U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS
This repository is under review for potential modification in compliance with Administration directives.

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

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

Targets

Primary TargetPharmacologyConditionPotency

Cmax

ValueDoseCo-administeredAnalytePopulation
487 ng/mL
300 mg 1 times / day multiple, oral
SURUFATINIB plasma
Homo sapiens
456 ng/mL
300 mg 1 times / day multiple, oral
SURUFATINIB plasma
Homo sapiens

AUC

ValueDoseCo-administeredAnalytePopulation
4810 ng × h/mL
300 mg 1 times / day multiple, oral
SURUFATINIB plasma
Homo sapiens
4770 ng × h/mL
300 mg 1 times / day multiple, oral
SURUFATINIB plasma
Homo sapiens

T1/2

ValueDoseCo-administeredAnalytePopulation
26.6 h
300 mg 1 times / day multiple, oral
SURUFATINIB plasma
Homo sapiens

PubMed

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