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

Stem definitionDrug idCAS RN
tyrosine kinase inhibitors 5680 1448169-71-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • futibatinib
  • lytgobi
  • TAS-120
Futibatinib is a small molecule kinase inhibitor of FGFR 1, 2, 3, and 4 with IC50 values of less than 4 nM. Futibatinib covalently binds FGFR. Constitutive FGFR signaling can support the proliferation and survival of malignant cells. Futibatinib inhibited FGFR phosphorylation and downstream signaling and decreased cell viability in cancer cell lines with FGFR alterations including FGFR fusions/rearrangements, amplifications, and mutations. Futibatinib demonstrated anti-tumor activity in mouse and rat xenograft models of human tumors with activating FGFR genetic alterations.
  • Molecular weight: 418.46
  • Formula: C22H22N6O3
  • CLOGP: 1.96
  • LIPINSKI: 0
  • HAC: 9
  • HDO: 1
  • TPSA: 108.39
  • ALOGS: -4.02
  • ROTB: 6
  • Status: ONP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
July 4, 2023 EMA TAIHO PHARMA NETHERLANDS B.V.
Sept. 30, 2022 FDA TAIHO ONCOLOGY

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01EN04 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
PROTEIN KINASE INHIBITORS
Fibroblast growth factor receptor (FGFR) tyrosine kinase inhibitors
MeSH PA D000970 Antineoplastic Agents

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

DiseaseRelationSNOMED_IDDOID
Intrahepatic cholangiocarcinoma indication 109842005 DOID:4928




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
4MG LYTGOBI TAIHO ONCOLOGY N214801 Sept. 30, 2022 RX TABLET ORAL 9108973 Feb. 23, 2033 METHOD OF TREATING INTRAHEPATIC CHOLANGIOCARCINOMA

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
4MG LYTGOBI TAIHO ONCOLOGY N214801 Sept. 30, 2022 RX TABLET ORAL Sept. 30, 2027 NEW CHEMICAL ENTITY
4MG LYTGOBI TAIHO ONCOLOGY N214801 Sept. 30, 2022 RX TABLET ORAL Sept. 30, 2029 TREATMENT OF ADULT PATIENTS WITH PREVIOUSLY TREATED, UNRESECTABLE, LOCALLY ADVANCED OR METASTATIC INTRAHEPATIC CHOLANGIOCARCINOMA HARBORING FIBROBLAST GROWTH FACTOR RECEPTOR 2 (FGFR2) GENE FUSIONS OR OTHER REARRANGEMENTS

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Fibroblast growth factor receptor 3 Kinase INHIBITOR IC50 8.79 SCIENTIFIC LITERATURE DRUG LABEL
Fibroblast growth factor receptor 1 Kinase INHIBITOR IC50 8.74 SCIENTIFIC LITERATURE DRUG LABEL
Fibroblast growth factor receptor 2 Kinase INHIBITOR IC50 8.85 SCIENTIFIC LITERATURE DRUG LABEL
Fibroblast growth factor receptor 4 Kinase INHIBITOR IC50 8.79 SCIENTIFIC LITERATURE DRUG LABEL
Tyrosine-protein kinase BTK Kinase IC50 7.02 CHEMBL

External reference:

IDSource
TAW PDB_CHEM_ID
CHEMBL3701238 ChEMBL_ID
C000713257 MESH_SUPPLEMENTAL_RECORD_UI
9786 IUPHAR_LIGAND_ID
DB15149 DRUGBANK_ID
019197 NDDF
4041794 VANDF
C5139845 UMLSCUI
10879 INN_ID
D11725 KEGG_DRUG
71621331 PUBCHEM_CID
2628190 RXNORM
361969 MMSL
40947 MMSL
d09927 MMSL
4B93MGE4AL UNII

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
LYTGOBI HUMAN PRESCRIPTION DRUG LABEL 1 64842-0120 TABLET 4 mg ORAL NDA 27 sections