rovalpituzumab tesirine

Rovalpituzumab tesirine is a first-in-class antibody-drug conjugate (ADC) designed to target delta-like protein 3 (DLL3), a transmembrane protein highly expressed on the surface of small cell lung cancer (SCLC) cells but largely absent in normal tissues. The drug consists of a humanized IgG1 monoclonal antibody (SC16) that specifically binds DLL3, linked via a protease-cleavable linker to a cytotoxic pyrrolobenzodiazepine (PBD) dimer toxin. Upon binding to DLL3-expressing tumor cells, the ADC is internalized and the PBD payload is released inside the cell, where it cross-links DNA, causing irreparable DNA damage, cell cycle arrest at G2–M phase, and apoptosis. The PBD toxin can also exert a bystander effect by diffusing into adjacent tumor cells. Rovalpituzumab tesirine was originally developed by Stemcentrx and later acquired by AbbVie for further development in SCLC and other solid tumors[1][3][4][5][6].

Other names

Rova-TSC16LDSC-16LDSC 16LD