Sirolimus protein-bound particles (Fyarro)
Mechanism of action
From the NCI Drug Dictionary: The macrolide antibiotic rapamycin bound to nanoparticle albumin with immunosuppressant (see sirolimus) and potential antiangiogenic and antineoplastic activities. Rapamycin binds to the immunophilin FK Binding Protein-12 (FKBP-12) to generate a complex that binds to and inhibits the activation of the mammalian Target Of Rapamycin (mTOR), a key regulatory kinase. In turn, inhibition of mTOR may result in the inhibition of the phosphatidylinositol 3 (PI-3) kinase/Akt pathway and vascular endothelial cell growth factor (VEGF) secretion, which may result in decreased tumor cell proliferation and tumor angiogenesis. The binding of water-insoluble rapamycin to nanoparticle albumin permits the albumin-mediated endocytosis of rapamycin by tumor cells and endothelial cells.
Diseases for which it is used
History of changes in FDA indication
- 2021-11-22: Approved for adult patients with locally advanced unresectable or metastatic malignant perivascular epithelioid cell tumor (PEComa). (Based on AMPECT)
Also known as
- Code name: ABI-009
- Generic names: nab-rapamycin, nab-sirolimus
- Brand name: Fyarro