Preferred Label : FRa/TRPV6 Bispecific Ligand-drug Conjugate CBP-1019;
NCIt synonyms : Bispecific Ligand/Topoisomerase Inhibitor Conjugate CBP-1019; FRa/TRPV6 Bispecific Ligand-exatecan Conjugate CBP-1019; FOLR1/TRPV6 Bispecific Ligand-drug Conjugate CBP-1019;
NCIt definition : A bispecific ligand-drug conjugate composed of dual ligands that target human folate
receptor alpha (FRa; FolRa; FOLR1) and transient receptor potential cation channel
subfamily V member 6 (TRPV6; CaT1; CATL), conjugated to the camptothecin analog and
topoisomerase 1 inhibitor exatecan, with potential antineoplastic activity. Upon administration
of FRa/TRPV6 bispecific ligand-drug conjugate CBP-1019, the dual ligands target and
bind to FRa and/or TRPV6 expressed on tumor cells. Upon binding and internalization,
exatecan is released and inhibits DNA topoisomerase 1 activity, thereby inhibiting
DNA replication and resulting in cell cycle arrest and apoptosis in tumor cells expressing
FRa and/or TRPV6. FRa is a glycosylphosphatidylinositol linked cell-surface glycoprotein
that is widely expressed in certain cancers while its expression is limited in normal
tissues. The TRPV6 ion channel plays a key role in calcium homeostasis and is highly
selective for calcium compared to other cations; it is overexpressed in a variety
of tumors and initiates tumor cell growth, proliferation and metastases.;
Molecule name : CBP 1019; CBP-1019;
NCI Metathesaurus CUI : CL1907552;
Origin ID : C200554;
UMLS CUI : C5854562;
Semantic type(s)
- concept_is_in_subset
- has_target
