Details of how to report adverse events are available at the bottom of the page.
For full information on a Roche medicine, please see the relevant Summary of Product Characteristics.
Itovebi, in combination with palbociclib and fulvestrant, is indicated for the treatment of adult patients with PIK3CA-mutated, ER-positive, HER2-negative, locally advanced or metastatic breast cancer, following recurrence on or within 12 months of completing adjuvant endocrine treatment.1
Patients previously treated with a CDK4/6 inhibitor in the (neo)adjuvant setting should have had an interval of at least 12 months between termination of CDK4/6 inhibitor treatment and the detection of recurrence.1
In pre/perimenopausal women and in men, endocrine therapy should be combined with a luteinising hormone-releasing hormone agonist.1
.
If you have any questions or require further information, please click the appropriate button below to contact our team.
INAVO120 is a Phase III, randomised, double-blind, placebo-controlled, multicentre, global study assessing the efficacy and safety of Itovebi + palbociclib and fulvestrant vs placebo + palbociclib and fulvestrant in patients with PIK3CA-mutated endocrine-resistant HR+/HER2– LA or mBC.1,3
*Patients were enrolled between 29 January 2020 and 14 September 2023.3 †Premenopausal or perimenopausal women and men received a luteinising hormone–releasing hormone agonist for hormone suppression for the duration of the trial intervention.3 ‡PIK3CA mutation status was prospectively determined in a central laboratory using the FoundationOne® Liquid CDx assay on ctDNA or in local laboratories using various validated PCR or NGS assays on tumour tissue or plasma; in China, the PredicineCARE next-generation sequencing assay (Huidu) was used.3 §As assessed by the investigator according to RECIST 1.1.3
Baseline disease characteristics were generally balanced between both arms of the study.3
INAVO120: Outcomes and implications for eligible patients
Discover key outcomes from the INAVO120 trial and how Itovebi could benefit your patients with PIK3CA-mutated ER+/HER2– LA or mBC who display resistance to endocrine therapy.
6-min watch
Itovebi: Practical guidance for AE management
Learn how to proactively monitor and manage key AEs to help your patients access the potential benefits of Itovebi.
12-min watch
Itovebi + palbociclib and fulvestrant demonstrated a significantly longer PFS vs. placebo + palbociclib and fulvestrant.3
Adapted from Turner et al. 2024.3
21.3-month median follow-up in the Itovebi group and 21.5-month median follow-up in the placebo group.3
*As assessed by investigator according to RECIST 1.1.3
Itovebi + palbociclib and fulvestrant demonstrated a significant OS benefit vs. placebo + palbociclib and fulvestrant.4
Adapted from Jhaveri et al. 2025.4
34.2-month median follow-up in the Itovebi group and 32.3-month median follow-up in the placebo group.4
An ORR* of 62.7% was observed in patients receiving Itovebi + palbociclib and fulvestrant, compared to 28.0% in those receiving placebo + palbociclib and fulvestrant.4
ORR was assessed for significance based on the protocol-defined hierarchical statistical testing once OS reached statistical significance at the updated analyses (CCOD: 15 November 2024).4
Adapted from Jhaveri et al. 2025.4
34.2-month median follow-up in the Itovebi group and 32.3-month median follow-up in the placebo group.4
*Per RECIST 1.1. ORR is defined as the proportion of patients with a CR or PR on two consecutive occasions ≥4 weeks apart, as determined by the investigator.1
34.2-month median follow-up in the Itovebi group and 32.3-month median follow-up in the placebo group.4
*Per RECIST 1.1. ORR is defined as the proportion of patients with a CR or PR on two consecutive occasions ≥4 weeks apart, as determined by the investigator.1
Adverse drug reactions observed in patients treated with Itovebi1
Grading according to CTCAE version 5.0.1
*No Grade 4 events were observed.1 †Includes hyperglycaemia, blood glucose increased, hyperglycaemic crisis, glycated serum protein increased, glucose tolerance impaired, diabetes mellitus, Type 2 diabetes mellitus and glycosylated haemoglobin increased.1 ‡Adverse reaction reported during post-marketing experience. The frequency category was estimated as the upper limit of the 95% confidence interval calculated on the basis of the total number of patients exposed to Itovebi in clinical trials.1 §Includes aphthous ulcer, glossitis, glossodynia, lip ulceration, mouth ulceration, mucosal inflammation and stomatitis.1 ¶Includes rash, rash erythematous, rash maculo-papular, rash papular, rash pruritic and rash pustular.1 #Includes dry skin, skin fissures, xerosis and xeroderma.1 **Includes dermatitis, dermatitis acneiform and dermatitis bullous.1
Management of AEs may require temporary interruption, dose reduction or discontinuation of Itovebi.1
Permanent discontinuation of Itovebi due to an adverse reaction occured in 3.1% of patients.1
The adverse reactions leading to permanent discontinuation of Itovebi include:1
- Hyperglycaemia: 1.2%
- Stomatitis: 0.6%
- Alanine transaminase increased: 0.6%
- Weight decreased: 0.6%
*Itovebi treatment should be permanently discontinued if patients are unable to tolerate the 3 mg dose.1
Itovebi offers continuous once-daily dosing1
Itovebi should be taken in combination with palbociclib and fulvestrant on a 28-day cycle1
- Itovebi: 9 mg taken orally once daily (at the same time of day with or without food) until disease progression or unacceptable toxicity.
The tablets should be swallowed whole and not chewed, crushed, dissolved or divided1 - Palbociclib: 125 mg taken orally once daily for 21 consecutive days followed by 7 days off treatment1
- Fulvestrant: 500 mg administered intramuscularly on Cycle 1, Days 1 and 15, then on Day 1 of every 28-day cycle thereafter1
If a dose of Itovebi is missed, it can be taken within 9 hours of the usual time. After more than 9 hours, skip that day and resume the next day at the usual time. If vomiting occurs after taking the Itovebi dose, do not take again, just resume the next day at the usual time1
Refer to the full SmPC for palbociclib and fulvestrant for more dosing information.1
- Treatment with Itovebi should be initiated by a physician experienced in the use of anticancer therapies. Patients should be selected for treatment with Itovebi based on the presence of one or more PIK3CA mutations1
- Treatment of pre/perimenopausal women and men with Itovebi should also include an LHRH agonist in accordance with local clinical practice1
Itovebi is available in 9 mg and 3 mg tablets1
HOW ITOVEBI IS SUPPLIED
- Itovebi 3 mg film-coated tablets: Approximately 6 mm in diameter1
- Itovebi 9 mg film-coated tablets: Approximately 13 mm in length and 6 mm in width1
- Itovebi is packaged in an aluminium/aluminium perforated unit-dose blisters in cartons of 28 × 1 film-coated tablets1
DOSE REDUCTION OF ITOVEBI FOR ADVERSE REACTIONS1
Tablets not actual size.
- Itovebi is contraindicated in those with hypersensitivity to the active substance (inavolisib) or to any of the excipients listed in Section 6.1 of the SmPC. Itovebi treatment should be permanently discontinued if patients are unable to tolerate the 3 mg daily dose1
- No dose adjustment of Itovebi is required in patients ≥65 years of age1
- For patients with mild renal impairment (eGFR 60 to <90 mL/min)1
- For patients with mild hepatic impairment (total bilirubin >ULN to ≤1.5 x ULN or AST >ULN and total bilirubin ≤ULN)1
- The recommended starting dose of Itovebi for patients with moderate renal impairment (eGFR 30 to <60 mL/min) is 6 mg orally once daily1
- Refer to the SmPC for more information in special populations1
Please see the SmPC for further details prior to initiating therapy.
Hyperglycaemia1
- Frequently reported in patients treated with Itovebi. Severe cases of hyperglycaemia, including ketoacidosis with fatal complications, have occurred
- Safety and efficacy in patients with T1DM and T2DM requiring ongoing anti-hyperglycaemic therapy is limited as these were excluded from the INAVO120 study
- Metformin premedication can be considered in patients with risk factors for hyperglycaemia
Stomatitis1
- Patients should be advised to start alcohol-free corticosteroid mouthwash at the first signs, or can be given as prophylaxis
Use in patients who previously received a CDK4/6 inhibitor1
- Information on efficacy is limited in patients who previously received a CDK4/6 inhibitor as part of neoadjuvant or adjuvant treatment. Efficacy may be lower in such patients
Lactose1
- Patients with rare hereditary problems of galactose intolerance, total lactase deficiency or glucose-galactose malabsorption should not take this medicine
Potential interaction with other medicinal products (no interaction studies done, based on in vitro signals)1
- Low likelihood of clinically relevant interactions between Itovebi and CYP inhibitors or inducers
- Use with caution in combination with sensitive CYP3A4 substrates with a narrow therapeutic index (e.g., alfentanil, astemizole, cisapride, cyclosporine, quinidine, sirolimus, tacrolimus)
- Use with caution in combination with sensitive substrates of these enzymes with a narrow therapeutic index (e.g., paclitaxel, warfarin, phenytoin, S-mephenytoin)
Effects on ability to drive and use machines1
- Itovebi has minor influence on the ability to drive or use machines because fatigue has been reported during treatment
Fertility, pregnancy and lactation1
- Itovebi is not recommended during pregnancy due to the potential risk to the foetus. Pregnancy status should be verified prior to initiating therapy. Patients and/or their partners are advised to use effective non-hormonal contraception during treatment and for 1 week after the last dose of Itovebi
- It is unknown whether Itovebi or its metabolites are excreted in human milk. Breastfeeding should be discontinued during treatment and for 1 week after the last dose of Itovebi
- No human data on the effect of Itovebi on fertility are available
For full prescribing and safety information please refer to Itovebi Summary of Product Characteristics.
Abbreviations
1L, first-line; AE, adverse event; AST, aspartate aminotransferase; C1D1/15, cycle 1 day 1 and 15; CCOD, clinical cut-off date; CDK4/6, cyclin-dependent kinase 4/6; CDx, companion diagnostic; CI, confidence interval; CR, complete response; CTCAE, Common Terminology Criteria for Adverse Events; ctDNA, circulating tumour DNA; DOR, duration of response; eGFR, estimated glomerular filtration rate; ER, oestrogen receptor; ESMO, European Society of Medical Oncology; HBA1c, haemoglobin A1c; HER2, human epidermal growth factor receptor 2; HR, hazard ratio; HR, hormone receptor; IM, intramuscular; LA, locally advanced; LHRH, luteinising hormone-releasing hormone; mBC, metastatic breast cancer; mOS, median overall survival; mPFS, median progression-free survival; NGS, next-generation sequencing; ORR, objective response rate; OS, overall survival; PCR, polymerase chain reaction; PFS, progression-free survival; PIK3CA, phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha; PO, orally; PR, partial response; Q4W, every 4 weeks; QD, once daily; RECIST, Response Evaluation Criteria In Solid Tumours; SmPC, Summary of Product Characteristics; T1DM, type 1 diabetes mellitus; T2DM, type 2 diabetes mellitus; ULN, upper limit of normal.
References
- Itovebi (inavolisib) Summary of Product Characteristics.
- ESMO. ESMO Living Guideline: Metastatic Breast Cancer. Version 1.2. Available at: https://www.esmo.org/guidelines/living-guidelines/esmo-living-guideline-metastatic-breast-cancer/. Accessed February 2026.
- Turner NC, et al. N Engl J Med. 2024;391(17):1584–96.
- Jhaveri KL, et al. N Engl J Med. 2025;393(2):151–61.