Antibody
RCSB PDB 6OGE
Payload
PubChem CID 11343137
Trastuzumab emtansine
Kadcyla
- Mechanism of action
- HER2-targeted antibody-drug conjugate
- In plain language
- A HER2-targeting antibody with a cell-killing chemotherapy drug chemically attached, delivering that chemotherapy directly inside HER2-positive cancer cells.
- How it works
- The trastuzumab antibody component binds HER2 receptors on tumor cell surfaces, triggering receptor-mediated internalization of the antibody-drug conjugate. Once inside the cell, lysosomal proteolytic degradation releases the cytotoxic payload (DM1, a maytansinoid) still attached to lysine residues. DM1 binds tubulin and disrupts microtubule assembly, causing mitotic arrest and apoptotic cell death. The conjugate retains trastuzumab's intrinsic anti-HER2 activity.
- Therapeutic applications
- Indicated for HER2-positive metastatic breast cancer in patients who previously received trastuzumab and a taxane, and as adjuvant treatment of HER2-positive early breast cancer with residual invasive disease after neoadjuvant taxane- and trastuzumab-based therapy.
- Class
- Antibody-drug conjugate
- Therapeutic area
- Oncology
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