trastuzumab deBouganin

Trastuzumab deBouganin (T-deB) is an investigational antibody-drug conjugate (ADC) consisting of the HER2-targeting monoclonal antibody trastuzumab chemically conjugated to deBouganin, a de-immunized (T-cell epitope-depleted) variant of the plant-derived type I ribosome-inactivating protein (RIP) bouganin. Developed with a drug-to-antibody ratio (DAR) of approximately 2, trastuzumab deBouganin targets HER2-expressing cancer cells. Upon internalization, the deBouganin payload binds and deadenylates the sarcin/ricin loop of the 28S subunit of ribosomal RNA, thereby inhibiting protein synthesis and inducing apoptosis. Unlike microtubule-inhibiting ADCs such as ado-trastuzumab emtansine (T-DM1), trastuzumab deBouganin is unaffected by common resistance mechanisms, including multidrug resistance (MDR) efflux pump overexpression, Bcl-2-mediated anti-apoptotic resistance, and HER2-HER3 dimerization, and it demonstrates high potency against tumor cells with cancer stem cell properties.

Other names

deBouganin-trastuzumab conjugatetrastuzumab-deBouganintrastuzumab-deBouganin conjugate