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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

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

Structure Descriptors

Smiles

[*]NC(=O)[C@@H]1CC[C@@H](CN2C(=O)CC(SCCC(=O)N(C)[C@@H](C)C(=O)O[C@H]3CC(=O)N(C)c4cc(C\C(=C\C=C\[C@@H](OC)[C@@]5(O)C[C@H](OC(=O)N5)[C@@H](C)[C@@H]6O[C@@]36C)\C)cc(OC)c4Cl)C2=O)CC1