Emtansine is the combination of DM1, a cytotoxic maytansinoid, and the stable MCC linker.1
DM1=derivative of maytansine; MCC=4-(N-maleimidomethyl) cyclohexane-1-carboxylate.
HER2+ antitumor activities1,14
1. HER2 binding: Selectively binds to the HER2 receptor at subdomain IV.
2. HER2+ antitumor activities
DM1* cytotoxic activity1
3. Internalization: once bound, the KADCYLA/HER2 receptor complex is internalized via endocytosis.
4. DM1 release: KADCYLA undergoes proteolytic degradation inside the target cell and releases the active chemotherapy, DM1.
5. DM1 cytotoxicity: DM1 binds to microtubules and inhibits their polymerization, causing cell-cycle arrest and cell death.
*Cytotoxic DM1-containing catabolites (primarily lysine-bound emtansine).1
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