Preferred Label : Encapsulated Rapamycin;
NCIt synonyms : Encapsulated Sirolimus; Microencapsulated Rapamycin;
NCIt definition : An orally bioavailable nanoparticle-based formulation composed of sub-micron particles
of the macrolide antibiotic rapamycin incorporated into a pH-sensitive poly(methyl
methacrylate) polymer, with potential immunomodulating and antineoplastic activities.
Upon oral administration of the encapsulated rapamycin, the nanoparticle specifically
delivers rapamycin at the tumor site. Rapamycin binds to the immunophilin FK Binding
Protein-12 (FKBP-12) to generate a complex that binds to and inhibits the activation
of the serine/threonine kinase mammalian target of rapamycin (mTOR), a key regulatory
kinase. This may suppress mTORC1 activity. In addition, inhibition of mTOR may modulate
central memory CD8 T cells, CD3 /CD56 natural killer (NK) cells and CD8 T-cell responses.
This may kill tumor cells. Compared to the administration of rapamycin alone, this
formulation improves oral bioavailability of rapamycin with more consistent rapamycin
levels, thereby allowing for administration of lower rapamycin dosage, which improves
and minimizes rapamycin's toxicity. Upregulated in some tumors, mTOR is a serine/threonine
kinase involved in regulating cellular proliferation, motility, and survival that
is located downstream of the PI3K/Akt signaling pathway.;
Molecule name : eRapa (TM);
NCI Metathesaurus CUI : CL1407680;
Origin ID : C173879;
UMLS CUI : C5420424;
Semantic type(s)
- concept_is_in_subset
- has_target
