◎ Sugi Atlas

Atlas / Drug / Futibatinib

Futibatinib

drug
On this page

Also known as Fgfr-in-1LytgobiTas 120Tas-120US9108973, 2

Summary

Futibatinib (CHEMBL3701238) is an approved small molecule (ATC L01EN04) targeting FGFR1, FGFR2, and FGFR3; indicated across 8 conditions including cholangiocarcinoma and neoplasm; with CIViC clinical evidence for 29 variant-indication associations (e.g. FGFR2::v Fusion OR FGFR2::? Fusion in intrahepatic cholangiocarcinoma).

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: L01EN04
  • Targets: 4 (FGFR1, FGFR2, FGFR3…)
  • Indications: 8 conditions
  • Clinical trials: 21
  • Precision-oncology evidence (CIViC): 29 variant–indication associations
  • Chemistry: 418.4 Da · C22H22N6O3

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL3701238
NameFutibatinib
TypeSmall molecule
Max phase4
FDA approvedyes
PubChem CID71621331
ATCL01EN04
Molecular formulaC22H22N6O3
Molecular weight418.4
InChIKeyKEIPNCCJPRMIAX-HNNXBMFYSA-N

SMILES: COC1=CC(=CC(=C1)C#CC2=NN(C3=NC=NC(=C23)N)[C@H]4CCN(C4)C(=O)C=C)OC

IUPAC name: 1-[(3S)-3-[4-amino-3-[2-(3,5-dimethoxyphenyl)ethynyl]pyrazolo[3,4-d]pyrimidin-1-yl]pyrrolidin-1-yl]prop-2-en-1-one

Also known as: Fgfr-in-1, Futibatinib, Lytgobi, Tas 120, Tas-120, TAS-120, US9108973, 2, FUTIBATINIB

Patent coverage: 368 distinct patent families (813 SureChEMBL compound mentions), from 1 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

GeneTargetActionpAffinityCancer dependencyUniProt
FGFR1fibroblast growth factor receptor 1Inhibition8.4411.5%P11362
FGFR2fibroblast growth factor receptor 2Inhibition8.961.7%P21802
FGFR3fibroblast growth factor receptor 3Inhibition9.30.5%P22607
FGFR4fibroblast growth factor receptor 4Inhibition8.470.7%P22455

Broader ChEMBL bioactivity targets: 6 (assay-derived). Sample: Fibroblast growth factor receptor 3, Vascular endothelial growth factor receptor 2, Fibroblast growth factor receptor 1, Fibroblast growth factor receptor 4, Fibroblast growth factor receptor 2, Tyrosine-protein kinase BTK.

Bioactivity

ChEMBL activities: 66 potent at pChembl ≥ 5 of 66 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
FGFR39.49IC500.32nMCHEMBL_ACT_29152193
FGFR29.44IC500.36nMCHEMBL_ACT_29152151
FGFR39.37IC500.43nMCHEMBL_ACT_29152169
FGFR39.31IC500.49nMCHEMBL_ACT_29152187
FGFR19.31IC500.49nMCHEMBL_ACT_29164266
FGFR39.3IC500.5nMCHEMBL_ACT_17685606
FGFR39.3IC500.5nMCHEMBL_ACT_28225997
FGFR39.28IC500.53nMCHEMBL_ACT_24354972
FGFR29.12IC500.75nMCHEMBL_ACT_29152139
FGFR29.11IC500.77nMCHEMBL_ACT_29152157
FGFR29IC501nMCHEMBL_ACT_25084773
FGFR28.96IC501.1nMCHEMBL_ACT_17685555
FGFR28.96IC501.1nMCHEMBL_ACT_27006023
FGFR28.96IC501.1nMCHEMBL_ACT_28185125
FGFR28.96IC501.1nMCHEMBL_ACT_28225841
FGFR28.89IC501.3nMCHEMBL_ACT_24688099
FGFR28.89IC501.3nMCHEMBL_ACT_25036477
FGFR28.89IC501.3nMCHEMBL_ACT_26025564
FGFR28.89IC501.3nMCHEMBL_ACT_29152328
FGFR28.89IC501.3nMCHEMBL_ACT_29164298
FGFR28.85IC501.4nMCHEMBL_ACT_29064071
FGFR38.8IC501.6nMCHEMBL_ACT_24688101
FGFR38.8IC501.6nMCHEMBL_ACT_25036478
FGFR38.8IC501.6nMCHEMBL_ACT_25084825
FGFR38.8IC501.6nMCHEMBL_ACT_26025579
FGFR38.8IC501.6nMCHEMBL_ACT_29064072
FGFR38.8IC501.6nMCHEMBL_ACT_29152336
FGFR38.8IC501.6nMCHEMBL_ACT_29164306
FGFR28.74IC501.8nMCHEMBL_ACT_25084775
FGFR18.74IC501.8nMCHEMBL_ACT_25084824

Target pathways

Aggregated over 4 target gene(s): FGFR1, FGFR2, FGFR3, FGFR4.

Top Reactome pathways

55 total, by targets touching each:

PathwayTargetsGenes
PI3K Cascade4FGFR1, FGFR2, FGFR3, FGFR4
PIP3 activates AKT signaling4FGFR1, FGFR2, FGFR3, FGFR4
Constitutive Signaling by Aberrant PI3K in Cancer4FGFR1, FGFR2, FGFR3, FGFR4
RAF/MAP kinase cascade4FGFR1, FGFR2, FGFR3, FGFR4
PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling4FGFR1, FGFR2, FGFR3, FGFR4
betaKlotho-mediated ligand binding1FGFR4
Signaling by FGFR1 amplification mutants1FGFR1
Signaling by activated point mutants of FGFR11FGFR1
FGFR4 mutant receptor activation1FGFR4
Signaling by activated point mutants of FGFR31FGFR3
FGFR4 ligand binding and activation1FGFR4
FGFR1b ligand binding and activation1FGFR1
FGFR3b ligand binding and activation1FGFR3
FGFR3c ligand binding and activation1FGFR3
FGFR1c ligand binding and activation1FGFR1
FGFR1c and Klotho ligand binding and activation1FGFR1
FGFR2c ligand binding and activation1FGFR2
FGFR2b ligand binding and activation1FGFR2
Signaling by FGFR2 amplification mutants1FGFR2
t(4;14) translocations of FGFR31FGFR3
Activated point mutants of FGFR21FGFR2
NCAM signaling for neurite out-growth1FGFR1
Signal transduction by L11FGFR1
Phospholipase C-mediated cascade: FGFR11FGFR1
Phospholipase C-mediated cascade; FGFR21FGFR2
Phospholipase C-mediated cascade; FGFR31FGFR3
Phospholipase C-mediated cascade; FGFR41FGFR4
Downstream signaling of activated FGFR11FGFR1
SHC-mediated cascade:FGFR11FGFR1
PI-3K cascade:FGFR11FGFR1

Dominant GO biological processes

GO termTargets
protein phosphorylation4
positive regulation of cell population proliferation4
fibroblast growth factor receptor signaling pathway4
positive regulation of MAPK cascade4
positive regulation of phospholipase activity3
peptidyl-tyrosine phosphorylation3
protein autophosphorylation3
skeletal system morphogenesis3
positive regulation of cell communication3
positive regulation of signaling3
positive regulation of ERK1 and ERK2 cascade3
negative regulation of transcription by RNA polymerase II2
MAPK cascade2
skeletal system development2
angiogenesis2

Indications & clinical

Indications

8 indications (3 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

IndicationTrial phaseMONDOEFO
cholangiocarcinoma4MONDO:0019087EFO:0005221
neoplasm4MONDO:0005070EFO:0000616
soft tissue sarcoma3MONDO:0018078EFO:1001968
biliary tract neoplasm3MONDO:0005304EFO:0003891
hepatocellular carcinoma2MONDO:0007256EFO:0000182
non-small cell lung carcinoma1MONDO:0005233EFO:0003060

2 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 21.

Phase distribution

PhaseTrials
PHASE210
PHASE14
PHASE33
PHASE1/PHASE22
PHASE2/PHASE31
Not specified1

Top trials by phase / activity

NCTPhaseStatusTitle
NCT05615818PHASE3RECRUITINGPersonalized Medicine for Advanced Biliary Cancer Patients
NCT06506955PHASE2/PHASE3ENROLLING_BY_INVITATIONFutibatinib in Patients Previously Enrolled in an Antecedent Futibatinib as Monotherapy or Combination Therapy.
NCT03784014PHASE3COMPLETEDMolecular Profiling of Advanced Soft-tissue Sarcomas
NCT04093362PHASE3TERMINATEDFutibatinib Versus Gemcitabine-Cisplatin Chemotherapy as First-Line Treatment of Patients With Advanced Cholangiocarcinoma Harboring FGFR2 Gene Rearrangements
NCT02693535PHASE2RECRUITINGTAPUR: Testing the Use of Food and Drug Administration (FDA) Approved Drugs That Target a Specific Abnormality in a Tumor Gene in People With Advanced Stage Cancer
NCT02813135PHASE1/PHASE2RECRUITINGEuropean Proof-of-Concept Therapeutic Stratification Trial of Molecular Anomalies in Relapsed or Refractory Tumors
NCT03767075PHASE2RECRUITINGA Modular Multi-Basket Trial to Improve Personalized Medicine in Cancer Patients (Basket of Baskets)
NCT05727176PHASE2RECRUITINGStudy of Futibatinib in Patients With Advanced Cholangiocarcinoma With FGFR2 Fusion or Rearrangement
NCT05945823PHASE2ACTIVE_NOT_RECRUITINGPhase 2 Futibatinib in Combination With PD-1 Antibody Based Standard of Care in Solid Tumors
NCT06263153PHASE2RECRUITINGFutibatinib in Combination With Durvalumab Prior to Cystectomy for the Treatment of Muscle-Invasive Bladder Cancer Patients Who Are Ineligible for Cisplatin-based Therapy
NCT02052778PHASE1/PHASE2COMPLETEDA Study of TAS-120 in Patients With Advanced Solid Tumors
NCT04024436PHASE2TERMINATEDA Study of TAS-120 in Patients With Metastatic Breast Cancer
NCT04189445PHASE2TERMINATEDFutibatinib in Patients With Specific FGFR Aberrations
NCT04601857PHASE2TERMINATEDFutibatinib and Pembrolizumab Combination in the Treatment of Advanced or Metastatic Urothelial Carcinoma
NCT04828486PHASE2COMPLETEDFutibatinib and Pembrolizumab for Treatment of Advanced or Metastatic FGF19 Positive BCLC Stage A, B, or C Liver Cancer
NCT05036681PHASE2TERMINATEDA Phase II Study of Futibatinib and Pembrolizumab in Metastatic Microsatellite Stable Endometrial Carcinoma
NCT04999761PHASE1RECRUITINGAB122 Platform Study
NCT05827614PHASE1ACTIVE_NOT_RECRUITINGStudy of the CHK1 Inhibitor BBI-355, an ecDNA-directed Therapy (ecDTx), and the RNR Inhibitor BBI-825, in Subjects With Tumors With Oncogene Amplifications
NCT07594548PHASE1NOT_YET_RECRUITINGFutibatinib With Paclitaxel and Ramucirumab for the Treatment of Locally Advanced or Unresectable Gastric, Gastroesophageal Junction, or Esophageal Adenocarcinoma
NCT04965818PHASE1TERMINATEDPhase 1b/2 Study of Futibatinib in Combination With Binimetinib in Patients With Advanced KRAS Mutant Cancer
NCT04507503Not specifiedAPPROVED_FOR_MARKETINGExpanded Access Study of TAS-120 in Patients With Advanced Cholangiocarcinoma Harboring FGFR2 Gene Rearrangements

Clinical evidence (CIViC)

Variant × indication × effect (29 predictive associations from 31 curated evidence items):

VariantIndicationEffectTherapyLevelCIViC
FGFR2::v Fusion OR FGFR2::? FusionIntrahepatic CholangiocarcinomaSensitivity/ResponseFutibatinibCIViC AEID11609 +1
FGFR2::v FusionCholangiocarcinomaSensitivity/ResponseFutibatinibCIViC BEID12489 +1
FGFR2::BICC1 FusionIntrahepatic CholangiocarcinomaSensitivity/ResponseFutibatinibCIViC BEID11610
FGFR1 M563TUrothelial CarcinomaSensitivity/ResponseFutibatinibCIViC CEID11636
FGFR1::PLAG1 FusionHead And Neck CancerSensitivity/ResponseFutibatinibCIViC CEID11639
FGFR1::TACC1 FusionGlioblastomaSensitivity/ResponseFutibatinibCIViC CEID11634
FGFR2 AmplificationGastric AdenocarcinomaSensitivity/ResponseFutibatinibCIViC CEID11637
FGFR2 AmplificationTriple-receptor Negative Breast CancerSensitivity/ResponseFutibatinibCIViC CEID11648
FGFR2 Amplification AND FGFR2::? FusionCholangiocarcinomaSensitivity/ResponseFutibatinibCIViC CEID11642
FGFR2 C383RCholangiocarcinomaSensitivity/ResponseFutibatinibCIViC CEID11631
FGFR2 W290CCholangiocarcinomaSensitivity/ResponseFutibatinibCIViC CEID11633
FGFR2 Y375CCancer Of Unknown Primary OriginSensitivity/ResponseFutibatinibCIViC CEID11640
FGFR2::BICC1 FusionCholangiocarcinomaSensitivity/ResponseFutibatinibCIViC CEID11629
FGFR2::CCDC6 FusionCholangiocarcinomaSensitivity/ResponseFutibatinibCIViC CEID11646
FGFR2::DBP FusionCholangiocarcinomaSensitivity/ResponseFutibatinibCIViC CEID11628
FGFR2::FILIP1 FusionCholangiocarcinomaSensitivity/ResponseFutibatinibCIViC CEID11630
FGFR2::KIAA1217 FusionIntrahepatic CholangiocarcinomaSensitivity/ResponseFutibatinibCIViC CEID11611
FGFR2::KIAA1217 FusionCholangiocarcinomaSensitivity/ResponseFutibatinibCIViC CEID11647
FGFR2::NRAP FusionCholangiocarcinomaSensitivity/ResponseFutibatinibCIViC CEID11641
FGFR2::POC1B FusionCholangiocarcinomaSensitivity/ResponseFutibatinibCIViC CEID11627
FGFR2::TNS1 FusionCholangiocarcinomaSensitivity/ResponseFutibatinibCIViC CEID11644
FGFR2::TTC28 FusionCholangiocarcinomaSensitivity/ResponseFutibatinibCIViC CEID11645
FGFR2::WAC FusionCholangiocarcinomaSensitivity/ResponseFutibatinibCIViC CEID11643
FGFR2::v Fusion OR FGFR2::? FusionCholangiocarcinomaSensitivity/ResponseFutibatinibCIViC CEID11632
FGFR3 S249CUrothelial CarcinomaSensitivity/ResponseFutibatinibCIViC CEID11635
FGFR3::TACC3 FusionGastric AdenocarcinomaSensitivity/ResponseFutibatinibCIViC CEID11638
FGFR3 Y373C AND FGFR3 N540KUrothelial CarcinomaResistanceErdafitinib + FutibatinibCIViC CEID12704
FGFR1 AmplificationBreast CancerSensitivity/ResponseFutibatinibCIViC DEID12547
FGFR3::TACC3 Fusion AND FGFR3 N540KCancerResistanceErdafitinib + FutibatinibCIViC DEID12706

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

91 molecules share ≥1 primary target. Top 60 by shared-target count:

MoleculeSourceStatusShared targets
CrizotinibChEMBL + PubChemPhase 4 (approved)FGFR1, FGFR2, FGFR3, FGFR4
PAZOPANIBChEMBL + PubChemPhase 4 (approved)FGFR1, FGFR2, FGFR3, FGFR4
BRIGATINIBChEMBLPhase 4 (approved)FGFR1, FGFR2, FGFR3, FGFR4
ERDAFITINIBChEMBLPhase 4 (approved)FGFR1, FGFR2, FGFR3, FGFR4
FEDRATINIBChEMBLPhase 4 (approved)FGFR1, FGFR2, FGFR3, FGFR4
INFIGRATINIBChEMBLPhase 4 (approved)FGFR1, FGFR2, FGFR3, FGFR4
LENVATINIBChEMBLPhase 4 (approved)FGFR1, FGFR2, FGFR3, FGFR4
NINTEDANIBChEMBLPhase 4 (approved)FGFR1, FGFR2, FGFR3, FGFR4
NINTEDANIB ESYLATEChEMBLPhase 4 (approved)FGFR1, FGFR2, FGFR3, FGFR4
PEMIGATINIBChEMBLPhase 4 (approved)FGFR1, FGFR2, FGFR3, FGFR4
PONATINIBChEMBLPhase 4 (approved)FGFR1, FGFR2, FGFR3, FGFR4
SUNITINIBChEMBLPhase 4 (approved)FGFR1, FGFR2, FGFR3, FGFR4
VANDETANIBChEMBLPhase 4 (approved)FGFR1, FGFR2, FGFR3, FGFR4
BRIVANIBChEMBLPhase 3FGFR1, FGFR2, FGFR3, FGFR4
CEDIRANIBChEMBLPhase 3FGFR1, FGFR2, FGFR3, FGFR4
DOVITINIBChEMBLPhase 3FGFR1, FGFR2, FGFR3, FGFR4
LESTAURTINIBChEMBLPhase 3FGFR1, FGFR2, FGFR3, FGFR4
LINIFANIBChEMBLPhase 3FGFR1, FGFR2, FGFR3, FGFR4
SEMAXANIBChEMBLPhase 3FGFR1, FGFR2, FGFR3, FGFR4
E-7090ChEMBLPhase 2FGFR1, FGFR2, FGFR3, FGFR4
FEXAGRATINIBChEMBLPhase 2FGFR1, FGFR2, FGFR3, FGFR4
FGFR INHIBITOR DEBIO 1347ChEMBLPhase 2FGFR1, FGFR2, FGFR3, FGFR4
FISOGATINIBChEMBLPhase 2FGFR1, FGFR2, FGFR3, FGFR4
LIRAFUGRATINIBChEMBLPhase 2FGFR1, FGFR2, FGFR3, FGFR4
OSI-632ChEMBLPhase 2FGFR1, FGFR2, FGFR3, FGFR4
R-406ChEMBLPhase 2FGFR1, FGFR2, FGFR3, FGFR4
REBASTINIBChEMBLPhase 2FGFR1, FGFR2, FGFR3, FGFR4
RESIGRATINIBChEMBLPhase 2FGFR1, FGFR2, FGFR3, FGFR4
SEGIGRATINIBChEMBLPhase 2FGFR1, FGFR2, FGFR3, FGFR4
SU-014813ChEMBLPhase 2FGFR1, FGFR2, FGFR3, FGFR4
TANDUTINIBChEMBLPhase 2FGFR1, FGFR2, FGFR3, FGFR4
TOZASERTIBChEMBLPhase 2FGFR1, FGFR2, FGFR3, FGFR4
AfatinibPubChemApprovedFGFR1, FGFR2, FGFR3, FGFR4
GefitinibPubChemApprovedFGFR1, FGFR2, FGFR3, FGFR4
IdelalisibPubChemApprovedFGFR1, FGFR2, FGFR3, FGFR4
SelumetinibPubChemApprovedFGFR1, FGFR2, FGFR3, FGFR4
AXITINIBChEMBLPhase 4 (approved)FGFR1, FGFR2, FGFR3
CERITINIBChEMBLPhase 4 (approved)FGFR2, FGFR3, FGFR4
DASATINIBChEMBLPhase 4 (approved)FGFR1, FGFR2, FGFR3
MIDOSTAURINChEMBLPhase 4 (approved)FGFR1, FGFR2, FGFR3
SORAFENIBChEMBLPhase 4 (approved)FGFR1, FGFR2, FGFR3
AT-9283ChEMBLPhase 2FGFR1, FGFR2, FGFR3
BMS-754807ChEMBLPhase 2FGFR1, FGFR2, FGFR3
DERAZANTINIBChEMBLPhase 2FGFR1, FGFR2, FGFR3
DORAMAPIMODChEMBLPhase 2FGFR1, FGFR2, FGFR4
FORETINIBChEMBLPhase 2FGFR1, FGFR2, FGFR3
LUCITANIBChEMBLPhase 2FGFR1, FGFR2, FGFR3
MK-2461ChEMBLPhase 2FGFR1, FGFR2, FGFR3
ROGARATINIBChEMBLPhase 2FGFR1, FGFR3, FGFR4
ENTRECTINIBChEMBLPhase 4 (approved)FGFR1, FGFR3
ALISERTIBChEMBLPhase 3FGFR1, FGFR3
MOTESANIBChEMBLPhase 3FGFR1, FGFR4
CENISERTIBChEMBLPhase 2FGFR1, FGFR3
CEP-11981ChEMBLPhase 2FGFR1, FGFR3
ILORASERTIBChEMBLPhase 2FGFR1, FGFR3
RX-518ChEMBLPhase 2FGFR1, FGFR2
REGORAFENIBChEMBL + PubChemPhase 4 (approved)FGFR1
CABOZANTINIBChEMBLPhase 4 (approved)FGFR1
CAPIVASERTIBChEMBLPhase 4 (approved)FGFR1
ERLOTINIBChEMBLPhase 4 (approved)FGFR2

About this page

Generated deterministically by Sugi Atlas from primary biomedical databases via BioBTree. Every record on this page traces to a primary source.

Generated
Atlas version
v1.1.2
BioBTree
v2.0.2

Sources 30

This page pulls from 30 datasets indexed by BioBTree:

chebichembl_activitychembl_moleculechembl_targetcivic_evidenceclingen_dosageclinical_trialsdepmapefoensemblentrezgogoparentgtopdbgtopdb_interactiongtopdb_ligandhgncmeshmondomsigdbpatent_compoundpharmgkbpharmgkb_guidelinepubchempubchem_activityreactomereactomeparentrefseqtranscriptuniprot