Everolimus is a mammalian target of rapamycin (mTOR) kinase inhibitor used to treat various types of malignancies. It is currently used as an immunosuppressant to prevent rejection of organ transplants.
- Mechanism
- Curator reviewed
Everolimus is a mTOR inhibitor that binds with high affinity to the FK506 binding protein-12 (FKBP-12), thereby forming a drug complex that inhibits the activation of mTOR. This inhibition reduces the activity of effectors downstream, which leads to a blockage in the progression of cells from G1 into S phase, and subsequently inducing cell growth arrest and apoptosis. Everolimus also inhibits the expression of hypoxia-inducible factor, leading to a decrease in the expression of vascular endothelial growth factor. The result of everolimus inhibition of mTOR is a reduction in cell proliferation, angiogenesis, and glucose uptake.
- Primary indication
- Everolimus is indicated for the treatment of postmenopausal women with advanced hormone receptor-positive, HER2-negative breast cancer (advanced HR+ BC) in combination with exemestane, after failure of treatment with letrozole or anastrozole.Curator reviewed · 16 structured indications
- Formula / weight
- C53H83NO14 · 958.24 g/mol (avg)
- First approval
- Canada, 2009 · United States, 2009 · European Union, 2016
- Code names
- RAD-001 · RAD-666 · SDZ-RAD
- Brand names
Resolves to
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Which drugs share a target with Everolimus, and which of those have an active Phase 3 trial?
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