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

Stem definitionDrug idCAS RN
tyrosine kinase inhibitors 5347 936091-26-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • fedratinib
  • fedratinib hydrochloride
  • SAR302503
  • SAR-302503
  • TG101348
  • TG-101348
  • FEDR
  • inrebic
Fedratinib is an oral kinase inhibitor with activity against wild type and mutationally activated Janus Associated Kinase 2 (JAK2) and FMS-like tyrosine kinase 3 (FLT3). Fedratinib is a JAK2-selective inhibitor with higher inhibitory activity for JAK2 over family members JAK1, JAK3 and TYK2. Abnormal activation of JAK2 is associated with myeloproliferative neoplasms (MPNs), including myelofibrosis and polycythemia vera.
  • Molecular weight: 524.68
  • Formula: C27H36N6O3S
  • CLOGP: 6.25
  • LIPINSKI: 2
  • HAC: 9
  • HDO: 3
  • TPSA: 108.48
  • ALOGS: -4.74
  • ROTB: 10

  • Status: ONP

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

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Feb. 8, 2021 EMA CELGENE EUROPE BV
Aug. 16, 2019 FDA IMPACT

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01EJ02 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
PROTEIN KINASE INHIBITORS
Janus-associated kinase (JAK) inhibitors

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Myelofibrosis indication 52967002 DOID:4971
Primary myelofibrosis indication 307651005
Post-polycythaemia vera myelofibrosis indication 871540009
Post-essential thrombocythaemia myelofibrosis indication 871541008

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.42 acidic
pKa2 8.9 Basic
pKa3 5.69 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 INREBIC IMPACT N212327 Aug. 16, 2019 RX CAPSULE ORAL Aug. 16, 2024 NEW CHEMICAL ENTITY
EQ 100MG BASE INREBIC IMPACT N212327 Aug. 16, 2019 RX CAPSULE ORAL Aug. 16, 2026 INDICATED FOR THE TREATMENT OF ADULT PATIENTS WITH INTERMEDIATE-2 OR HIGH-RISK PRIMARY OR SECONDARY (POST-POLYCYTHEMIA VERA OR POST-ESSENTIAL THROMBOCYTHEMIA) MYELOFIBROSIS (MF)

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Tyrosine-protein kinase JAK2 Kinase INHIBITOR IC50 8.52 SCIENTIFIC LITERATURE DRUG LABEL
Receptor-type tyrosine-protein kinase FLT3 Kinase INHIBITOR IC50 7.82 SCIENTIFIC LITERATURE DRUG LABEL
Tyrosine-protein kinase JAK3 Kinase INHIBITOR IC50 5.99 SCIENTIFIC LITERATURE
Tyrosine-protein kinase JAK1 Kinase INHIBITOR IC50 6.97 SCIENTIFIC LITERATURE
Non-receptor tyrosine-protein kinase TYK2 Kinase INHIBITOR IC50 6.39 SCIENTIFIC LITERATURE

External reference:

IDSource
1374744-69-0 SECONDARY_CAS_RN
4038661 VANDF
C3886623 UMLSCUI
2TA PDB_CHEM_ID
CHEMBL1287853 ChEMBL_ID
CHEMBL4297216 ChEMBL_ID
DB12500 DRUGBANK_ID
D10630 KEGG_DRUG
C528327 MESH_SUPPLEMENTAL_RECORD_UI
5716 IUPHAR_LIGAND_ID
9707 INN_ID
6L1XP550I6 UNII
16722836 PUBCHEM_CID
2197490 RXNORM
321679 MMSL
37321 MMSL
d09354 MMSL
018090 NDDF
789359000 SNOMEDCT_US
789368003 SNOMEDCT_US
895592002 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Inrebic HUMAN PRESCRIPTION DRUG LABEL 1 59572-720 CAPSULE 100 mg ORAL NDA 30 sections