SURUFATINIB

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 Search

SMILES

CN(C)CCNS(=O)(=O)CC1=CC=CC(NC2=NC=CC(OC3=CC=C4NC(C)=CC4=C3)=N2)=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
Sources: https://www.ncbi.nlm.nih.gov/pubmed/30833272 | https://clinicaltrials.gov/ct2/show/NCT02588170

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 Target	Pharmacology	Condition	Potency
Vascular endothelial growth factor receptor 1 41 Target ID: CHEMBL1868 Sources: http://cancerres.aacrjournals.org/content/77/13_Supplement/4187.short	Inhibitor 8297
Vascular endothelial growth factor receptor 2 104 Target ID: CHEMBL279 Sources: http://cancerres.aacrjournals.org/content/77/13_Supplement/4187.short	Inhibitor 8297
Vascular endothelial growth factor receptor 3 41 Target ID: CHEMBL1955 Sources: http://cancerres.aacrjournals.org/content/77/13_Supplement/4187.short	Inhibitor 8297
Fibroblast growth factor receptor 1 45 Target ID: CHEMBL3650 Sources: http://cancerres.aacrjournals.org/content/77/13_Supplement/4187.short	Inhibitor 8297
Macrophage colony stimulating factor receptor 24 Target ID: CHEMBL1844 Sources: http://cancerres.aacrjournals.org/content/77/13_Supplement/4187.short	Inhibitor 8297

PubMed

Title	Date	PubMed
Sulfatinib, a novel kinase inhibitor, in patients with advanced solid tumors: results from a phase I study.	2017 Jun 27	28159938
Emerging multitarget tyrosine kinase inhibitors in the treatment of neuroendocrine neoplasms.	2018 Sep	29769293
Surufatinib in Advanced Well-Differentiated Neuroendocrine Tumors: A Multicenter, Single-Arm, Open-Label, Phase Ib/II Trial.	2019 Jun 15	30833272

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

Name

Type

Language

SURUFATINIB

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

SULFATINIB

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