Sorry, you need to enable JavaScript to visit this website.

RAPAMUNE® (sirolimus) Highlights

HIGHLIGHTS OF PRESCRIBING INFORMATION

These highlights do not include all the information needed to use RAPAMUNE safely and effectively. See full prescribing information for RAPAMUNE.

RAPAMUNE (sirolimus) oral solution
RAPAMUNE (sirolimus) tablets, for oral use
Initial U.S. Approval: 1999

WARNING: IMMUNOSUPPRESSION, USE IS NOT RECOMMENDED IN LIVER OR LUNG TRANSPLANT PATIENTS

See full prescribing information for complete boxed warning.

  • Increased susceptibility to infection and the possible development of lymphoma and other malignancies may result from immunosuppression (5.1). Only physicians experienced in immunosuppressive therapy and management of renal transplant patients should use Rapamune for prophylaxis of organ rejection in patients receiving renal transplants.
  • The safety and efficacy of Rapamune as immunosuppressive therapy have not been established in liver or lung transplant patients, and therefore, such use is not recommended (5.2, 5.3).
    Liver Transplantation – Excess mortality, graft loss, and hepatic artery thrombosis (5.2).
    Lung Transplantation – Bronchial anastomotic dehiscence (5.3).

RECENT MAJOR CHANGES

Warnings and Precautions, Male Infertility (5.16) 7/2019
Warnings and Precautions, Immunizations (5.19) 7/2019

INDICATIONS AND USAGE

  • Rapamune is an mTOR inhibitor immunosuppressant indicated for the prophylaxis of organ rejection in patients aged ≥13 years receiving renal transplants:
    • Patients at low- to moderate-immunologic risk: Use initially with cyclosporine (CsA) and corticosteroids. CsA withdrawal is recommended 2–4 months after transplantation (1.1).
    • Patients at high-immunologic risk: Use in combination with CsA and corticosteroids for the first 12 months following transplantation (1.1). Safety and efficacy of CsA withdrawal has not been established in high risk patients (1.1, 1.2, 14.3).
  • Rapamune is an mTOR inhibitor indicated for the treatment of patients with lymphangioleiomyomatosis (1.3).

DOSAGE AND ADMINISTRATION

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 Rapamune 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:

  • Rapamune and CsA Combination Therapy: One loading dose of 6 mg on day 1, followed by daily maintenance doses of 2 mg (2.2).
  • Rapamune Following CsA Withdrawal: 2–4 months post-transplantation, withdraw CsA over 4–8 weeks (2.2).

In renal transplant patients at high-immunologic risk:

  • Rapamune 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 Rapamune dose is 2 mg/day (2.4).
  • Adjust the Rapamune dose to achieve sirolimus trough concentrations between 5–15 ng/mL (2.4).
  • Hepatic impairment: Reduce maintenance dose in patients with hepatic impairment (2.7, 8.6, 12.3).

Therapeutic drug monitoring is recommended for all patients (2.5, 5.17).

DOSAGE FORMS AND STRENGTHS

  • Oral Solution: 60 mg per 60 mL in amber glass bottle (3.1).
  • Tablets: 0.5 mg, 1 mg, 2 mg (3.2).

CONTRAINDICATIONS

Hypersensitivity to Rapamune (4).

WARNINGS AND PRECAUTIONS

  • Hypersensitivity Reactions (5.4)
  • Angioedema (5.5)
  • Fluid Accumulation and Impairment of Wound Healing (5.6)
  • Hyperlipidemia (5.7)
  • Decline in Renal Function (5.8)
  • Proteinuria (5.9)
  • Latent Viral Infections (5.10)
  • Interstitial Lung Disease/Non-Infectious Pneumonitis (5.11)
  • De Novo Use Without Cyclosporine (5.12)
  • Increased Risk of Calcineurin Inhibitor-Induced Hemolytic Uremic Syndrome/ Thrombotic Thrombocytopenic Purpura/ Thrombotic Microangiopathy (5.13)
  • Embryo-Fetal Toxicity: Can cause fetal harm. Use of highly effective contraception is recommended for females of reproductive potential during treatment and for 12 weeks after final dose of Rapamune (5.15, 8.1)
  • Male Infertility: Azoospermia or oligospermia may occur (5.16, 13.1)
  • Immunizations: Avoid live vaccines (5.19)

ADVERSE REACTIONS

Prophylaxis of organ rejection in patients receiving renal transplants: Most common adverse reactions (incidence ≥30%) are peripheral edema, hypertriglyceridemia, hypertension, hypercholesterolemia, creatinine increased, abdominal pain, diarrhea, headache, fever, urinary tract infection, anemia, nausea, arthralgia, pain, and thrombocytopenia (6).

Lymphangioleiomyomatosis: Most common adverse reactions (incidence ≥20%) are stomatitis, diarrhea, abdominal pain, nausea, nasopharyngitis, acne, chest pain, peripheral edema, upper respiratory tract infection, headache, dizziness, myalgia, and hypercholesterolemia (6.6).


To report SUSPECTED ADVERSE REACTIONS, contact Pfizer Inc. at 1-800-438-1985 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.

DRUG INTERACTIONS

  • 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).
  • See full prescribing information for complete list of clinically significant drug interactions (12.3).

USE IN SPECIFIC POPULATIONS

  • Pregnancy: Based on animal data can cause fetal harm (5.15, 8.1).
  • Lactation: Potential for serious adverse effects in breastfed infants based on mechanism of action (8.2).
  • Females and Males of Reproductive Potential: May impair fertility (8.1. 8.3, 13.1).

See 17 for PATIENT COUNSELING INFORMATION and Medication Guide.

Revised: 8/2019

What's New

No Current Announcements.

Contact Pfizer Medical

Report an Adverse Event
1-800-438-1985

Meet Our Team

Contact Pfizer

Need to report an Adverse Event, Side Effect or Product Quality Concern?

Contact Pfizer Safety to report an adverse event, side effect or concern about the quality of a Pfizer product: (800) 438-1985

You may also contact the U.S. Food and Drug Administration (FDA) directly to report adverse events or product quality concerns at 1-800-FDA-1088 or www.fda.gov/MedWatch

Have a Medical Question on a Pfizer Prescription Medicine?
Contact Pfizer Medical Information to speak with a professional regarding your medical question on a Pfizer prescription product: (800) 438-1985
Have a Question on a Pfizer Over-the-Counter Product?
For Pfizer Consumer Healthcare non-prescription or over-the-counter products such as Advil, Centrum, Nexium or Thermacare, call (800) 322-3129
Have a Question about Pfizer Clinical Trials?
If you are looking for information about Pfizer studies currently recruiting new patients in your area, you can begin your search on our website. For questions about a Pfizer Clinical Trial, call (800) 718-1021 or email [email protected]
Need Information on Pfizer’s Patient Assistance Programs?

Pfizer RxPathways® connects eligible patients, regardless of their insurance status, to a range of assistance programs that offer insurance support, co-pay help, and medicines for free or at a savings. For more information, please call (844) 989-7284 or visit www.PfizerRxPathways.com.

Eligible patients can register for valuable savings offers for nearly 40 brand name medications. Visit www.MyPfizerBrands.com for more information.