Rap-hRS7

Rap-hRS7 is an experimental immuno-RNase developed by Immunomedics (now part of Gilead Sciences) for the treatment of TROP-2-expressing epithelial cancers. It is constructed using the proprietary 'Dock-and-Lock' (DNL) platform, which enables the site-specific conjugation of a humanized anti-TROP-2 monoclonal antibody (hRS7) with a mutant human pancreatic ribonuclease (Rap). The hRS7 component selectively targets the Tumor-associated calcium signal transducer 2 (TROP-2) antigen, which is frequently overexpressed in various solid tumors, including breast, lung, and pancreatic cancers. Upon binding to the cell surface and subsequent internalization, the ribonuclease moiety is delivered into the cytoplasm. Once inside, the RNase evades the cytosolic ribonuclease inhibitor and degrades cellular RNA, leading to the inhibition of protein synthesis and the induction of apoptosis. This therapeutic approach aims to leverage the high specificity of monoclonal antibodies to deliver a potent enzymatic payload directly to malignant cells while minimizing off-target systemic toxicity.

Other names

hRS7-RaphRS-7-RaphRS 7-Rapanti-TROP-2-RNase fusion proteinanti-TROP2-RNase fusion proteinanti-TROP 2-RNase fusion proteinhRS7-RNasehRS-7-RNasehRS 7-RNase