What Are the Indications and Contraindications of Alpelisib (阿培利司)? A Comprehensive Guide

What Are the Indications and Contraindications of Alpelisib (阿培利司)? A Comprehensive Guide

For patients with advanced breast cancer, particularly those with PIK3CA mutations, Alpelisib (阿培利司, brand name: Piqray) represents an important targeted therapy option. This article examines its approved uses, key restrictions, and important safety considerations to help patients and caregivers make informed treatment decisions.

Key Approved Uses of Alpelisib

Alpelisib is a PI3Kα inhibitor specifically designed for:
✔ HR-positive, HER2-negative, PIK3CA-mutated advanced or metastatic breast cancer
✔ Cases where endocrine therapy alone has failed
✔ Used in combination with fulvestrant (not as monotherapy)

Clinical benefits:

• Progression-free survival: ~11 months (vs. 5.7 months with fulvestrant alone)

• Tumor response rate: ~35% in clinical trials

Who Should NOT Take Alpelisib? Key Contraindications

1. Absolute Contraindications

• Severe hypersensitivity to alpelisib or its components

• Severe hepatic impairment (Child-Pugh Class C)

• Uncontrolled Type 1/2 diabetes (risk of severe hyperglycemia)

2. High-Risk Populations Requiring Caution

• Pregnant women: Potential fetal harm (Category D)

• Breastfeeding mothers: Discontinue nursing during treatment

• Elderly patients: Higher risk of side effects like rash/diarrhea

• Renal impairment: Dose adjustments may be needed

Critical Drug Interactions

Alpelisib interacts significantly with:

• Strong CYP3A4 inhibitors (e.g., ketoconazole): ↑ Alpelisib toxicity

• Strong CYP3A4 inducers (e.g., rifampin): ↓ Alpelisib effectiveness

• BCRP substrates (e.g., rosuvastatin): May require dose reduction

Always inform your oncologist about ALL medications/supplements you take.

Monitoring Requirements During Treatment

Due to common side effects, patients need regular:
✔ Blood glucose tests (weekly for first month, then monthly)
✔ Liver function tests (baseline and periodically)
✔ Skin checks (for rashes, which affect ~50% of patients)

Q&A: Addressing Patient Concerns

Q1: How do I know if I have a PIK3CA mutation?

A: Your oncologist will order tumor genetic testing (e.g., tissue biopsy or liquid biopsy).

Q2: What if I develop severe hyperglycemia?

A: Your doctor may:

• Start antidiabetic medications

• Reduce alpelisib dose

• Temporarily halt treatment

Q3: Are there financial assistance programs?

A: Yes—manufacturer programs may help with costs (~¥20,000-¥30,000/month). Ask your healthcare team.

Key Takeaways

• Alpelisib is highly specific for PIK3CA+ HR+/HER2- breast cancer.

• Strict contraindications exist for liver/diabetes patients.

• Vigilant monitoring is crucial for safety.

Consult your oncologist to determine if alpelisib is appropriate for your case.

For personalized advice, contact Dingxiang Medical Service.

English Translation

Alpelisib (阿培利司): Indications & Contraindications

Alpelisib (Piqray) is approved for:
✔ PIK3CA-mutated, HR+/HER2- advanced breast cancer
✔ Combined with fulvestrant after endocrine therapy failure

Avoid if:
✖ Severe liver disease
✖ Uncontrolled diabetes
✖ Known hypersensitivity

Requires regular glucose/liver monitoring.