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

Stem definitionDrug idCAS RN
tyrosine kinase inhibitors 5459 872511-34-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • infigratinib
  • infigratinib phosphate
  • truseltiq
  • BGJ-398
  • NVP-BGJ398
Infigratinib is a small molecule kinase inhibitor of FGFR with IC50 values of 1.1, 1, 2, and 61 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively. The major human metabolites of infigratinib, BHS697 and CQM157, have similar in vitro binding affinities for FGFR1, FGFR2, and FGFR3 compared to infigratinib. Infigratinib inhibited FGFR signaling and decreased cell proliferation in cancer cell lines with activating FGFR amplifications, mutations, or fusions. Constitutive FGFR signaling can support the proliferation and survival of malignant cells. Infigratinib had anti-tumor activity in mouse and rat xenograft models of human tumors with activating FGFR2 or FGFR3 alterations, including two patient-derived xenograft models of cholangiocarcinoma that expressed FGFR2-TTC28 or FGFR2-TRA2B fusions. Infigratinib demonstrated brain-to-plasma concentration ratios (based on AUC0-inf) of 0.682 in rats after a single oral dose.
  • Molecular weight: 560.48
  • Formula: C26H31Cl2N7O3
  • CLOGP: 5.44
  • LIPINSKI: 1
  • HAC: 10
  • HDO: 2
  • TPSA: 95.09
  • ALOGS: -4.27
  • ROTB: 8

  • Status: OFM

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

Drug dosage:

None

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Bocci G, Oprea TI, Benet LZ

Approvals:

DateAgencyCompanyOrphan
June 28, 2019 FDA QED THERAP

FDA Adverse Event Reporting System (Female)

None

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
Hyperphosphataemia 32.96 23.70 4 3 6372 79738009

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01EN03 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
PROTEIN KINASE INHIBITORS
Fibroblast growth factor receptor (FGFR) tyrosine kinase inhibitors
MeSH PA D000970 Antineoplastic Agents
CHEBI has role CHEBI:35610 antineoplastic agents
CHEBI has role CHEBI:63457 FGFR inhibitors

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

DiseaseRelationSNOMED_IDDOID
Unresectable locally advanced or metastatic cholangiocarcinoma with FGFR2 fusion indication 312104005




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
100MG TRUSELTIQ HELSINN HLTHCARE N214622 May 28, 2021 DISCN CAPSULE ORAL May 28, 2026 NEW CHEMICAL ENTITY
25MG TRUSELTIQ HELSINN HLTHCARE N214622 May 28, 2021 DISCN CAPSULE ORAL May 28, 2026 NEW CHEMICAL ENTITY
100MG TRUSELTIQ HELSINN HLTHCARE N214622 May 28, 2021 DISCN CAPSULE ORAL May 28, 2028 FOR TREATMENT OF ADULTS WITH PREVIOUSLY TREATED, UNRESECTABLE LOCALLY ADVANCED OR METASTATIC CHOLANGIOCARCINOMA WITH A FIBROBLAST GROWTH FACTOR RECEPTOR 2 (FGFR2) FUSION OR OTHER REARRANGEMENT AS DETECTED BY AN FDA-APPROVED TEST
25MG TRUSELTIQ HELSINN HLTHCARE N214622 May 28, 2021 DISCN CAPSULE ORAL May 28, 2028 FOR TREATMENT OF ADULTS WITH PREVIOUSLY TREATED, UNRESECTABLE LOCALLY ADVANCED OR METASTATIC CHOLANGIOCARCINOMA WITH A FIBROBLAST GROWTH FACTOR RECEPTOR 2 (FGFR2) FUSION OR OTHER REARRANGEMENT AS DETECTED BY AN FDA-APPROVED TEST

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Fibroblast growth factor receptor 1 Kinase INHIBITOR 8.99 DRUG LABEL DRUG LABEL
Tyrosine-protein kinase ABL1 Kinase IC50 5.64 CHEMBL
Mast/stem cell growth factor receptor Kit Kinase IC50 6.12 CHEMBL
Proto-oncogene tyrosine-protein kinase Src Kinase IC50 5.53 CHEMBL
Tyrosine-protein kinase Lck Kinase IC50 5.60 CHEMBL
Tyrosine-protein kinase Yes Kinase IC50 5.96 CHEMBL
Tyrosine-protein kinase Fyn Kinase IC50 5.72 CHEMBL
Serine/threonine-protein kinase B-raf Kinase IC50 5.38 CHEMBL
Receptor-type tyrosine-protein kinase FLT3 Kinase IC50 5.49 CHEMBL
Proto-oncogene tyrosine-protein kinase receptor Ret Kinase IC50 5.47 CHEMBL
Vascular endothelial growth factor receptor 1 Kinase IC50 5.82 CHEMBL
Vascular endothelial growth factor receptor 2 Kinase INHIBITOR IC50 6.74 IUPHAR
Vascular endothelial growth factor receptor 3 Kinase IC50 5.68 CHEMBL
Platelet-derived growth factor receptor alpha Kinase IC50 5.57 CHEMBL
Insulin receptor Kinase IC50 5.47 CHEMBL
Tyrosine-protein kinase JAK2 Kinase IC50 5.54 CHEMBL
Macrophage-stimulating protein receptor Kinase IC50 5.54 CHEMBL
Angiopoietin-1 receptor Kinase IC50 5.69 CHEMBL
Hepatocyte growth factor receptor Kinase IC50 5.52 CHEMBL
Tyrosine-protein kinase Lyn Kinase IC50 6.52 CHEMBL
Cytoplasmic tyrosine-protein kinase BMX Kinase IC50 5.47 CHEMBL
ALK tyrosine kinase receptor Kinase IC50 5.51 CHEMBL
Ephrin type-B receptor 1 Kinase IC50 5.52 CHEMBL
BDNF/NT-3 growth factors receptor Kinase IC50 5.50 CHEMBL
Non-receptor tyrosine-protein kinase TYK2 Kinase IC50 5.48 CHEMBL
Proto-oncogene tyrosine-protein kinase ROS Kinase IC50 5.49 CHEMBL
Smoothened homolog GPCR Ki 7.33 CHEMBL
Fibroblast growth factor receptor 3 Kinase INHIBITOR 8.70 DRUG LABEL
Fibroblast growth factor receptor 2 Kinase INHIBITOR 9 DRUG LABEL
Fibroblast growth factor receptor 4 Kinase INHIBITOR 7.21 DRUG LABEL
Tyrosine-protein kinase SYK Kinase IC50 5.27 CHEMBL
Fibroblast growth factor receptor 4, FGFR-4, EC 2.7.10.1 Unclassified IC50 6.27 CHEMBL

External reference:

IDSource
D11589 KEGG_DRUG
A4055ME1VK UNII
1310746-10-1 SECONDARY_CAS_RN
C3254591 UMLSCUI
CHEBI:63451 CHEBI
07J PDB_CHEM_ID
CHEMBL1852688 ChEMBL_ID
53235510 PUBCHEM_CID
DB11886 DRUGBANK_ID
CHEMBL1834657 ChEMBL_ID
10032 INN_ID
7877 IUPHAR_LIGAND_ID
018743 NDDF
018752 NDDF
1162483003 SNOMEDCT_US
1162514000 SNOMEDCT_US
4040560 VANDF
2550729 RXNORM
347055 MMSL
39550 MMSL
d09752 MMSL
C568950 MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
TRUSELTIQ HUMAN PRESCRIPTION DRUG LABEL 1 72730-101 CAPSULE 125 mg ORAL NDA 17 sections
TRUSELTIQ HUMAN PRESCRIPTION DRUG LABEL 1 72730-111 CAPSULE 100 mg ORAL NDA 17 sections
TRUSELTIQ HUMAN PRESCRIPTION DRUG LABEL 1 72730-202 CAPSULE 75 mg ORAL NDA 17 sections
TRUSELTIQ HUMAN PRESCRIPTION DRUG LABEL 1 72730-506 CAPSULE 50 mg ORAL NDA 17 sections