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

Stem definitionDrug idCAS RN
tyrosine kinase inhibitors 5327 1346242-81-6

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • erdafitinib
  • balversa
  • JNJ-42756493
  • G-024
Erdafitinib inhibited FGFR phosphorylation and signaling and decreased cell viability in cell lines expressing FGFR genetic alterations, including point mutations, amplifications, and fusions. Erdafitinib demonstrated antitumor activity in FGFR-expressing cell lines and xenograft models derived from tumor types, including bladder cancer.
  • Molecular weight: 446.56
  • Formula: C25H30N6O2
  • CLOGP: 4.27
  • LIPINSKI: 0
  • HAC: 8
  • HDO: 1
  • TPSA: 77.33
  • ALOGS: -4.53
  • ROTB: 9

  • Status: ONP

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

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
April 12, 2019 FDA JANSSEN BIOTECH

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

None

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Metastatic urothelial carcinoma indication 458321000124102

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.52 Basic
pKa2 2.13 Basic
pKa3 0.47 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
3MG BALVERSA JANSSEN BIOTECH N212018 April 12, 2019 RX TABLET ORAL 9464071 April 28, 2031 TREATMENT OF ADULTS WITH LOCALLY ADVANCED OR METASTATIC UROTHELIAL CARCINOMA THAT HAS SUSCEPTIBLE FGFR3 OR FGFR2 GENETIC ALTERATIONS AND PROGRESSED DURING OR FOLLOWING PRIOR PLATINUM-CONTAINING CHEMOTHERAPY
4MG BALVERSA JANSSEN BIOTECH N212018 April 12, 2019 RX TABLET ORAL 9464071 April 28, 2031 TREATMENT OF ADULTS WITH LOCALLY ADVANCED OR METASTATIC UROTHELIAL CARCINOMA THAT HAS SUSCEPTIBLE FGFR3 OR FGFR2 GENETIC ALTERATIONS AND PROGRESSED DURING OR FOLLOWING PRIOR PLATINUM-CONTAINING CHEMOTHERAPY
5MG BALVERSA JANSSEN BIOTECH N212018 April 12, 2019 RX TABLET ORAL 9464071 April 28, 2031 TREATMENT OF ADULTS WITH LOCALLY ADVANCED OR METASTATIC UROTHELIAL CARCINOMA THAT HAS SUSCEPTIBLE FGFR3 OR FGFR2 GENETIC ALTERATIONS AND PROGRESSED DURING OR FOLLOWING PRIOR PLATINUM-CONTAINING CHEMOTHERAPY

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
3MG BALVERSA JANSSEN BIOTECH N212018 April 12, 2019 RX TABLET ORAL April 12, 2024 NEW CHEMICAL ENTITY
4MG BALVERSA JANSSEN BIOTECH N212018 April 12, 2019 RX TABLET ORAL April 12, 2024 NEW CHEMICAL ENTITY
5MG BALVERSA JANSSEN BIOTECH N212018 April 12, 2019 RX TABLET ORAL April 12, 2024 NEW CHEMICAL ENTITY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Fibroblast growth factor receptor 1 Kinase INHIBITOR IC50 8.92 SCIENTIFIC LITERATURE DRUG LABEL
Fibroblast growth factor receptor 2 Kinase INHIBITOR IC50 8.60 SCIENTIFIC LITERATURE DRUG LABEL
Fibroblast growth factor receptor 3 Kinase INHIBITOR IC50 8.52 SCIENTIFIC LITERATURE DRUG LABEL
Fibroblast growth factor receptor 4 Kinase INHIBITOR IC50 8.24 SCIENTIFIC LITERATURE DRUG LABEL
Vascular endothelial growth factor receptor 2 Kinase INHIBITOR IC50 7.43 SCIENTIFIC LITERATURE DRUG LABEL

External reference:

IDSource
2123125 RXNORM
017965 NDDF
4038332 VANDF
36736 MMSL
d09237 MMSL
787731007 SNOMEDCT_US
787742003 SNOMEDCT_US
890E37NHMV UNII
10147 INN_ID
67462786 PUBCHEM_CID
DB12147 DRUGBANK_ID
D10927 KEGG_DRUG
CHEMBL3545376 ChEMBL_ID
9039 IUPHAR_LIGAND_ID
C000604580 MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
BALVERSA HUMAN PRESCRIPTION DRUG LABEL 1 59676-030 TABLET, FILM COATED 3 mg ORAL NDA 17 sections
BALVERSA HUMAN PRESCRIPTION DRUG LABEL 1 59676-040 TABLET, FILM COATED 4 mg ORAL NDA 17 sections
BALVERSA HUMAN PRESCRIPTION DRUG LABEL 1 59676-050 TABLET, FILM COATED 5 mg ORAL NDA 17 sections