Alpelisib: PI3K Inhibitor for Breast Cancer
Alpelisib is a kinase inhibitor that specifically targets the alpha isoform of phosphatidylinositol 3-kinase (PI3K). It is a targeted therapy designed for breast cancer patients whose tumors harbor a mutation in the PIK3CA gene.
By inhibiting the PI3K signaling pathway, Alpelisib reduces tumor cell proliferation and helps overcome resistance to endocrine therapy. On Unifarm, you can find details regarding original medications (such as Piqray) containing this active ingredient.
Indications
- Breast Cancer: Treatment of postmenopausal women and men with hormone receptor-positive (HR+), human epidermal growth factor receptor 2-negative (HER2-) advanced or metastatic breast cancer.
- Specific Mutation: Indicated for patients with a PIK3CA mutation as detected by an approved test.
- Combination Therapy: Used in combination with fulvestrant following progression on or after an endocrine-based regimen.
Dosage and administration
The medication is taken orally once daily. Tablets come in different strengths (e.g., 50 mg, 150 mg, 200 mg).
Standard Regimen:
- Recommended Dose: 300 mg (two 150 mg tablets) taken once daily.
- Administration: Must be taken with food to ensure proper absorption.
Tablets should be swallowed whole; do not chew, crush, or split them. If adverse reactions occur, the dosage may be reduced sequentially to 250 mg or 200 mg daily.
- Severe hypersensitivity to Alpelisib (e.g., anaphylaxis, Stevens-Johnson syndrome).
- Pregnancy (can cause fetal harm).
- Breastfeeding (not recommended during treatment and for 1 week after the last dose).
Treatment generally requires monitoring of fasting plasma glucose (FPG) and HbA1c. Common adverse reactions include:
- Metabolic: Hyperglycemia (high blood sugar), weight loss.
- Dermatologic: Rash (including maculopapular rash), dry skin, alopecia.
- Gastrointestinal: Diarrhea, nausea, vomiting, stomatitis.
- Renal: Increased creatinine levels.
- General: Fatigue, decreased appetite.
