Selective immunosuppressant, mTOR inhibitor
ATC code: L04AA10 (Sirolimus)
Brand names
Rapamune
Sirolimus (rapamycin) binds FKBP-12 and blocks the mTORC1 complex (mammalian target of rapamycin complex 1), halting T-cell progression from G1 to S phase and suppressing cytokine-driven proliferation. It is used after kidney transplantation, in lymphangioleiomyomatosis, and in neuroendocrine tumours. Sirolimus is a CYP3A4 and P-glycoprotein substrate with a very narrow therapeutic window (target trough 4–12 ng/mL depending on indication). Strong CYP3A4 inhibitors or inducers shift concentrations sharply, so therapy proceeds under whole-blood level monitoring.
Second line
mTOR inhibitor for maintenance immunosuppression after organ transplantation. AEMPS positions sirolimus as an alternative or adjunct to calcineurin inhibitors to reduce nephrotoxicity.
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FDA Category C. mTOR inhibitors show embryo- and fetotoxicity in animal models. Human experience in transplant recipients is limited; AEMPS requires effective contraception during and 12 weeks after therapy. When pregnancy is established, switching to tacrolimus or cyclosporine under the transplant team is preferred.
Not compatible. Hale L4. No human milk transfer data; potential immunosuppressive effect on the infant. AEMPS contraindicates breastfeeding during sirolimus therapy.
Reference information, not a clinical decision. Discuss feeding pauses or changes with your physician or an IBCLC.
Sirolimus is evaluated for the following indications with varying evidence strength: Maintenance immunosuppression after organ transplantation (evidence tier A). See the full indication matrix with dosing and citations above on this page.
Common side effects of Sirolimus (≥ 1 in 100): Hypertriglyceridaemia and hypercholesterolaemia, Hypertension, Anaemia, thrombocytopenia, leukopenia, Oedema, Stomatitis and mouth ulcers, Acne. See the Safety section for uncommon and serious reactions.
FDA category C. FDA Category C. mTOR inhibitors show embryo- and fetotoxicity in animal models. Human experience in transplant recipients is limited; AEMPS requires effective contraception during and 12 weeks after therapy. When pregnancy is established, switching to tacrolimus or cyclosporine under the transplant team is preferred.
Not compatible. Hale L4. No human milk transfer data; potential immunosuppressive effect on the infant. AEMPS contraindicates breastfeeding during sirolimus therapy.
Sirolimus is contraindicated in: Hypersensitivity to sirolimus; Severe active infections; Severe hypertriglyceridaemia; Co-administration with grapefruit and grapefruit juice. Full list in the Safety section.