Mechanism of action
From the NCI Drug Dictionary: A natural macrocyclic lactone produced by the bacterium Streptomyces hygroscopicus, with immunosuppressant properties. In cells, sirolimus binds to the immunophilin FK Binding Protein-12 (FKBP-12) to generate an immunosuppressive complex that binds to and inhibits the activation of the mammalian target of rapamycin (mTOR), a key regulatory kinase. This results in inhibition of T lymphocyte activation and proliferation that occurs in response to antigenic and cytokine (IL-2, IL-4, and IL-15) stimulation and inhibition of antibody production.
Diseases for which it is used
Also known as
- Code names: AY 22989, SILA 9268A, SLM, WY-090217
- Generic names: RAPA, rapamycin
- Brand name: Rapamune