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Substance Name: Trastuzumab emtansine [USAN:INN]
RN: 1018448-65-1
UNII: SE2KH7T06F
Notes
- 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)
Molecular Weight
- 973.5557
Classification Codes
- Antimitotic Agents
- Antineoplastic Agents
- Antineoplastic Agents, Immunological
- Mitosis Modulators
- Treatment of Cancer
- Tubulin Modulators
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Links to Resources
NLM Resources (File Locators)
Other Resources (Internet Locators)
Names and Synonyms
Name of Substance
- Trastuzumab emtansine [USAN:INN]
Synonyms
- Ado-trastuzumab emtansine
- Kadcyla
- PRO 132365
- PRO132365
- T-DM 1
- T-DM1
- Trastuzumab conjugate with emtasine
- Trastuzumab emtansine
- Trastuzumab-DM1
- Trastuzumab-MCC-DM 1
- Trastuzumab-MCC-DM1
- Trastuzumab-MCC-DM1 antibody-drug conjugate
- UNII-SE2KH7T06F
Systematic Name
- Immunoglobulin G1, anti-(human p185neu receptor) (human-mouse monoclonal rhuMab HER2 gamma1-chain), disulfide with human-mouse monoclonal rhuMab HER2 light chain, dimer, tetraamide with N2'-(3-((1-((4-carboxycyclohexyl)methyl)-2,5-dioxo-3-pyrrolidinyl)thio)-1-oxopropyl)-N2'-deacetylmaytansine
Registry Numbers
CAS Registry Number
- 1018448-65-1
FDA UNII
- SE2KH7T06F
System Generated Number
- 1018448651