Inavolisib
Inavolisib is a targeted cancer therapy that inhibits the phosphatidylinositol 3-kinase (PI3K) pathway, specifically targeting the mutated form of the PI3Kα catalytic subunit encoded by the PIK3CA gene. By degrading the mutant p110α protein, it inhibits tumor cell proliferation in cancers harboring PIK3CA mutations. This medication is used in the treatment of certain solid tumors with PIK3CA mutations, most notably hormone receptor-positive, HER2-negative breast cancer.
Inavolisib is a PI3K inhibitor that targets and degrades mutated PI3Kα to treat PIK3CA-mutated cancers.
Key facts at a glance
- ATC
- L01EM06
- RxNorm
- 2695422
- Generic
- Inavolisib
- Class
- atc-l01
- Brands
- Itovebi
- 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.
Inavolisib is indicated for the treatment of adults with PIK3CA-mutated, hormone receptor-positive, HER2-negative locally advanced or metastatic breast cancer who have progressed following endocrine-based therapy. Testing for PIK3CA mutations is required prior to treatment initiation.
Inavolisib is a PI3K inhibitor with predominant activity against the PI3Kα isoform. It selectively binds to and induces degradation of the mutated p110α catalytic subunit of PI3K (encoded by the PIK3CA gene), thereby inhibiting downstream signaling pathways including AKT phosphorylation. This leads to inhibition of tumor cell growth and proliferation in PIK3CA-mutated cancer cells.
Common adverse reactions may include hyperglycemia, rash, and gastrointestinal symptoms. As a PI3K inhibitor, it requires regular monitoring of blood glucose levels. The medication should be taken consistently with or without food, and dose modifications may be necessary based on tolerability. Patients should be advised about potential drug interactions and the importance of adherence to the prescribed dosing schedule.
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