enasidenib Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
5251 1446502-11-9

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • enasidenib
  • enasidenib mesylate
  • AG-221
  • CC-90007 Free Base
  • CC-90007
  • AG-221 mesylate
Enasidenib is a small molecule inhibitor of the isocitrate dehydrogenase 2 (IDH2) enzyme. Enasidenib targets the mutant IDH2 variants R140Q, R172S, and R172K at approximately 40-fold lower concentrations than the wild-type enzyme in vitro. Inhibition of the mutant IDH2 enzyme by enasidenib led to decreased 2-hydroxyglutarate (2-HG) levels and induced myeloid differentiation in vitro and in vivo in mouse xenograft models of IDH2 mutated AML. In blood samples from patients with AML with mutated IDH2, enasidenib decreased 2-HG levels, reduced blast counts and increased percentages of mature myeloid cells.
  • Molecular weight: 473.38
  • Formula: C19H17F6N7O
  • CLOGP: 3.76
  • LIPINSKI: 0
  • HAC: 8
  • HDO: 3
  • TPSA: 108.74
  • ALOGS: -4.11
  • ROTB: 8

  • Status: ONP

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

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Aug. 1, 2017 FDA CELGENE CORP

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
Differentiation syndrome 223.32 37.61 35 1101 876 46684050
Death 205.33 37.61 116 1020 335432 46349494
Acute myeloid leukaemia 151.63 37.61 41 1095 15737 46669189
Platelet count decreased 43.12 37.61 28 1108 99996 46584930
Acute myeloid leukaemia recurrent 41.29 37.61 9 1127 1387 46683539

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
Death 274.88 42.43 187 1354 357096 29593841
Differentiation syndrome 267.22 42.43 47 1494 1113 29949824
Acute myeloid leukaemia 257.28 42.43 75 1466 17931 29933006
Full blood count decreased 51.63 42.43 22 1519 15695 29935242
Platelet count decreased 43.51 42.43 39 1502 106090 29844847
Decreased appetite 42.54 42.43 45 1496 149865 29801072

Pharmacologic Action:

SourceCodeDescription
ATC L01XX59 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
OTHER ANTINEOPLASTIC AGENTS
Other antineoplastic agents
FDA MoA N0000193614 Isocitrate Dehydrogenase 2 Inhibitors
FDA EPC N0000193615 Isocitrate Dehydrogenase 2 Inhibitor
CHEBI has role CHEBI:35610 cytostatic
CHEBI has role CHEBI:145410 ec 1.1.1.42 inhibitors

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Acute myeloid leukemia, disease indication 91861009

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 4.77 Basic
pKa2 2.61 Basic
pKa3 0.4 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 100MG BASE IDHIFA CELGENE CORP N209606 Aug. 1, 2017 RX TABLET ORAL Aug. 1, 2022 NEW CHEMICAL ENTITY
EQ 50MG BASE IDHIFA CELGENE CORP N209606 Aug. 1, 2017 RX TABLET ORAL Aug. 1, 2022 NEW CHEMICAL ENTITY
EQ 100MG BASE IDHIFA CELGENE CORP N209606 Aug. 1, 2017 RX TABLET ORAL Aug. 1, 2024 TREATMENT OF ADULT PATIENTS WITH RELAPSED OR REFRACTORY ACUTE MYELOID LEUKEMIA WITH AN ISOCITRATE DEHYDROGENULLSE-2 (IDH2) MUTATION AS DETECTED BY AN FDA-APPROVED TEST
EQ 50MG BASE IDHIFA CELGENE CORP N209606 Aug. 1, 2017 RX TABLET ORAL Aug. 1, 2024 TREATMENT OF ADULT PATIENTS WITH RELAPSED OR REFRACTORY ACUTE MYELOID LEUKEMIA WITH AN ISOCITRATE DEHYDROGENULLSE-2 (IDH2) MUTATION AS DETECTED BY AN FDA-APPROVED TEST

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Isocitrate dehydrogenase [NADP], mitochondrial Enzyme INHIBITOR IC50 7 SCIENTIFIC LITERATURE DRUG LABEL

External reference:

IDSource
1650550-25-6 SECONDARY_CAS_RN
4036873 VANDF
C3827168 UMLSCUI
CHEBI:145374 CHEBI
69Q PDB_CHEM_ID
CHEMBL3989908 ChEMBL_ID
CHEMBL3989931 ChEMBL_ID
89683805 PUBCHEM_CID
D10901 KEGG_DRUG
DB13874 DRUGBANK_ID
C000605269 MESH_SUPPLEMENTAL_RECORD_UI
8960 IUPHAR_LIGAND_ID
10162 INN_ID
3T1SS4E7AG UNII
1940331 RXNORM
32972 MMSL
d08627 MMSL
017290 NDDF
017291 NDDF
763038001 SNOMEDCT_US
763583008 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Idhifa HUMAN PRESCRIPTION DRUG LABEL 1 59572-705 TABLET, FILM COATED 50 mg ORAL NDA 29 sections
Idhifa HUMAN PRESCRIPTION DRUG LABEL 1 59572-710 TABLET, FILM COATED 100 mg ORAL NDA 29 sections