ivosidenib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
5292 1448347-49-6

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • ivosidenib
  • tibsovo
  • AG-120
Ivosidenib is a small molecule inhibitor that targets the mutant isocitrate dehydrogenase 1 (IDH1) enzyme. Susceptible IDH1 mutations are defined as those leading to increased levels of 2-hydroxyglutarate(2-HG) in the leukemia cells and where efficacy is predicted by 1) clinically meaningful remissions with the recommended dose of ivosidenib and/or 2) inhibition of mutant IDH1 enzymatic activity at concentrations of ivosidenib sustainable at the recommended dosage according to validated methods. The most common of such mutations are R132H and R132C substitutions.
  • Molecular weight: 582.97
  • Formula: C28H22ClF3N6O3
  • CLOGP: 2.11
  • LIPINSKI: 2
  • HAC: 9
  • HDO: 1
  • TPSA: 119.29
  • ALOGS: -4.45
  • ROTB: 7

  • Status: ONP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
July 20, 2018 FDA AGIOS PHARMS INC

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

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
Differentiation syndrome 102.10 66.46 13 43 1100 29573371

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
Differentiation syndrome 157.74 84.07 20 77 2034 64496601

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01XX62 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
OTHER ANTINEOPLASTIC AGENTS
Other antineoplastic agents
MeSH PA D000970 Antineoplastic Agents
MeSH PA D004791 Enzyme Inhibitors
CHEBI has role CHEBI:35610 antineoplastic agents
CHEBI has role CHEBI:145410 IDP1 inhibitors

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Acute myeloid leukemia, disease indication 91861009




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 13.43 acidic
pKa2 0.21 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
250MG TIBSOVO SERVIER N211192 July 20, 2018 RX TABLET ORAL 10610125 June 21, 2030 A METHOD OF TREATING A CANCER CHARACTERIZED BY AN IDH1 MUTATION WHERE THE CANCER IS NEWLY DIAGNOSED ACUTE MYELOID LEUKEMIA (AML) AND WHERE THE MUTANT IDH1 HAS THE ABILITY TO CONVERT ALPHA-KETOGLUTARATE INTO 2-HYDROXYGLUTARATE (2-HG)
250MG TIBSOVO SERVIER N211192 July 20, 2018 RX TABLET ORAL 10610125 June 21, 2030 A METHOD OF TREATING A CANCER CHARACTERIZED BY AN IDH1 MUTATION WHERE THE CANCER IS RELAPSED OR REFRACTORY ACUTE MYELOID LEUKEMIA (AML) AND WHERE THE MUTANT IDH1 HAS THE ABILITY TO CONVERT ALPHA-KETOGLUTARATE INTO 2-HYDROXYGLUTARATE (2-HG)
250MG TIBSOVO SERVIER N211192 July 20, 2018 RX TABLET ORAL 10717764 Jan. 18, 2033 A METHOD OF TREATING PREVIOUSLY TREATED, LOCALLY ADVANCED OR METASTATIC CHOLANGIOCARCINOMA CHARACTERIZED BY AN IDH1 MUTATION
250MG TIBSOVO SERVIER N211192 July 20, 2018 RX TABLET ORAL 9850277 Jan. 18, 2033 A METHOD OF TREATING A CANCER CHARACTERIZED BY AN IDH1 MUTATION WHEREIN THE CANCER IS PREVIOUSLY TREATED, LOCALLY ADVANCED OR METASTATIC CHOLANGIOCARCINOMA
250MG TIBSOVO SERVIER N211192 July 20, 2018 RX TABLET ORAL 9850277 Jan. 18, 2033 A METHOD OF TREATING A CANCER CHARACTERIZED BY AN IDH1 MUTATION WHERE THE CANCER IS ACUTE MYELOGENOUS LEUKEMIA (AML)
250MG TIBSOVO SERVIER N211192 July 20, 2018 RX TABLET ORAL 9850277 Jan. 18, 2033 A METHOD OF TREATING A CANCER CHARACTERIZED BY AN IDH1 MUTATION WHERE THE CANCER IS NEWLY DIAGNOSED ACUTE MYELOID LEUKEMIA (AML)
250MG TIBSOVO SERVIER N211192 July 20, 2018 RX TABLET ORAL 9850277 Jan. 18, 2033 A METHOD OF TREATING A CANCER CHARACTERIZED BY AN IDH1 MUTATION WHERE THE CANCER IS RELAPSED OR REFRACTORY ACUTE MYELOID LEUKEMIA (AML)
250MG TIBSOVO SERVIER N211192 July 20, 2018 RX TABLET ORAL 9474779 Aug. 19, 2033 A METHOD OF TREATING A CANCER CHARACTERIZED BY AN IDH1 MUTATION WHEREIN THE CANCER IS PREVIOUSLY TREATED, LOCALLY ADVANCED OR METASTATIC CHOLANGIOCARCINOMA
250MG TIBSOVO SERVIER N211192 July 20, 2018 RX TABLET ORAL 9474779 Aug. 19, 2033 A METHOD OF TREATING A CANCER CHARACTERIZED BY AN IDH1 MUTATION WHERE THE CANCER IS ACUTE MYELOGENOUS LEUKEMIA (AML)
250MG TIBSOVO SERVIER N211192 July 20, 2018 RX TABLET ORAL 9474779 Aug. 19, 2033 A METHOD OF TREATING A CANCER CHARACTERIZED BY AN IDH1 MUTATION WHERE THE CANCER IS NEWLY DIAGNOSED ACUTE MYELOID LEUKEMIA (AML)
250MG TIBSOVO SERVIER N211192 July 20, 2018 RX TABLET ORAL 9474779 Aug. 19, 2033 A METHOD OF TREATING A CANCER CHARACTERIZED BY AN IDH1 MUTATION WHERE THE CANCER IS RELAPSED OR REFRACTORY ACUTE MYELOID LEUKEMIA (AML)
250MG TIBSOVO SERVIER N211192 July 20, 2018 RX TABLET ORAL 10799490 March 13, 2035 A METHOD OF TREATING ACUTE MYELOGENOUS LEUKEMIA (AML) IN A SUBJECT BY ADMINISTERING A PHARMACEUTICAL COMPOSITION WHERE THE AML IS CHARACTERIZED BY THE PRESENCE OF A MUTANT ALLELE OF IDH1 AND THE AML IS NEWLY DIAGNOSED
250MG TIBSOVO SERVIER N211192 July 20, 2018 RX TABLET ORAL 10799490 March 13, 2035 A METHOD OF TREATING ACUTE MYELOGENOUS LEUKEMIA (AML) IN A SUBJECT BY ADMINISTERING A PHARMACEUTICAL COMPOSITION WHERE THE AML IS CHARACTERIZED BY THE PRESENCE OF A MUTANT ALLELE OF IDH1 AND WHERE THE AML IS RELAPSED/REFRACTORY
250MG TIBSOVO SERVIER N211192 July 20, 2018 RX TABLET ORAL 9968595 March 13, 2035 A METHOD OF TREATING A CANCER CHARACTERIZED BY AN IDH1 MUTATION WHERE THE CANCER IS NEWLY DIAGNOSED ACUTE MYELOID LEUKEMIA (AML)
250MG TIBSOVO SERVIER N211192 July 20, 2018 RX TABLET ORAL 9968595 March 13, 2035 A METHOD OF TREATING A CANCER CHARACTERIZED BY AN IDH1 MUTATION WHERE THE CANCER IS RELAPSED OR REFRACTORY ACUTE MYELOID LEUKEMIA (AML)
250MG TIBSOVO SERVIER N211192 July 20, 2018 RX TABLET ORAL 9968595 March 13, 2035 TREATMENT OF ACUTE MYELOID LEUKEMIA (AML) WITH AN IDH1 MUTATION
250MG TIBSOVO SERVIER N211192 July 20, 2018 RX TABLET ORAL 10980788 June 7, 2039 A METHOD OF TREATING PREVIOUSLY TREATED, LOCALLY ADVANCED OR METASTATIC CHOLANGIOCARCINOMA CHARACTERIZED BY THE PRESENCE OF A MUTANT ALLELE OF IDH1 BY ADMINISTERING A ONCE DAILY 500 MG ORAL DOSE TO A SUBJECT THAT HAS NOT INGESTED A HIGH-FAT MEAL
250MG TIBSOVO SERVIER N211192 July 20, 2018 RX TABLET ORAL 10980788 June 7, 2039 TREATING NEWLY DIAGNOSED ACUTE MYELOGENOUS LEUKEMIA (AML) CHARACTERIZED BY THE PRESENCE OF A MUTANT ALLELE OF IDH1 BY ADMINISTERING A ONCE DAILY 500 MG ORAL DOSE TO A SUBJECT THAT HAS NOT INGESTED A HIGH-FAT MEAL
250MG TIBSOVO SERVIER N211192 July 20, 2018 RX TABLET ORAL 10980788 June 7, 2039 TREATING RELAPSED/REFRACTORY ACUTE MYELOGENOUS LEUKEMIA (AML) CHARACTERIZED BY THE PRESENCE OF A MUTANT ALLELE OF IDH1 BY ADMINISTERING A ONCE DAILY 500 MG ORAL DOSE TO A SUBJECT THAT HAS NOT INGESTED A HIGH-FAT MEAL

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
250MG TIBSOVO SERVIER N211192 July 20, 2018 RX TABLET ORAL May 2, 2022 TREATMENT OF ADULT PATIENTS WITH NEWLY-DIAGNOSED ACUTE MYELOID LEUKEMIA (AML) WHO ARE >= 75 YEARS OLD OR WHO HAVE COMORBIDITIES THAT PRECLUDE USE OF INTENSIVE INDUCTION CHEMOTHERAPY
250MG TIBSOVO SERVIER N211192 July 20, 2018 RX TABLET ORAL July 20, 2023 NEW CHEMICAL ENTITY
250MG TIBSOVO SERVIER N211192 July 20, 2018 RX TABLET ORAL Aug. 25, 2024 FOR THE TREATMENT OF ADULT PATIENTS WITH PREVIOUSLY TREATED, LOCALLY ADVANCED OR METASTATIC CHOLANGIOCARCINOMA WITH AN IDH1 MUTATION AS DETECTED BY AN FDA-APPROVED TEST
250MG TIBSOVO SERVIER N211192 July 20, 2018 RX TABLET ORAL July 20, 2025 INDICATED FOR THE TREATMENT OF ADULT PATIENTS WITH RELAPSED OR REFRACTORY ACUTE MYELOID LEUKEMIA (AML) WITH A SUSCEPTIBLE ISOCITRATE DEHYDROGENASE-1 (IDH1) MUTATION AS DETECTED BY AN FDA-APPROVED TEST
250MG TIBSOVO SERVIER N211192 July 20, 2018 RX TABLET ORAL May 2, 2026 TX OF NEWLY-DIAGNOSED ACUTE MYELOID LEUKEMIA WITH A SUSCEPTIBLE ISOCITRATE DEHYDROGENASE-1 MUTATION AS DETECTED BY AN FDA-APPROVED TEST IN ADULT PTS WHO ARE >=75 YRS OLD OR WHO HAVE COMORBIDITIES THAT PRECLUDE USE OF INTENSIVE INDUCTION CHEMOTHERAPY
250MG TIBSOVO SERVIER N211192 July 20, 2018 RX TABLET ORAL Aug. 25, 2028 TREATMENT OF ADULT PATIENTS WITH PREVIOUSLY TREATED, LOCALLY ADVANCED OR METASTATIC CHOLANGIOCARCINOMA WITH AN ISOCITRATE DEHYDROGENASE-1 (IDH1) MUTATION AS DETECTED BY AN FDA-APPROVED TEST

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Isocitrate dehydrogenase [NADP] cytoplasmic Enzyme INHIBITOR IC50 7.15 SCIENTIFIC LITERATURE DRUG LABEL

External reference:

IDSource
Q2PCN8MAM6 UNII
C4682397 UMLSCUI
CHEBI:145430 CHEBI
CHEMBL3989958 ChEMBL_ID
71657455 PUBCHEM_CID
DB14568 DRUGBANK_ID
D11090 KEGG_DRUG
9217 IUPHAR_LIGAND_ID
2049873 RXNORM
285271 MMSL
34590 MMSL
d08845 MMSL
773137008 SNOMEDCT_US
773232006 SNOMEDCT_US
4037715 VANDF
017647 NDDF
C000627630 MESH_SUPPLEMENTAL_RECORD_UI
10225 INN_ID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Tibsovo HUMAN PRESCRIPTION DRUG LABEL 1 71334-100 TABLET, FILM COATED 250 mg ORAL NDA 28 sections
Tibsovo HUMAN PRESCRIPTION DRUG LABEL 1 71334-100 TABLET, FILM COATED 250 mg ORAL NDA 28 sections
TIBSOVO HUMAN PRESCRIPTION DRUG LABEL 1 72694-617 TABLET, FILM COATED 250 mg ORAL NDA 31 sections
TIBSOVO HUMAN PRESCRIPTION DRUG LABEL 1 72694-617 TABLET, FILM COATED 250 mg ORAL NDA 31 sections