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Surufatinib

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Also known as Hmpl-012SulfatinibSurufatinib

Summary

Surufatinib (CHEMBL4297190) is a phase-3 clinical-stage small molecule (ATC L01EX24) targeting FGFR1 and KDR; indicated across 28 conditions including neoplasm and neuroendocrine neoplasm.

At a glance

  • Status: Max clinical phase 3 (not approved)
  • Modality: Small molecule
  • ATC class: L01EX24
  • Targets: 2 (FGFR1, KDR)
  • Indications: 28 conditions
  • Clinical trials: 82
  • Chemistry: 480.6 Da · C24H28N6O3S

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL4297190
NameSurufatinib
TypeSmall molecule
Max phase3
FDA approvedno
PubChem CID52920501
ATCL01EX24
Molecular formulaC24H28N6O3S
Molecular weight480.6
InChIKeyTTZSNFLLYPYKIL-UHFFFAOYSA-N

SMILES: CC1=CC2=C(N1)C=CC(=C2)OC3=NC(=NC=C3)NC4=CC=CC(=C4)CS(=O)(=O)NCCN(C)C

IUPAC name: N-[2-(dimethylamino)ethyl]-1-[3-[[4-[(2-methyl-1H-indol-5-yl)oxy]pyrimidin-2-yl]amino]phenyl]methanesulfonamide

Also known as: Hmpl-012, HMPL-012, Sulfatinib, Surufatinib, SURUFATINIB, SULFATINIB, Sulfatinib; Surufatinib

Patent coverage: 250 distinct patent families (654 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 615 (94%) 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 1Inhibition7.2811.5%P11362
KDRkinase insert domain receptorInhibition7.681.1%P35968

Broader ChEMBL bioactivity targets: 8 (assay-derived). Sample: Vascular endothelial growth factor receptor 1, Vascular endothelial growth factor receptor 3, Receptor-type tyrosine-protein kinase FLT3, Vascular endothelial growth factor receptor 2, Fibroblast growth factor receptor 1, BDNF/NT-3 growth factors receptor, Tyrosine-protein kinase Mer, Macrophage colony-stimulating factor 1 receptor.

Bioactivity

ChEMBL activities: 14 potent at pChembl ≥ 5 of 14 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
FLT19IC501nMCHEMBL_ACT_26132410
KDR9IC501nMCHEMBL_ACT_26132412
FLT49IC501nMCHEMBL_ACT_26132413
FLT49IC501nMCHEMBL_ACT_26187719
FLT18.7IC502nMCHEMBL_ACT_26187716
MERTK8.4IC504nMCHEMBL_ACT_26132409
FGFR17.82IC5015nMCHEMBL_ACT_26132415
FGFR17.82IC5015nMCHEMBL_ACT_26187720
KDR7.62IC5024nMCHEMBL_ACT_26187717
NTRK27.39IC5041nMCHEMBL_ACT_26132416
NTRK27.39IC5041nMCHEMBL_ACT_26187721
FLT37.17IC5067nMCHEMBL_ACT_26132414
FLT37.17IC5067nMCHEMBL_ACT_26187722
P095817.1IC5079nMCHEMBL_ACT_26132417

Target pathways

Aggregated over 2 target gene(s): FGFR1, KDR.

Top Reactome pathways

29 total, by targets touching each:

PathwayTargetsGenes
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
Neuropilin interactions with VEGF and VEGFR1KDR
VEGF binds to VEGFR leading to receptor dimerization1KDR
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
Signaling by membrane-tethered fusions of PDGFRA or PDGFRB1KDR
Epithelial-Mesenchymal Transition (EMT) during gastrulation1FGFR1
Formation of paraxial mesoderm1FGFR1
High laminar flow shear stress activates signaling by PIEZO1 and PECAM1:CDH5:KDR in endothelial cells1KDR

Dominant GO biological processes

GO termTargets
angiogenesis2
positive regulation of mesenchymal cell proliferation2
protein phosphorylation2
positive regulation of cell population proliferation2
mesenchymal cell proliferation2
cell migration2
peptidyl-tyrosine phosphorylation2
positive regulation of MAPK cascade2
positive regulation of blood vessel endothelial cell migration2
protein autophosphorylation2
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction2
calcium ion homeostasis2
stem cell proliferation2
positive regulation of stem cell proliferation2
positive regulation of endothelial cell chemotaxis2

Indications & clinical

Indications

28 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
neoplasm3MONDO:0005070EFO:0000616
neuroendocrine neoplasm3MONDO:0019496EFO:1001901
neuroendocrine carcinoma3MONDO:0002120MONDO:0002120
pancreatic neuroendocrine tumor3MONDO:0019954EFO:1000045
thyroid gland carcinoma2MONDO:0015075EFO:0002892
non-small cell lung carcinoma2MONDO:0005233EFO:0003060
head and neck cancer2MONDO:0005627EFO:0006859
hepatocellular carcinoma2MONDO:0007256EFO:0000182
gastric adenocarcinoma2MONDO:0005036EFO:0000503
sarcoma2MONDO:0005089EFO:0000691
small cell lung carcinoma2MONDO:0008433EFO:0000702
exocrine pancreatic carcinoma2MONDO:0005192EFO:0002618
pancreatic neoplasm2MONDO:0021040EFO:0003860
colorectal neoplasm2MONDO:0005335EFO:0004142
breast neoplasm2MONDO:0021100MONDO:0007254
osteosarcoma2MONDO:0009807EFO:0000637
soft tissue sarcoma2MONDO:0018078EFO:1001968
carcinoma2MONDO:0004993EFO:0000313
malignant pancreatic neoplasm2MONDO:0009831EFO:1000359
intrahepatic cholangiocarcinoma2MONDO:0003210EFO:1001961
nasopharyngeal carcinoma2MONDO:0015459MONDO:0015459
liver disorder1MONDO:0005154EFO:0001421
kidney disorder1MONDO:0005240EFO:0003086
triple-negative breast carcinoma1MONDO:0005494EFO:0005537
pancreatic ductal adenocarcinoma1MONDO:0005184MONDO:0005184

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

Clinical trials

Total trials: 82.

Phase distribution

PhaseTrials
PHASE248
PHASE1/PHASE214
PHASE18
Not specified7
PHASE33
PHASE41
PHASE2/PHASE31

Top trials by phase / activity

NCTPhaseStatusTitle
NCT07272512PHASE4RECRUITINGProspective Multicenter Real-world Study of Surufatinib in Patients With Advanced Neuroendocrine Neoplasms
NCT07436741PHASE3NOT_YET_RECRUITINGSurufatinib Plus Gemcitabine and Nab-paclitaxel vs. Gemcitabine Plus Nab-paclitaxel in Neoadjuvant Therapy for High - Risk Resectable or Borderline Resectable Pancreatic Cancer
NCT02588170PHASE3COMPLETEDPhase III Study of Surufatinib in Treating Advanced Extrapancreatic Neuroendocrine Tumors
NCT02589821PHASE3COMPLETEDPhase III Study of Surufatinib in Treating Advanced Pancreatic Neuroendocrine Tumors
NCT03873532PHASE2/PHASE3UNKNOWNA Trial Evaluating Surufatinib Efficacy and Safety in Biliary Tract Carcinoma Patients
NCT05165407PHASE2RECRUITINGSintilimab Combined With IBI310 and Surufatinib for the Treatment of G3-NET and NEC (NESSIE)
NCT05218889PHASE1/PHASE2RECRUITINGSurufatinib Plus Camrelizumab and AS in First Line Treatment of Advanced Metastatic Pancreatic Cancer
NCT05472948PHASE2RECRUITINGSurufatinib and Sintilimab in Combination With Capecitabine for Metastatic Adenocarcinoma of Small Intestine or Appendix Carcinoma
NCT05481476PHASE2ACTIVE_NOT_RECRUITINGSurufatinib Combined With Sintilimab and AG in First-line Therapy of Patients With Locally Advanced or Metastatic Pancreatic Cancer
NCT05590572PHASE1/PHASE2NOT_YET_RECRUITINGA Study of Sulfatinib on Relapsed or Refractory Drug Resistant Osteosarcoma
NCT05652283PHASE2ACTIVE_NOT_RECRUITINGPamiparib Combined With Surufatinib for the Neoadjuvant Treatment of Unresectable Ovarian Cancer
NCT05722977PHASE2NOT_YET_RECRUITINGSurufatinib and Envafolimab as Second or More-line Therapy in Advanced Soft Tissue Sarcoma Patients
NCT05839275PHASE1/PHASE2RECRUITINGThe Combination of Radiotherapy，Surufatinib and Sintilimab in High-Risk Localized Soft Tissue Sarcoma
NCT05882630PHASE1/PHASE2NOT_YET_RECRUITINGSurufatinib Combined With Serplulimab Plus Chemotherapy in the Treatment of Extensive-stage Small Cell Lung Cancer
NCT05908747PHASE2ACTIVE_NOT_RECRUITINGEfficacy and Safety of Surufatinib Combined With Gemcitabine and Albumin-bound Paclitaxel in the Peri-operative Treatment of Pancreatic Cancer
NCT05969171PHASE2RECRUITINGA Single-center, Prospective, Two Cohort Study of Surufatinib Combined With AG or AG in the First-line Treatment of Locally Advanced or Metastatic Pancreatic Cancer
NCT05988372PHASE2NOT_YET_RECRUITINGSurufatinib and Serplulimab Combined With AG Regimen Compare With AG Regimen as Conversion Therapy for Patients With Locally Advanced Pancreatic Cancer (SAGE)
NCT05989425PHASE2RECRUITINGSurufatinib as Neoadjuvant Treatment for Locally Advanced or Metastatic Differentiated Thyroid Cancer
NCT06062485PHASE2NOT_YET_RECRUITINGSurufatinib Combined With Toripalimab and AG Regiments for First-line Treatment of Unresectable or Relapsing Metastatic Ampullary Carcinoma
NCT06158516PHASE2NOT_YET_RECRUITINGA Study of Surufatinib as Adjuvant Therapy for Pancreatic Neuroendocrine Tumors
NCT06239532PHASE2ACTIVE_NOT_RECRUITINGHAIC Sequential TAE Combined With Tislelizumab and Surufatinib in Unresectable Intrahepatic Cholangiocarcinoma
NCT06329947PHASE2NOT_YET_RECRUITINGA Phase II Study of Surufatinib Combined With Camrelizumab and mFOLFOX6 as Second-line Treatment for Advanced PRAD
NCT06414915PHASE2NOT_YET_RECRUITINGSurufatinib Combined With Tislelizumab in Advanced Lung Cancer With Neuroendocrine Differentiation
NCT06447636PHASE2NOT_YET_RECRUITINGPerioperative Surufatinib Plus Sintilimab Combined With Chemotherapy in Gastric/Gastroesophageal Junction Adenocarcinoma
NCT06531291PHASE2NOT_YET_RECRUITINGSurufatinib Combined With Serplulimab and Standard Chemotherapy as First-line Treatment in Advanced Solid Tumors With Neuroendocrine Differentiation
NCT06654947PHASE2NOT_YET_RECRUITINGA Single-arm, Open-label, Prospective Clinical Study of Surufatinib Combined With Immunotherapy and Chemotherapy for Unresectable or Metastatic Biliary Tract Cancer.
NCT06656559PHASE2NOT_YET_RECRUITINGEndoscopic Retrograde Cholangiopancreatography With Radiofrequency Ablation (ERCP-RFA) Combined With Envafolimab and Surufatinib Sequential Therapy for Unresectable Biliary Tract Carcinoma
NCT06708858PHASE2RECRUITINGPhase Ⅱ Clinical Study of Surufatinib Combined With Gemcitabine and Cisplatin Plus Durvalumab/Pembrolizumab Regimen in the Treatment of Advanced Biliary Tract Cancer
NCT06719700PHASE2RECRUITINGConcurrent Chemoradiotherapy Combined With Toripalimab and Surufatinib in the Treatment of Limited-Stage Small Cell Lung Cancer
NCT07086456PHASE2RECRUITINGCombination of Concurrent Chemoradiotherapy With Surufatinib and Tislelizumab in Patients With Locally Advanced Non-Small Cell Lung Cancer
NCT07086469PHASE2RECRUITINGSurufatinib in Combination With Neoadjuvant Chemo-immunotherapy and Concurrent Chemoradiotherapy for Patients With Unresectable Locally Advanced Esophageal Squamous Cell Carcinoma
NCT07156019PHASE2NOT_YET_RECRUITINGSintilimab in Combination With Surufatinib and Temozolomide in the Advanced Neuroendocrine Carcinoma
NCT07279532PHASE2NOT_YET_RECRUITINGClinical Study of Adjuvant Surufatinib Therapy for Postoperative High-risk Neuroendocrine Tumors Based on the Ninth Edition of the AJCC Staging System
NCT07357623PHASE2RECRUITINGSurufatinib Combined With Chemo Versus Surufatinib in the Treatment of Pulmonary Neuroendocrine Tumors
NCT07469956PHASE2NOT_YET_RECRUITINGSurufatinib Plus mFOLFIRINOX and PD-1 Inhibitor as the Neoadjuvant Therapy for High-risk or Borderline Resectable Pancreatic Cancer
NCT07609121PHASE2NOT_YET_RECRUITINGHypofractionated Chemoradiotherapy With Tislelizumab and Surufatinib for Unresectable Stage III NSCLC
NCT02549937PHASE1/PHASE2COMPLETEDA Multi-Center, Open-Label Study of Surufatinib (HMPL-012) in Patients With Advanced Solid Tumors
NCT02614495PHASE2COMPLETEDStudy of Sulfatinib in Treating Advanced Medullary Thyroid Carcinoma and Iodine-refractory Differentiated Thyroid Carcinoma
NCT02966821PHASE2COMPLETEDStudy of Surufatinib as Second-line Treatment in Patients With Biliary Tract Carcinoma
NCT04169672PHASE2COMPLETEDStudy of Surufatinib Single Agent or Surufatinib Combined With Toripalimab in Patients 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.

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

MoleculeSourceStatusShared targets
CrizotinibChEMBL + PubChemPhase 4 (approved)FGFR1, KDR
GefitinibChEMBL + PubChemPhase 4 (approved)FGFR1, KDR
PAZOPANIBChEMBL + PubChemPhase 4 (approved)FGFR1, KDR
REGORAFENIBChEMBL + PubChemPhase 4 (approved)FGFR1, KDR
AXITINIBChEMBLPhase 4 (approved)FGFR1, KDR
BRIGATINIBChEMBLPhase 4 (approved)FGFR1, KDR
CABOZANTINIBChEMBLPhase 4 (approved)FGFR1, KDR
DASATINIBChEMBLPhase 4 (approved)FGFR1, KDR
ENTRECTINIBChEMBLPhase 4 (approved)FGFR1, KDR
ERDAFITINIBChEMBLPhase 4 (approved)FGFR1, KDR
FEDRATINIBChEMBLPhase 4 (approved)FGFR1, KDR
FUTIBATINIBChEMBLPhase 4 (approved)FGFR1, KDR
INFIGRATINIBChEMBLPhase 4 (approved)FGFR1, KDR
LENVATINIBChEMBLPhase 4 (approved)FGFR1, KDR
MIDOSTAURINChEMBLPhase 4 (approved)FGFR1, KDR
NICLOSAMIDEChEMBLPhase 4 (approved)FGFR1, KDR
NINTEDANIBChEMBLPhase 4 (approved)FGFR1, KDR
NINTEDANIB ESYLATEChEMBLPhase 4 (approved)FGFR1, KDR
PONATINIBChEMBLPhase 4 (approved)FGFR1, KDR
SORAFENIBChEMBLPhase 4 (approved)FGFR1, KDR
SUNITINIBChEMBLPhase 4 (approved)FGFR1, KDR
TIVOZANIBChEMBLPhase 4 (approved)FGFR1, KDR
UPADACITINIBChEMBLPhase 4 (approved)FGFR1, KDR
VANDETANIBChEMBLPhase 4 (approved)FGFR1, KDR
ALISERTIBChEMBLPhase 3FGFR1, KDR
BRIVANIBChEMBLPhase 3FGFR1, KDR
CEDIRANIBChEMBLPhase 3FGFR1, KDR
DOVITINIBChEMBLPhase 3FGFR1, KDR
LESTAURTINIBChEMBLPhase 3FGFR1, KDR
LINIFANIBChEMBLPhase 3FGFR1, KDR
MOTESANIBChEMBLPhase 3FGFR1, KDR
ORANTINIBChEMBLPhase 3FGFR1, KDR
SEMAXANIBChEMBLPhase 3FGFR1, KDR
AG-13958ChEMBLPhase 2FGFR1, KDR
AT-9283ChEMBLPhase 2FGFR1, KDR
CENISERTIBChEMBLPhase 2FGFR1, KDR
CEP-11981ChEMBLPhase 2FGFR1, KDR
DANUSERTIBChEMBLPhase 2FGFR1, KDR
DORAMAPIMODChEMBLPhase 2FGFR1, KDR
ENMD-2076ChEMBLPhase 2FGFR1, KDR
FEXAGRATINIBChEMBLPhase 2FGFR1, KDR
FGFR INHIBITOR DEBIO 1347ChEMBLPhase 2FGFR1, KDR
FORETINIBChEMBLPhase 2FGFR1, KDR
ILORASERTIBChEMBLPhase 2FGFR1, KDR
LUCITANIBChEMBLPhase 2FGFR1, KDR
MK-2461ChEMBLPhase 2FGFR1, KDR
OSI-632ChEMBLPhase 2FGFR1, KDR
R-406ChEMBLPhase 2FGFR1, KDR
RAF-265ChEMBLPhase 2FGFR1, KDR
REBASTINIBChEMBLPhase 2FGFR1, KDR
RX-518ChEMBLPhase 2FGFR1, KDR
SU-014813ChEMBLPhase 2FGFR1, KDR
TANDUTINIBChEMBLPhase 2FGFR1, KDR
TOCERANIBChEMBLPhase 2FGFR1, KDR
TOZASERTIBChEMBLPhase 2FGFR1, KDR
AfatinibPubChemApprovedFGFR1, KDR
BinimetinibPubChemApprovedFGFR1, KDR
SelumetinibPubChemApprovedFGFR1, KDR
GENTIAN VIOLETChEMBL + PubChemPhase 4 (approved)KDR
ABEMACICLIBChEMBLPhase 4 (approved)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
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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