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Inavolisib is a PI3K drug that also destroys the mutant protein, approved in 2024 with palbociclib and fulvestrant for PIK3CA-mutant breast cancer.
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.
PI3Kα-selective inhibitor that promotes degradation of mutant p110α. Connects to PIK3CA / PI3K-alpha.
1.Inavolisib binds mutant and wild-type PI3Kα
Background: ADC sequencing, Antigen escape (antigen loss, lineage switch), BCG-unresponsive, Castration-resistant prostate cancer (CRPC), Circulating tumour DNA (ctDNA). Also on OnCo: Resistance: how tumours escape each drug class · Lines of therapy.
Source: www.fda.gov/drugs/resources-information-approved-drugs/oncology-cancer-hematologic-malignancies-approval-notifications. Doses are for orientation; the current label governs.
Oral, self-administered, so it is a Part D drug: covered through a stand-alone Part D plan or Medicare Advantage drug benefit, usually on the specialty tier with 25 to 33% coinsurance until the annual cap ($2,000 in 2025, $2,100 in 2026). FDA-approved October 2024.
Covered for FDA-labelled and NCCN-listed uses, but almost always behind prior authorisation confirming diagnosis, biomarker and line of therapy; dispensed through a specialty pharmacy. PIK3CA mutation and endocrine-resistant disease per the label.
Part D out-of-pocket capped at $2,000 (2025) / $2,100 (2026). Medicare patients cannot use manufacturer co-pay cards; charity funds (PAN, HealthWell, CancerCare) and the Extra Help subsidy are the routes.
Sources: Medicare.gov: Drug coverage (Part D) · Medicare.gov: Costs for Medicare drug coverage (annual out-of-pocket cap). Not medical or financial advice; verify with your plan.
Sources: NICE search: inavolisib. Funding decisions are indication-specific and change monthly; verify with NICE and your treating team.
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PIK3CA-mutant HR+/HER2- endocrine-resistant advanced breast cancer with palbociclib and fulvestrant (INAVO120) source
OS benefit added to label source
| Region | Year | Indication |
|---|---|---|
| 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 |
| Adverse event |
|---|
| Neutropenia |
| Hyperglycaemia |
| Stomatitis |
| Diarrhoea |
| Rash |
| Fatigue |
INAVO120 triplet: most common grade 3-4 (from palbociclib). Events listed without rates were not read from a primary source; see the label. Blank cells mean the figure was not sourced, not that it is zero.
| Country | Reimbursement | List price | Assistance |
|---|---|---|---|
| United States | Medicare Part D (oral); commercial plans per formulary, often with prior authorisation | not disclosed | genentech-access.com |
| United Kingdom | NICE: appraisal for PIK3CA-mutant HR+ breast cancer (2025-26) | not disclosed | - |
List prices are manufacturer or Medicare figures where publicly disclosed; net prices after rebates are usually lower. Reimbursement changes; check the payer.
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Query for this drug: (TITLE:"Inavolisib" OR ABSTRACT:"Inavolisib" OR TITLE:"Itovebi" OR ABSTRACT:"Itovebi") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about Inavolisib, not a curated reading list.
Shares Hyperglycaemia (PI3K/AKT inhibitor class effect), 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, PI3K/AKT-pathway inhibitor + endocrine therapy (± CDK4/6), PIK3CA mutation.
Shares Hyperglycaemia (PI3K/AKT inhibitor class effect), PI3K/AKT-pathway inhibitor + endocrine therapy (± CDK4/6), Molecular-progression switching beyond ESR1, PIK3CA mutation.
Shares 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, 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, A Study to Test Inavolisib Treatments in Participants With Early-Stage, PIK3CA-Mutated Breast Cancer, To Study the Effect of Inavolisib in Combination With Fulvestrant in Participants With Breast Cancer.
Shares PI3K, AKT and mTOR inhibitors, HR-positive metastatic breast cancer after CDK4/6 inhibitors, Hormonal therapy roadmap: removing the ovaries → tamoxifen → oral degraders switched by a blood test, PIK3CA / PI3K-alpha.
Shares A Study to Test Inavolisib Treatments in Participants With Early-Stage, PIK3CA-Mutated Breast Cancer, A Study Evaluating the Efficacy and Safety of Multiple Treatment Combinations in Participants With Breast Cancer, HR-positive metastatic breast cancer after CDK4/6 inhibitors, Hormonal therapy roadmap: removing the ovaries → tamoxifen → oral degraders switched by a blood test.
Shares PI3K, AKT and mTOR inhibitors, HR-positive metastatic breast cancer after CDK4/6 inhibitors, Hormonal therapy roadmap: removing the ovaries → tamoxifen → oral degraders switched by a blood test, PIK3CA / PI3K-alpha.
Shares HR-positive metastatic breast cancer after CDK4/6 inhibitors, Hormonal therapy roadmap: removing the ovaries → tamoxifen → oral degraders switched by a blood test, PIK3CA / PI3K-alpha, PI3K / AKT / mTOR.
Shares A Study Evaluating the Efficacy and Safety of Multiple Treatment Combinations in Participants With Breast Cancer, Tumor-agnostic Precision Immuno-oncology and Somatic Targeting Rational for You (TAPISTRY) Platform Study, HR-positive metastatic breast cancer after CDK4/6 inhibitors, Roche / Genentech.