Alpelisib
Alpelisib is an oral targeted therapy that inhibits PI3Kα, a protein involved in cell growth and survival. It is specifically used to treat hormone receptor-positive, HER2-negative advanced breast cancer in patients whose tumors have PIK3CA mutations, often in combination with fulvestrant.
Alpelisib is a PI3K inhibitor used for HR+/HER2- breast cancer with PIK3CA mutations.
Key facts at a glance
- ATC
- L01EM03
- RxNorm
- 2169285
- Generic
- Alpelisib
- Class
- atc-l01
- Brands
- Piqray, Vijoice
- Availability
- rx
- Lactation
- unknown
- Routes
- oral
- Forms
- tablet
- Regions
- US, EU, CN, JP
- Monitoring
- —
This page is for informational purposes only.
Do not use this information to diagnose yourself or to replace a physician's advice. Always consult a qualified healthcare provider before starting, stopping, or changing any medication. If you believe you are experiencing a medical emergency, call your local emergency number immediately.
Dosage and administration
- Usual dose
- 500mg twice daily
- Maximum
- consult physician
- Frequency
- every 12 hours
- Instructions
- Follow physician instructions
- Duration limits
- as prescribed
- Monitoring
- standard
- Usual dose
- 250mg twice daily
- Maximum
- consult physician
- Frequency
- every 12 hours
- Instructions
- Follow physician instructions
- Duration limits
- as prescribed
- Monitoring
- standard
- Usual dose
- 400mg daily
- Maximum
- consult physician
- Frequency
- once daily
- Instructions
- Follow physician instructions
- Duration limits
- as prescribed
- Monitoring
- standard
Overdose information
Special Populations
10 groupspregnancy
first trimesteravoid if possible
avoid use during pregnancy unless benefits outweigh risks; discuss with healthcare provider
regular fetal monitoring and ultrasound assessments
Use of this medication in this population requires careful consideration of risks and benefits.
pregnancy
second trimesteravoid if possible
continue avoidance; consider discontinuing therapy if pregnancy occurs
regular fetal monitoring
Use of this medication in this population requires careful consideration of risks and benefits.
pregnancy
third trimesteravoid if possible
avoid use near delivery; discuss delivery planning with oncology and obstetrics teams
fetal growth monitoring and non-stress tests
Use of this medication in this population requires careful consideration of risks and benefits.
lactation
breastfeedingcontraindicated
do not breastfeed during treatment and for at least 1 week after last dose
monitor infant for adverse reactions
Use of this medication in this population requires careful consideration of risks and benefits.
geriatric
elderly 65 plusno adjustment required
no overall differences in safety or efficacy observed; monitor for adverse reactions
regular monitoring of blood glucose and for signs of toxicity
Use with caution and monitor for adverse effects.
pediatric_age
children adolescentsnot recommended
safety and efficacy not established in pediatric patients; do not use in children under 18
not applicable
Use of this medication in this population requires careful consideration of risks and benefits.
renal_impairment
mildno adjustment required
no dose adjustment needed for mild renal impairment
standard monitoring
renal_impairment
moderateno adjustment required
use with caution; no dose adjustment based on population PK analysis
monitor renal function periodically
Use with caution and monitor for adverse effects.
hepatic_impairment
mildno adjustment required
no dose adjustment needed for mild hepatic impairment
standard monitoring
hepatic_impairment
moderateno adjustment required
use with caution; no dose adjustment based on PK studies
monitor liver function tests
Use with caution and monitor for adverse effects.
Statistics and clinical data
Drug class
Alpelisib is a phosphatidylinositol-3-kinase (PI3K) alpha inhibitor
FDA approval year
FDA approved Alpelisib (Piqray) for breast cancer treatment
Common uses
Primary therapeutic indication
Additional uses
Second FDA-approved indication for rare disease
Treatment of HR-positive, HER2-negative, PIK3CA-mutated advanced or metastatic breast cancer in combination with fulvestrant in men and postmenopausal women who have progressed on or after endocrine therapy.
Alpelisib inhibits phosphatidylinositol-3-kinase alpha (PI3Kα), blocking the PI3K/Akt signaling pathway. This pathway is hyperactive in tumors with PIK3CA mutations, driving cancer cell growth and survival. By inhibiting this pathway, Alpelisib helps control tumor growth.
Requires confirmation of PIK3CA mutation through an FDA-approved test before starting treatment. Common side effects include hyperglycemia, rash, diarrhea, and nausea. May cause severe skin reactions; discontinue if severe. Regular blood glucose monitoring is required. Women of reproductive potential should use effective contraception during and after treatment.
Contraindications
Conditions and patient states where this medication should be avoided or used with caution.
Do not use (1)
Known allergy to this medication or its components
Use caution (1)
Consult healthcare provider for benefits vs risks assessment
Official drug label
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This information is for educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment.
This content is for general informational and educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the guidance of a qualified healthcare provider with any questions you have about a medical condition, and never disregard professional medical advice or delay seeking it because of something you read here.
If you think you may have a medical emergency, call your local emergency number or go to the nearest emergency department immediately.
Medically reviewed by WellAlly Editorial Team Last reviewed July 26, 2026. · Read our editorial policy