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ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › PROTEIN KINASE INHIBITORS › Mammalian target of rapamycin (mTOR) kinase inhibitors
sirolimus
L01EG04
Forms & Strengths
- Oral tablet: 0.5 mg, 1 mg, 2 mg
- Oral solution: 1 mg/mL
Adult Dosing
- Renal transplant (de novo): Loading dose 6 mg once, then 2 mg PO daily adjusted to target trough levels
- Renal transplant (maintenance): 2 mg PO daily, adjusted based on therapeutic drug monitoring
- Lymphangioleiomyomatosis (LAM): Initial 2 mg PO daily, target trough 5-15 ng/mL
Pediatric Dosing
- Children >= 13 years (renal transplant): Loading dose 3 mg/m2, then 1 mg/m2/day PO adjusted to target trough levels
Indications
- Prophylaxis of organ rejection in renal transplantation
- Lymphangioleiomyomatosis (LAM)
Mechanism of Action
- Inhibits mammalian target of rapamycin (mTOR) kinase
- Suppresses cytokine-driven T-cell proliferation
- Inhibits calcineurin-independent signal transduction pathways
Contraindications
- Hypersensitivity to sirolimus or its derivatives
- Lung transplantation (increased mortality, graft loss, and bronchial anastomotic dehiscence)
- Liver transplantation (associated with hepatic artery thrombosis and graft loss)
Adverse Reactions
- Peripheral edema, hypertension, hyperlipidemia, hypercholesterolemia
- Thrombocytopenia, leukopenia, anemia
- Diarrhea, nausea, abdominal pain
- Increased risk of infections and malignancies (lymphomas, skin cancers)
- Interstitial lung disease / pneumonitis
- Impaired wound healing
Drug Interactions
- Strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin) significantly increase sirolimus exposure
- Strong CYP3A4 inducers (e.g., rifampin, St. John's wort) significantly decrease sirolimus concentrations
- Cyclosporine increases sirolimus blood concentrations (administer 4 hours apart)
- Live vaccines (avoid concomitant use due to immunosuppression)
Curated Content: Needs Vetting Before Put to Clinical Use