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Tucatinib significantly enhances its anti-tumor effect by combining with other drugs such as trastuzumab, providing a new treatment option for patients with HER2-positive cancer.
Tucatinib is a kinase inhibitor used in combination with trastuzumab and capecitabine. It is suitable for the treatment of adult patients with HER2-positive breast cancer:
Advanced unresectable or metastatic breast cancer Adenocarcinoma (including patients with brain metastases)
Patients with metastatic disease who have received at least one anti-HER2 regimen in the past
Tucatinib is a HER2 tyrosine kinase inhibitor, passed: < /p>
1. Inhibit HER2 and HER3 phosphorylation
2. Block downstream MAPK and AKT signaling pathways
3. Inhibit tumor cell proliferation
4. Combination with trastuzumab can enhance anti-tumor activity Sex
Recommended dose: 300 mg orally, twice a day (approximately 12 hours apart), with trastuzumab Combined with capecitabine
Can be taken with food or on an empty stomach
Swallow the tablet whole and do not chew, crush or break it
If you miss a dose ≤12 hours, you can take it again, and if you skip the dose if >12 hours
No risk after vomiting If you need to take a supplement, take the next dose as originally planned
Hepatic insufficiency:
Child-Pugh C grade: reduce the dose to 200 mg twice a day
Adverse reaction management:
First reduction: 250 mg twice daily
Second reduction: 200 mg twice daily
Third reduction: 150 mg twice daily
Intolerable 15 0mg should be permanently discontinued
Incidence rate ≥20%:
Diarrhea (81%, 12% grade 3), hand-foot syndrome (63%), nausea (58%), fatigue Strain, hepatotoxicity (42%), vomiting, stomatitis, loss of appetite, abdominal pain, headache, anemia, rash
Important Precautions
Severe diarrhea: incidence rate 25%, may lead to dehydration, acute kidney injury or even Death
Hepatotoxicity: 8% of patients had ALT>5×ULN, 6% had AST>5×ULN
Important monitoring
Before treatment and every 3 Weekly: liver function (ALT/AST/bilirubin), complete blood count
Regular monitoring: electrocardiogram (QT interval), electrolytes, renal function
Drug interactions
Avoid combined use: strong potency CYP3A inducers/moderate CYP2C8 inducers
Use with caution: CYP3A/P-gp substrate drugs (the dosage may need to be reduced)
Strong CYP2C8 inhibitors: the dosage needs to be reduced to 100 mg twice daily
< p>Patient educationAvoid grapefruit, star fruit, and pomegranate
See a doctor immediately for diarrhea ≥ 4 times/day
Pay attention to symptoms of hepatotoxicity (jaundice, deepening of urine, etc.)
Contact with capsule powder Wash the skin immediately after
Pregnancy/breastfeeding
Pregnancy: There is a risk of teratogenesis, effective contraception is required during treatment and 1 week after stopping the drug
Breastfeeding: During treatment And breastfeeding is prohibited for 1 week after stopping the drug
Liver and kidney insufficiency
Child-PughC: reduce the dose to 200 mg twice a day
Severe renal impairment: not recommended (capecitabine is contraindicated)< /p>
Elderly patients
Patients aged ≥65 years have a higher incidence of serious adverse reactions (34% vs 24%)
Pediatric medication
The safety and effectiveness have not been established.