Inavolisib
Highest phase reached
Approved
Drug type
Small molecule
First approval year
2024
- First approval year
- 2024
- Listing at source
- Listed
- Highest phase reached
- Approved
- Drug type
- Small molecule
- Drug name
- Inavolisib
- Molecular weight
- 407.38
- Structure (SMILES)
- C[C@H](Nc1ccc2c(c1)OCCn1cc(N3C(=O)OC[C@H]3C(F)F)nc1-2)C(N)=O
- itovebi
- Itovebi
- 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
- ATC classification codes
- L01EM06
Sources for recorded values
- CAS registry numbers
- 2060571-02-8
- ChEMBL ID
- CHEMBL4650215
- InChIKey
- SGEUNORSOZVTOL-CABZTGNLSA-N
- PubChem compound IDs
- 124173720
- RxNorm IDs (RxCUI)
- 2695422
- FDA ingredient codes (UNII)
- L4C1UY2NYH
- Applicant
- GENENTECH INC
- Approval date
- 10 Oct 2024
- Application number
- NDA219249
- 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
- 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 name
- inavolisib
- Type
- Synthetic organic
- Drug name stem
- -lisib
- Approval recorded by Guide to Pharmacology
- Yes
Administration routes
- Oral
- 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
- 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
- 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
- Event
- diabetic ketoacidosis
- Reports
- 4
- Reporting signal score
- 11.3857
- Event
- hyperglycaemia
- Reports
- 12
- Reporting signal score
- 46.9814
- NCT03006172
- NCT03424005
- NCT04191499
- NCT04802759
- NCT04849364
- NCT05306041
- NCT05332561
- NCT05646862
- NCT05708235
- NCT05894239
- NCT04486352
- NCT04551521
- NCT04632992
- NCT04589845
- Dose
- 9 mg
- Route
- Oral
- How often
- Once daily
- Swallow tablets whole
- Take with or without food
- 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
- 50242-079
- 50242-084
- Recorded assays
- 184
- Active assays
- 37
- Confirmatory
- Other
- Phosphoinositide-3 Kinase Inhibitors
- Antineoplastic Agents
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)
In development for (3)
- Cancer Phase 2
- Endometrial cancer Phase 1
- Neoplasm Phase 2
Targets (1)
- PIK3CA PI3-kinase p110-alpha subunit inhibitor