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Herceptin (trastuzumab)
HER2-targeted antibody-drug conjugate delivering microtubule inhibitor DM1 to HER2-overexpressing cells.
KADCYLA is a HER2-targeted antibody-drug conjugate combining trastuzumab with the microtubule inhibitor DM1, indicated for HER2-positive metastatic breast cancer after prior trastuzumab and taxane therapy, and for adjuvant treatment of early breast cancer with residual disease after neoadjuvant therapy. The drug demonstrates a 4-day half-life with linear two-compartment pharmacokinetics and requires CYP3A4 inhibitor avoidance due to increased DM1 exposure risk. Body weight-based dosing of 3.6 mg/kg every 3 weeks is appropriate without adjustment for most covariates. HER2-positive status via FDA-authorized testing is required for patient selection.
At a glance
| Generic name | trastuzumab |
|---|---|
| Sponsor | Roche |
| Drug class | Antibody-drug conjugate (ADC) |
| Target | HER2 receptor, subdomain IV |
| Modality | Monoclonal antibody |
| Therapeutic area | Oncology |
| Phase | FDA-approved |
| First approval | 1998 |
| Annual revenue | 2900 |
Mechanism of action
Ado-trastuzumab emtansine is composed of trastuzumab, a humanized anti-HER2 IgG1 antibody, conjugated to DM1, a small molecule microtubule inhibitor. Upon binding to subdomain IV of the HER2 receptor, the conjugate undergoes receptor-mediated internalization and lysosomal degradation, releasing DM1-containing cytotoxic catabolites intracellularly. DM1 binding to tubulin disrupts microtubule networks, resulting in cell cycle arrest and apoptotic cell death. Additionally, the antibody component inhibits HER2 receptor signaling, mediates antibody-dependent cell-mediated cytotoxicity, and inhibits shedding of the HER2 extracellular domain in HER2-overexpressing breast cancer cells.
Approved indications
- HER2-positive carcinoma of breast
- HER2-positive colon cancer
- HER2-positive rectal cancer
- HER2-positive salivary gland tumors
- Human epidermal growth factor 2 positive gastric cancer
- Secondary malignant neoplasm of female breast
- Secondary malignant neoplasm of stomach
Common side effects
- DIARRHOEA
- NAUSEA
- Diarrhoea
- FATIGUE
- Fatigue
- Nausea
- ALOPECIA
- Alopecia
- RASH
- ARTHRALGIA
- VOMITING
- ASTHENIA
Drug interactions
- Strong CYP3A4 inhibitors (ketoconazole, itraconazole, clarithromycin, atazanavir, indinavir, nefazodone, nelfinavir, ritonavir, saquinavir, telithromycin, voriconazole)
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| FDA label | Mechanism, indications, dosing, boxed warnings, drug interactions |
| SEC EDGAR | Revenue + earnings |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Herceptin CI brief — competitive landscape report
- Herceptin updates RSS · CI watch RSS
- Roche portfolio CI