Tucatinib (Tukysa)
Targeted Therapy · Approved since 2020
Description
Tucatinib is an oral tyrosine kinase inhibitor specifically designed to target HER2-positive tumors, including HER2-positive metastatic colorectal cancer. This selective HER2 inhibitor is used in combination with trastuzumab and chemotherapy regimens like mFOLFOX6 for the treatment of HER2-amplified colorectal cancers. Tucatinib demonstrates activity against both extracranial disease and brain metastases in HER2-positive solid tumors. The drug is specifically indicated for patients whose tumors harbor HER2 amplification or overexpression, which occurs in approximately 2-5% of colorectal cancers.
Mechanism of Action
Tucatinib selectively inhibits the HER2 protein tyrosine kinase by binding to the ATP-binding site of the HER2 receptor, blocking downstream signaling pathways that promote tumor cell proliferation and survival. Unlike other HER2-targeted agents, tucatinib has high selectivity for HER2 over EGFR, reducing off-target effects while maintaining potent anti-HER2 activity. The drug effectively crosses the blood-brain barrier, making it particularly valuable for treating or preventing CNS metastases in HER2-positive cancers.
Molecular Targets
Side Effects
Not all side effects are listed. Side effects vary by individual. Always consult your oncologist.
Clinical Trials
Quick Info
| Brand Name | Tukysa |
| Category | Targeted Therapy |
 Status | FDA Approved |
 EMA Status | EMA Approved |
 Spain Access | Hospital use approved in CRC |
| Administration | Oral |
| Year Approved | 2020 |
| Clinical Trials | 12 |
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Medical Disclaimer
This information is for educational purposes only and should not replace professional medical advice. Always consult your healthcare team before making treatment decisions.