Preferred Label : Rinatabart Sesutecan;
NCIt synonyms : ADC PRO1184; Anti-FRalpha/Exatecan ADC PRO1184;
NCIt definition : An antibody-drug conjugate (ADC) composed of a human monoclonal antibody targeting
folate receptor alpha (FRa; FolRa; FOLR1) conjugated, via a cleavable hydrophilic
linker, to the camptothecin analog and topoisomerase 1 inhibitor exatecan, with potential
antineoplastic activity. Upon administration of rinatabart sesutecan, 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,
and leading to cell cycle arrest and tumor cell apoptosis. 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.;
UNII : C56LJ7JC3W;
CAS number : 2853518-95-1;
Drug name : Rina-S;
Molecule name : PRO 1184; PRO-1184; GEN-1184; GEN 1184;
NCI Metathesaurus CUI : CL1912851;
Origin ID : C192818;
UMLS CUI : C5785439;
Semantic type(s)
concept_is_in_subset
has_target