How close are we to a real anti-aging pill?

What is Rapamycin?

Rapamycin and its cousin medicines (“rapalogs”) are currently prescription medications for organ transplant recipients and also cancer patients with the names of sirolimus (Rapamune), deforolimus (Ridaforolimus), everolimus, and temsirolimus (a rapamycin pro-drug).

But there is an indication that using it “off-label” could be an anti-aging breakthrough.

When a drug is used off-label, it means a physician has prescribed it for an approved use other than what it was developed for. For example, Wellbutrin is a brand drug developed for depression, but over the years it’s been found to aid smokers in quitting and work as a second-line treatment for ADHD.

How did Rapamycin get a reputation as an anti-aging drug? It was first discovered from a soil sample on Easter Island (Rapa Nui). This antifungal metabolite of Streptomyces hygroscopicus was subsequently found to have immunosuppressive and anti-proliferative properties in animal studies. Now years later, the mode of action of rapamycin has been identified in great detail and is proven to be an anti-aging drug and a lot more.

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Proven health benefits and safety of Rapamycin

Rapamycin and the rapalogs have been used in healthy volunteers, and even in pregnant women without detrimental effects. They have minimal side effects — which can be reversed by discontinuation of the drug.

Rapamycin and the rapalogs are well proven to have the following impressive health effects (and I have 88 scientific studies for this section — too numerous to cite):

• Rapamycin extends life span in diverse species from yeast to mammals. Even at safe doses, they have no noticeable side effects.
• It and other rapalogs are consistently shown to suppress the process of cell deterioration with age (a.k.a. geroconversion).
• It prevents age-related diseases such as atherosclerosis, neurodegeneration, and retinopathy, cardiopathy in mice and primates including humans.
• It prevents cancer in mice and in humans.
• It decreases obesity in mice and humans.
• It prevents all age-related diseases in general.
• In some studies, rapamycin improves metabolic parameters.

After many years of research and animal studies, rapamycin was recently investigated as an anti-aging drug in a small human clinical trial.

Mechanism of action of Rapamycin

The molecular mechanisms of action that have been well studied are quite complex. I feel you deserve to know just a few of the key abbreviations that may become more popular in years to come:

• mTOR = mammalian Target Of Rapamycin. This is a protein with enzyme activity that controls cell growth, proliferation, and survival. This protein activity is upregulated in cancer. The rapalogs target this enzyme; they bind to it and block many of mTOR functions.
• mTORC1 = mammalian Target Of Rapamycin Complex 1. It contains mTOR and other enzymes that together break apart RNA and DNA chains (genetic code). mTORC1 regulates many cellular functions that are required for cell growth, cell proliferation, mRNA biogenesis, protein and fat synthesis, energy metabolism and autophagy (a “self-eating” detox process your body undergoes to clean out damaged cells and regenerate new ones)
• mTORC2 = mammalian Target Of Rapamycin Complex 2. It enzymes that are not sensitive to rapamycin and plays countering metabolic roles.

Figure. Effects of rapamycin in various diseases including cancer, diabetes, tuberous sclerosis complex, lymphangioleiomyomatosis, neurodegenerative diseases, and aging. FDA-approved cases are described. Source: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3972801/

In summary

Now after decades of intense research on rapamycin, mTOR, and mTORC1, the direction of this research continues to be the implementation of anti-aging drugs that can delay age-related diseases.

The dilemma is that we don’t have long-term studies yet for the FDA to give their approval, though it’s certainly been demonstrated to be safe in many medical situations.

Some authors suggest the ideal anti-aging formula includes a nutrient-rich plant-based diet and physical exercise.

Anti-aging pill or not, there’s nothing holding you back from working on your diet and getting exercise. And it may not be too far down the road that off-label use for rapamycin could include a common anti-aging pill.

Sources:

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3. Veroux M, Corona D, Veroux P. Pregnancy under everolimus-based immunosuppression — Transpl Int. 2011;24:e115–117
4. Sifontis NM, Coscia LA, Constantinescu S, Lavelanet AF, Moritz MJ, Armenti VT. Pregnancy outcomes in solid organ transplant recipients with exposure to mycophenolate mofetil or sirolimus — Transplantation. 2006;82:1698–1702
5. Morrisett JD, Abdel-Fattah G, Hoogeveen R, Mitchell E, Ballantyne CM, Pownall HJ, Opekun AR, Jaffe JS, Oppermann S, Kahan BD. Effects of sirolimus on plasma lipids, lipoprotein levels, and fatty acid metabolism in renal transplant patients — J Lipid Res. 2002;43:1170-1180
6. Liu Y, Diaz V, Fernandez E, Strong R, Ye L, Baur JA, Lamming DW, Richardson A, Salmon AB. Rapamycin-induced metabolic defects are reversible in both lean and OBESE mice — Aging (Albany NY) 2014;6:742–754
7. Blagosklonny MV. Geroconversion: irreversible step to cellular senescence — Cell Cycle. 014;13(23):3628-35. Review. PubMed PMID: 25483060
8. Leontieva OV, Demidenko ZN, Blagosklonny MV. Dual mTORC1/C2 inhibitors suppress cellular geroconversion (a senescence program) — Oncotarget. 2015 Sep 15;6(27):23238-48. PubMed PMID: 26177051
9. Singh M, Jensen MD, Lerman A, Kushwaha S, Rihal CS, Gersh BJ, Behfar A, Tchkonia T, Thomas RJ, Lennon RJ, Keenan LR, Moore AG, Kirkland JL. Effect of Low-Dose Rapamycin on Senescence Markers and Physical Functioning in Older Adults with Coronary Artery Disease: Results of a Pilot Study — J Frailty Aging. 2016;5:204–207
10. Blagosklonny MV. Koschei the immortal and anti-aging drugs — Cell Death Dis. 2014 Dec 4;5:e1552. Review. PubMed PMID: 25476900