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Rapamycin (Sirolimus)

Rapamune

Macrolide mTORC1 inhibitor, FDA-approved for transplant rejection and LAM; weekly off-label dosing extends lifespan in mice and showed benefits in the PEARL human trial.

◆ Editorial note

Macrolide small molecule. FKBP12/mTORC1 inhibitor.

§ 01   Overview

Overview

Macrolide mTORC1 inhibitor, FDA-approved for transplant rejection and LAM; weekly off-label dosing extends lifespan in mice and showed benefits in the PEARL human trial.

FDA-approved for transplant rejection (1999) and LAM (2015). PEARL RCT (2025) is the first human longevity-endpoint trial.

§ 02   Mechanism

Mechanism of action

Rapamycin forms a complex with FKBP12 that inhibits mTORC1, dampening cell growth and protein synthesis pathways and activating autophagy. Intermittent dosing preserves mTORC1 recovery and appears to avoid mTORC2-related metabolic side effects.

  • 01Extends mouse lifespan (Harrison 2009 and later)
  • 02Improves physical and cognitive markers (PEARL trial)
  • 03Potential senomorphic + autophagy-inducing effects

§ 03   Dosing

Dosing protocol

Standard Protocol

Dose Range
6 mg weekly (off-label longevity protocols)
Route
Oral
Timing
Same day weekly
Frequency
Weekly
Cycle
Continuous; reassess IGF-1, lipids, glucose

§ 04   Evidence

Evidence & research

Established

FDA-approved for transplant rejection (1999) and LAM (2015). PEARL RCT (2025) is the first human longevity-endpoint trial.

FDA Status

FDA-approved (Rapamune NDA 021083) for transplant rejection and LAM.

§ 06   News

In the news

4 articles from the last 12 months · updates hourly

§ 07   Sourcing

Sourcing & supply

Regulatory status

FDA-approved

This compound has an FDA approval for at least one indication. Brand pharmacy channels exist. Compounding may or may not be available depending on shortage status.

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§ 09   Safety

Safety & side effects

Side effects

  • 01Mouth ulcers
  • 02Immunosuppression at higher / daily dosing
  • 03Dyslipidemia and glucose elevations

Contraindications

  • 01Active infection
  • 02Pregnancy

§ 10   Questions

Rapamycin (Sirolimus) FAQ

What is Rapamycin (Sirolimus)?
Macrolide mTORC1 inhibitor, FDA-approved for transplant rejection and LAM; weekly off-label dosing extends lifespan in mice and showed benefits in the PEARL human trial. Rapamycin forms a complex with FKBP12 that inhibits mTORC1, dampening cell growth and protein synthesis pathways and activating autophagy. Intermittent dosing preserves mTORC1 recovery and appears to avoid mTORC2-related metabolic side effects.
What is Rapamycin (Sirolimus) used for?
Reported uses include extends mouse lifespan (harrison 2009 and later), improves physical and cognitive markers (pearl trial), and potential senomorphic + autophagy-inducing effects. Evidence strength is rated Established — see the evidence section for detail.
How is Rapamycin (Sirolimus) dosed?
Commonly referenced dosing is 6 mg weekly (off-label longevity protocols), administered Oral. This is educational reference only; consult a licensed clinician before use.
What are the side effects of Rapamycin (Sirolimus)?
Commonly reported side effects include mouth ulcers, immunosuppression at higher / daily dosing, and dyslipidemia and glucose elevations. This list is not exhaustive.
Is Rapamycin (Sirolimus) legal?
This compound has an FDA approval for at least one indication. Brand pharmacy channels exist. Compounding may or may not be available depending on shortage status. FDA status: FDA-approved (Rapamune NDA 021083) for transplant rejection and LAM..

§ 11   References

Selected references

  1. 01

    Harrison Nature — mouse lifespan

    PMID: 19587680

  2. 02

    PEARL trial

    PMID: 40188830 (NCT04488601)

This site is for educational and research purposes only. It does not constitute medical advice. Always consult a qualified healthcare provider before using any peptide or supplement.