Preferred Label : Fibroblast Activation Protein Alpha-activated Doxorubicin Prodrug AVA6000;
NCIt synonyms : FAP-activated Doxorubicin Prodrug AVA6000;
NCIt related terms : AVA-6000;
NCIt definition : A prodrug of the anthracycline antineoplastic antibiotic doxorubicin composed of doxorubicin
covalently bonded to the dipeptide N-(pyridine-4-carbonyl)-D-Ala-L-Pro, with potential
antineoplastic activity. Upon administration, fibroblast activation protein alpha
(FAP)-activated doxorubicin prodrug AVA6000 is hydrolyzed by FAP, which is overexpressed
on cancer-associated fibroblasts (CAFs) in the tumor microenvironment (TME). Doxorubicin
is released in the TME, and intercalates into DNA and interacts with topoisomerase
II. This leads to an inhibition of DNA replication and repair, and prevents RNA and
protein synthesis. By targeting the delivery of doxorubicin directly to the tumor,
AVA6000 may result in less systemic toxicities. FAP, a membrane-bound protease, is
overexpressed on CAFs in various tumors but minimally expressed on normal, healthy
cells.;
UNII : 7XPB9B6MUA;
CAS number : 1841402-73-0;
Molecule name : AVA-6000; AVA 6000;
NCI Metathesaurus CUI : CL1799097;
Origin ID : C190682;
UMLS CUI : C5777101;
Semantic type(s)
- concept_is_in_subset
- has_target
