Drug

Inavolisib

Approved medicine

ClassPI3-kinase p110-alpha subunit inhibitorResearchOngoing clinical research

Also known as Itovebi, (2S)-2-((2-((4S)-4-(difluoromethyl)-2-oxo-3-oxazolidinyl)-5,6-dihydroimidazo(1,2-D)(1,4)benzoxazepin-9-yl)amino)propanamide, propanamide, 2-((2-((4S)-4-(difluoromethyl)-2-oxo-3-oxazolidinyl)-5,6-dihydroimidazo(1,2-D)(1,4)benzoxazepin-9-yl)amino)-, (2S)-.

RxNorm2695422 ChEMBLCHEMBL4650215UNIIL4C1UY2NYH

Active clinical trials

PIK3CA

Primary target

Regulatory events

Latest activity

beta

Recent clinical, regulatory, research and industry developments relating to this drug.

A Phase Ib/II, Open-Label, Multicenter, Randomized Umbrella Study Evaluating the Efficacy and Safety of Multiple Treatment Combinations in Patients With Breast Cancer (MORPHEUS-BREAST CANCER)

Clinical trial2026-08-05Results expected Q2 2029 · ClinicalTrials.gov

A Phase II, Open-Label, Multicenter Study Evaluating the Safety and Efficacy of Neoadjuvant Treatment With Inavolisib Combinations in Patients With Untreated, Early-stage, PIK3CA-Mutated Breast Cancer

Clinical trial2026-07-16Results expected Q3 2027 · ClinicalTrials.gov

A Phase II, Multicenter, Randomized, Double-Blind, Placebo-Controlled Study Evaluating the Efficacy and Safety of Inavolisib Plus Ribociclib Plus Fulvestrant Versus Placebo Plus Ribociclib Plus Fulvestrant in Patients With Endocrine- Resistant Hormone-Receptor-Positive, HER2-Negative Advanced Breast Cancer With Chromosome 8P Loss and Without a PIK3CA Mutation

Clinical trial2026-07-13Results expected Q4 2028 · ClinicalTrials.gov

A Multicenter, Single Arm Study to Evaluate the Preliminary Efficacy and Safety Profile of Inavolisib in Previously Treated Pancreatic Ductal Adenocarcinoma Patients

Clinical trial2026-07-10Results expected Q2 2028 · ClinicalTrials.gov

An Open-Label, Multicenter Extension Study in Patients Previously Enrolled in a Genentech and/or F. Hoffmann-La Roche Ltd Sponsored Study

Clinical trial2026-07-10Results expected Q1 2033 · ClinicalTrials.gov

A Phase 1, Open-Label, Single-Dose Study to Evaluate the Effect of Moderate or Severe Hepatic Impairment on the Pharmacokinetics of Inavolisib

Clinical trial2026-07-07Results expected Q3 2026 · ClinicalTrials.gov

A Phase II, Randomized, Open-Label Study Evaluating Two Inavolisib Dose Levels in Combination With Fulvestrant in Participants With PIK3CA-Mutated, HR-Positive, HER2-Negative Locally Advanced or Metastatic Breast Cancer

Clinical trial2026-07-07Results expected Q4 2028 · ClinicalTrials.gov

A Phase II, Randomized, Multicenter, Open-Label Study Evaluating the Efficacy and Safety of the Combination of Inavolisib Plus Enzalutamide Versus Physician's Choice of ARPI or Docetaxel in Patients With Metastatic Castration-Resistant Prostate Cancer

Clinical trial2026-07-06Results expected Q1 2028 · ClinicalTrials.gov

A Phase III, Multicenter, Randomized, Double-Blind, Placebo-Controlled Study Evaluating the Efficacy and Safety of Inavolisib Plus a CDK4/6 Inhibitor and Letrozole Versus Placebo Plus a CDK4/6 Inhibitor and Letrozole in Patients With Endocrine-Sensitive PIK3CA-Mutated, Hormone Receptor-Positive, HER2-Negative Advanced Breast Cancer

Clinical trial2026-07-02Results expected Q2 2032 · ClinicalTrials.gov

A Phase III, Multicenter, Randomized, Double-Blind, Placebo-Controlled Study Evaluating the Efficacy and Safety of Inavolisib in Combination With Phesgo Versus Placebo in Combination With Phesgo As Maintenance Therapy After First Line Induction Therapy in Participants With PIK3CA-Mutated HER2-Positive Locally Advanced or Metastatic Breast Cancer

Clinical trial2026-06-29Results expected Q4 2026 · ClinicalTrials.gov

A Phase III, Multicenter, Randomized, Open-Label Study Evaluating the Efficacy and Safety of Inavolisib Plus Fulvestrant Versus Alpelisib Plus Fulvestrant in Patients With Hormone Receptor-Positive, HER2-Negative, PIK3CA Mutated, Locally Advanced or Metastatic Breast Cancer Who Progressed During or After CDK4/6 Inhibitor and Endocrine Combination Therapy

Clinical trial2026-06-24Results expected Q4 2026 · ClinicalTrials.gov

Approval: Itovebi (EMA)

Regulatory2025-07-18EMA

Profile

Identifiers & mechanism

Canonical identifiers, marketed brand names and mechanism, resolved across RxNorm, ChEMBL and ATC.

Canonical name

Inavolisib

Aliases & brands

Itovebi(2S)-2-((2-((4S)-4-(difluoromethyl)-2-oxo-3-oxazolidinyl)-5,6-dihydroimidazo(1,2-D)(1,4)benzoxazepin-9-yl)amino)propanamidepropanamide, 2-((2-((4S)-4-(difluoromethyl)-2-oxo-3-oxazolidinyl)-5,6-dihydroimidazo(1,2-D)(1,4)benzoxazepin-9-yl)amino)-, (2S)-

RxNorm CUI

2695422

ChEMBL ID

CHEMBL4650215

UNII

L4C1UY2NYH

Primary mechanism

PI3-kinase p110-alpha subunit inhibitor

Regulatory jurisdictions

ema

Pharmacology & targets

1 target

Known molecular targets and mechanisms supported by curated pharmacology databases.

Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform

PIK3CA · P42336

INHIBITORPI3-kinase p110-alpha subunit inhibitor

Regulatory timeline

1 event

The complete regulatory record, grouped by authority — approvals, safety advisories and label changes. Each authority shows its most recent events; expand one to read its full history.

Earliest approval

2025-07-18

Latest approval

2025-07-18

Authorities

EMA

Total events

emaEuropean Medicines Agency· 1 event

2025-07-18Approval

Approval: Itovebi (EMA)

Indication: Itovebi, in combination with palbociclib and fulvestrant, is indicated for the treatment of adult patients with PIK3CA-mutated, oestrogen receptor (ER)-positive, HER2-negative,… Show full indication

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 5.1). Patients previously treated with a CDK 4/6 inhibitor in the (neo)adjuvant setting should have had an interval of at least 12 months between termination of CDK 4/6 inhibitor treatment and the detection of recurrence. In pre/perimenopausal women and in men, endocrine therapy should be combined with a luteinising hormone releasing hormone (LHRH) agonist.

Evidence ↗