Rapamycin

What it is

• Rapamycin is another name for sirolimus, which is sold under the brand name Rapamune.
• Sirolimus belongs to a class of drugs called immunosuppressants.
• The label calls sirolimus an mTOR inhibitor immunosuppressant.

Sources: MedlinePlus (NIH): Sirolimus: MedlinePlus Drug Information ↗ · DailyMed (FDA drug label): DailyMed - SIROLIMUS tablet, sugar coated ↗

How it's thought to work

It works by suppressing the body's immune system. In lab studies, mTOR inhibitors like sirolimus blocked certain growth factors that may affect blood vessel growth, scar-forming cells, and vessel leakiness.

Sources: MedlinePlus (NIH): Sirolimus: MedlinePlus Drug Information ↗ · DailyMed (FDA drug label): DailyMed - SIROLIMUS tablet, sugar coated ↗

What people use it for

• It is used with other medicines to prevent rejection of kidney transplants.
• It is also used to treat lymphangioleiomyomatosis, a rare lung condition.
• It is sometimes used to prevent organ rejection in people with heart, pancreas, or intestinal transplants.

Source: MedlinePlus (NIH): Sirolimus: MedlinePlus Drug Information ↗

What the research has found so far

Extends lifespan in mice. Human studies so far are small.

On Rapamycin and aging, PubMed lists 25 trials in people, 36 studies that watched people over time, 1,020 animal and lab studies. See the counts and searches

Side effects and risks

• Common side effects listed include stomach pain, headache, constipation, diarrhea, nausea, joint or muscle pain, mouth sores, and acne.
• In transplant patients, the most common reactions (30% or more) included swelling in the limbs, high blood fats, high blood pressure, fever, urinary infection, anemia, and low platelets.
• Sirolimus may raise the risk of cancer, especially lymphoma or skin cancer.
• Cholesterol and triglycerides rose more often in sirolimus patients than in placebo patients.
• Reports include slow or delayed wound healing.
• Serious lung disease, some fatal, has occurred in people on regimens including sirolimus.
• It may cause too little or no sperm in men.
• Sirolimus has been linked to allergic reactions and swelling under the skin called angioedema.
• Increased protein in the urine was commonly seen in patients switched to sirolimus.

Sources: MedlinePlus (NIH): Sirolimus: MedlinePlus Drug Information ↗ · DailyMed (FDA drug label): DailyMed - SIROLIMUS tablet, sugar coated ↗

Who should be careful, and drug interactions

• People should not become pregnant while taking it, and it may harm the fetus.
• Birth control is described for before, during, and 12 weeks after treatment.
• It may lower fertility in men and women.
• The label says breastfed infants could have serious effects.
• The page lists cimetidine, St. John's wort, and cannabidiol as products that may interact with it.
• The page says cyclosporine is taken 4 hours before sirolimus.
• The label says to avoid strong CYP3A4/P-gp inducers or inhibitors, which change sirolimus levels.
• Using ACE inhibitors with sirolimus may raise the risk of angioedema.
• Taking sirolimus with cholesterol drugs called HMG-CoA reductase inhibitors led to muscle-related reactions.
• The page says to tell doctors about high cholesterol or triglycerides, diabetes, or liver disease.
• The page says to tell the doctor or dentist about sirolimus before surgery.
• The label says live vaccines should be avoided.
• The page says to avoid grapefruit juice with this medicine.
• People with a BMI over 30 may be at higher risk of abnormal wound healing.
• It is contraindicated in people with a hypersensitivity (allergy) to sirolimus.

Sources: MedlinePlus (NIH): Sirolimus: MedlinePlus Drug Information ↗ · DailyMed (FDA drug label): DailyMed - SIROLIMUS tablet, sugar coated ↗

Amounts used in studies

What studies or labels describe, not a recommendation.

• It comes as a tablet and a liquid solution taken by mouth once a day.
• The label lists tablets of 0.5 mg, 1 mg, and 2 mg.
• For kidney transplant patients at low to moderate risk, the label lists a 6 mg loading dose on day 1, then 2 mg daily.
• For high-risk kidney transplant patients, the label lists a loading dose of up to 15 mg, then 5 mg daily.
• For lymphangioleiomyomatosis, the label lists an initial dose of 2 mg a day.

Sources: MedlinePlus (NIH): Sirolimus: MedlinePlus Drug Information ↗ · DailyMed (FDA drug label): DailyMed - SIROLIMUS tablet, sugar coated ↗

Roughly what it costs

We don't have prices for this yet.

Questions to ask your doctor

• Is Rapamycin a sensible option for me, given my health and the medicines I take?
• Could Rapamycin interact with any medicine or supplement I already take?
• What side effects should I watch for, and when should I stop or call you?
• Would Rapamycin be used for its approved purpose, or off-label for aging?
• How would we tell whether it is helping, and when should we review it?