Preferred Label : PSMA/FRa Bispecific Peptide-drug Conjugate CBP-1018;
NCIt synonyms : FRa/PSMA Bispecific Peptide-drug Conjugate CBP-1018; PSMA/FRa Bispecific PDC CBP-1018; FOLR1/PSMA Bispecific Peptide-drug Conjugate CBP-1018;
NCIt definition : A bispecific peptide-drug conjugate (PDC) composed of dual ligands that target human
prostate-specific membrane antigen (PSMA) and human folate receptor alpha (FRa; FolRa;
FOLR1) conjugated, via the cathepsin B-cleavable MC-Val-Cit-PABC linker, to the auristatin
derivative and potent microtubule disrupting agent monomethyl auristatin E (MMAE),
with potential antineoplastic activity. Upon administration of PSMA/FRa bispecific
PDC CBP-1018, the dual ligands target and bind to FRa and PSMA expressed on tumor
cells. Upon binding, internalization, and enzymatic cleavage, MMAE is released. MMAE
binds to tubulin and inhibits microtubule polymerization, which may result in G2/M
phase cell cycle arrest and apoptosis in FRa- and PSMA-expressing tumor cells. PSMA
is expressed on the membrane of prostatic epithelial cells and overexpressed on prostate
tumor cells as well as a variety of other solid tumors. FRa is a glycosylphosphatidylinositol
linked cell-surface glycoprotein that is widely expressed in certain cancers while
its expression is limited in normal tissues.;
Molecule name : CBP-1018; CBP 1018;
NCI Metathesaurus CUI : CL1663608;
Origin ID : C181019;
UMLS CUI : C5556784;
Semantic type(s)
- concept_is_in_subset
- has_target
