- Approval Id
- a02017f03fbc31b5
- Drug Approval Emc Name
- Itovebi 9 mg Film-Coated Tablet
- Drug Name
- Itovebi 9 mg Film-Coated Tablet
- Company Address
- Hexagon Place, 6 Falcon Way, Shire Park, Welwyn Garden City, Hertfordshire, AL7 1TW
- Company Website
- http://www.roche.co.uk
- Company Telephone
- +44 (0)1707 366 000
- Company Fax
- +44 (0)1707 384555
- Company Medical Info Direct Line
- +44 (0)800 328 1629
- Company Medical Info Email
- [email protected]
- Company Customer Care Direct Line
- +44 (0)800 731 5711
- Company Medical Info Fax
- +44 (0)1707 384555
- Atc Code
- L01EM06
- Legal Category
- Prescription only medicine
- Authorisation Holder
- 7. Marketing authorisation holder Roche Products Limited 6 Falcon Way, Shire Park Welwyn Garden City AL7 1TW United Kingdom
- Authorisation Number
- 8. Marketing authorisation number(s) PL 00031/0946 PL 00031/0947
- Authorisation Date
- 9. Date of first authorisation/renewal of the authorisation 26 November 2025
- Instruction Authorisation Holder
- 7. Marketing authorisation holder Roche Products Limited 6 Falcon Way, Shire Park Welwyn Garden City AL7 1TW United Kingdom
- Instruction Authorisation Number
- 8. Marketing authorisation number(s) PL 00031/0946 PL 00031/0947
- Instruction Authorisation Date
- 9. Date of first authorisation/renewal of the authorisation 26 November 2025
- Instruction Composition
- 2. Qualitative and quantitative composition Itovebi 3 mg film-coated tablets Each film-coated tablet contains 3 mg of inavolisib. Excipient(s) with known effect Each film-coated tablet contains 22 mg of lactose. Itovebi 9 mg film-coated tablets Each film-coated tablet contains 9 mg of inavolisib. Excipient(s) with known effect Each film-coated tablet contains 66 mg of lactose. For the full list of excipients, see section 6.1.
- Instruction Dosage Form
- 3. Pharmaceutical form Film-coated tablet (tablet). Itovebi 3 mg film-coated tablets Red, round convex-shaped film-coated tablet with an “INA 3” debossing on one side. Approximate diameter: 6 mm. Itovebi 9 mg film-coated tablets Pink, oval film-coated tablet with an “INA 9” debossing on one side. Approximate size: 13 mm (length), 6 mm (width).
- Instruction Clinical Particulars
- 4. Clinical particulars 4.1 Therapeutic indications Itovebi, in combination with palbociclib and fulvestrant, is indicated for the treatment of adult patients with PIK3CA-mutated, oestrogen receptor (ER)-positive, HER2-negative, locally advanced or metastatic breast cancer, following recurrence on or within 12 months of completing adjuvant endocrine treatment (see section
- Instruction Pharmacology
- 5. Pharmacological properties 5.1 Pharmacodynamic properties Pharmacotherapeutic group: Antineoplastic agents, PI3K inhibitors, ATC Code: L01EM06 Mechanism of action Inavolisib is an inhibitor of the phosphatidylinositol-4,5-bisphosphate 3-kinase (PI3K) catalytic subunit alpha isoform protein (p110α; encoded by the PIK3CA gene). In addition, inavolisib promotes the degradation of mutated p110α (mutant degrader). The PI3K signalling pathway is commonly dysregulated in HR-positive breast cancer, often due to activating PIK3CA mutations. With its dual mechanism of action, inavolisib inhibits the activity of downstream PI3K pathway targets, including AKT, resulting in reduced cellular proliferation and induction of apoptosis in PIK3CA-mutated breast cancer cell lines. Clinical efficacy and safety Locally advanced or metastatic breast cancer The patients in this setting, based on data from the INAVO120 study, are defined as endocrine-resistant patients (disease recurrence on or within 12 months of adjuvant endocrine treatment completion) who have not received prior treatment for their locally advanced or metastatic disease. INAVO120 The efficacy of Itovebi in combination with palbociclib and fulvestrant was evaluated in a Phase 3, randomised, double-blind, placebo-controlled study in adult patients with PIK3CA-mutated, HR-positive, HER2-negative, locally advanced or metastatic breast cancer whose disease progressed during or within 12 months of completing adjuvant endocrine therapy (endocrine-resistant) and who have not received prior systemic therapy for locally advanced or metastatic disease. The study included patients who received prior (neo)adjuvant endocrine therapy including a CDK4/6 inhibitor if the progression event was > 12 months since completion of the CDK4/6 inhibitor portion of (neo)adjuvant therapy, and who had HbA1C < 6% and fasting blood glucose < 126 mg/dL. The study excluded patients with Type 1 diabetes mellitus or Type 2 diabetes mellitus requiring ongoing anti-hyperglycaemic therapy at the start of study treatment, patients who received prior treatment with fulvestrant (except as part of neoadjuvant therapy with treatment duration ≤ 6 months), and patients with known and untreated, or active CNS metastases (progressing or requiring anticonvulsants or corticosteroids for symptomatic control). PIK3CA mutation status was prospectively determined through testing of plasma-derived circulating tumour DNA (ctDNA) using a next-generation sequencing (NGS) assay (FoundationOne® Liquid CDx assay or PredicineCARETM) performed at a central laboratory (87.4%), or in local laboratories (12.6%) using various validated polymerase chain reaction (PCR) or NGS assays on tumour tissue or plasma. The following PIK3CA mutations at the indicated amino acid positions were eligible for inclusion: H1047D/I/L/N/P/Q/R/T/Y, G1049A/C/D/R/S, E545A/D/G/K/L/Q/R/V, E453A/D/G/K/Q/V, E542A/D/G/K/Q/R/V, K111N/R/E, Q546E/H/K/L/P/R, G106A/D/R/S/V, N345D/H/I/K/S/T/Y, G118D, C420R, R88Q, and M1043I/T/V. At least one eligible PIK3CA mutation was identified in at least one of these amino acid positions in each of the enrolled patient specimens. Based on results from the central FoundationOne® Liquid CDx assay, the most common PIK3CA alterations were short variants at amino acids H1047 (n=115, 42.6%), E545 (n=58, 21.5%), and E542 (n=39, 14.4%). There were 25 patients whose specimens harboured more than one PIK3CA alterations (i.e., multiple PIK3CA mutations), and 33 with less common PIK3CA alterations. A total of 325 patients were randomised 1:1 to receive either Itovebi 9 mg (n=161) or placebo (n=164) orally once daily, in combination with palbociclib and fulvestrant, until disease progression or unacceptable toxicity. In addition, pre/perimenopausal women and men received an LHRH agonist throughout therapy. Randomisation was stratified by presence of visceral disease (yes or no), endocrine resistance (primary or secondary), and geographic region (North America/Western Europe, Asia, other). The baseline demographic and disease characteristics were: median age 54 years (range: 27 to 79 years, 18.2% were ≥ 65 years of age); 98.2% female; 38.2% pre/perimenopausal; 58.8% White, 38.2% Asian, 2.5% unknown, 0.6% Black or African American;
- Instruction Pharmaceutical Particulars
- 6. Pharmaceutical particulars 6.1 List of excipients Itovebi 3 mg and 9 mg tablet core Lactose monohydrate Magnesium stearate (E470b) Microcrystalline cellulose (E460) Sodium starch glycolate Itovebi 3 mg film-coating Polyvinyl alcohol, partially hydrolysed Titanium dioxide (E 171) Macrogol Talc (E 553b) Iron oxide red (E 172) Itovebi 9 mg film-coating Polyvinyl alcohol, partially hydrolysed Titanium dioxide (E 171) Macrogol Talc (E 553b) Iron oxide red (E 172) Iron oxide yellow (E 172) 6.2 Incompatibilities Not applicable. 6.3 Shelf life 2 years. 6.4 Special precautions for storage This medicinal product does not require any special storage conditions. 6.5 Nature and contents of container Alu/Alu (aluminium/aluminium) perforated unit-dose blisters in cartons of 28 × 1 film-coated tablets. 6.6 Special precautions for disposal and other handling Any unused medicinal product or waste material should be disposed of in accordance with local requirements.
- Instruction Content
- ## Composition
2. Qualitative and quantitative composition Itovebi 3 mg film-coated tablets Each film-coated tablet contains 3 mg of inavolisib. Excipient(s) with known effect Each film-coated tablet contains 22 mg of lactose. Itovebi 9 mg film-coated tablets Each film-coated tablet contains 9 mg of inavolisib. Excipient(s) with known effect Each film-coated tablet contains 66 mg of lactose. For the full list of excipients, see section 6.1.
## Pharmaceutical Form
3. Pharmaceutical form Film-coated tablet (tablet). Itovebi 3 mg film-coated tablets Red, round convex-shaped film-coated tablet with an “INA 3” debossing on one side. Approximate diameter: 6 mm. Itovebi 9 mg film-coated tablets Pink, oval film-coated tablet with an “INA 9” debossing on one side. Approximate size: 13 mm (length), 6 mm (width).
## Clinical Particulars
4. Clinical particulars 4.1 Therapeutic indications Itovebi, in combination with palbociclib and fulvestrant, is indicated for the treatment of adult patients with PIK3CA-mutated, oestrogen receptor (ER)-positive, HER2-negative, locally advanced or metastatic breast cancer, following recurrence on or within 12 months of completing adjuvant endocrine treatment (see section
## Pharmacological Properties
5. Pharmacological properties 5.1 Pharmacodynamic properties Pharmacotherapeutic group: Antineoplastic agents, PI3K inhibitors, ATC Code: L01EM06 Mechanism of action Inavolisib is an inhibitor of the phosphatidylinositol-4,5-bisphosphate 3-kinase (PI3K) catalytic subunit alpha isoform protein (p110α; encoded by the PIK3CA gene). In addition, inavolisib promotes the degradation of mutated p110α (mutant degrader). The PI3K signalling pathway is commonly dysregulated in HR-positive breast cancer, often due to activating PIK3CA mutations. With its dual mechanism of action, inavolisib inhibits the activity of downstream PI3K pathway targets, including AKT, resulting in reduced cellular proliferation and induction of apoptosis in PIK3CA-mutated breast cancer cell lines. Clinical efficacy and safety Locally advanced or metastatic breast cancer The patients in this setting, based on data from the INAVO120 study, are defined as endocrine-resistant patients (disease recurrence on or within 12 months of adjuvant endocrine treatment completion) who have not received prior treatment for their locally advanced or metastatic disease. INAVO120 The efficacy of Itovebi in combination with palbociclib and fulvestrant was evaluated in a Phase 3, randomised, double-blind, placebo-controlled study in adult patients with PIK3CA-mutated, HR-positive, HER2-negative, locally advanced or metastatic breast cancer whose disease progressed during or within 12 months of completing adjuvant endocrine therapy (endocrine-resistant) and who have not received prior systemic therapy for locally advanced or metastatic disease. The study included patients who received prior (neo)adjuvant endocrine therapy including a CDK4/6 inhibitor if the progression event was > 12 months since completion of the CDK4/6 inhibitor portion of (neo)adjuvant therapy, and who had HbA1C < 6% and fasting blood glucose < 126 mg/dL. The study excluded patients with Type 1 diabetes mellitus or Type 2 diabetes mellitus requiring ongoing anti-hyperglycaemic therapy at the start of study treatment, patients who received prior treatment with fulvestrant (except as part of neoadjuvant therapy with treatment duration ≤ 6 months), and patients with known and untreated, or active CNS metastases (progressing or requiring anticonvulsants or corticosteroids for symptomatic control). PIK3CA mutation status was prospectively determined through testing of plasma-derived circulating tumour DNA (ctDNA) using a next-generation sequencing (NGS) assay (FoundationOne® Liquid CDx assay or PredicineCARETM) performed at a central laboratory (87.4%), or in local laboratories (12.6%) using various validated polymerase chain reaction (PCR) or NGS assays on tumour tissue or plasma. The following PIK3CA mutations at the indicated amino acid positions were eligible for inclusion: H1047D/I/L/N/P/Q/R/T/Y, G1049A/C/D/R/S, E545A/D/G/K/L/Q/R/V, E453A/D/G/K/Q/V, E542A/D/G/K/Q/R/V, K111N/R/E, Q546E/H/K/L/P/R, G106A/D/R/S/V, N345D/H/I/K/S/T/Y, G118D, C420R, R88Q, and M1043I/T/V. At least one eligible PIK3CA mutation was identified in at least one of these amino acid positions in each of the enrolled patient specimens. Based on results from the central FoundationOne® Liquid CDx assay, the most common PIK3CA alterations were short variants at amino acids H1047 (n=115, 42.6%), E545 (n=58, 21.5%), and E542 (n=39, 14.4%). There were 25 patients whose specimens harboured more than one PIK3CA alterations (i.e., multiple PIK3CA mutations), and 33 with less common PIK3CA alterations. A total of 325 patients were randomised 1:1 to receive either Itovebi 9 mg (n=161) or placebo (n=164) orally once daily, in combination with palbociclib and fulvestrant, until disease progression or unacceptable toxicity. In addition, pre/perimenopausal women and men received an LHRH agonist throughout therapy. Randomisation was stratified by presence of visceral disease (yes or no), endocrine resistance (primary or secondary), and geographic region (North America/Western Europe, Asia, other). The baseline demographic and disease characteristics were: median age 54 years (range: 27 to 79 years, 18.2% were ≥ 65 years of age); 98.2% female; 38.2% pre/perimenopausal; 58.8% White, 38.2% Asian, 2.5% unknown, 0.6% Black or African American;
## Pharmaceutical Particulars
6. Pharmaceutical particulars 6.1 List of excipients Itovebi 3 mg and 9 mg tablet core Lactose monohydrate Magnesium stearate (E470b) Microcrystalline cellulose (E460) Sodium starch glycolate Itovebi 3 mg film-coating Polyvinyl alcohol, partially hydrolysed Titanium dioxide (E 171) Macrogol Talc (E 553b) Iron oxide red (E 172) Itovebi 9 mg film-coating Polyvinyl alcohol, partially hydrolysed Titanium dioxide (E 171) Macrogol Talc (E 553b) Iron oxide red (E 172) Iron oxide yellow (E 172) 6.2 Incompatibilities Not applicable. 6.3 Shelf life 2 years. 6.4 Special precautions for storage This medicinal product does not require any special storage conditions. 6.5 Nature and contents of container Alu/Alu (aluminium/aluminium) perforated unit-dose blisters in cartons of 28 × 1 film-coated tablets. 6.6 Special precautions for disposal and other handling Any unused medicinal product or waste material should be disposed of in accordance with local requirements.
- Company Detail Path
- /organization/roche-products-limited
