Last reviewed · How we verify
Tukysa (tukysa)
Tukysa blocks the activity of ERBB2 and ERBB3 proteins, which are involved in cancer cell growth and spread.
Tukysa is a small molecule kinase inhibitor developed by Seattle Genetics, targeting the ERBB2/ERBB3 pathway. It is a patented medication approved by the FDA in 2020 for the treatment of metastatic human epidermal growth factor 2 positive carcinoma of breast. Tukysa works by inhibiting the activity of the ERBB2 and ERBB3 proteins, which are involved in the growth and spread of cancer cells. As a result, it helps to slow down or stop the growth of cancer cells. Tukysa is a commercial product with a proprietary formulation.
At a glance
| Generic name | tukysa |
|---|---|
| Sponsor | Pfizer |
| Drug class | Kinase Inhibitor [EPC] |
| Target | ERBB2/ERBB3 |
| Modality | Monoclonal antibody |
| Therapeutic area | Oncology |
| Phase | FDA-approved |
| First approval | 2020 |
| Annual revenue | 463 |
Mechanism of action
Tucatinib is tyrosine kinase inhibitor of HER2. In vitro, tucatinib inhibits phosphorylation of HER2 and HER3, resulting in inhibition of downstream MAPK and AKT signaling and cell proliferation, and showed anti-tumor activity in HER2 expressing tumor cells. In vivo, tucatinib inhibited the growth of HER2 expressing tumors. The combination of tucatinib and trastuzumab showed increased anti-tumor activity in vitro and in vivo compared to either drug alone.
Approved indications
- Metastatic human epidermal growth factor 2 positive carcinoma of breast
Common side effects
- Diarrhea
- Palmar-plantar erythrodysesthesia syndrome
- Nausea
- Vomiting
- Stomatitis
- Hepatotoxicity
- Decreased appetite
- Anemia
- Rash
- Abdominal pain
- Headache
- Fatigue
Key clinical trials
- Canadian Profiling and Targeted Agent Utilization Trial (CAPTUR) (PHASE2)
- Phase Ib/II Study of Zanidatamab Plus Tucatinib and Chemotherapy in HER2-Positive Advanced Breast Cancer (PHASE1,PHASE2)
- A Study of Tucatinib Plus Trastuzumab Deruxtecan in HER2+ Breast Cancer (PHASE2)
- Study of Tucatinib and Doxil in Participants With Human Epidermal Growth Factor Receptor 2 Positive (HER2+) Metastatic Breast Cancer (PHASE2)
- TAPUR: Testing the Use of Food and Drug Administration (FDA) Approved Drugs That Target a Specific Abnormality in a Tumor Gene in People With Advanced Stage Cancer (PHASE2)
- Secondary BRain Metastases Prevention After Isolated Intracranial Progression on Trastuzumab/Pertuzumab or T-DM1 in Patients With aDvanced Human Epidermal Growth Factor Receptor 2+ brEast Cancer With the Addition of Tucatinib (PHASE2)
- A Study of Disitamab Vedotin With Other Anticancer Drugs in Solid Tumors (PHASE2)
- A Study of Tucatinib or Placebo With Trastuzumab and Pertuzumab for Metastatic HER2+ Breast Cancer (PHASE3)
Patents
| Patent | Expiry | Type |
|---|---|---|
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 |
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
| FDA Orange Book | Patents + exclusivity |
| 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:
- Tukysa CI brief — competitive landscape report
- Tukysa updates RSS · CI watch RSS
- Pfizer portfolio CI