Pyrotinib Application Scope

HER2-positive advanced or metastatic breast cancer — usually in patients previously treated with anthracycline/taxane and often alongside capecitabine or trastuzumab. It’s also studied as neoadjuvant therapy.

Pyrotinib Characteristics

Ingredients:
- Active: Pyrotinib maleate (irreversible dual EGFR/HER2/HER4 tyrosine kinase inhibitor)
Properties:
- Small-molecule pan-ErbB (HER1/2/4) TKI
- Irreversibly inhibits receptor phosphorylation, downregulating HER2 protein and signaling
Packaging Specification:
- Strength: Typically 80 mg oral tablets
- Package type: Bottles of 100 tablets (e.g., “80 mg × 100”)
Storage:
- For tablets: store at controlled room temperature (manufacturer specifics not public)
- For research-grade formulation: −20 °C storage (lab reference)
Expiry Date: Unknown
Executive Standard:
- Approved by China’s NMPA with standards aligned to Chinese pharmaceutical regulations
- Recognized by national guidelines (e.g., CSCO)
Approval Number: Approved by China’s NMPA in August 2018 for use with capecitabine in HER2-positive metastatic breast cancer
Date of Revision: Unknown
Manufacturer: Developed and marketed by Jiangsu Hengrui Medicine Co., Ltd.

Guidelines for the Use of Pyrotinib

Dosage and Administration:
- Standard dosing: 400 mg orally once daily (typically 21-day cycles with breakfast)
- Dose adjustments: Reduced to 320 mg or 240 mg if adverse effects occur
Adverse Reactions:
Common adverse events:
- Diarrhea: up to ~80% of patients; some grade ≥3 (~16–25%)
- Hematologic: anemia (~69%), neutropenia, leukopenia, thrombocytopenia (~30–70%)
- Gastrointestinal: nausea/vomiting (~63%)
- Others: fatigue (~51%), elevated liver enzymes, skin rash/itching, hypomagnesemia, upper respiratory infections (~5–36%)
Contraindications: No explicit formal contraindications published; likely contraindicated in patients with known hypersensitivity to pyrotinib components.
Precautions:
- Manage diarrhea: standard antidiarrheal treatment (e.g., loperamide) is essential
- Monitor blood counts and manage cytopenias with dose modifications
- Liver function: watch for enzyme elevations and bilirubin increase (~5%)
- Skin reactions: rash or pruritus require supportive care
- Rare respiratory events (e.g., pneumonitis) — monitor cough or dyspnea

Pyrotinib Interactions

Drug Interactions:
CYP3A4 metabolism: concomitant use of strong CYP3A4 inhibitors or inducers could alter plasma levels—avoid or adjust dosing
Antidiarrheals: loperamide used to control diarrhea; no known severe interaction.
Trastuzumab/capecitabine combos: widely used; no concerning interaction signals yet

Note:

If there is a new packaging for the drug, the new packaging shall prevail. The above information is sourced from DengYue Medicine.
It is only for internal discussion among medical staff and does not serve as a basis for medication. For specific medication guidelines, please consult the attending physician.