Proposed mechanism of action of KADCYLA

Multiple antitumor activities from a single agent

Proposed mechanism of action for KADCYLA, based on preclinical models1,2,6

Dual antitumor activity with HER2 suppression and the release of DM1 inside HER2-targeted cells

HER2+ antitumor activities1,2,5

1. HER2 binding

  • Selectively binds to the HER2 receptor at subdomain IV

2. HER2+ antitumor activities

  • Suppresses ligand-independent HER2 downstream signaling (antiproliferative and apoptotic effects)
  • Triggers the antibody-dependent cell-mediated cytotoxicity (ADCC) immune response
  • Inhibits HER2 shedding

DM1* cytotoxic activity1

3. Internalization

  • Once bound, the KADCYLA/HER2 receptor complex is internalized via endocytosis

4. DM1 release

  • KADCYLA is degraded inside the tumor to release DM1

5. DM1 cytotoxicity

  • DM1 binds to microtubules and inhibits their polymerization, causing cell-cycle arrest and cell death

*Cytotoxic DM1-containing catabolites (primarily lysine-bound emtansine).1

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How KADCYLA was studied

Learn more about the KADCYLA clinical trial design.

Prescribing Information

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