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Inavolisib

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

INAVO120: PFS 15.0 vs 7.3 months in endocrine-resistant PIK3CA-mutant HR+/HER2- breast cancer; OS benefit reported 2025. Roche/Genentech.

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Inavolisib
PubChem
Mechanism, step by step
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1.Inavolisib binds mutant and wild-type PI3Kα

Modality
Small-molecule PI3Kα inhibitor and degrader
Mechanism
PI3Kα-selective inhibitor that promotes degradation of mutant p110α.
Brand / code
Itovebi
Dosing & schedule
Route
Oral
Schedule
9 mg once daily with palbociclib and fulvestrant
Dose modifications
Reduce to 6 then 3 mg for hyperglycaemia, stomatitis, diarrhoea
Monitoring
Fasting glucose weekly for 4 weeks then every 4 weeks; HbA1c; oral care

Source: www.fda.gov/drugs/resources-information-approved-drugs/oncology-cancer-hematologic-malignancies-approval-notifications. Doses are for orientation; the current label governs.

Medicare
Part D (self-administered)

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.

Commercial insurance
covered with prior authorisation

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.

Assistance programmes

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.

Appraisal in progressSearch NICE
Notes
Recently licensed; a NICE appraisal is scheduled or in progress. Interim access may be possible via the CDF interim funding route once NICE issues positive draft guidance.

Sources: NICE search: inavolisib. Funding decisions are indication-specific and change monthly; verify with NICE and your treating team.

Regulatory

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  1. 10 Oct 2024ApprovalUS

    PIK3CA-mutant HR+/HER2- endocrine-resistant advanced breast cancer with palbociclib and fulvestrant (INAVO120) source

  2. Jun 2025Label changeUS

    OS benefit added to label source

Approvals

RegionYearIndication
US2024PIK3CA-mutant HR+/HER2- advanced breast cancer with palbociclib and fulvestrant

Safety

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Toxicity profile
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.

Cost & access

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Cost & access
CountryReimbursement
United StatesMedicare Part D (oral); commercial plans per formulary, often with prior authorisation
United KingdomNICE: appraisal for PIK3CA-mutant HR+ breast cancer (2025-26)

List prices are manufacturer or Medicare figures where publicly disclosed; net prices after rebates are usually lower. Reimbursement changes; check the payer.

Trials

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ClinicalTrials.gov · phase 2/3
refreshed 2026-09-06
28 studies15 recruiting24 Phase 25 Phase 3
Search “Inavolisib” on ClinicalTrials.gov →
Counts are from a name search and may include unrelated studies; up to 100 studies are summarised.

Recruiting now (live from ClinicalTrials.gov)

Recruiting trials near you · live from ClinicalTrials.gov
Inavolisib
intervention: Inavolisib
Open on ClinicalTrials.gov →

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Latest papers

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Literature trend45 papers in the last 12 months+105% vs prior 12How this is computed
Latest papers · live from Europe PMC
Open in Europe PMC

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.

Connected

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