Mechanism of Action

See how ENHERTU delivers the cytotoxic agent directly to HER2-positive mBC cells:

ENHERTU is a specifically engineered HER2-directed antibody-drug
conjugate (ADC)1,2

HER2-directed monoclonal antibody

HER2-directed mAb1

  • Provides targeted delivery of cytotoxic agent1,2
HER2-directed monoclonal antibody

Potent cytotoxic agent1,2

  • Novel topoisomerase I inhibitor payload, known as DXd1,2,a
  • Upon release, membrane-permeable DXd causes DNA damage and apoptotic cell death, resulting in destruction of HER2+ tumor cells and surrounding cells of variable HER2 expression1,3

Enzyme-cleavable linker1

  • Attaches DXd to the antibody1
  • Cleaved specifically by lysosomal enzymes1

ENHERTU has a stable and homogeneous drug-to-antibody ratio of ~8 molecules of cytotoxic agent per antibody1,2

aIC50 of DXd topoisomerase I inhibitory activity = 0.31 μmol/L.2

IC, inhibitory concentration; mAb, monoclonal antibody; mBC, metastatic breast cancer.

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