TUKYSA TUCATINIB 图卡替尼妥卡替尼

Tucatinib is an oral small molecule tyrosine kinase inhibitor, mainly used to treat HER2-positive breast cancer, especially advanced patients with brain metastases or ineffective with other treatment options. It selectively inhibits the activity of HER2 protein and blocks tumor cell growth signals. It is often used in combination with trastuzumab and capecitabine to improve efficacy.

1. Mechanism of action and indications
Mechanism of action: Tucatinib targets the tyrosine kinase domain of HER2 protein, inhibits its abnormal activation, reduces downstream signal transduction, and thus delays tumor progression.
‌Indications: HER2-positive metastatic breast cancer (including brain metastases);
Combined with trastuzumab and capecitabine for patients who have failed anti-HER2 treatment in the past.
2. Clinical efficacy and usage
Efficacy characteristics: Clinical trials have shown that the combination regimen can significantly prolong progression-free survival, and has outstanding effects on patients with brain metastases.
‌Dosage‌:
The recommended dose is 300 mg orally twice a day;
It needs to be taken with food to improve absorption stability.
3. Common side effects and treatment
‌Common reactions‌:
Diarrhea (can be controlled by antidiarrheal drugs);
Fatigue, nausea, hand-foot syndrome (such as skin desquamation).
‌Serious risks‌:
Hepatotoxicity (liver function needs to be monitored regularly);
Interstitial lung disease (if dyspnea occurs, stop the drug immediately and seek medical attention).
4. Precautions for use
‌Contraindicated groups‌: Those who are allergic to the ingredients and patients with moderate to severe liver damage are prohibited;
‌Special groups‌:
Pregnant women need to assess the risk, and the drug needs to be discontinued or breastfeeding needs to be stopped during lactation;
Effective contraceptive measures need to be taken during medication.
‌Drug interactions‌: The dose needs to be adjusted when used in combination with CYP3A4 enzyme inhibitors or inducers, and the doctor needs to be informed of the drugs being used in advance.
5. Medical treatment and follow-up guidance
Tucatinib is a prescription drug and must be used strictly in accordance with the doctor’s instructions. During treatment, liver function, blood routine and imaging should be regularly reviewed to evaluate the efficacy. If serious side effects or disease progression occur, the regimen should be adjusted in a timely manner. Patients should not increase or decrease the dose or stop taking the drug on their own to avoid affecting the treatment effect or increasing the risk of toxicity.