inavolisib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
phosphatidylinositol 3-kinase inhibitors, antineoplastics 5836 2060571-02-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • inavolisib
  • GDC-0077
  • RG6114
  • RO7113755
Inavolisib is an inhibitor of phosphatidylinositol 3-kinase (PI3K) with inhibitory activity predominantly against PI3Kα. In vitro, inavolisib induced the degradation of mutated PI3K catalytic alpha subunit p110α (encoded by the PIK3CA gene), inhibited phosphorylation of the downstream target AKT, reduced cellular proliferation, and induced apoptosis in PIK3CA-mutated breast cancer cell lines. In vivo, inavolisib reduced tumor growth in PIK3CA-mutated, estrogen receptor-positive, breast cancer xenograft models.
  • Molecular weight: 407.38
  • Formula: C18H19F2N5O4
  • CLOGP: 1.82
  • LIPINSKI: 0
  • HAC: 9
  • HDO: 2
  • TPSA: 111.71
  • ALOGS:
  • ROTB: 5
  • Status: ONP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
9 mg O

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

None

Approvals:

DateAgencyCompanyOrphan
Oct. 10, 2024 FDA Genentech (Roche)
July 18, 2025 EMA Roche Registration GmbH

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Hyperglycaemia 291.45 57.18 67 535 50903 90576942
Blood glucose increased 115.30 57.18 37 565 95209 90532636

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Hyperglycaemia 107.62 55.27 30 386 85060 110503823
Blood glucose increased 74.12 55.27 25 391 132471 110456412

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01EM06 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
PROTEIN KINASE INHIBITORS
Phosphatidylinositol-3-kinase (Pi3K) inhibitors
MeSH PA D000081082 Phosphoinositide-3 Kinase Inhibitors
MeSH PA D000970 Antineoplastic Agents
MeSH PA D004791 Enzyme Inhibitors
FDA EPC N0000175605 Kinase Inhibitor
FDA MoA N0000194130 Phosphoinositide 3-Kinase alpha Inhibitors
CHEBI has role CHEBI:35610 antineoplastic agent

Related Drugs by ATC class:

L01EM Phosphatidylinositol-3-kinase (Pi3K) inhibitors 4 drugs
alpelisibcopanlisibduvelisibidelalisib

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Locally advanced or metastatic breast cancer indication 254837009 DOID:1612




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
3MG ITOVEBI GENENTECH INC N219249 Oct. 10, 2024 RX TABLET ORAL 8343955 Sept. 27, 2030 COMBINATION WITH PALBOCICLIB AND FULVESTRANT FOR TREATMENT OF ADULTS WITH ENDOCRINE-RESISTANT PIK3CA-MUTATED HR-POSITIVE HER2-NEGATIVE LOCALLY ADVANCED OR METASTATIC BREAST CANCER FOLLOWING RECURRENCE ON OR AFTER COMPLETING ADJUVANT ENDOCRINE THERAPY
9MG ITOVEBI GENENTECH INC N219249 Oct. 10, 2024 RX TABLET ORAL 8343955 Sept. 27, 2030 COMBINATION WITH PALBOCICLIB AND FULVESTRANT FOR TREATMENT OF ADULTS WITH ENDOCRINE-RESISTANT PIK3CA-MUTATED HR-POSITIVE HER2-NEGATIVE LOCALLY ADVANCED OR METASTATIC BREAST CANCER FOLLOWING RECURRENCE ON OR AFTER COMPLETING ADJUVANT ENDOCRINE THERAPY
3MG ITOVEBI GENENTECH INC N219249 Oct. 10, 2024 RX TABLET ORAL 11760753 July 1, 2036 COMBINATION WITH PALBOCICLIB AND FULVESTRANT FOR TREATMENT OF ADULTS WITH ENDOCRINE-RESISTANT PIK3CA-MUTATED HR-POSITIVE HER2-NEGATIVE LOCALLY ADVANCED OR METASTATIC BREAST CANCER FOLLOWING RECURRENCE ON OR AFTER COMPLETING ADJUVANT ENDOCRINE THERAPY
3MG ITOVEBI GENENTECH INC N219249 Oct. 10, 2024 RX TABLET ORAL 9650393 July 1, 2036 COMBINATION WITH PALBOCICLIB AND FULVESTRANT FOR TREATMENT OF ADULTS WITH ENDOCRINE-RESISTANT PIK3CA-MUTATED HR-POSITIVE HER2-NEGATIVE LOCALLY ADVANCED OR METASTATIC BREAST CANCER FOLLOWING RECURRENCE ON OR AFTER COMPLETING ADJUVANT ENDOCRINE THERAPY
9MG ITOVEBI GENENTECH INC N219249 Oct. 10, 2024 RX TABLET ORAL 11760753 July 1, 2036 COMBINATION WITH PALBOCICLIB AND FULVESTRANT FOR TREATMENT OF ADULTS WITH ENDOCRINE-RESISTANT PIK3CA-MUTATED HR-POSITIVE HER2-NEGATIVE LOCALLY ADVANCED OR METASTATIC BREAST CANCER FOLLOWING RECURRENCE ON OR AFTER COMPLETING ADJUVANT ENDOCRINE THERAPY
9MG ITOVEBI GENENTECH INC N219249 Oct. 10, 2024 RX TABLET ORAL 9650393 July 1, 2036 COMBINATION WITH PALBOCICLIB AND FULVESTRANT FOR TREATMENT OF ADULTS WITH ENDOCRINE-RESISTANT PIK3CA-MUTATED HR-POSITIVE HER2-NEGATIVE LOCALLY ADVANCED OR METASTATIC BREAST CANCER FOLLOWING RECURRENCE ON OR AFTER COMPLETING ADJUVANT ENDOCRINE THERAPY
3MG ITOVEBI GENENTECH INC N219249 Oct. 10, 2024 RX TABLET ORAL 12410189 June 14, 2038 COMBINATION WITH PALBOCICLIB AND FULVESTRANT FOR TREATMENT OF ADULTS WITH ENDOCRINE-RESISTANT PIK3CA-MUTATED HR-POSITIVE HER2-NEGATIVE LOCALLY ADVANCED OR METASTATIC BREAST CANCER FOLLOWING RECURRENCE ON OR AFTER COMPLETING ADJUVANT ENDOCRINE THERAPY
9MG ITOVEBI GENENTECH INC N219249 Oct. 10, 2024 RX TABLET ORAL 12410189 June 14, 2038 COMBINATION WITH PALBOCICLIB AND FULVESTRANT FOR TREATMENT OF ADULTS WITH ENDOCRINE-RESISTANT PIK3CA-MUTATED HR-POSITIVE HER2-NEGATIVE LOCALLY ADVANCED OR METASTATIC BREAST CANCER FOLLOWING RECURRENCE ON OR AFTER COMPLETING ADJUVANT ENDOCRINE THERAPY

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
3MG ITOVEBI GENENTECH INC N219249 Oct. 10, 2024 RX TABLET ORAL Oct. 10, 2029 NEW CHEMICAL ENTITY
9MG ITOVEBI GENENTECH INC N219249 Oct. 10, 2024 RX TABLET ORAL Oct. 10, 2029 NEW CHEMICAL ENTITY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform Kinase INHIBITOR IC50 10.42 DRUG LABEL DRUG LABEL
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform Kinase INHIBITOR Ki 7.74 IUPHAR
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform Kinase INHIBITOR Ki 7.91 IUPHAR
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform Kinase INHIBITOR Ki 7 IUPHAR

External reference:

IDSource
MWF PDB_CHEM_ID
CHEMBL4650215 ChEMBL_ID
C000723546 MESH_SUPPLEMENTAL_RECORD_UI
DB15275 DRUGBANK_ID
4043515 VANDF
C5446307 UMLSCUI
CHEBI:758122 CHEBI
11204 INN_ID
124173720 PUBCHEM_CID
43338 MMSL
d10228 MMSL
9636 IUPHAR_LIGAND_ID
L4C1UY2NYH UNII
2695422 RXNORM
933451381000036107 SNOMEDCT_US
D11942 KEGG_DRUG
019886 NDDF
L4C1UY2NYH INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Itovebi HUMAN PRESCRIPTION DRUG LABEL 1 50242-079 TABLET, FILM COATED 9 mg ORAL NDA 31 sections
Itovebi HUMAN PRESCRIPTION DRUG LABEL 1 50242-079 TABLET, FILM COATED 9 mg ORAL NDA 31 sections
Itovebi HUMAN PRESCRIPTION DRUG LABEL 1 50242-084 TABLET, FILM COATED 3 mg ORAL NDA 31 sections
Itovebi HUMAN PRESCRIPTION DRUG LABEL 1 50242-084 TABLET, FILM COATED 3 mg ORAL NDA 31 sections