Article

Trastuzumab emtansine in advanced HER2-positive breast cancer


 

Trastuzumab emtansine is an antibody drug conjugate composed of trastuzumab (T) linked to a highly potent cytotoxic derivative of maytansine (DM1) by a stable linker (a nonreducible thioether, SMCC).1 DM1 binds to intracellular tubulin and prevents the assembly of microtubules, resulting in cell death. Trastuzumab targets the conjugate to the human epidermal growth factor receptor 2 (HER2) protein and the stable linker releases the cytotoxic agent only when the compound is internalized through receptor endocytosis. Trastuzumab emtansine (T-DM1) has been in found to be active in trastuzumab- and lapatinib-resistant disease, as well as in trastuzumab-naïve tumors...

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