Rapamycin, an antiaging drug: Benefits and risks to health and longevity

In longevity studies, scientists have been getting more interested in the potential anti-aging benefits of rapamycin.

Currently, this drug is being used to treat specific lung diseases, prevent organ-transplant rejection and coat coronary stents. 

A drug originally developed as an immunosuppressant and used in organ transplantation, rapamycin has recently taken center stage for its potential to extend lifespan and promote health in the aging population.

Rapamycin was found to extend the lifespan of mice in an experiment in 2009. Since then, numerous clinical studies have been trying to discover the exact contribution and function of rapamycin in longevity and treating age-related diseases. 

How does rapamycin work?

Rapamycin refers to a compound released by a bacterium that is scientifically called Streptomyces hygroscopicus. 

Historically speaking, rapamycin was first isolated from a soil sample found on Easter Island in 1972. The name “rapamycin,” in fact, came from the word Rapa Nui, which is the island’s native name. In clinical terms, rapamycin is also referred to as Sirolimus and is being sold under the brand name “Rapamune” [1].

The compound was originally used as an antifungal; however, it is presently commonly used as an immunosuppressant in clinics, which helps prevent organ rejection during transplant surgery–following the 1999 approval of the United States Food and Drug Administration in the use of Rapamune for kidney transplant patients [2]. 

Moreover, rapamycin is also used as an anti-proliferative that potentially inhibits cell growth, including the growth of malignant or cancerous cells.

Mechanism of action

Rapamycin is found to function as a blocker of cells to stop them from growing and multiplying. Consequently, it becomes an effective drug in preventing cancer cells from spreading in the body.

The compound can disrupt cell growth by promoting the inhibition of the mammalian target of rapamycin (mTOR). mTOR refers to a signaling pathway that contributes to cell synthesis and metabolism–basically, rapamycin can interrupt mTOR [3]. 

mechanism of action

The mTOR pathway is known to be involved in the formation of numerous health diseases, primarily different types of cancer and Alzheimer’s disease. With the function of rapamycin, it can potentially treat such fatal health conditions. 

Additionally, rapamycin can suppress the immune system of kidney transplant patients in order to keep the body from rejecting the donor’s kidney [4]. 

How rapamycin affects cellular aging

Rapamycin’s impact on cellular aging is multifaceted. It reduces the production of harmful free radicals, which can accelerate cellular damage and aging.

Additionally, rapamycin enhances the functioning of mitochondria, the energy powerhouses of cells, and reduces inflammation, a major driver of age-related diseases.

Rapamycin influences the balance between cell proliferation and cell senescence. It promotes the survival of healthy cells while discouraging the replication of damaged and senescent cells, which can contribute to aging and disease progression.

What are the benefits of rapamycin?

Scientists are still investigating the use of rapamycin for longevity. They are looking at how rapamycin can either slow the aging process or prevent age-related diseases. 

Meanwhile, rapamycin’s function in prolonging the lifespan of many species of mice [5], yeast [6] and fruit flies (Drosophila melanogaster) [7] are well-tested and experimented with. 

1. Anti-aging

Numerous animal studies have been conducted for years on rapamycin in dogs, worms, fruit flies, mice and rats, and the results showed are quite promising in anti-aging.

However, rapamycin’s beneficial effects on humans are still lacking and being investigated. 

The anti-aging effects of rapamycin on animal studies are what keep scientists intrigued. Rapamycin can potentially help prevent age-related diseases, improve the quality of life of patients, and extend lifespans. 

Furthermore, many scientists believe that rapamycin can be an effective anti-aging drug if it is administered to people before they even develop diseases associated with aging. Rapamycin can potentially increase both the health and lifespan of humans [8]. 

However, rapamycin is not a compound that can magically cure age-related diseases. It can only be a supplement that will be taken alongside a healthy lifestyle and diet.

What is lacking in anti-aging studies involving rapamycin? It is determining the actual causes of aging to fully understand the anti-aging capabilities of rapamycin. 

Some of the major causes of why the body degenerates and develops age-related diseases are a halt in cell division, a loss of stem cells, damaged DNA and shortened telomeres, which are all cell-function related that threaten health and lifespan.

2. Increased longevity and lifespan

In terms of longevity, rapamycin enhances autophagy, a process that removes unnecessary, abnormal and damaged components within cells and prevents cells from stress [9]. In short, autophagy keeps your cells healthy.

Rapamycin can improve autophagy in the body when it inhibits mTOR. It simultaneously boosts the process and disrupts unhealthy cell growth.

As a result, the body can delay the onset of the aging process and age-related diseases, giving people a longer and healthier life. Hence, many researchers are positive that we might be able to use rapamycin for longevity in the future. 

3. Used to treat cancer

The mTOR encourages cell growth and proliferation that affects the body’s function to remediate cellular damage through autophagy.

When this happens, the body may develop various diseases, including cancer which is the uncontrolled growth of cells. 

Interestingly, rapamycin’s ability to inhibit mTOR can also impact tumor proliferation by disrupting it.

The inhibition of mTOR through rapamycin induces tumor cell apoptosis or cell death and angiogenesis, which is the process of supplying tumors with the network of blood vessels they need to acquire nutrients. 

Rapalogs, which are rapamycin derivatives, are approved in the United States for the treatment of certain types of cancer, particularly renal cancer [10].

used to treat cancer

4. Skin aging

The most visible sign of aging can be seen in one’s skin health. Creams made from rapamycin are scientifically produced and prescribed to treat certain skin conditions, such as vascular anomalies, facial angiofibroma and psoriasis in children and young adults.

Moreover, rapamycin may also potentially lessen the signs of aging on the skin, including sun spots and wrinkles [11]. 

Research suggests that topical rapamycin application may reduce sagging skin and photoaging and enhance dermal volume on hands, thereby slowing the process of skin aging. However, a topical rapamycin cream to be added to cosmetics can be far from reality today [12]. 

Recommended dosage of rapamycin

There is an appropriate dosage of rapamycin, depending on where to use it. 

For kidney transplants

Rapamycin should be taken orally by the patients as a tablet or liquid solution for those unable to swallow pills. Your doctor may advise you to take the rapamycin pills with food or a large glass of water or orange juice.

Take note, though, that rapamycin is not safe to take with grapefruit juice and should be taken at the same time and in the same way every day. You should also consult with your physician about the frequency and certain special instructions. 

For cancer patients

Rapamycin treatment is commonly given through an IV, and it usually takes around 30 minutes to be administered.

Your rapamycin dose depends on how your body tolerates it, the side effects experienced and the impact on your current medical condition, as per the advice of a medical professional. 

What is the downside of rapamycin?

Using rapamycin may cause side effects [13, 14] and the severity may vary from one person to another. Generally, rapamycin’s side effects are mild but for some, it can be really life-threatening.

  • Immunosuppression: Rapamycin’s primary use in organ transplantation is as an immunosuppressant, which means it dampens the immune system’s response. This can make individuals more susceptible to infections, including viral, bacterial, and fungal diseases.
  • Gastrointestinal disturbances: Some people experience gastrointestinal issues such as diarrhea, nausea, and abdominal discomfort while taking rapamycin.
  • Skin problems: Skin-related side effects, like rash and acne, have been reported in some cases.
  • Metabolic effects: Rapamycin may impact metabolism, potentially leading to increased cholesterol levels and insulin resistance.

The immunosuppressive properties of rapamycin, while useful in preventing organ rejection, raise concerns in the context of anti-aging.

A weakened immune system could increase susceptibility to infections and compromise the body’s ability to fend off diseases.

Therefore, using rapamycin for anti-aging purposes requires careful monitoring and management to mitigate these risks.

The long-term safety of rapamycin for anti-aging purposes is an area of ongoing research. While it has shown promise in extending lifespan and improving health in animal studies, the effects of prolonged rapamycin use in humans are not yet fully understood.

This uncertainty underscores the importance of medical supervision and regular health assessments for individuals using rapamycin as an anti-aging intervention.

Risks to health and longevity 

While rapamycin may help kidney transplant patients, it may increase the risk of infection for some other people as it can notably suppress the immune system. Suppressing the immune system brought by rapamycin may significantly impair wound healing. 

Some other risks of using rapamycin include insulin resistance, high cholesterol and interstitial lung disease.

Using rapamycin can have negative effects on glucose metabolism that may cause diabetes-like effects. 

Most importantly, the greatest risk of taking rapamycin as an antiaging drug is the lack of human research.

There is still no strong evidence from clinical trials that may prove its health and longevity claims, especially when taken over a long period of time. 

As mentioned several times before, there are many successful research studies on animals in relation to rapamycin’s antiaging effects; however, there are only a few human studies to back it up. 

Not to mention, few human studies have mostly been conducted among small groups of patients and treatment regimens vary significantly between studies. Hence, there are still inconsistencies among the results. 

Although, some scientists may argue that there may be little to no risk of adverse effects from using rapamycin to fight aging; however, we still can’t determine how much rapamycin should we take and when to schedule and the varying effects of these two variables on a person. 

One thing we know for sure is that rapamycin has the potential to prolong longevity, improve quality of life and slow down aging but it is still early to celebrate yet. 

Final takeaways

Rapamycin’s ability to extend lifespan and enhance immune function in various model organisms is nothing short of extraordinary. It offers hope for a future where individuals can enjoy longer lives and healthier and more vibrant ones.

However, this optimism is tempered by the need for caution. Rapamycin’s immunosuppressive properties and potential side effects, such as gastrointestinal disturbances and metabolic effects, raise legitimate concerns. The long-term safety and efficacy of rapamycin in humans are still subjects of ongoing research.

As research continues to unveil its mysteries, the key lies in balancing the potential benefits and the associated risks. Only through informed decisions and careful oversight can we hope to harness the full potential of rapamycin.

FAQs

Is it safe to take rapamycin?

The safety of taking rapamycin for antiaging purposes is still being studied, and it should only be used under medical supervision and with regular monitoring due to potential side effects.

What does rapamycin do to your body?

Rapamycin inhibits mTOR, a protein that regulates cell growth and metabolism, which can slow down cellular aging processes.

What are the side effects of rapamycin in humans?

Common side effects of rapamycin in humans may include immunosuppression, gastrointestinal disturbances (such as diarrhea and nausea), skin problems (like rash and acne), and metabolic effects like increased cholesterol levels and insulin resistance.

[1] https://pubmed.ncbi.nlm.nih.gov/12742462/ 
[2] https://www.accessdata.fda.gov/drugsatfda_docs/nda/99/21083A.cfm 
[3] https://www.uptodate.com/contents/pharmacology-of-mammalian-mechanistic-target-of-rapamycin-mtor-inhibitors 
[4] https://pubmed.ncbi.nlm.nih.gov/33037985/ 
[5] https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3434687/ 
[6] https://pubmed.ncbi.nlm.nih.gov/19458476/
[7] https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2824086/ 
[8] https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6814615/ 
[9] https://www.sciencedirect.com/science/article/pii/S0014579310000360 
[10] https://aacrjournals.org/mct/article/15/3/347/92052/The-Enigma-of-Rapamycin-DosageRapamycin-Dosage 
[11] https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6949048/ 
[12] https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6925069/ 
[13] https://www.lifespan.io/topic/rapamycin-benefits-side-effects/ 
[14] https://www.naturemedclinic.com/weighing-the-anti-aging-benefits-of-rapamycin-against-possible-side-effects/

Photograph: drazenphoto/Envato
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