termsTerm
DM1
aka mertansine, emtansine payload, mertansine, emtansine
DM1 is the maytansine-derived payload in Kadcyla: a tubulin blocker held by a non-cleavable linker, so it stays in the cell it entered.
DM1 (mertansine) is released as a lysine-linker-payload catabolite after the antibody is degraded in the lysosome. That catabolite is charged and not membrane permeable, so trastuzumab emtansine has little bystander killing and needs high, uniform HER2 expression to work. Thrombocytopenia and raised liver enzymes are characteristic.
Category
ADC chemistry