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Itovebi (INAVOLISIB)
Itovebi works by blocking a specific enzyme called PIK3CA, which is involved in the growth and spread of cancer cells.
Itovebi (inavolisib) is a small molecule kinase inhibitor developed by Genentech Inc. It is used to treat endocrine-resistant, PIK3CA-mutated, hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative, locally advanced or metastatic breast cancer. Itovebi was approved by the FDA in 2025 and is currently patented. Key safety considerations include its half-life of 15 hours and bioavailability of 76%. As a patented drug, there are currently no generic manufacturers.
At a glance
| Generic name | INAVOLISIB |
|---|---|
| Sponsor | Genentech Inc |
| Drug class | Kinase Inhibitor [EPC] |
| Modality | Small molecule |
| Therapeutic area | Oncology |
| Phase | FDA-approved |
| First approval | 2025 |
Mechanism of action
Inavolisib is an inhibitor of phosphatidylinositol 3-kinase (PI3K) with inhibitory activity predominantly against PI3Kα. In vitro, inavolisib induced the degradation of mutated PI3K catalytic alpha subunit p110α (encoded by the PIK3CA gene), inhibited phosphorylation of the downstream target AKT, reduced cellular proliferation, and induced apoptosis in PIK3CA -mutated breast cancer cell lines. In vivo, inavolisib reduced tumor growth in PIK3CA -mutated, estrogen receptor-positive, breast cancer xenograft models. The combination of inavolisib with palbociclib and fulvestrant increased tumor growth inhibition compared to each treatment alone or the doublet combinations.
Approved indications
- endocrine-resistant, PIK3CA-mutated, hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative, locally advanced or metastatic breast cancer
Common side effects
- Decreased neutrophils
- Decreased hemoglobin
- Increased fasting glucose
- Decreased platelets
- Decreased lymphocytes
- Stomatitis
- Diarrhea
- Decreased calcium
- Fatigue
- Decreased potassium
- Increased creatinine
- Increased ALT
Key clinical trials
- A Study to Evaluate the Effectiveness and Safety of Inavolisib in Participants With Endocrine-resistant, PIK3CA-mutated, Hormone Receptor-positive, HER2-negative Locally Advanced or Metastatic Breast Cancer
- A Study Evaluating Single-agent Inavolisib, Inavolisib Plus Atezolizumab, and Inavolisib Plus Pembrolizumab in PIK3CA-Mutated Cancers (PHASE1)
- A Study Evaluating the Efficacy and Safety of Inavolisib + Palbociclib + Fulvestrant vs Placebo + Palbociclib + Fulvestrant in Participants With PIK3CA-Mutant, Hormone Receptor-Positive, HER2-Negative, Locally Advanced or Metastatic Breast Cancer (PHASE2,PHASE3)
- To Study the Effect of Inavolisib in Combination With Fulvestrant in Participants With Breast Cancer (PHASE2)
- A Study Evaluating the Efficacy and Safety of Multiple Treatment Combinations in Patients With Metastatic or Locally Advanced Breast Cancer (PHASE1,PHASE2)
- A Study Evaluating the Efficacy and Safety of Multiple Treatment Combinations in Participants With Breast Cancer (PHASE1,PHASE2)
- A Rollover Study for Participants Previously Enrolled in a Genentech and/or F. Hoffman-La Roche Sponsored Study (PHASE3)
- A Study to Evaluate the Effect of Moderate or Severe Hepatic Impairment on the Pharmacokinetics (PK) of Inavolisib (PHASE1)
Patents
| Patent | Expiry | Type |
|---|---|---|
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| FDA label | Mechanism, indications, dosing, boxed warnings, drug interactions |
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
| FDA Orange Book | Patents + exclusivity |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Itovebi CI brief — competitive landscape report
- Itovebi updates RSS · CI watch RSS
- Genentech Inc portfolio CI