Rinatabart Sesutecan

**Semantic type:** Pharmacologic Substance

**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.

**Synonyms:** - ADC PRO1184 - Anti-FRalpha/Exatecan ADC PRO1184 - GEN 1184 - GEN-1184 - GEN1184 - PRO 1184 - PRO-1184 - PRO1184 - RINATABART SESUTECAN - Rina-S