stress – like all cancer cells. The drive for that mechanism of action is reactive oxygen species (ROS). The more oxidative phosphorylation stress, the more ROS is made. More ROS attracts PNC27. In most cancers, tumor suppressing genes are inactivated. PNC27 drawn in by ROS changes this.
Therein is the specific targeting of the peptide PNC27 to cancer cells alone genotypic for B-53 gene which is the most comprehensive cancer killing gene for apoptosis, reducing proliferation, like that.
Uses for i-RGD
Thus, i-RGD is used with chemo to increase the chemo effect in the cancer tissue while sparing non-cancer tissue. It doesn’t have to be conjugated to the chemo for it to work. It is however not recommended as a standalone therapy (mostly because this has not been studied in human and nonhuman models), so must be used in conjunction with chemo given concurrently.
Thymosin alpha is used in a standalone fashion without chemo; and also lowers the doses of chemotherapy used. It is synergistic with i-RGD, so using them together along with chemotherapy is now allowing us to drop chemotherapy as low as 1/40 standard dosing to achieve as much as 40 times greater results with 40 times less side effects.
Numerous studies, human and animal, essentially every cancer type has been studied. Impressive, promising results.
Administration of i-RGD
Thymosin alpha is best dosed daily for treating cancer or Lyme disease. It is best dosed twice a week when treating chronic viruses.
PNC27 half life is so short that it must be dosed either multiple times a day or as a continuous IV infusion. The latter causes significant tumor lysis syndrome in humans.
Risks of i-RGD
Essentially no side effects. But since cancer apoptosis can be dramatic, the greatest risk tends to be tumor lysis syndrome. Especially with iRGD.
Because PNC27 causes essentially 100% apoptosis of the cancer cells because of great specificity and great killing enabled by the potentiation of the tumor suppression gene process, tumor lysis syndrome occurs much less.
As cell lysis syndrome happens way less in animals, it makes using these peptides in veterinary cancers particularly exciting.