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Sirolimus

    Brands

    DEA Class; Rx

    Common Brand Names; Rapamune

    • Immunosuppressants

    sirolimus topical (Rx)

    Brand and Other Names: Hyftor
    • Classes: Dermatologics, mTOR Inhibitors

    sirolimus protein bound (Rx)

    Brand and Other Names: Fyarro
    • Classes: Antineoplastics, mTOr Kinase Inhibitor
     

    Immunosuppressant; analog of tacrolimus
    Oral formulations for prophylaxis of organ rejection in renal transplant patients and for lymphangioleiomyomatosis; topical gel for facial angiofibroma associated with tuberous sclerosis
    Acts synergistically with other immunosuppressants with little overlapping toxicity; may reduce the incidence of chronic rejection

    Indicated for kidney transplant rejection prophylaxis.

    For the treatment of lymphangioleiomyomatosis.
    For the treatment of facial angiofibroma associated with tuberous sclerosis complex.
    For the management of heart transplant rejection prophylaxis.

    Indicated for treatment of facial angiofibroma associated with tuberous sclerosis

    Indicated for locally advanced or metastatic malignant perivascular epithelioid cell tumor (PEComa)

    Hypersensitivity to sirolimus or macrolide antibiotics

    Concomitant live vaccines

    • Peripheral edema, w/ corticosteroids (54-58%)
    • Hypertriglyceridemia (45-57%; up to 90% when used with or following cyclosporine)
    • Hypercholesterolemia (43-46%; up to 90% when used with or following cyclosporine)
    • Constipation (36-38%)
    • Arthralgia (25-31%)
    • Thrombocytopenia (14-30%)
    • Rash (10-20%)
    • Hypertension (45-49%)
    • Increased creatinine (39-40%)
    • Abdominal pain (29-36%)
    • Diarrhea (25-35%)
    • Headache (34%)
    • Fever (23-34%)
    • Urinary tract infection (26-33%)
    • Anemia (23-33%)
    • Nausea (25-31%)
    • Arthralgia (25-31%)
    • Pain (29-33%)
    • Acne (22%)
    • Edema (18-20%)
    • Sepsis (<20%)
    • Lymphocele (<20%)
    • Venous thromboembolism (<20%)
    • Tachycardia (<20%)
    • Stomatitis (<20%)
    • Thrombotic thrombocytopenic purpura/hemolytic uremic syndrome (<20%)
    • Leukopenia (<20%)
    • Abnormal healing (<20%)
    • Increased lactic dehydrogenase (<20%)
    • Hypokalemia (<20%)
    • Hypophoaphatemia (<20%)
    • Hyperglycemia (<20%)
    • Diabetes mellitus (<20%)
    • Bone necrosis (<20%)
    • Pneumonia (<20%)
    • Epistaxis (<20%)
    • Melanoma (<20%)
    • Squamous cell carcinoma (<20%)
    • Basal cell carcinoma (<20%)
    • Pyelonephritis (<20%)
    • Ovarian cysts (<20%)
    • Menstrual disorders (amenorrhea and menorrhagia) (<20%)

    Hypersensitivity reactions, including anaphylactic/anaphylactoid reactions, angioedema, exfoliative dermatitis, and hypersensitivity vasculitis, have been associated with the administration of this drug

    Not for liver or lung transplant

    Exposure to sunlight and ultraviolet (UV) light should be limited by wearing protective clothing and using a broad spectrum sunscreen with a high protection factor

    Progressive multifocal leukoencephalopathy (PML), sometimes fatal, have been reported; commonly presents with hemiparesis, apathy, confusion, cognitive deficiencies, and ataxia

    Based on animal studies and mechanism of action, therapy may cause fetal harm when administered to a pregnant woman; in animal studies, mTOR inhibitors caused embryo- fetal toxicity when administered during period of organogenesis at maternal exposures that were equal to or less than human exposures at recommended lowest starting dose; advise pregnant women of potential risk to a fetus; advise women of childbearing potential to avoid becoming pregnant and to use effective contraception while on therapy and for 12 weeks after ending treatment

    Associated with development of angioedema; concomitant use of other drugs known to cause angioedema, such as angiotensin-converting enzyme (ACE) inhibitors, may increase risk of developing angioedema; elevated sirolimus levels (with/without concomitant ACE inhibitors) may potentiate angioedema; in some cases, angioedema has resolved upon discontinuation or therapy dose reduction

    Consult lab regarding type of assay for drug monitoring; whole blood concentrations are being measured by various chromatographic and immunoassay methodologies; sample concentration values from different assays may not be interchangeable

    Can cause fetal harm when administered to pregnant women based on animal studies and the mechanism of action

    Data are not available regarding the presence in human milk, the effects on breastfed infants, or the effects on milk production

    Adults

    40 mg per day PO; 800 mg (2.5 cm) per day for topical gel.

    Geriatric

    40 mg per day PO; 800 mg (2.5 cm) per day for topical gel.

    Adolescents

    40 mg per day PO; 800 mg (2.5 cm) per day for topical gel.

    Children

    12 years: 800 mg (2.5 cm) per day for topical gel; safety and efficacy of oral formulations have not been established.
    6 to 11 years: 600 mg (2 cm) per day for topical gel; safety and efficacy of oral formulations have not been established.
    1 to 5 years: Safety and efficacy have not been established.

    Infants

    Safety and efficacy have not been established.

    Neonates

    Safety and efficacy have not been established.

    Sirolimus 

    tablet

    • 0.5mg
    • 1mg
    • 2mg

    oral solution

    • 1mg/mL

    topical gel

    • 0.2%

    injection, lyophilized powder for reconstitution

    • 100mg/vial