Sirolimus: uses, dosing, side effects & brands
Sirolimus is a kinase inhibitor sold in the U.S. under 4 brand and generic names, for lymphangioleiomyomatosis and perivascular epithelioid cell neoplasms. Below: what the FDA label says, every product that contains it, what the pills look like, and its recall record.
Key facts
- Drug class
- Kinase Inhibitor
- Treats (across its forms)
- Lymphangioleiomyomatosis and Perivascular Epithelioid Cell Neoplasms
- Available as
- Solution · Injectable · Topical
- Sold as
- 4 products — Sirolimus, Fyarro and Hyftor, and others
- Prescription?
- Prescription only
- Generic available?
- Yes
- What the pharmacy pays
- about $49 for a 30-count supply — not your price
- Boxed warning
- Boxed warning
How Sirolimus is dosed
From the FDA label for Sirolimus (application ANDA211406). Other sirolimus products — different forms, different strengths — are dosed differently. Follow the label for the one you were prescribed.
Sirolimus oral solution is to be administered orally once daily, consistently with or without food [ see Dosage and Administration (2.5) , Clinical Pharmacology (12.3) ]. Renal Transplant Patients: Administer once daily by mouth, consistently with or without food ( 2 ). Administer the initial dose as soon as possible after transplantation and 4 hours after CsA ( 2.1 , 7.1 ). Adjust the sirolimus maintenance dose to achieve sirolimus trough concentrations within the target-range ( 2.5 ). Hepatic impairment: Reduce maintenance dose in patients with hepatic impairment ( 2.7 , 8.6 , 12.3 ). In renal transplant patients at low-to moderate-immunologic risk : Sirolimus Oral Solution and CsA Combination Therapy: One loading dose of 6 mg on day 1, followed by daily maintenance doses of 2 mg ( 2.2 ). Sirolimus Oral Solution Following CsA Withdrawal: 2 to 4 months post-transplantation, withdraw CsA over 4 to 8 weeks ( 2.2 ). In renal transplant patients at high-immunologic risk: Sirolimus Oral Solution and CsA Combination Therapy (for the first 12 months post-transplantation): One loading dose of up to 15 mg on day 1, followed by daily maintenance doses of 5 mg ( 2.3 ). Lymphangioleiomyomatosis Patients: Administer once daily by mouth, consistently with or without food ( 2 ). Recommended initial sirolimus dose is 2 mg/day ( 2.4 ). Adjust the sirolimus dose to achieve sirolimus trough…
Everything below is the FDA label for Sirolimus (solution). Sirolimus is also sold as injectable and topical, and those are different medicines to take — follow the label for the one you were prescribed.
Sirolimus side effects
The following adverse reactions are discussed in greater detail in other sections of the label. Increased susceptibility to infection, lymphoma, and malignancy [ see Boxed Warning , Warnings and Precautions (5.1) ] Excess mortality, graft loss, and hepatic artery thrombosis in liver transplant patients [ see Boxed Warning , Warnings and Precautions (5.2) ] Bronchial anastomotic dehiscence in lung transplant patients [ see Boxed Warning , Warnings and Precautions (5.3) ] Hypersensitivity reactions [ see Warnings and Precautions (5.4) ] Exfoliative dermatitis [ see Warnings and Precautions (5.4) ] Angioedema [ see Warnings and Precautions (5.5) ] Fluid accumulation and impairment of wound healing [ see Warnings and Precautions (5.6) ] Hypertriglyceridemia, hypercholesterolemia [ see Warnings and Precautions (5.7) ] Decline in renal function in long-term combination of cyclosporine with sirolimus [ see Warnings and Precautions (5.8) ] Proteinuria [ see Warnings and Precautions (5.9) ] Interstitial lung disease [ see Warnings and Precautions (5.11) ] Increased risk of calcineurin inhibitor-induced HUS/TTP/TMA [ see Warnings and Precautions (5.13) ]. Embryo-fetal toxicity [see Warnings and Precautions ( 5.15 )] Male infertility [see Warnings and Precautions ( 5.16 )] The most common (≥ 30%) adverse reactions observed with sirolimus in clinical studies for organ rejection…
Who shouldn’t take Sirolimus
Sirolimus oral solution is contraindicated in patients with a hypersensitivity to sirolimus [ see Warnings and Precautions (5.4) ]. Hypersensitivity to sirolimus ( 4 ).
Sirolimus drug interactions
Sirolimus is known to be a substrate for both cytochrome P-450 3A4 (CYP3A4) and p-glycoprotein (P-gp). Inducers of CYP3A4 and P-gp may decrease sirolimus concentrations whereas inhibitors of CYP3A4 and P-gp may increase sirolimus concentrations. Avoid concomitant use with strong CYP3A4/P-gp inducers or strong CYP3A4/P-gp inhibitors that decrease or increase sirolimus concentrations ( 7.4 , 12.3 ). Therapeutic drug monitoring and dose reduction for sirolimus should be considered when sirolimus is co-administered with cannabidiol ( 5.21 , 7.5 ). See full prescribing information for complete list of clinically significant drug interactions ( 12.3 ). 7.1 Use with Cyclosporine Cyclosporine, a substrate and inhibitor of CYP3A4 and P-gp, was demonstrated to increase sirolimus concentrations when co-administered with sirolimus. In order to diminish the effect of this interaction with cyclosporine, it is recommended that sirolimus be taken 4 hours after administration of cyclosporine oral solution (MODIFIED) and/or cyclosporine capsules (MODIFIED). If cyclosporine is withdrawn from combination therapy with sirolimus, higher doses of sirolimus are needed to maintain the recommended sirolimus trough concentration ranges [ see Dosage and Administration (2.2) , Clinical Pharmacology (12.3) ]. 7.2 Strong Inducers and Strong Inhibitors of CYP3A4 and P-gp Avoid concomitant use of sirolimus with strong inducers (e.g., rifampin, rifabutin) and strong inhibitors (e.g., ketoconazole, voriconazole, itraconazole, erythromycin, telithromycin, clarithromycin) of CYP3A4 and P-gp. Alternative agents with lesser interaction potential with sirolimus should be considered [see Warnings and Precautions ( 5.20 ), Clinical Pharmacology ( 12.3 )]. 7.3 Grapefruit Juice Because grapefruit juice inhibits the CYP3A4-mediated metabolism of sirolimus, it must not be taken with or be used for dilution of sirolimus [ see Dosage and Administration (2.9) , Drug Interactions (7.3) , Clinical Pharmacology (12.3) ]. 7.4 Weak and Moderate Inducers or Inhibitors of CYP3A4 and P-gp Exercise caution when using sirolimus with drugs or agents that are modulators of CYP3A4 and P-gp. The dosage of sirolimus and/or the co-administered drug may need to be adjusted [ see Clinical Pharmacology (12.3) ]. Drugs that could increase sirolimus blood concentrations: Bromocriptine, cimetidine, cisapride, clotrimazole, danazol, diltiazem, fluconazole, letermovir, protease inhibitors (e.g., HIV and hepatitis C that include drugs such as ritonavir, indinavir, boceprevir, and telaprevir), metoclopramide, nicardipine, troleandomycin, verapamil Drugs and other agents that could decrease sirolimus concentrations: Carbamazepine, phenobarbital, phenytoin, rifapentine, St. John's Wort ( Hypericum perforatum ) Drugs with concentrations that could increase when given with sirolimus: Verapamil 7.5 Cannabidiol The blood levels of sirolimus may increase upon concomitant use with cannabidiol. When cannabidiol and sirolimus are co-administered, closely monitor for an increase in sirolimus blood levels and for adverse reactions suggestive of sirolimus toxicity. A dose reduction of sirolimus should be considered as needed when sirolimus is co-administered with cannabidiol [see Dosage and Administration ( 2.5 ) and Warnings and Precautions ( 5.21 )].
Every sirolimus product we track (4)
Same active ingredient — different manufacturer, form, price and FDA recall record. That last one is what our independent score measures.
| # | Drug | Rating | Type | Form | Generic? | Pharmacy pays | |
|---|---|---|---|---|---|---|---|
| 1 | 66/100 | Prescription | Solution | Generic | $49 | View → | |
| 2 | Not yet rated | Prescription | Injectable | Generic | $49 | View → | |
| 3 | Not yet rated | Prescription | Topical | Generic | $49 | View → | |
| 4 | Not yet rated | Prescription | Solution | Generic | $49 | View → |
What sirolimus pills look like
Imprint codes, colour and shape from the FDA’s labelling data. Match the imprint on your pill — or search any imprint.
| Imprint | Strength | Colour | Shape | Maker |
|---|---|---|---|---|
| 1 | 0.5 mg | yellow | round | — |
| Y;7 | 0.5 mg | gray | round | — |
| Y;77 | 1 mg | white | round | — |
| Y;71 | 2 mg | yellow | round | — |
| RAPAMUNE;05;MG | 0.5 mg | brown | triangle | — |
| RAPAMUNE;1;MG | 1 mg | white | triangle | — |
| RAPAMUNE;2;MG | 2 mg | yellow | triangle | — |
Sirolimus recalls
From the FDA Enforcement database. A recall covers specific lots — not the drug as a whole.
Can you crush or split sirolimus?
At least one sirolimusproduct is labelled to be swallowed whole — crushing an extended-release tablet releases the whole day’s dose at once. Which applies depends on the form you were given.
What each sirolimus label says about crushing, splitting and chewingHow long sirolimus keeps
No sirolimus label we read sets a separate limit for after opening, but they do specify how it must be stored — and the stability behind any date assumes those conditions.
Does sirolimus expire? The in-use limits and storage rules from its labelsSirolimus and breastfeeding
From LactMed, the US National Library of Medicine’s Drugs and Lactation Database — quoted, not rewritten.
Full LactMed record for sirolimus: levels in milk, effects in breastfed infants, and the drugs it would consider insteadBecause almost no information is available on the use of oral sirolimus during breastfeeding, an alternate drug may be preferred, especially while nursing a newborn or preterm infant.
National Institute of Child Health and Human Development, record revised August 15, 2025. LactMed states its information is not a substitute for professional judgement.
What people report to the FDA about sirolimus
The FDA Adverse Event Reporting System (FAERS) collects reports from patients and clinicians. It holds 13,670 reports naming sirolimus, and the FDA flagged 86% of those reports as serious. The effects reported most often — leaving out reports about overdose, misuse or the condition being treated, which dominate the raw list for common medicines:
- diarrhoea551 reports
- pyrexia550 reports
- pneumonia502 reports
- acute kidney injury429 reports
- thrombotic microangiopathy377 reports
- transplant rejection371 reports
- cytomegalovirus infection350 reports
- nausea324 reports
Read these as a signal, not a rate. A report does not mean sirolimus caused the effect — anyone can file one, and many describe people taking several medicines for several conditions. Crucially there is no denominator: FAERS does not record how many people took the drug, so these counts cannot be turned into “X% of patients” — a bigger number often just means a more widely used or more talked-about drug. Duplicates exist, and publicity drives reporting. For what is actually established, read the FDA label section above.
Source: openFDA drug/event (FAERS), retrieved July 26, 2026.
Related calculators
Frequently asked questions
What is Sirolimus?
Sirolimus is an mTOR inhibitor immunosuppressive agent. Sirolimus is a macrocyclic lactone produced by Streptomyces hygroscopicus.
What kind of drug is sirolimus?
The FDA classifies sirolimus as a kinase inhibitor. Kinase inhibitors block protein kinases, the enzymes that relay 'grow and divide' signals inside cells. By shutting down the overactive kinase signals that a tumor depends on, they help slow or stop cancer cells from multiplying. If you are checking whether it is safe to combine with something else, the class is what matters — two drugs from the same class usually should not be stacked.
Can you take sirolimus with other medicines?
It depends on the medicine. We check it against the FDA labels rather than guessing: our interaction checker searches each drug's own label for the other and quotes what it says, naming the section it came from. Run sirolimus against whatever else you take — and remember that a label not naming a drug is not the same as that combination being safe.
What brand names is sirolimus sold under?
We track 4 sirolimus-containing products in the U.S.: Sirolimus, Fyarro, Hyftor and Rapamune. They are the same active ingredient; they differ in form, manufacturer, price and FDA recall record.
What forms does sirolimus come in?
Across the brands we track, sirolimus is currently marketed as solution, injectable and topical, per the FDA's National Drug Code Directory. Each form is dosed differently — follow the label for the exact product you were prescribed.
Is there a generic sirolimus?
Yes. Our catalog lists 1 generic sirolimus product alongside the brand versions. A generic has the same active ingredient and must meet the FDA's bioequivalence standard; it usually costs less. Ask your pharmacist which one your plan covers.
Has sirolimus been recalled?
The FDA's Enforcement database lists 1 recall record whose product description mentions sirolimus. The most recent: Sirolimus Tablets 1mg Tablets 100-count bottle (May 1, 2024). A recall applies to specific lots, not to the drug as a whole — check the record for the affected lot numbers.
Cite this page
- APA
- pharmaranks. (2026, July 24). Sirolimus: uses, dosing, side effects & brands. https://pharmaranks.com/drugs/sirolimus
- MLA
- “Sirolimus: uses, dosing, side effects & brands.” pharmaranks, 24 July 2026, https://pharmaranks.com/drugs/sirolimus.
We summarise public FDA and NIH sources — for a clinical claim, cite the primary source we link to as well.
Sources: FDA openFDA drug label, National Drug Code Directory, and Enforcement (recall) database. This page reproduces public FDA data and is not medical advice. Dosing is set by your prescriber.
Read the full FDA label for sirolimus on DailyMed (NIH) ↗ — including its boxed warning in full.