ALPESIB 150 mg (Alpelisib): Uses, Dosage, Side Effects & Breast Cancer Treatment
ALPESIB 150 mg (Alpelisib): Uses, Dosage, Side Effects & Breast Cancer Treatment
ALPESIB 150 mg contains alpelisib, an oral targeted anticancer medicine that belongs to the PI3K inhibitor class. Alpelisib is used in combination with fulvestrant for appropriately selected adults with hormone receptor-positive (HR-positive), HER2-negative, PIK3CA-mutated advanced or metastatic breast cancer following progression on or after endocrine-based therapy.
The product details provided identify ALPESIB 150 MG as alpelisib in tablet form with a 28-tablet pack size.
Alpelisib is a molecularly targeted medicine. Rather than acting broadly on rapidly dividing cells, it targets a specific signalling pathway that can become abnormally activated when certain mutations occur in the PIK3CA gene.
This makes biomarker testing an important part of patient selection. In the FDA-approved indication, the presence of a qualifying PIK3CA mutation is determined using an FDA-approved test.
What Is ALPESIB 150 mg?
ALPESIB 150 mg contains alpelisib, a selective inhibitor of the PI3K alpha pathway.
The product information provided is:
- Product Name: ALPESIB 150 MG
- Generic Name: Alpelisib
- Strength: 150 mg
- Dosage Form: Tablets
- Pack Size: 28 Tablets
Alpelisib belongs to a group of targeted medicines known as PI3K inhibitors.
The PI3K pathway is involved in important cellular processes such as:
- Cell growth
- Cell proliferation
- Cell survival
- Cellular metabolism
- Signal transmission
In some breast cancers, mutations in PIK3CA can lead to abnormal activation of the PI3K pathway. Alpelisib inhibits PI3K alpha, helping interfere with signalling that contributes to cancer-cell growth.
What Is Alpelisib Used For?
Alpelisib is used in combination with fulvestrant for appropriately selected adults with:
- Hormone receptor-positive (HR-positive) breast cancer
- HER2-negative breast cancer
- PIK3CA-mutated disease
- Locally advanced or metastatic disease
- Disease that has progressed following endocrine-based therapy
The FDA indication specifies adults with HR-positive, HER2-negative, PIK3CA-mutated advanced or metastatic breast cancer following progression on or after an endocrine-based regimen.
Current EMA information similarly describes its use with fulvestrant in postmenopausal women and men with HR-positive, HER2-negative, locally advanced or metastatic breast cancer carrying a PIK3CA mutation after progression following endocrine therapy.
Patient-Friendly Explanation
Alpelisib is a targeted medicine used for certain advanced breast cancers where testing shows a specific PIK3CA mutation.
It works by blocking a growth-signalling pathway that can become overactive because of this mutation.
Medical Explanation
Alpelisib selectively inhibits the alpha isoform of phosphatidylinositol-3-kinase (PI3K), encoded by the PIK3CA gene. In PIK3CA-mutated breast cancer, abnormal PI3K signalling can contribute to malignant-cell proliferation and survival. Inhibition of this pathway reduces downstream signalling associated with tumour growth.
How Does Alpelisib Work?
Understanding alpelisib requires understanding the PI3K/AKT/mTOR signalling pathway.
The PI3K pathway is an intracellular signalling system that helps regulate:
- Cellular growth
- Metabolism
- Proliferation
- Survival
- Protein synthesis
The PIK3CA gene provides instructions for the catalytic alpha subunit of PI3K.
When certain activating PIK3CA mutations occur, the PI3K pathway can become excessively active.
A simplified pathway is:
PIK3CA mutation → abnormal PI3K-alpha activity → downstream signalling → cell growth and survival
Alpelisib acts by inhibiting PI3K alpha:
Alpelisib → PI3K-alpha inhibition → reduced downstream signalling → reduced cancer-cell growth and survival
This targeted mechanism distinguishes alpelisib from conventional chemotherapy.
Alpelisib is therefore particularly relevant when molecular testing confirms an appropriate PIK3CA mutation.
The FDA-approved companion diagnostic framework identifies specific PIK3CA mutations associated with eligibility for alpelisib treatment.
Alpelisib is used with fulvestrant, an endocrine therapy, because the two medicines target complementary biological mechanisms in HR-positive breast cancer.
The therapeutic objective is to interfere with both hormone-driven signalling and PI3K pathway activation in appropriately selected patients.
Key Indications
HR-Positive Breast Cancer
Alpelisib is used for breast cancer that expresses hormone receptors.
Patient-friendly:
The cancer cells use hormone-related signalling, and treatment combines endocrine therapy with targeted pathway inhibition.
Medical:
Alpelisib is administered with fulvestrant in the approved treatment setting.
HER2-Negative Breast Cancer
The approved breast-cancer indication requires the disease to be HER2-negative.
HER2 status is determined through appropriate diagnostic testing.
PIK3CA-Mutated Breast Cancer
The presence of an appropriate PIK3CA mutation is a key factor in determining eligibility.
Molecular testing is therefore important before treatment.
Advanced or Metastatic Disease
Alpelisib is used for appropriately selected patients with locally advanced or metastatic breast cancer following progression on endocrine-based treatment.
ALPESIB 150 mg Dosage and Administration
The dose must be determined by the treating oncologist.
For the FDA-approved breast-cancer indication, the recommended alpelisib dose is:
300 mg once daily with food.
This corresponds to two 150 mg tablets once daily when using the 150 mg strength.
Administration Guidance
- Take alpelisib exactly as prescribed.
- Take it once daily at approximately the same time.
- Take the medicine with food.
- Swallow tablets whole.
- Do not chew, crush or split tablets unless specifically instructed by the applicable product information.
- Do not independently change the dose.
- Treatment may be interrupted, reduced or discontinued if clinically significant adverse reactions occur.
Dose Modification
Dose interruption or reduction may be required for adverse reactions, particularly significant hyperglycemia, severe diarrhea or other clinically important toxicities.
Missed Dose
If a dose is missed, follow the instructions provided by the treating healthcare professional or the applicable product information.
Do not automatically take an extra dose to compensate for a missed dose.
Alpelisib Side Effects
Alpelisib can cause adverse reactions, some of which require active monitoring and treatment.
Common Side Effects
Reported adverse effects include:
- Increased blood glucose
- Diarrhea
- Rash
- Nausea
- Fatigue
- Decreased appetite
- Weight loss
- Vomiting
- Stomatitis
- Increased creatinine
- Increased liver enzymes
- Increased lipase
- Decreased lymphocyte count
- Anaemia
- Hair loss
These effects are identified among the common adverse reactions in FDA and EMA product information.
Less Common Side Effects
Other possible reactions include:
- Colitis
- Pneumonitis
- Hypersensitivity reactions
- Changes in calcium levels
- Changes in blood-cell counts
- Pancreatic enzyme abnormalities
- Renal-function changes
Serious Side Effects
Important serious risks include:
- Severe hyperglycemia
- Diabetic ketoacidosis
- Severe hypersensitivity
- Severe cutaneous adverse reactions
- Pneumonitis
- Severe diarrhea or colitis
- Significant dehydration
- Acute kidney injury secondary to severe diarrhea
The FDA specifically warns about severe hyperglycemia, severe cutaneous reactions, pneumonitis and diarrhea/colitis.
When to Seek Medical Attention
Prompt medical assessment may be required for:
- Very high blood glucose or symptoms of hyperglycemia
- Severe thirst or frequent urination
- Confusion or marked weakness
- Severe diarrhea
- Blood or mucus in stool
- Severe abdominal pain
- Difficulty breathing
- New persistent cough
- Widespread rash, blistering or skin peeling
- Facial swelling or other severe allergic symptoms
Drug Interactions
Alpelisib can interact with other medicines and may alter drug exposure.
Medicines Requiring Particular Attention
The FDA label identifies important interactions involving:
- Strong CYP3A4 inducers
- BCRP inhibitors
Strong CYP3A4 inducers should be avoided with alpelisib. BCRP inhibitors should also be avoided where possible; if no alternative exists, closer monitoring may be necessary.
Food Considerations
Alpelisib should be taken with food, which is an important administration requirement.
Supplement Considerations
Patients should tell their healthcare professional about:
- Herbal products
- Traditional medicines
- Vitamins
- High-dose supplements
- Unregulated cancer supplements
Do not begin a new supplement during treatment without discussing it with the treating team.
Warnings and Precautions
Hyperglycemia
One of the most important safety concerns with alpelisib is increased blood glucose.
Before treatment, fasting plasma glucose and HbA1c should be assessed, and glucose abnormalities should be addressed. During treatment, blood glucose should be monitored periodically.
Severe hyperglycemia can sometimes lead to serious metabolic complications.
Skin Reactions
Alpelisib can cause serious cutaneous reactions, including severe drug-related skin reactions.
Patients should report significant rash, blistering, peeling skin or mucosal involvement promptly.
Diarrhea and Colitis
Diarrhea is common and can sometimes become severe.
Severe diarrhea may cause dehydration and acute kidney injury. Colitis can also occur.
Patients should promptly notify their healthcare professional if significant diarrhea develops.
Lung Considerations
Alpelisib can rarely cause pneumonitis or interstitial lung disease.
New or worsening respiratory symptoms should be medically evaluated.
Liver Considerations
Liver enzyme abnormalities may occur, so clinical monitoring may be appropriate depending on the patient's circumstances.
Kidney Considerations
Renal problems can occur, particularly when severe diarrhea causes dehydration.
Adequate fluid management and medical monitoring are important when significant gastrointestinal toxicity develops.
Pregnancy and Breastfeeding
Alpelisib can cause fetal harm and should not be used during pregnancy unless specifically determined appropriate by the treating physician. The FDA recommends counselling patients about potential fetal risk and effective contraception.
Patients who may become pregnant should discuss contraception and pregnancy planning with their healthcare professional.
The FDA prescribing information advises against breastfeeding during alpelisib treatment.
Special Populations
Elderly Patients
Older adults may receive alpelisib when clinically appropriate. Treatment decisions should consider:
- Overall health
- Diabetes or glucose-control status
- Kidney function
- Other medicines
- Treatment tolerance
Pediatric Patients
The breast-cancer indication is an adult indication. Pediatric use should not be extrapolated from adult dosing and should only occur under appropriate specialist guidance and an approved indication.
Alpelisib also has a separate FDA-approved indication for certain patients aged 2 years and older with severe manifestations of PIK3CA-related overgrowth spectrum (PROS), using indication-specific formulations and dosing.
Renal Impairment
Patients with kidney impairment should inform their healthcare professional before treatment.
Kidney function becomes particularly important when severe diarrhea or dehydration occurs.
Hepatic Impairment
Patients with liver impairment should be evaluated individually before and during therapy. Monitoring may be appropriate based on hepatic function and concomitant treatment.
Storage of ALPESIB 150 mg
Store ALPESIB 150 mg according to the specific instructions printed on its packaging.
General medicine-storage precautions include:
- Keep tablets in their original packaging.
- Protect from inappropriate heat and moisture.
- Keep out of direct environmental exposure where applicable.
- Keep out of reach of children.
- Do not use damaged or visibly altered tablets.
- Follow the specific storage conditions supplied with the product.
For reference, the FDA labeling for alpelisib tablets specifies controlled room-temperature storage of 20°C to 25°C (68°F to 77°F), with permitted excursions between 15°C and 30°C.
Frequently Asked Questions About ALPESIB 150 mg
1. What is ALPESIB 150 mg used for?
ALPESIB 150 mg contains alpelisib, a targeted PI3K inhibitor used in combination with fulvestrant for appropriately selected adults with PIK3CA-mutated HR-positive, HER2-negative advanced or metastatic breast cancer.
2. What is alpelisib?
Alpelisib is a targeted anticancer medicine that inhibits PI3K alpha.
3. Is alpelisib a chemotherapy drug?
Alpelisib is a targeted kinase inhibitor rather than conventional cytotoxic chemotherapy.
4. How does alpelisib work?
It inhibits PI3K alpha activity, interfering with abnormal signalling associated with PIK3CA-mutated cancer cells.
5. What is the usual dose of alpelisib?
For the approved breast-cancer indication, the recommended dose is 300 mg once daily with food, equivalent to two 150 mg tablets.
6. Does alpelisib need to be taken with food?
Yes. The approved product information specifies administration with food.
7. What are the common side effects of alpelisib?
Common adverse effects include hyperglycemia, diarrhea, rash, nausea, fatigue, decreased appetite, weight loss and laboratory abnormalities.
8. Can alpelisib cause high blood sugar?
Yes. Hyperglycemia is one of the most important adverse effects associated with alpelisib and requires glucose monitoring.
9. Can alpelisib cause diarrhea?
Yes. Diarrhea is common and can become severe in some patients.
10. What is a PIK3CA mutation?
A PIK3CA mutation is a genetic alteration that can activate the PI3K signalling pathway and contribute to cancer-cell growth.
11. Is alpelisib used for breast cancer?
Yes. It is used for specific PIK3CA-mutated HR-positive, HER2-negative advanced or metastatic breast cancer in combination with fulvestrant.
12. Is alpelisib used alone?
For the approved breast-cancer indication, alpelisib is used in combination with fulvestrant rather than as standalone therapy.
13. Can alpelisib cause skin reactions?
Yes. Serious cutaneous adverse reactions can occur and require prompt medical assessment.
14. Can alpelisib affect the lungs?
Pneumonitis and interstitial lung disease are recognized risks. New respiratory symptoms should be evaluated.
15. Can alpelisib cure breast cancer?
It should not be described as a guaranteed cure. It is a targeted treatment intended to control appropriately selected advanced or metastatic breast cancer.
Global Medicine Information & Support by RootAid Pharma
RootAid Pharma provides pharmaceutical information and specialty-medicine support for individuals and organizations seeking information about prescription and high-value medicines.
Our medicine-information resources can help international visitors understand:
- Oncology medicines
- Targeted cancer therapies
- Breast cancer medicines
- Generic and brand medicine information
- Therapeutic classes
- Medicine indications
- Dosage information
- Safety considerations
- Drug interactions
- Prescription-related support
- International medicine information
For medicines such as alpelisib, treatment should be supervised by a qualified oncologist.
RootAid Pharma can provide medicine-related information and supply assistance where legally and operationally applicable. Availability, prescription requirements, import regulations and local requirements may vary between countries.
RootAid Pharma does not replace a physician, oncologist or pharmacist and does not claim to manufacture ALPESIB or alpelisib.
Suggested Internal Links
- Oncology Medicines
- Breast Cancer Medicines
- Targeted Cancer Medicines
- PI3K Inhibitors
- Hormone Receptor Positive Breast Cancer
- Prescription Support
- Upload Prescription
- Global Medicine Information
- Contact RootAid Pharma
Medical Disclaimer
This article is provided for general educational and informational purposes only. It does not replace professional medical advice, diagnosis, individualized treatment planning or official prescribing information.
Alpelisib is a prescription medicine intended for specific patients with appropriate clinical and molecular indications. Dose, treatment duration, monitoring and dose adjustments must be determined by a qualified healthcare professional.
Approved indications, formulations, dosing recommendations, contraindications and regulatory requirements may differ between countries and may change over time. Patients should consult the official product information applicable to their location.
Do not start, stop, increase or reduce alpelisib without medical advice.
Need help after reading this?
Talk to our support team for sourcing guidance, product availability, and global delivery assistance.