Products
Sirolimus (rapamycin) is commercially available as coated tablets and as an oral solution (Rapamune). It has been approved in many countries since 2000.
Structure and properties
Sirolimus (C51H79NO13, Mr = 914.2 g/mol) is a large, lipophilic and complex molecule. It is a macrocyclic lactone extracted from. This fungus was originally identified in a soil sample from the Easter Islands (Rapa Nui). Sirolimus exists as a white powder that is insoluble in water.
Effects
Sirolimus (ATC L04AA10) has immunosuppressive properties. It inhibits the activation of T lymphocytes. The effects are due to binding to the intracellular protein FKBP12 (FK Binding Protein-12). The rapamycin-FKBP12 complex blocks the kinase mTor (mammalian Target Of Rapamycin), inhibiting T-cell proliferation.
Indications
For prevention of organ rejection after transplantation.
Dosage
According to the SmPC. The drug is taken once daily, regardless of meals. It should always be administered at the same time of day and always either with or without food to avoid fluctuations.
Contraindications
- Hypersensitivity
For complete precautions, see the drug label.
Interactions
Sirolimus is a substrate of CYP3A4 and P-glycoprotein. Corresponding drug-drug interactions are possible and pose a risk for graft rejection.
Adverse effects
The most common potential adverse effects include peripheral edema, hypertriglyceridemia, hypertension, hypercholesterolemia, abdominal pain, diarrhea, headache, fever, urinary tract infection, anemia, nausea, joint pain, aches, and thrombocythemia.
