Preferred Label : Anti-FRalpha/Exatecan ADC LY4170156;
NCIt synonyms : ADC LY4170156; Antibody-drug Conjugate LY4170156; Anti-FRa ADC LY4170156;
NCIt definition : An antibody-drug conjugate (ADC) composed of a Fc-silenced, humanized immunoglobulin
G1 (IgG1) monoclonal antibody targeting folate receptor alpha (FRa; FolRa; FOLR1)
linked, via a dipeptide cleavable linker and a polysarcosine hydrophobicity masking
agent, to the camptothecin analog and topoisomerase 1 inhibitor exatecan, with potential
antineoplastic activity. Upon administration of anti-FRalpha/exatecan ADC LY4170156,
the antibody moiety targets and binds to FRa expressed on tumor cells. Upon binding,
cellular uptake and linker cleavage, exatecan is released. Exatecan inhibits DNA topoisomerase
I activity, thereby inhibiting DNA replication and generating DNA single- and double-strand
breaks. This leads to cell cycle arrest and tumor cell apoptosis. In addition, exatecan
is able to induce a bystander effect on neighboring cells in the tumor environment.
This inhibits the proliferation of FRa-expressing tumor cells. 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 : LY 4170156; LY-4170156;
Origin ID : C207085;
concept_is_in_subset
- has_target
