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Details

Stereochemistry ACHIRAL
Molecular Formula C24H28N6O3S
Molecular Weight 480.583
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of SURUFATINIB

SMILES

CN(C)CCNS(=O)(=O)CC1=CC(NC2=NC(OC3=CC4=C(NC(C)=C4)C=C3)=CC=N2)=CC=C1

InChI

InChIKey=TTZSNFLLYPYKIL-UHFFFAOYSA-N
InChI=1S/C24H28N6O3S/c1-17-13-19-15-21(7-8-22(19)27-17)33-23-9-10-25-24(29-23)28-20-6-4-5-18(14-20)16-34(31,32)26-11-12-30(2)3/h4-10,13-15,26-27H,11-12,16H2,1-3H3,(H,25,28,29)

HIDE SMILES / InChI
Molecular Formula C24H28N6O3S
Molecular Weight 480.583
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description

Sulfatinib (previously known as HMPL-012) was developed as a small-molecule inhibitor targeting vascular endothelial growth factor receptors 1 and 3, fibroblast growth factor receptor 1 and colony-stimulating factor 1 receptor with potential antineoplastic and anti-angiogenic activities. Sulfatinib has shown encouraging antitumor activity and manageable toxicities in patients with advanced neuroendocrine tumors (NET). The drug is participating in two ongoing phases III studies, validating the efficacy of surufatinib in patients with NETs. In addition, in November 2018, Hutchison MediPharma completed a phase II trial of sulfatinib, for the treatment of patients with biliary tract cancer. This drug is also participating in the phase II trial that is currently in recruiting status in treating advanced medullary thyroid carcinoma.

Originator

Approval Year

Unknown
149124
Targets

Targets

Primary TargetPharmacologyConditionPotency
Inhibitor
8504
Inhibitor
8504
Inhibitor
8504
Inhibitor
8504
Inhibitor
8504
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
487 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/30833272/
300 mg 1 times / day multiple, oral
dose: 300 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
SURUFATINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
456 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/37074571/
300 mg 1 times / day multiple, oral
dose: 300 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
SURUFATINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
4810 ng × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/30833272/
300 mg 1 times / day multiple, oral
dose: 300 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
SURUFATINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
4770 ng × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/37074571/
300 mg 1 times / day multiple, oral
dose: 300 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
SURUFATINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
26.6 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/37074571/
300 mg 1 times / day multiple, oral
dose: 300 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
SURUFATINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
PubMed

PubMed

TitleDatePubMed
Surufatinib in Advanced Well-Differentiated Neuroendocrine Tumors: A Multicenter, Single-Arm, Open-Label, Phase Ib/II Trial.
2019-06-15
Emerging multitarget tyrosine kinase inhibitors in the treatment of neuroendocrine neoplasms.
2018-09
Sulfatinib, a novel kinase inhibitor, in patients with advanced solid tumors: results from a phase I study.
2017-06-27

Sample Use Guides

In Vivo Use Guide
SULFATINIB (HMPL-012) 300 mg once a day (QD) will be orally administrated on a 28-day cycle
Route of Administration: Oral
Substance Class Chemical
Created
by admin
on Mon Mar 31 22:17:18 GMT 2025
Edited
by admin
on Mon Mar 31 22:17:18 GMT 2025
Record UNII
B2K5L1L8S9
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
SULFATINIB
Preferred Name English
SURUFATINIB
USAN   INN  
Official Name English
surufatinib [INN]
Common Name English
Surufatinib [WHO-DD]
Common Name English
BENZENEMETHANESULFONAMIDE, N-(2-(DIMETHYLAMINO)ETHYL)-3-((4-((2-METHYL-1H-INDOL-5-YL)OXY)-2-PYRIMIDINYL)AMINO)-
Systematic Name English
SURUFATINIB [USAN]
Common Name English
HMPL-012
Code English
N-(2-(DIMETHYLAMINO) ETHYL)-1-(3-((4-(2-METHYL-1H-INDOL-5-YLOXY) PYRIMIDIN-2-YL) AMINO) PHENYL) METHANESULFONAMIDE
Common Name English
Classification Tree Code System Code
FDA ORPHAN DRUG 710319
Created by admin on Mon Mar 31 22:17:19 GMT 2025 , Edited by admin on Mon Mar 31 22:17:19 GMT 2025
NCI_THESAURUS C93259
Created by admin on Mon Mar 31 22:17:18 GMT 2025 , Edited by admin on Mon Mar 31 22:17:18 GMT 2025
NCI_THESAURUS C129825
Created by admin on Mon Mar 31 22:17:18 GMT 2025 , Edited by admin on Mon Mar 31 22:17:18 GMT 2025
Code System Code Type Description
PUBCHEM
52920501
Created by admin on Mon Mar 31 22:17:18 GMT 2025 , Edited by admin on Mon Mar 31 22:17:18 GMT 2025
PRIMARY
CAS
1816307-67-1
Created by admin on Mon Mar 31 22:17:18 GMT 2025 , Edited by admin on Mon Mar 31 22:17:18 GMT 2025
SUPERSEDED
USAN
HI-176
Created by admin on Mon Mar 31 22:17:19 GMT 2025 , Edited by admin on Mon Mar 31 22:17:19 GMT 2025
PRIMARY
NCI_THESAURUS
C116066
Created by admin on Mon Mar 31 22:17:18 GMT 2025 , Edited by admin on Mon Mar 31 22:17:18 GMT 2025
PRIMARY
CAS
1308672-74-3
Created by admin on Mon Mar 31 22:17:18 GMT 2025 , Edited by admin on Mon Mar 31 22:17:18 GMT 2025
PRIMARY
DRUG BANK
DB15106
Created by admin on Mon Mar 31 22:17:19 GMT 2025 , Edited by admin on Mon Mar 31 22:17:19 GMT 2025
PRIMARY
SMS_ID
100000181191
Created by admin on Mon Mar 31 22:17:19 GMT 2025 , Edited by admin on Mon Mar 31 22:17:19 GMT 2025
PRIMARY
FDA UNII
B2K5L1L8S9
Created by admin on Mon Mar 31 22:17:19 GMT 2025 , Edited by admin on Mon Mar 31 22:17:19 GMT 2025
PRIMARY
INN
10349
Created by admin on Mon Mar 31 22:17:18 GMT 2025 , Edited by admin on Mon Mar 31 22:17:18 GMT 2025
PRIMARY
ChEMBL
CHEMBL3545251
Created by admin on Mon Mar 31 22:17:18 GMT 2025 , Edited by admin on Mon Mar 31 22:17:18 GMT 2025
PRIMARY
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Related Record Type Details
Structure of SURUFATINIB
ACTIVE MOIETY
NIH
NCATS
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