trastuzumab-maytansinoid conjugate

A **trastuzumab-maytansinoid conjugate** is a class of antibody-drug conjugates (ADCs) designed to target HER2-overexpressing cancer cells. It consists of the humanized anti-HER2 monoclonal antibody trastuzumab covalently linked to a maytansinoid cytotoxic payload, such as DM1 (emtansine) or DM4, via a chemical linker (which can be non-cleavable like SMCC or cleavable like SPP or SPDB). The most prominent and clinically approved representative of this class is trastuzumab emtansine (T-DM1, marketed as Kadcyla). Upon binding to HER2 on the surface of tumor cells, the conjugate undergoes receptor-mediated endocytosis and lysosomal degradation, releasing active maytansinoid catabolites. These catabolites bind to tubulin, disrupting microtubule dynamics and inducing mitotic arrest and apoptosis. Trastuzumab-maytansinoid conjugates are primarily developed for the treatment of HER2-positive breast cancer, and have been investigated in other HER2-expressing malignancies such as gastric cancer, non-small cell lung cancer, and salivary gland cancer.

Brand names

Kadcyla

Other names

ado-trastuzumab emtansinetrastuzumab emtansinetrastuzumab-MCC-DM1trastuzumab-MCC-DM-1trastuzumab-MCC-DM 1trastuzumab-maytansinoid ADCtrastuzumab-maytansinoid conjugates