The first HER2-targeted antibody-drug conjugate

KADCYLA: A single agent with 3 components1-3

*Emtansine is the combination of DM1, a cytotoxic maytansinoid, and the stable MCC linker.1

DM1=derivative of maytansine; MCC=4-(N-maleimidomethyl) cyclohexane-1-carboxylate.

In preclinical studies
KADCYLA maintains the HER2 suppression and anticancer activities of trastuzumab while delivering cytotoxic DM1 to HER2-expressing cells1

Monoclonal antibody

  • Many normal cells express HER24
    • HER2-positive (HER2+) cancer cells can express up to 100 times more HER2 than normal cells
  • Trastuzumab selectively binds to HER2 receptors1
    • Suppresses downstream signaling pathways to inhibit tumor cell proliferation and survival1,5
    • Triggers antibody-dependent cell-mediated cytotoxicity (ADCC)1
    • Inhibits HER2 shedding1

Linker

  • MCC linker stabilizes KADCYLA in circulation to release DM1 after entering the target cell1,3

Cytotoxic agent

  • A microtubule inhibitory agent that induces cell cycle arrest and cell death
  • Provides cytotoxicity previously unavailable for clinical use
    • DM1, a maytansinoid, is approximately 20 to 200 times more potent than taxanes and vinca alkaloids1,2

Proposed mechanism of action

KADCYLA delivers multiple HER2-targeted antitumor activities.

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Prescribing Information

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