Substance Name: Trastuzumab emtansine [USAN:INN]
RN: 1018448-65-1
UNII: SE2KH7T06F

Designed to deliver antimicrotubule agent DM1 to HER2-positive cells.

Designed to deliver antimicrotubule agent DM1 to HER2-positive cells

NCI: An antibody-drug conjugate (ADC) consisting of the recombinant anti-epidermal growth factor receptor 2 (HER2) monoclonal antibody trastuzumab conjugated to the maytansinoid DM1 via a nonreducible thioether linkage (MCC) with potential antineoplastic activity. The trastuzumab moiety of this ADC binds to HER2 on tumor cell surface surfaces; upon internalization, the DM1 moiety is released and binds to tubulin, thereby disrupting microtubule assembly/disassembly dynamics and inhibiting cell division and the proliferation of cancer cells that overexpress HER2. Linkage of antibody and drug through a nonreducible linker has been reported to contribute to the improved efficacy and reduced toxicity of this ADC compared to similar ADCs constructed with reducible linkers. (NCI Thesaurus)