# Inavolisib

Source: https://onco.cc/drugs/inavolisib/  
OnCo record `inavolisib` (Treatment). Data CC BY-NC 4.0, attribute "Data from OnCo (onco.cc)"; commercial use needs a licence.

## TL;DR

Inavolisib is a PI3K drug that also destroys the mutant protein, approved in 2024 with palbociclib and fulvestrant for PIK3CA-mutant breast cancer.

## Summary

Inavolisib is a PI3K-alpha-selective inhibitor that also promotes degradation of the mutant p110-alpha protein, combining enzyme blockade with removal of the target. It is taken as 9 mg once daily with palbociclib and fulvestrant, and was approved in 2024 for PIK3CA-mutant HR-positive, HER2-negative advanced breast cancer on INAVO120, where the triplet improved progression-free survival to 15.0 versus 7.3 months in endocrine-resistant disease, with an overall survival benefit reported in 2025. Roche/Genentech developed it. Hyperglycaemia, stomatitis, neutropenia and rash are the main adverse events. INAVO120 enrolled patients relapsing during or soon after adjuvant endocrine therapy, so its value in other PIK3CA-mutant settings is still being defined. For a newcomer: a PI3K drug that both blocks and destroys the mutant protein.

## Fields

- Kind: Treatment
- Status: approved
- Last checked: 2026-09-04
- Brand: Itovebi
- Modality: Small-molecule PI3Kα inhibitor and degrader
- Mechanism: PI3Kα-selective inhibitor that promotes degradation of mutant p110α.
- Approvals: US 2024: PIK3CA-mutant HR+/HER2- advanced breast cancer with palbociclib and fulvestrant; EU 2025: PIK3CA-mutant ER+/HER2- mBC with palbociclib + fulvestrant; 18 Jul 2025
- Dosing: Oral; 9 mg once daily with palbociclib and fulvestrant

## Sources

- Wikipedia: https://en.wikipedia.org/wiki/Inavolisib
- FDA label (DailyMed): https://dailymed.nlm.nih.gov/dailymed/search.cfm?query=Inavolisib

## Connected records

- pairings: [PI3K/AKT-pathway inhibitor + endocrine therapy (± CDK4/6)](https://onco.cc/pairings/pi3k-pathway-plus-endocrine/)
- biomarkers: [PIK3CA mutation](https://onco.cc/biomarkers/pik3ca-hotspot-mutation/)
- cancers: [HER2-positive breast cancer](https://onco.cc/cancers/breast-her2-positive/), [HR-positive / HER2-negative breast cancer](https://onco.cc/cancers/breast-hr-positive/), [HR-positive metastatic breast cancer after CDK4/6 inhibitors](https://onco.cc/cancers/hr-positive-metastatic-post-cdk46/)
- technologies: [PI3K, AKT and mTOR inhibitors](https://onco.cc/technologies/pi3k-akt-mtor-inhibitors/), [Small-molecule kinase inhibitors](https://onco.cc/technologies/kinase-inhibitors/)
- targets: [PIK3CA / PI3K-alpha](https://onco.cc/targets/pik3ca/)
- companies: [Roche / Genentech](https://onco.cc/companies/roche-genentech/)
- terms: [Hyperglycaemia (PI3K/AKT inhibitor class effect)](https://onco.cc/terms/hyperglycaemia/), [PTEN loss](https://onco.cc/terms/pten-loss/)
- trials: [A Phase II Study Evaluating the Efficacy and Safety of Inavolisib Plus Ribociclib Plus Fulvestrant Versus Placebo Plus Ribociclib Plus Fulvestrant in Participants With Advanced Breast Cancer](https://onco.cc/trials/nct07405801/), [A Phase II, Single-arm Study to Evaluate the Efficacy and Safety of Inavolisib in Combination With Eribulin in Pretreated Advanced Triple-negative Breast Cancer](https://onco.cc/trials/nct07441512/), [A Study Evaluating the Efficacy and Safety of Inavolisib Plus CDK4/6 Inhibitor and Letrozole vs Placebo + CDK4/6i and Letrozole in Participants With Endocrine-Sensitive PIK3CA-Mutated, Hormone Receptor-Positive, HER2-Negative Advanced Breast Cancer](https://onco.cc/trials/nct06790693/), [A Study Evaluating the Efficacy and Safety of Inavolisib Plus Fulvestrant Compared With Alpelisib Plus Fulvestrant in Participants With HR-Positive, HER2-Negative, PIK3CA Mutated, Locally Advanced or Metastatic Breast Cancer Post CDK4/6i and Endocrine Combination Therapy](https://onco.cc/trials/nct05646862/), [A Study Evaluating the Efficacy and Safety of Multiple Treatment Combinations in Participants With Breast Cancer](https://onco.cc/trials/nct04802759/), [A Study to Evaluate the Efficacy and Safety of Inavolisib in Combination With Phesgo Versus Placebo in Combination With Phesgo in Participants With PIK3CA-Mutated HER2-Positive Locally Advanced or Metastatic Breast Cancer](https://onco.cc/trials/nct05894239/), [A Study to Test Inavolisib Treatment in Participants With Metastatic Castration-Resistant Prostate Cancer](https://onco.cc/trials/nct07287150/), [A Study to Test Inavolisib Treatments in Participants With Early-Stage, PIK3CA-Mutated Breast Cancer](https://onco.cc/trials/nct07054190/), [INAVO120](https://onco.cc/trials/inavo120/), [To Study the Effect of Inavolisib in Combination With Fulvestrant in Participants With Breast Cancer](https://onco.cc/trials/nct07368998/), [Tumor-agnostic Precision Immuno-oncology and Somatic Targeting Rational for You (TAPISTRY) Platform Study](https://onco.cc/trials/nct04589845/)
- ideas: [Molecular-progression switching beyond ESR1](https://onco.cc/ideas/idea-ctdna-switch-generalised/)
- pathways: [Breast cancer (KEGG map)](https://onco.cc/pathways/breast-cancer-signalling/), [PI3K / AKT / mTOR](https://onco.cc/pathways/pi3k-akt-mtor/)
- people: [Komal Jhaveri](https://onco.cc/people/komal-jhaveri/)
- roadmaps: [Hormonal therapy roadmap: removing the ovaries → tamoxifen → oral degraders switched by a blood test](https://onco.cc/roadmaps/hormonal-therapy-roadmap/)

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