Rapamycin: a quick history

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Well known for having over 800+ monolithic human statues, the Island of Rapa Nui (also known as the Easter Island) lies in the middle of the South Pacific Ocean, about 1300 miles from its nearest inhabited neighbor.

But it turns out that the moai statues aren’t the only wonders of this island. There’s another gem present there – rapamycin. The ‘rapa’ in rapamycin, is derived from ‘Rapa’ Nui.

Georges Nógrády along with other fellow scientists, carried out an expedition to Rapa Nui in 1964 and was baffled upon seeing that the island’s inhabitants walked barefoot but never got tetanus, even when there were so many horses around (tetanus and horses usually go hand in hand).

The curious scientists then made 67 divisions of the island, took samples of the soil, and added each to a vial.  Eventually, these vials found a home in the Ayerst Pharmaceuticals in Montreal. 5 years on, in 1969, it came to light that one of these samples had a bacterium with rapamycin-producing abilities (At that time, it was an unknown compound).

Fast forward to the late 80s, rapamycin and ‘rapalogs’ (compounds with similar structures to rapamycin) were being studied as powerful immunosuppressants that could be used for preventing organ rejection in transplant recipients.

Let’s TORC about mTOR

1993 and 1994 were the years where independent labs made multiple successive breakthroughs, leading up to a huge discovery. They found that rapamycin acts on a highly-conserved, alien protein complex. We now know that this protein complex is mTOR, and it has two components – mTORC1 and mTORC2.

 David Sabatini was one of the scientists who worked on the discovery of mTOR.  Now nicknamed as the ‘mTOR man’. Dr. Sabatini brings highly informative  podcasts and presentations on mTOR and its discovery.  If you’d like to dive in, it’s a great idea to check these out!

What has rapamycin shown so far?

In 1994, Rapamycin received FDA approval for the prevention of organ rejection. However, its efficacy for the treatment of other diseases is still undergoing research. Bearing that in mind, here’s an outline of some of the most significant benefits of Rapamycin, evident in both human and animal studies.

  • In 2009, rapamycin became known as the first molecule which was proven to extend a mammal’s lifespan, even when administered during the later stages of life.
  • In 2010, Rapamycin displayed promising potential in the elimination of cognitive deficits and reduced amyloid-beta in a mouse model of Alzheimer’s.
  • In 2014, rapamycin showed promising results in boosting the human immune system.
  • In 2020, rapamycin administration in mice showed improvement in oral health.

The promising animal and human data have encouraged more exploration into the marvels of Rapamycin. Right now, there are over 200 Rapamycin human clinical trials registered at clinicaltrials.gov. AgelessRx.com will also be conducting their own clinical trial soon. This trial is known as PEARL.
Rapamycin boasts an impressive safety profile when administered in small doses. Many individuals have also provided promising anecdotal evidence, suggesting that Rapamycin can help with a wide range of issues such as autoimmune conditions to arthritis, and much more.