Drug reference
Rapamycin
Macrolide · Antiproliferative agent
Also known as Sirolimus
MacrolideAntiproliferative agent
CDSCO approvedSchedule H
EXCRETION
—
not curated
INTERACTIONS
—
none in our sources
PREGNANCY
—
not curated
Mechanism
Rapamycin (sirolimus) is a hydrophobic macrolide that binds to the cytosolic immunophilin FKBP12. The resulting FKBP12-sirolimus complex then inhibits the mammalian target of rapamycin (mTOR) kinase. This inhibition leads to the suppression of cell cycle progression and also affects various signaling pathways, including those where PKB (Akt) regulates mTOR and impacts proteins like Bad, important in apoptosis.
Indications
Prevention of in-stent restenosis (in drug-eluting intravascular stents)
Pharmacokinetics
Protein binding
Binds to intracellular proteins (e.g., FKBP12)
Metabolism
Metabolized by CYP3A4
Side effects
Serious
- Stent thrombosis (associated with drug-eluting stents, sometimes after discontinuation of antiplatelet therapy)
Related guidelines
Other Macrolide drugs
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Continue into a citation-backed clinical answer with the drug context already attached.
Sources: Katzung, Nelson, Harriet Lane·Verified: 2026-05-10 · House clinical team