Rapamycin

Rapamycin is also known as Sirolimus or Rapamune, and it's in the group of macrolides.

Rapamycin was first found in a soil sample on Easter Island in 1972. It was produced by a soil bacterium streptomyces hygroscopicus. It was first produced as an antifungal agent because it was effective in reducing the growth of yeast, but it was later discovered that it also has an immunosuppressive function with antiproliferative properties due to the capacity of inhibit mTOR and was approved by the FDA as an immunosuppressant for organ transplants in 1999. It is the first drug that researchers were able to identify its target biochemically and was named mTOR “mammalian target of rapamycin.

In a recent study, there was evidence that review that rapamycin is a universal anti-aging drug, that helps prolong lifespan in yeast, mammals and also suppresses cell senescence and also helps to delay the onset of age-related diseases.

It’s known rapamycin has an effective immunosuppressive function with the capacity to disrupt cytokines signaling that helps to assist the growth of lymphocytes and also in differentiation. It also helps in suppressing cellular hyperfunction which leads to the delay of all diseases that have to do with aging. The obstruction of mTORC1 by rapamycin suppresses aging by the increase in autophagy, which indulges the elimination of misfolded proteins and Impaired organelles like mitochondria, preventing the accumulation and associated with aging and related diseases. Nevertheless, it is still unknown if the outcome of late-life treatment is equal to lifelong treatment or even if brief treatment at a younger age is sufficient for long-term benefits.

Due to this mechanism of action of rapamycin and also in scientific research done in yeast and mammals. so it is known as a potential inducer of autophagy. Researchers have also discovered that rapamycin exposure helps to increase the production of histone a protein that is found in DNA and helps to over-turn the age-related loss.

In a recent study that was done at UCL Institute of Healthy Ageing, on fruit flies’ rapamycin was said to be given to both male and female fruit flies it was found that rapamycin helped to prolong the lifespan and slowed age-related intestinal pathologies in female flies but these changes were not found in the male files. In research that was done at Max Planck Institute for Biology of Ageing to clinically determine the dose of rapamycin that can be given to see a therapeutic effect and whether rapamycin can be used long-term without any adverse effects; it was relieved that the lower doses have undesired side-effects. Young fruit flies received rapamycin for two weeks, it appeared to have protected them against age-related changes in the intestine and also helped to prolong their lives whereas the rapamycin was administered to mice for three months starting at three months of age which is similar to early adulthood in humans, improvements were seen in the intestine of the mice. It is also observed that the effect of the drug can still be observed six months after the cancellation of rapamycin. In this research, the researchers were able to observe that brief treatment in early adulthood produces enough protection as continuous treatment. And the use of rapamycin in early life has the strongest effect when compared to middle age.

In an interview that was done by Life Extension with pharmacist Ross Pelton about his book on Rapamycin mTOR, autophagy and treating mTOR syndrome. In this book, he explained how rapamycin works and how it has the ability to increase median life expectancy by up to 60% in an experiment that was carried out on animal models. Furthermore, a clinical trial that was done on people older than 65 years with the use of Everlimus which is also a derivative of Rapamycin revealed that it has the capability to fortify their immune system. And also how rapamycin reduces body mass and body weight in the cells of the animal models in the animal experiment that was carried out. Pharmacist Ross Pelton also experienced weight loss of about 15 pounds when taking Rapamycin but this trial is yet to be done on humans. Pelton also explains how physicians are observing that administering 5-6 mg of rapamycin just once weekly helps to partly inhibit mTOR, which helps allows autophagy to express itself on a periodic basis. It gets to a point when mTOR and autophagy balance each other favorably and this allows every cell in the helps to undergo detoxification, revitalization, and renewal.

In conclusion, based on the pharmacodynamics and the chemical properties of rapamycin it is shown that rapamycin is indeed a potential anti-aging drug. Which has only been tested in mice and flies and has shown to prolong lifespan but is irreversible; it has yet to test in humans.

(Article by: Dr. Thiago Freire and Quadri Halimat Morenikeji)