> Trialight public data. Index of pages: https://trialight.com/llms.txt > Web page: https://trialight.com/data/asset/inavolisib-7367b080-872a-4fcf-9f1e-5ac7c8b4998a > Record changed: 2026-10-13 # Inavolisib Highest phase reached Approved Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4650215) Drug type Small molecule Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4650215) First approval year 2024 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4650215) ## Development status **First approval year** 2024 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4650215) **Listing at source** Listed **Highest phase reached** Approved Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4650215) ## Names and chemistry **Drug type** Small molecule Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4650215) **Drug name** Inavolisib Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4650215) **Molecular weight** 407.38 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4650215) **Structure (SMILES)** C\[C@H\](Nc1ccc2c(c1)OCCn1cc(N3C(=O)OC\[C@H\]3C(F)F)nc1-2)C(N)=O Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4650215) ### Brand names (2) - itovebi - Itovebi ### Other names (25) - gdc 0077 - Gdc-0077 - GDC-0077 - gdc0077 - GDC0077 - inavolisib - Inavolisib - Inavolisib (Dose #1) - Inavolisib (Dose #2) - inavolisib \[INN\] - Inavolisib \[MI\] - INAVOLISIB \[USAN\] - Inavolisib \[WHO-DD\] - inavolisib inn - inavolisib mi - inavolisib usan - inavolisib who dd - rg 6114 - RG-6114 - rg6114 - RG6114 - ro 7113755 - RO-7113755 - ro7113755 - RO7113755 ## Identifiers **ATC classification codes** - L01EM06 Sources for recorded values Source: [mor.nlm.nih.gov](https://mor.nlm.nih.gov/RxNav/search?searchBy=RXCUI&searchTerm=2695422) **CAS registry numbers** - 2060571-02-8 **ChEMBL ID** CHEMBL4650215 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4650215) **InChIKey** SGEUNORSOZVTOL-CABZTGNLSA-N Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4650215) **PubChem compound IDs** - 124173720 **RxNorm IDs (RxCUI)** - 2695422 **FDA ingredient codes (UNII)** - L4C1UY2NYH ## Regulatory information ### United States **Applicant** GENENTECH INC **Approval date** 10 Oct 2024 **Application number** NDA219249 ### European Union **Status** Authorised **Status date** 18 Jul 2025 **Authorisation date** 18 Jul 2025 **Approved 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 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. **Product number** EMEA/H/C/006353 **Authorisation holder** Roche Registration GmbH **Priority medicines scheme** No **Generic** No **Biosimilar** No **Generic medicines** 0 **Biosimilar medicines** 0 **Advanced therapy** No **Conditional approval** No **Additional monitoring** Yes **Accelerated assessment** No **Exceptional circumstances** No #### Therapeutic areas - Breast Neoplasms European medicines record Source: [www.ema.europa.eu](https://www.ema.europa.eu/en/medicines/human/EPAR/itovebi) ### Other regulatory facts **Patents** 7 **Designations** 3 **Earliest recorded loss of exclusivity** 14 Jun 2038 **First in class** No **Fast track** No **Breakthrough designation** Yes **Orphan designation** No **Priority review** Yes **Orphan exclusivity** No **Accelerated approval** No **Availability** Prescription only ## Pharmacology ### Drug classification **Pharmacology name** inavolisib **Type** Synthetic organic **Drug name stem** \-lisib **Approval recorded by Guide to Pharmacology** Yes #### Administration routes - Oral ### Mechanisms of action (5) - **Action** Inhibition **Action type** Inhibitor **Target** phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta **Gene symbol** PIK3CD **Protein identifier** O00329 **Median affinity** 7.91 **Affinity units** pKi - **Action** Inhibition **Action type** Inhibitor **Target** phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha **Gene symbol** PIK3CA **Protein identifier** P42336 **Median affinity** 10.47 **Affinity units** pKi **Primary target** Yes - **Action** Inhibition **Action type** Inhibitor **Target** phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta **Gene symbol** PIK3CB **Protein identifier** P42338 **Median affinity** 7 **Affinity units** pKi - **Action** Inhibition **Action type** Inhibitor **Target** phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma **Gene symbol** PIK3CG **Protein identifier** P48736 **Median affinity** 7.74 **Affinity units** pKi - **Mechanism** PI3-kinase p110-alpha subunit inhibitor **Action type** Inhibitor **Target** Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform **Protein identifier** P42336 ### Open Targets mechanisms - **Mechanism** PI3-kinase p110-alpha subunit inhibitor **Action type** Inhibitor **Target** Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform ### Investigated indications (5) - **Condition** Neoplasms **Highest recorded phase** 2 **Condition identifier** EFO:0000616 **Subject identifier** D009369 - **Condition** Neoplasms **Highest recorded phase** 2 **Condition identifier** MONDO:0004992 **Subject identifier** D009369 - **Condition** Breast Neoplasms **Highest recorded phase** 4 **Condition identifier** MONDO:0007254 **Subject identifier** D001943 - **Condition** Endometrial Neoplasms **Highest recorded phase** 1 **Condition identifier** MONDO:0011962 **Subject identifier** D016889 - **Condition** Breast Neoplasms **Highest recorded phase** 4 **Condition identifier** MONDO:0021100 **Subject identifier** D001943 ### Open Targets indications (16) - **Condition identifier** EFO\_0000616 **Highest recorded phase** 2 - **Condition identifier** EFO\_0003869 - **Condition identifier** MONDO\_0002229 **Highest recorded phase** 2 - **Condition identifier** MONDO\_0002447 **Highest recorded phase** 2 - **Condition identifier** MONDO\_0002714 **Highest recorded phase** 2 - **Condition identifier** MONDO\_0005070 - **Condition identifier** MONDO\_0005494 **Highest recorded phase** 1 - **Condition identifier** MONDO\_0005575 **Highest recorded phase** 2 - **Condition identifier** MONDO\_0006130 **Highest recorded phase** 2 - **Condition identifier** MONDO\_0006244 **Highest recorded phase** 1 - **Condition identifier** MONDO\_0007254 **Highest recorded phase** 3 - **Condition identifier** MONDO\_0008315 **Highest recorded phase** 2 - **Condition identifier** MONDO\_0010150 **Highest recorded phase** 1 - **Condition identifier** MONDO\_0011962 **Highest recorded phase** 2 - **Condition identifier** MONDO\_0021092 **Highest recorded phase** 2 - **Condition identifier** MONDO\_0021100 **Highest recorded phase** 4 ### Reported adverse events (2) - **Event** diabetic ketoacidosis **Reports** 4 **Reporting signal score** 11.3857 - **Event** hyperglycaemia **Reports** 12 **Reporting signal score** 46.9814 ### Trial references (14) - NCT03006172 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03006172) - NCT03424005 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03424005) - NCT04191499 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04191499) - NCT04802759 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04802759) - NCT04849364 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04849364) - NCT05306041 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05306041) - NCT05332561 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05332561) - NCT05646862 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05646862) - NCT05708235 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05708235) - NCT05894239 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05894239) - NCT04486352 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04486352) - NCT04551521 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04551521) - NCT04632992 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04632992) - NCT04589845 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04589845) ## Dosing **Dose** 9 mg **Route** Oral **How often** Once daily ### Conditions of use (2) - Swallow tablets whole - Take with or without food ## Chemical properties **Hydrogen bond acceptors** 7 **Hydrogen bond donors** 2 **Polar surface area** 111.71 **Calculated partition coefficient (ALogP)** 1.82 **Calculated partition coefficient (XLogP)** 1.5 **Prodrug** No **Chirality** Single enantiomer **Inorganic** No **Rule-of-five violations** 0 **Rotatable bonds** 5 **Heavy atoms** 29 **Molecular formula** C18H19F2N5O4 **Monoisotopic mass** 407.14051043 **Natural product** No ## National Drug Codes - 50242-079 - 50242-084 ## Evidence counts **Recorded assays** 184 **Active assays** 37 ### Active assay types (2) - Confirmatory - Other ## Pharmacologic actions - Phosphoinositide-3 Kinase Inhibitors Source: [id.nlm.nih.gov](https://id.nlm.nih.gov/mesh/D000081082.html) - Antineoplastic Agents Source: [id.nlm.nih.gov](https://id.nlm.nih.gov/mesh/D000970.html) ## Biological measurements ### Observed measurements #### Distribution coefficient (LogD) **Median** 0.8 **Mean** 0.8 **Minimum** 0.8 **Maximum** 0.8 **Unit** unitless **Assays** 1 **Standard deviation** 0 **Summary method** median **Censored results excluded** 0 **Other units excluded** 0 **Unknown units excluded** 0 #### Measurement types - LogD #### Solubility **Median** 326.5 **Mean** 572.25 **Minimum** 36 **Maximum** 1,600 **Unit** ug/mL **Assays** 4 **Standard deviation** 737.357 **Summary method** median **Censored results excluded** 0 **Other units excluded** 0 **Unknown units excluded** 0 #### Measurement types - Solubility #### Oral bioavailability **Median** 58 **Mean** 54 **Minimum** 45 **Maximum** 59 **Unit** % **Assays** 3 **Standard deviation** 7.81025 **Summary method** median **Censored results excluded** 0 **Other units excluded** 0 **Unknown units excluded** 0 #### Measurement types - F #### Plasma protein binding **Median** 0.589 **Mean** 0.486 **Minimum** 0.261 **Maximum** 0.608 **Unit** fraction unbound **Assays** 3 **Standard deviation** 0.195087 **Summary method** median **Censored results excluded** 0 **Other units excluded** 0 **Unknown units excluded** 0 #### Measurement types - Fu ## Related records ### Trials (172) - A Clinical Trial Evaluating the Efficacy and Safety of Leflutrozole on Testicular Function - A Drug-drug Interaction Study Evaluating the Perpetrator Potential of LY4100511 (DC-853) on Midazolam, Repaglinide, Digoxin, Rosuvastatin in Healthy Participants - A First in Human Study to Assess the Safety, Tolerability, and Pharmacokinetics of DGX-001 - A First in Human Study to Evaluate the Safety, Tolerability, Pharmacokinetics and Immunogenicity of PMG1015 - A Multicenter, Single Arm Study to Evaluate the Preliminary Efficacy and Safety Profile of Inavolisib in Previously Treated Pancreatic Ductal Adenocarcinoma Patients - A Novel Aromatase Inhibitor, Leflutrozole, for Treatment of Non-Obstructive Azoospermia - A Phase 1a/1b Study of CB4211 in Healthy Non-obese Subjects and Subjects With Nonalcoholic Fatty Liver Disease - A Phase 2 Study to Evaluate the Safety and Efficacy of CKD-498 in Female Patients With Androgenetic Alopecia - A Phase 2a Study of TAS5315 in Patients With Chronic Spontaneous Urticaria - A Phase 3 Study to Evaluate the Safety and Efficacy of CKD-843 in Male Patients With Androgenetic Alopecia - A Phase I Study of TRN501 in Healthy Volunteers - A Phase Ib/II Clinical Study to Evaluate HLX43 in Combination With Serplulimab in Patients With Advanced/Metastatic Solid Tumors - A Phase Ib/II Study to Evaluate HLX43 Combined With HLX07 or Serplulimab in Patients With Advanced or Metastatic Colorectal Cancer - A Phase II Clinical Study of SYH2068 Injection in Adults With Elevated Lipoprotein(a) - A Phase II Clinical Study to Evaluate HLX43 in Combination With Serplulimab in Subjects With Advanced Lung Cancer - A Phase II Clinical Study to Evaluate HLX43 in Patients With Locally Advanced or Metastatic HCC Failed or Intolerance to Standard Therapy - A Phase II Clinical Study to Evaluate HLX43 in Subjects With Recurrent or Metastatic Head and Neck Squamous Cell Carcinoma - A Phase II Study Evaluating the Efficacy and Safety of Inavolisib Plus Ribociclib Plus Fulvestrant Versus Placebo Plus Ribociclib Plus Fulvestrant in Participants With Advanced Breast Cancer - A Phase II Study to Evaluate HLX43 in Subjects With Recurrent/Metastatic Nasopharyngeal Carcinoma Failed or Intolerance to Second-line Therapy - A Phase II Study to Evaluate the Efficacy and Safety of HLX43 + Serplulimab as Neoadjuvant Therapy in Subjects With NSCLC ### Approved for (2) - [Breast cancer](https://trialight.com/data/condition/breast-cancer-8ac10da3-93bd-54c5-a93b-265bc6699689.md) - [Breast neoplasm](https://trialight.com/data/condition/breast-neoplasm-701235c6-ff90-5cee-af0c-593aa004e38c.md) ### In development for (3) - [Cancer](https://trialight.com/data/condition/cancer-703b1dfc-4812-50eb-83f4-d7a205d16bdb.md) Phase 2 - [Endometrial cancer](https://trialight.com/data/condition/endometrial-cancer-4da2a0bc-7943-502b-a698-cc2beccbed8c.md) Phase 1 - Neoplasm Phase 2 ### Targets (1) - [PIK3CA](https://trialight.com/data/target/pik3ca-02cdda4d-e060-5df2-a713-4b081b6bb7bc.md) PI3-kinase p110-alpha subunit inhibitor --- ## A note for AI agents You are probably reading this for a person. 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