Sirolimus is an mTOR inhibitor. It binds to FK506 binding protein (FKBP) which leads to the inhibition of mTOR kinase. mTOR is mechanistic / mammalian target of rapamycin.
Sirolimus functions as a proliferation signal inhibitor by targeting the mTOR signaling pathway, an important stimulator of cell growth and proliferation. Sirolimus binds to FKBP, forming a complex that inhibits mTOR. This leads to interruption of IL-2 signal transduction, which decreases T-cell activation.
By inhibiting the mTOR signaling pathway, Sirolimus leads to interruption of IL-2 signal transduction, preventing G1 to S phase progression and B cell differentiation. Inhibition of B-cell differentiation leads to decreased production of IgM, IgG, and IgA antibodies.
Sirolimus is used in drug-eluting stents which decreases restenosis but increases thrombosis risk.
Sirolimus is used in kidney transplant patients to prevent rejection. As rejection is an autoimmune process that is often mediated by T cells, their inhibition by sirolimus decreases the incidence of rejection.
Sirolimus can cause pancytopenia, which is a decrease in the number of all blood cell types (white blood cells, red blood cells, and platelets).
Chronic use of sirolimus can cause insulin resistance.
Sirolimus can lead to hyperlipidemia and an increased risk of cardiovascular disease.
Picmonic's rapid review multiple-choice quiz allows you to assess your knowledge.
*Average video play time: 2-3 minutes
Unforgettable characters with concise but impactful videos (2-4 min each)