Drug intelligence / Profile preview

nab-sirolimus

Development stage
Approved
Lead developer
Aadi Bioscience
Modality
Nanoparticles → Drug Delivery Systems, Small Molecules
Administration
Intravenous
01

Overview

Nab-sirolimus is a nanoparticle, albumin-bound intravenous formulation of sirolimus, a macrolide antibiotic and mTOR (mammalian target of rapamycin) inhibitor. Developed to overcome the low water solubility of oral sirolimus, this formulation enables enhanced tumor penetration via albumin-mediated transport. Nab-sirolimus binds to FK Binding Protein 12 (FKBP12), forming a complex that inhibits mTOR activity, leading to suppression of the PI3K/Akt pathway and decreased secretion of vascular endothelial growth factor (VEGF). This results in reduced tumor cell proliferation and angiogenesis. Nab-sirolimus is approved in the United States for adults with locally advanced unresectable or metastatic malignant perivascular epithelioid cell tumor (PEComa), a rare sarcoma[5][6][8]. It has also been studied in other cancers such as sarcoma, brain cancer, and colorectal cancer[3].

Brand names
Fyarro
Other names
sirolimus protein-bound particlesnanoparticle albumin-bound sirolimus
02

Targets

Mechanistic target of rapamycin complex 1

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