rinatabart sesutecan

Rinatabart sesutecan is an investigational antibody-drug conjugate (ADC) targeting folate receptor alpha (FRα, also known as FOLR1), which is highly expressed in several solid tumors, including ovarian and endometrial cancers. The drug consists of a human monoclonal antibody that selectively binds to FRα, linked via a novel hydrophilic and cleavable linker (sesutecan) to the cytotoxic payload exatecan—a potent topoisomerase I inhibitor. Upon binding to FRα on tumor cells, the ADC is internalized and releases exatecan intracellularly through enzymatic cleavage of the linker. Exatecan then inhibits DNA topoisomerase I, causing DNA single-strand and double-strand breaks that lead to cell death. Rinatabart sesutecan has demonstrated robust anti-tumor activity in preclinical models across multiple tumor types and has shown promising efficacy in early-phase clinical trials for advanced ovarian cancer regardless of FRα expression levels[1][3][5][6][8]. The drug was originally developed by ProfoundBio (now a subsidiary of Genmab) and has received FDA fast track designation for high-grade serous or endometrioid platinum-resistant ovarian cancer[4][5]. It is currently being evaluated in Phase III trials for fallopian tube cancer, ovarian cancer, and peritoneal cancer[7].

Brand names

Rina-S

Other names

rinatabart sesutecan-ProfoundBioRina-S-ProfoundBio