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Catequentinib

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Also known as AL 3818Al-3818AL3818Anlotinib

Summary

Catequentinib (CHEMBL4303201) is a phase-3 clinical-stage small molecule targeting FGFR1, FLT1, and KDR; indicated across 61 conditions including non-small cell lung carcinoma and hepatocellular carcinoma.

At a glance

  • Status: Max clinical phase 3 (not approved)
  • Modality: Small molecule
  • Targets: 4 (FGFR1, FLT1, KDR…)
  • Indications: 61 conditions
  • Clinical trials: 292
  • Chemistry: 407.4 Da · C23H22FN3O3

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL4303201
NameCatequentinib
TypeSmall molecule
Max phase3
FDA approvedno
PubChem CID25017411
Molecular formulaC23H22FN3O3
Molecular weight407.4
InChIKeyKSMZEXLVHXZPEF-UHFFFAOYSA-N

SMILES: CC1=CC2=C(N1)C=CC(=C2F)OC3=C4C=C(C(=CC4=NC=C3)OCC5(CC5)N)OC

IUPAC name: 1-[[4-[(4-fluoro-2-methyl-1H-indol-5-yl)oxy]-6-methoxyquinolin-7-yl]oxymethyl]cyclopropan-1-amine

Also known as: AL 3818, Al-3818, AL-3818, AL3818, Anlotinib, Catequentinib, CATEQUENTINIB, ANLOTINIB, anlotinib

Parent form; salt/anhydrous children: CHEMBL5314570, CHEMBL5572229

Patent coverage: 554 distinct patent families (1,292 SureChEMBL compound mentions), from 4 matched compound structure(s). One matched structure accounts for 974 (75%) of the total. 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 1Inhibition7.711.5%P11362
FLT1fms related receptor tyrosine kinase 1Inhibition8.40.1%P17948
KDRkinase insert domain receptorInhibition7.351.1%P35968
FLT4fms related receptor tyrosine kinase 4Inhibition90.2%P35916

Broader ChEMBL bioactivity targets: 2 (assay-derived). Sample: Platelet-derived growth factor receptor beta, Vascular endothelial growth factor receptor 2.

Bioactivity

ChEMBL activities: 2 potent at pChembl ≥ 5 of 2 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
KDR9.7IC500.2nMCHEMBL_ACT_26137483
PDGFRB6.94IC50115nMCHEMBL_ACT_26137484

Target pathways

Aggregated over 4 target gene(s): FGFR1, FLT1, KDR, FLT4.

Top Reactome pathways

30 total, by targets touching each:

PathwayTargetsGenes
VEGF binds to VEGFR leading to receptor dimerization3FLT1, FLT4, KDR
Neuropilin interactions with VEGF and VEGFR2FLT1, KDR
High laminar flow shear stress activates signaling by PIEZO1 and PECAM1:CDH5:KDR in endothelial cells2FLT4, KDR
PI3K Cascade1FGFR1
PIP3 activates AKT signaling1FGFR1
Signaling by FGFR1 amplification mutants1FGFR1
Signaling by activated point mutants of FGFR11FGFR1
FGFR1b ligand binding and activation1FGFR1
FGFR1c ligand binding and activation1FGFR1
FGFR1c and Klotho ligand binding and activation1FGFR1
Integrin cell surface interactions1KDR
Constitutive Signaling by Aberrant PI3K in Cancer1FGFR1
NCAM signaling for neurite out-growth1FGFR1
VEGFA-VEGFR2 Pathway1KDR
Signal transduction by L11FGFR1
VEGFR2 mediated cell proliferation1KDR
Phospholipase C-mediated cascade: FGFR11FGFR1
Downstream signaling of activated FGFR11FGFR1
SHC-mediated cascade:FGFR11FGFR1
PI-3K cascade:FGFR11FGFR1
FRS-mediated FGFR1 signaling1FGFR1
Negative regulation of FGFR1 signaling1FGFR1
Signaling by FGFR1 in disease1FGFR1
RAF/MAP kinase cascade1FGFR1
PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling1FGFR1
Signaling by plasma membrane FGFR1 fusions1FGFR1
NOTCH4 Intracellular Domain Regulates Transcription1FLT4
Signaling by membrane-tethered fusions of PDGFRA or PDGFRB1KDR
Epithelial-Mesenchymal Transition (EMT) during gastrulation1FGFR1
Formation of paraxial mesoderm1FGFR1

Dominant GO biological processes

GO termTargets
angiogenesis4
protein phosphorylation4
positive regulation of cell population proliferation4
cell migration4
peptidyl-tyrosine phosphorylation4
positive regulation of MAPK cascade4
protein autophosphorylation4
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction3
blood vessel morphogenesis3
cell surface receptor protein tyrosine kinase signaling pathway3
positive regulation of cell migration3
cellular response to vascular endothelial growth factor stimulus3
vascular endothelial growth factor receptor signaling pathway3
vascular endothelial growth factor signaling pathway3
positive regulation of mesenchymal cell proliferation2

Indications & clinical

Indications

61 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
non-small cell lung carcinoma3MONDO:0005233EFO:0003060
hepatocellular carcinoma3MONDO:0007256EFO:0000182
small cell lung carcinoma3MONDO:0008433EFO:0000702
soft tissue sarcoma3MONDO:0018078EFO:1001968
sarcoma3MONDO:0005089EFO:0000691
leiomyosarcoma3MONDO:0005058EFO:0000564
synovial sarcoma3MONDO:0010434EFO:0001376
alveolar soft part sarcoma3MONDO:0011655EFO:0007143
ovarian cancer3MONDO:0008170MONDO:0008170
lung neoplasm3MONDO:0021117MONDO:0008903
kidney cancer3MONDO:0002367MONDO:0002367
lung carcinoma3MONDO:0005138EFO:0001071
renal cell carcinoma2MONDO:0005086EFO:0000681
neoplasm2MONDO:0005070EFO:0000616
esophageal squamous cell carcinoma2MONDO:0005580EFO:0005922
glioblastoma2MONDO:0018177EFO:0000519
lymphoma2MONDO:0005062EFO:0000574
bone neoplasm2MONDO:0019060EFO:0003820
breast neoplasm2MONDO:0021100EFO:0003869
nasopharyngeal neoplasm2MONDO:0005375EFO:0004252
rectal cancer2MONDO:0006519EFO:1000657
undifferentiated pleomorphic sarcoma2MONDO:0002142EFO:1001972
gastric neoplasm2MONDO:0021085MONDO:0001056
endometrium neoplasm2MONDO:0021251MONDO:0011962
carcinoid tumor2MONDO:0005369MONDO:0024503
squamous cell carcinoma2MONDO:0005096EFO:0000707
exocrine pancreatic carcinoma2MONDO:0005192EFO:0002618
glioma2MONDO:0021042MONDO:0100342
diffuse large B-cell lymphoma2MONDO:0018905EFO:0000403
neuroblastoma2MONDO:0005072EFO:0000621
triple-negative breast carcinoma2MONDO:0005494EFO:0005537
brainstem cancer2MONDO:0002912MONDO:0002912
head and neck squamous cell carcinoma2MONDO:0010150EFO:0000181
carcinoma2MONDO:0004993EFO:0000313
mesothelioma2MONDO:0005065EFO:0000588
melanoma2MONDO:0005105EFO:0000756
essential tremor2MONDO:0003233EFO:0003108
pancreatic neoplasm2MONDO:0021040EFO:0003860
endometrial carcinoma2MONDO:0002447EFO:1001512
gastrointestinal stromal tumor2MONDO:0011719MONDO:0011719
lung disorder2MONDO:0005275EFO:0003818
malignant pancreatic neoplasm2MONDO:0009831EFO:1000359
adrenal gland pheochromocytoma2MONDO:0004974EFO:0000239
clear cell renal carcinoma2MONDO:0005005EFO:0000349
lung adenocarcinoma2MONDO:0005061EFO:0000571
thyroid gland carcinoma2MONDO:0015075EFO:0002892
colorectal neoplasm2MONDO:0005335MONDO:0005575
nasopharyngeal carcinoma2MONDO:0015459MONDO:0015459
Ewing sarcoma1MONDO:0012817EFO:0000174
cholangiocarcinoma1MONDO:0019087EFO:0005221
plasma cell myeloma1MONDO:0009693EFO:0001378
liver disorder1MONDO:0005154HP:0001410

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

Clinical trials

Total trials: 292.

Phase distribution

PhaseTrials
PHASE2176
PHASE1/PHASE229
Not specified26
PHASE323
PHASE116
PHASE2/PHASE313
PHASE49

Top trials by phase / activity

NCTPhaseStatusTitle
NCT05830500PHASE4RECRUITINGStudy of Anlotinib in Patients With Advanced Medullary Thyroid Carcinoma
NCT06356675PHASE4NOT_YET_RECRUITINGA Single-arm Pilot Study of Tislelizumab Combined With Anlotinib in Patients With Advanced NSCLC With Driver-negative After Progression to Immunotherapy
NCT06506838PHASE4RECRUITINGAnlotinib Combined With Doxorubicin and Radiotherapy as Neoadjuvant Treatment for Soft Tissue Sarcoma
NCT06931145PHASE4NOT_YET_RECRUITINGBenmelstobart, Anlotinib and Chemotherapy as First-line Treatment for Extensive-stage Small-cell Lung Cancer
NCT06951841PHASE4NOT_YET_RECRUITINGProspective, Single-arm, Phase II Clinical Study of Irinotecan Hydrochloride Liposome Injection Combined With Platinum and Immune Checkpoint Inhibitors Combined With Anlotinib for the Maintenance of Extensive Small Cell Lung Cancer After First-line Induction
NCT07010393PHASE4NOT_YET_RECRUITINGGenotype-Driven Neoadjuvant Therapy for Locally Advanced Thyroid Cancer: A Real-World Cohort Study
NCT07358520PHASE4NOT_YET_RECRUITINGClinical Study on the Use of Huaier Granules for the Treatment of Proteinuria Related to Bevacizumab and Anlotinib in Lung Cancer Patients
NCT03755869PHASE4UNKNOWNStudy of Anlotinib in Non-squamous NSCLC Patients Who Failed First-Line（ALTER-L020）
NCT03799601PHASE4UNKNOWNDocetaxel Combined With Carboplatin Plus Anlotinib as First Line Treatment in NSCLC
NCT03016819PHASE3RECRUITINGPhase III Trial of Anlotinib, Catequentinib in Advanced Alveolar Soft Part Sarcoma, Leiomyosarcoma, Synovial Sarcoma (APROMISS)
NCT04322617PHASE2/PHASE3RECRUITINGAnlotinib Plus Immune Checkpoint Inhibitors for Lung Cancer
NCT04523272PHASE3ACTIVE_NOT_RECRUITINGA Study of TQB2450 Injection Combined With Anlotinib Hydrochloride Capsule Versus Sunitinib in Subjects With Advanced Renal Cancer
NCT04854668PHASE3ACTIVE_NOT_RECRUITINGA Study of Anlotinib Hydrochloride Capsule Combined With Chemotherapy as First-line Treatment in Subjects With RAS/BRAF Wild Metastatic Colorectal Cancer
NCT05828953PHASE2/PHASE3RECRUITINGAnlotinib Capsules in the Treatment for IPF/PF-ILDs
NCT05862337PHASE3RECRUITINGAnlotinib Hydrochloride Capsules Combined With Penpulimab Injection for the Treatment of Hepatocellular Carcinoma at High Risk of Recurrence.
NCT06048315PHASE3NOT_YET_RECRUITINGA Single Center, Single Arm Clinical Study on the Treatment of Advanced Non-small Cell Lung Cancer With Positive EGFR Sensitive Mutations and Failed EGFR TKIs With the Combination of Enrotinib and Paclitaxel Monoclonal Antibody
NCT06354530PHASE2/PHASE3RECRUITINGA Study of Neoadjuvant Therapy for the Treatment of Patients With Locally Advanced Esophageal Squamous Cell Carcinoma
NCT06469879PHASE3NOT_YET_RECRUITINGA Clinical Study of TQB2450 Combined With Anlotinib in Limited-Stage Small Cell Lung Cancer Patients
NCT06475599PHASE3NOT_YET_RECRUITINGAnlotinib Hydrochloride Capsules Combined With TQB2450 in the Treatment of Endometrial Cancer
NCT06662877PHASE2/PHASE3NOT_YET_RECRUITINGAnlotinib Plus Nab-Paclitaxels and S-1 for Patients with Advanced Biliary Tract Cancer As Second-Line Treatment
NCT07443397PHASE3RECRUITINGAnlotinib Plus Whole-Brain Radiotherapy for Brain Metastases in SCLC Patients.
NCT07540390PHASE3NOT_YET_RECRUITINGGAPP Induction and Concurrent Chemoradiotherapy for High-risk Locoregionally Advanced NPC.
NCT02029209PHASE2/PHASE3UNKNOWNTo Predict Efficacy by Detecting Circulating Endothelial Cell Subsets and Blood Perfusion Parameters Changes in Vivo Tumor in the Phase II/III Study of Anlotinib in Patients With Advanced Non-small Cell Lung Cancer
NCT02332499PHASE2/PHASE3COMPLETEDStudy of Anlotinib in Patients With Metastatic Colorectal Cancer（mCRC）(ALTER0703)
NCT02388919PHASE2/PHASE3COMPLETEDStudy of Anlotinib in Patients With Advanced Non-small Cell Lung Cancer（ALTER0303）
NCT02449343PHASE2/PHASE3UNKNOWNStudy of Anlotinib in Patients With Soft Tissue Sarcoma（STS）(ALTER0203)
NCT02461407PHASE2/PHASE3UNKNOWNStudy of Anlotinib in Patients With Gastric Cancer(ALTER0503)
NCT02584478PHASE3UNKNOWNPhase 1/2a/3 Evaluation of Adding AL3818 to Standard Platinum-Based Chemotherapy in Subjects With Recurrent or Metastatic Endometrial, Ovarian, Fallopian, Primary Peritoneal or Cervical Carcinoma (AL3818-US-002)
NCT02586337PHASE2/PHASE3UNKNOWNStudy of Anlotinib in Patients With Differentiated Thyroid Cancer(ALTER01032)
NCT02586350PHASE2/PHASE3COMPLETEDStudy of Anlotinib in Patients With Medullary Thyroid Carcinoma(ALTER01031)
NCT03866980PHASE3TERMINATEDA Study of Anti-PD-1 AK105 in Patients With Metastatic Nonsquamous Non-small Cell Lung Cancer
NCT03975036PHASE2/PHASE3UNKNOWNClinical Study on the Second-line and Above Treatment of Advanced Solid Tumor With Anlotinib Combined With Pd-1 Antibody
NCT04073537PHASE3UNKNOWNStudy of Anlotinib Hydrochloride Capsule Combined With Chemotherapy in Subjects With Squamous Non-small Cell Lung Cancer
NCT04073550PHASE3UNKNOWNStudy of Anlotinib Hydrochloride Capsule in Subjects With Small Cell Lung Cancer
NCT04234607PHASE3UNKNOWNA Study of TQB2450 or Placebo Combined With Anlotinib, Etoposide and Carboplatin Versus Etoposide and Carboplatin in Subjects With Extensive Small Cell Lung Cancer (ETER701)
NCT04325763PHASE3UNKNOWNA Study of TQB2450 in Subjects With Stage III Non-Small Cell Lung Cancer(NSCLC)
NCT04385550PHASE3UNKNOWNA Study of Anlotinib Hydrochloride Capsule Combined With AK105 Injection in Subject With Advanced Gastric and Gastro-oesophageal Junction Adenocarcinoma
NCT04405505PHASE3UNKNOWNA Study of TQB2450 Injection Combined With Anlotinib Hydrochloride Capsule Versus Paclitaxel for Injection (Albumin Bound) in Subjects With Triple Negative Breast Cancer (TNBC)
NCT04439890PHASE3UNKNOWNA Efficacy and Safety Study of Anlotinib Hydrochloride Capsule Combined With Chemotherapy Versus Placebo Combined With Chemotherapy as First-line Treatment in Subjects With Advanced Non-squamous Cell Non-small Cell Lung Cancer
NCT04665609PHASE3UNKNOWNThermal Ablation Combined With Anlotinib and TQB2450 Solution for HCC

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 0 clinical and 4 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

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.

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

MoleculeSourceStatusShared targets
CrizotinibChEMBL + PubChemPhase 4 (approved)FGFR1, FLT1, FLT4, KDR
GefitinibChEMBL + PubChemPhase 4 (approved)FGFR1, FLT1, FLT4, KDR
PAZOPANIBChEMBL + PubChemPhase 4 (approved)FGFR1, FLT1, FLT4, KDR
REGORAFENIBChEMBL + PubChemPhase 4 (approved)FGFR1, FLT1, FLT4, KDR
AXITINIBChEMBLPhase 4 (approved)FGFR1, FLT1, FLT4, KDR
CABOZANTINIBChEMBLPhase 4 (approved)FGFR1, FLT1, FLT4, KDR
ENTRECTINIBChEMBLPhase 4 (approved)FGFR1, FLT1, FLT4, KDR
FEDRATINIBChEMBLPhase 4 (approved)FGFR1, FLT1, FLT4, KDR
INFIGRATINIBChEMBLPhase 4 (approved)FGFR1, FLT1, FLT4, KDR
LENVATINIBChEMBLPhase 4 (approved)FGFR1, FLT1, FLT4, KDR
MIDOSTAURINChEMBLPhase 4 (approved)FGFR1, FLT1, FLT4, KDR
NINTEDANIBChEMBLPhase 4 (approved)FGFR1, FLT1, FLT4, KDR
NINTEDANIB ESYLATEChEMBLPhase 4 (approved)FGFR1, FLT1, FLT4, KDR
SORAFENIBChEMBLPhase 4 (approved)FGFR1, FLT1, FLT4, KDR
SUNITINIBChEMBLPhase 4 (approved)FGFR1, FLT1, FLT4, KDR
TIVOZANIBChEMBLPhase 4 (approved)FGFR1, FLT1, FLT4, KDR
VANDETANIBChEMBLPhase 4 (approved)FGFR1, FLT1, FLT4, KDR
BRIVANIBChEMBLPhase 3FGFR1, FLT1, FLT4, KDR
CEDIRANIBChEMBLPhase 3FGFR1, FLT1, FLT4, KDR
DOVITINIBChEMBLPhase 3FGFR1, FLT1, FLT4, KDR
LESTAURTINIBChEMBLPhase 3FGFR1, FLT1, FLT4, KDR
LINIFANIBChEMBLPhase 3FGFR1, FLT1, FLT4, KDR
MOTESANIBChEMBLPhase 3FGFR1, FLT1, FLT4, KDR
SEMAXANIBChEMBLPhase 3FGFR1, FLT1, FLT4, KDR
SURUFATINIBChEMBLPhase 3FGFR1, FLT1, FLT4, KDR
AT-9283ChEMBLPhase 2FGFR1, FLT1, FLT4, KDR
CENISERTIBChEMBLPhase 2FGFR1, FLT1, FLT4, KDR
DORAMAPIMODChEMBLPhase 2FGFR1, FLT1, FLT4, KDR
FORETINIBChEMBLPhase 2FGFR1, FLT1, FLT4, KDR
ILORASERTIBChEMBLPhase 2FGFR1, FLT1, FLT4, KDR
LUCITANIBChEMBLPhase 2FGFR1, FLT1, FLT4, KDR
MK-2461ChEMBLPhase 2FGFR1, FLT1, FLT4, KDR
OSI-632ChEMBLPhase 2FGFR1, FLT1, FLT4, KDR
R-406ChEMBLPhase 2FGFR1, FLT1, FLT4, KDR
RAF-265ChEMBLPhase 2FGFR1, FLT1, FLT4, KDR
REBASTINIBChEMBLPhase 2FGFR1, FLT1, FLT4, KDR
SU-014813ChEMBLPhase 2FGFR1, FLT1, FLT4, KDR
TANDUTINIBChEMBLPhase 2FGFR1, FLT1, FLT4, KDR
TOZASERTIBChEMBLPhase 2FGFR1, FLT1, FLT4, KDR
AfatinibPubChemApprovedFGFR1, FLT1, FLT4, KDR
SelumetinibPubChemApprovedFGFR1, FLT1, FLT4, KDR
BRIGATINIBChEMBLPhase 4 (approved)FGFR1, FLT4, KDR
DASATINIBChEMBLPhase 4 (approved)FGFR1, FLT1, KDR
ERLOTINIBChEMBLPhase 4 (approved)FLT1, FLT4, KDR
FRUQUINTINIBChEMBLPhase 4 (approved)FLT1, FLT4, KDR
PONATINIBChEMBLPhase 4 (approved)FGFR1, FLT1, KDR
QUIZARTINIBChEMBLPhase 4 (approved)FLT1, FLT4, KDR
ALISERTIBChEMBLPhase 3FGFR1, FLT1, KDR
CEP-1347ChEMBLPhase 3FLT1, FLT4, KDR
ORANTINIBChEMBLPhase 3FGFR1, FLT1, KDR
VATALANIBChEMBLPhase 3FLT1, FLT4, KDR
BFH-772ChEMBLPhase 2FLT1, FLT4, KDR
CEP-11981ChEMBLPhase 2FGFR1, FLT1, KDR
DANUSERTIBChEMBLPhase 2FGFR1, FLT4, KDR
DEFOSBARASERTIBChEMBLPhase 2FLT1, FLT4, KDR
IdelalisibPubChemApprovedFGFR1, FLT1, FLT4
ERDAFITINIBChEMBLPhase 4 (approved)FGFR1, KDR
FILGOTINIBChEMBLPhase 4 (approved)FLT1, FLT4
FUTIBATINIBChEMBLPhase 4 (approved)FGFR1, KDR
NICLOSAMIDEChEMBLPhase 4 (approved)FGFR1, 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
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Sources 30

This page pulls from 30 datasets indexed by BioBTree:

chebichembl_activitychembl_moleculechembl_targetcivic_evidenceclingen_dosageclinical_trialsdepmapefoensemblentrezgogoparentgtopdbgtopdb_interactiongtopdb_ligandhgncmeshmondomsigdbpatent_compoundpharmgkbpharmgkb_guidelinepubchempubchem_activityreactomereactomeparentrefseqtranscriptuniprot