Ailiyi Pyrotinib Maleate Tablets

1. Indications and Usage
Recurrent or Metastatic Breast Cancer:
Indicated in combination with capecitabine for the treatment of adult patients with HER2-positive recurrent or metastatic breast cancer who have not received or received trastuzumab in the setting of metastatic disease.
Early or Locally Advanced Breast Cancer:
Indicated in combination with trastuzumab and docetaxel for the neoadjuvant treatment of HER2-positive early or locally advanced breast cancer.
Prerequisite:
Patients should have received prior anthracycline- or taxane-based chemotherapy. HER2 status must be confirmed positive by a validated test.
2. Dosage and Administration
Route of Administration:
Oral Use ONLY.
Recommended Dosage:
Dose: Pyrotinib 400 mg administered orally once daily.
Cycle: Continue daily for 21 days as one cycle.
Administration Instructions:
Timing: Take within 30 minutes after a meal.
Administration: Swallow tablets whole with water; do not crush or chew.
Missed Dose:
If a dose is missed, do not take it. Resume at the regularly scheduled time for the next dose. Do not take extra tablets to make up for a missed dose.
3. Mechanism of Action
Irreversible Inhibition:
Pyrotinib is a small molecule tyrosine kinase inhibitor that irreversibly blocks the tyrosine kinase activity of EGFR and HER2.
Signal Pathway Blockade:
It inhibits the phosphorylation and activation of EGFR, HER2, HER3, and HER4, thereby blocking the PI3K/Akt and MAPK signaling pathways, which leads to the inhibition of tumor cell proliferation and induction of apoptosis.
4. Safety and Warnings
Diarrhea:
Diarrhea is the most common adverse reaction. Monitor patients for signs of diarrhea and provide supportive care (e.g., loperamide) as needed. Dose interruption or reduction may be required for severe cases.
Liver Function Impairment:
Elevations in ALT, AST, and bilirubin have been observed. Monitor liver function tests regularly. Contraindicated or not recommended in patients with moderate to severe hepatic impairment.
Embryo-Fetal Toxicity:
May cause fetal harm. Women of reproductive potential should use effective contraception during treatment and for at least 1 month after the last dose.
Cardiac Toxicity:
Monitor LVEF regularly during treatment.
5. Adverse Reactions
Most Common:
Diarrhea, hand-foot syndrome, vomiting, nausea, alopecia, increased ALT/AST, fatigue, and anemia.
6. Drug Interactions
CYP3A4 Modulators:
Pyrotinib is metabolized by CYP3A4. Concomitant use with strong CYP3A4 inhibitors or inducers should be monitored closely, and dose adjustment considered.
7. Pharmaceutical Information
Chemical Composition:
Active Ingredient: Pyrotinib Maleate (available in 80 mg and 160 mg strengths).
Storage:
Store in a tightly closed container in a dry place at a temperature not exceeding 25°C.