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Tinengotinib

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Also known as Tt 00420Tt-00420

Summary

Tinengotinib (CHEMBL5314430) is a phase-3 clinical-stage small molecule targeting FGFR1, FGFR3, and FLT1; indicated across 3 conditions including cholangiocarcinoma and neoplasm.

At a glance

  • Status: Max clinical phase 3 (not approved)
  • Modality: Small molecule
  • Targets: 7 (FGFR1, FGFR3, FLT1…)
  • Indications: 3 conditions
  • Clinical trials: 13
  • Chemistry: 394.9 Da · C20H19ClN6O

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL5314430
NameTinengotinib
TypeSmall molecule
Max phase3
FDA approvedno
PubChem CID137279257
Molecular formulaC20H19ClN6O
Molecular weight394.9
InChIKeyDQFCVOOFMXEPOC-UHFFFAOYSA-N

SMILES: CC1=C2C(=NN1)NC3=CC(=NC=C3C(=N2)C4=CC=CC=C4Cl)N5CCOCC5

IUPAC name: 4-[9-(2-chlorophenyl)-6-methyl-2,4,5,8,12-pentazatricyclo[8.4.0.03,7]tetradeca-1(14),3,6,8,10,12-hexaen-13-yl]morpholine

Also known as: Tinengotinib, Tt 00420, Tt-00420, TT-00420, TINENGOTINIB

Patent coverage: 47 distinct patent families (117 SureChEMBL compound mentions), from 3 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 1Inhibition8.6411.5%P11362
FGFR3fibroblast growth factor receptor 3Inhibition8.460.5%P22607
FLT1fms related receptor tyrosine kinase 1Inhibition8.620.1%P17948
KDRkinase insert domain receptorInhibition8.61.1%P35968
AURKAaurora kinase AInhibition8.9299.4% (common-essential)O14965
AURKBaurora kinase BInhibition8.4899.7% (common-essential)Q96GD4
JAK2Janus kinase 2Inhibition9.120.7%O60674

Bioactivity

No ChEMBL bioactivity rows at pChembl ≥ 5 (expected for biologics / antibodies).

Target pathways

Aggregated over 7 target gene(s): FGFR1, FGFR3, FLT1, KDR, AURKA, AURKB, JAK2.

Top Reactome pathways

144 total, by targets touching each:

PathwayTargetsGenes
Cell Cycle3AURKA, AURKB, JAK2
RAF/MAP kinase cascade3FGFR1, FGFR3, JAK2
Cell Cycle, Mitotic3AURKA, AURKB, JAK2
PI3K Cascade2FGFR1, FGFR3
PIP3 activates AKT signaling2FGFR1, FGFR3
Signal Transduction2AURKB, JAK2
APC/C-mediated degradation of cell cycle proteins2AURKA, AURKB
APC/C:Cdh1 mediated degradation of Cdc20 and other APC/C:Cdh1 targeted proteins in late mitosis/early G12AURKA, AURKB
Neuropilin interactions with VEGF and VEGFR2FLT1, KDR
VEGF binds to VEGFR leading to receptor dimerization2FLT1, KDR
Generic Transcription Pathway2AURKA, AURKB
Constitutive Signaling by Aberrant PI3K in Cancer2FGFR1, FGFR3
SUMOylation2AURKA, AURKB
SUMO E3 ligases SUMOylate target proteins2AURKA, AURKB
Transcriptional Regulation by TP532AURKA, AURKB
Metabolism of proteins2AURKA, AURKB
Regulation of mitotic cell cycle2AURKA, AURKB
SUMOylation of DNA replication proteins2AURKA, AURKB
Regulation of TP53 Activity2AURKA, AURKB
Post-translational protein modification2AURKA, AURKB
Regulation of TP53 Activity through Phosphorylation2AURKA, AURKB
PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling2FGFR1, FGFR3
RNA Polymerase II Transcription2AURKA, AURKB
Gene expression (Transcription)2AURKA, AURKB
Interleukin-6 signaling1JAK2
Hemostasis1JAK2
MAPK3 (ERK1) activation1JAK2
RAF-independent MAPK1/3 activation1JAK2
MAPK1 (ERK2) activation1JAK2
Prolactin receptor signaling1JAK2

Dominant GO biological processes

GO termTargets
protein phosphorylation7
positive regulation of cell population proliferation5
positive regulation of MAPK cascade5
protein autophosphorylation5
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction5
angiogenesis3
cell migration3
peptidyl-tyrosine phosphorylation3
negative regulation of gene expression3
apoptotic process3
cell differentiation3
positive regulation of cell migration3
negative regulation of apoptotic process3
negative regulation of transcription by RNA polymerase II2
MAPK cascade2

Indications & clinical

Indications

3 indications (0 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
cholangiocarcinoma3MONDO:0019087EFO:0005221
neoplasm1MONDO:0005070EFO:0000616

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

Clinical trials

Total trials: 13.

Phase distribution

PhaseTrials
PHASE1/PHASE24
PHASE24
PHASE32
PHASE12
Not specified1

Top trials by phase / activity

NCTPhaseStatusTitle
NCT05948475PHASE3RECRUITINGStudy of Tinengotinib VS. Physician’s Choice a Treatment of Subjects With FGFR-altered in Cholangiocarcinoma
NCT07328919PHASE3NOT_YET_RECRUITINGEfficacy and Safety of TT-00420 (Tinengotinib) Tablets Versus Chemotherapy in Patients With Advanced Intrahepatic Cholangiocarcinoma Harboring FGFR2 Fusions/Rearrangements or Mutations
NCT06057571PHASE2ACTIVE_NOT_RECRUITINGStudy of TT-00420 (Tinengotinib) in Subjects With Cholangiocarcinoma Who Failed or Relapsed to Chemotherapy and FGFR Inhibitor
NCT06457919PHASE1/PHASE2RECRUITINGA Study of Tinengotinib (TT-00420) in Combination With Standard Treatments in People With Prostate Cancer
NCT07052253PHASE2RECRUITINGA Phase II Clinical Study of AK104/AK112 in Combination With TT-00420 Tablet for Advanced HCC.
NCT07498478PHASE2RECRUITINGEfficacy and Safety of Tinengotinib Tablets Combined With Fulvestrant Injection in Patients With HR Positive and HER-2 Negative Recurrent or Metastatic Breast Cancer Who Have Failed Prior Treatment
NCT04742959PHASE1/PHASE2COMPLETEDStudy of TT-00420 (Tinengotinib) Tablet as Monotherapy and Combination Therapy in Patients With Advanced Solid Tumors
NCT04919642PHASE2COMPLETEDStudy to Evaluate the Efficacy and Safety of TT-00420 (Tinengotinib) in Cholangiocarcinoma
NCT05253053PHASE1/PHASE2COMPLETEDTo Evaluate Efficacy and Safety of TT-00420 (Tinengotinib) as Monotherapy and Combination Therapy in Patients With Advanced Solid Tumors
NCT06221774PHASE1/PHASE2UNKNOWNSafety and Efficacy of TT-00420 Tablets Combined With Toripalimab Injection in Advanced Urological Tumors
NCT03654547PHASE1COMPLETEDSafety of TT-00420 (Tinengotinib) Monotherapy in Patients With Advanced Solid Tumors and Triple Negative Breast Cancer
NCT04705922PHASE1COMPLETEDRelative Bioavailability Study and Food Effect Study of TT-00420 (Tinengotinib) Capsule and Tablet Formulations in Healthy Volunteers
NCT06370013Not specifiedAVAILABLERollover Study to Provide Continued Access to TT-00420 (Tinengotinib) for Subjects With Advanced Solid Tumors

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

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.

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

MoleculeSourceStatusShared targets
CrizotinibChEMBL + PubChemPhase 4 (approved)AURKA, AURKB, FGFR1, FGFR3, FLT1, JAK2, KDR
PAZOPANIBChEMBL + PubChemPhase 4 (approved)AURKA, AURKB, FGFR1, FGFR3, FLT1, JAK2, KDR
AXITINIBChEMBLPhase 4 (approved)AURKA, AURKB, FGFR1, FGFR3, FLT1, JAK2, KDR
DASATINIBChEMBLPhase 4 (approved)AURKA, AURKB, FGFR1, FGFR3, FLT1, JAK2, KDR
ENTRECTINIBChEMBLPhase 4 (approved)AURKA, AURKB, FGFR1, FGFR3, FLT1, JAK2, KDR
FEDRATINIBChEMBLPhase 4 (approved)AURKA, AURKB, FGFR1, FGFR3, FLT1, JAK2, KDR
MIDOSTAURINChEMBLPhase 4 (approved)AURKA, AURKB, FGFR1, FGFR3, FLT1, JAK2, KDR
SUNITINIBChEMBLPhase 4 (approved)AURKA, AURKB, FGFR1, FGFR3, FLT1, JAK2, KDR
LESTAURTINIBChEMBLPhase 3AURKA, AURKB, FGFR1, FGFR3, FLT1, JAK2, KDR
AT-9283ChEMBLPhase 2AURKA, AURKB, FGFR1, FGFR3, FLT1, JAK2, KDR
FORETINIBChEMBLPhase 2AURKA, AURKB, FGFR1, FGFR3, FLT1, JAK2, KDR
ILORASERTIBChEMBLPhase 2AURKA, AURKB, FGFR1, FGFR3, FLT1, JAK2, KDR
R-406ChEMBLPhase 2AURKA, AURKB, FGFR1, FGFR3, FLT1, JAK2, KDR
TOZASERTIBChEMBLPhase 2AURKA, AURKB, FGFR1, FGFR3, FLT1, JAK2, KDR
AfatinibPubChemApprovedAURKA, AURKB, FGFR1, FGFR3, FLT1, JAK2, KDR
SelumetinibPubChemApprovedAURKA, AURKB, FGFR1, FGFR3, FLT1, JAK2, KDR
GefitinibChEMBL + PubChemPhase 4 (approved)AURKB, FGFR1, FGFR3, FLT1, JAK2, KDR
NINTEDANIBChEMBLPhase 4 (approved)AURKB, FGFR1, FGFR3, FLT1, JAK2, KDR
SORAFENIBChEMBLPhase 4 (approved)AURKA, AURKB, FGFR1, FGFR3, FLT1, KDR
ALISERTIBChEMBLPhase 3AURKA, AURKB, FGFR1, FGFR3, FLT1, KDR
DOVITINIBChEMBLPhase 3AURKB, FGFR1, FGFR3, FLT1, JAK2, KDR
LINIFANIBChEMBLPhase 3AURKA, AURKB, FGFR1, FGFR3, FLT1, KDR
CENISERTIBChEMBLPhase 2AURKA, FGFR1, FGFR3, FLT1, JAK2, KDR
MK-2461ChEMBLPhase 2AURKA, FGFR1, FGFR3, FLT1, JAK2, KDR
OSI-632ChEMBLPhase 2AURKA, AURKB, FGFR1, FGFR3, FLT1, KDR
SU-014813ChEMBLPhase 2AURKB, FGFR1, FGFR3, FLT1, JAK2, KDR
IdelalisibPubChemApprovedAURKA, AURKB, FGFR1, FGFR3, FLT1, JAK2
REGORAFENIBChEMBL + PubChemPhase 4 (approved)AURKA, AURKB, FGFR1, FLT1, KDR
BRIGATINIBChEMBLPhase 4 (approved)AURKA, FGFR1, FGFR3, JAK2, KDR
CABOZANTINIBChEMBLPhase 4 (approved)AURKA, AURKB, FGFR1, FLT1, KDR
ERLOTINIBChEMBLPhase 4 (approved)AURKA, AURKB, FLT1, JAK2, KDR
INFIGRATINIBChEMBLPhase 4 (approved)FGFR1, FGFR3, FLT1, JAK2, KDR
LENVATINIBChEMBLPhase 4 (approved)AURKB, FGFR1, FGFR3, FLT1, KDR
PONATINIBChEMBLPhase 4 (approved)FGFR1, FGFR3, FLT1, JAK2, KDR
UPADACITINIBChEMBLPhase 4 (approved)AURKA, AURKB, FGFR1, JAK2, KDR
VANDETANIBChEMBLPhase 4 (approved)AURKB, FGFR1, FGFR3, FLT1, KDR
CEDIRANIBChEMBLPhase 3AURKB, FGFR1, FGFR3, FLT1, KDR
DEFACTINIBChEMBLPhase 3AURKA, AURKB, FLT1, JAK2, KDR
ORANTINIBChEMBLPhase 3AURKA, AURKB, FGFR1, FLT1, KDR
BMS-754807ChEMBLPhase 2AURKA, AURKB, FGFR1, FGFR3, JAK2
CEP-11981ChEMBLPhase 2AURKA, FGFR1, FGFR3, FLT1, KDR
DANUSERTIBChEMBLPhase 2AURKA, AURKB, FGFR1, JAK2, KDR
LUCITANIBChEMBLPhase 2AURKB, FGFR1, FGFR3, FLT1, KDR
REBASTINIBChEMBLPhase 2FGFR1, FGFR3, FLT1, JAK2, KDR
TANDUTINIBChEMBLPhase 2AURKB, FGFR1, FGFR3, FLT1, KDR
belumosudilChEMBL + PubChemPhase 4 (approved)AURKA, AURKB, FGFR1, JAK2
FostamatinibChEMBL + PubChemPhase 4 (approved)AURKA, AURKB, FGFR1, JAK2
NICLOSAMIDEChEMBLPhase 4 (approved)AURKA, FGFR1, JAK2, KDR
NINTEDANIB ESYLATEChEMBLPhase 4 (approved)FGFR1, FGFR3, FLT1, KDR
TIVOZANIBChEMBLPhase 4 (approved)AURKB, FGFR1, FLT1, KDR
BRIVANIBChEMBLPhase 3FGFR1, FGFR3, FLT1, KDR
SEMAXANIBChEMBLPhase 3FGFR1, FGFR3, FLT1, KDR
AZD-1480ChEMBLPhase 2AURKA, AURKB, FGFR1, JAK2
DEFOSBARASERTIBChEMBLPhase 2AURKA, AURKB, FLT1, KDR
ENMD-2076ChEMBLPhase 2AURKA, AURKB, FGFR1, KDR
FEXAGRATINIBChEMBLPhase 2AURKA, FGFR1, FGFR3, KDR
BinimetinibPubChemApprovedAURKA, AURKB, FGFR1, KDR
TrametinibPubChemApprovedAURKA, AURKB, FGFR1, JAK2
CERITINIBChEMBLPhase 4 (approved)FGFR3, JAK2, KDR
ERDAFITINIBChEMBLPhase 4 (approved)FGFR1, FGFR3, KDR

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