surufatinib   Click here for help

GtoPdb Ligand ID: 9769

Synonyms: HMPL-012 | HMPL012 | KDR-IN-1 | VEGFR2 inhibitor [WO2011060746]
Compound class: Synthetic organic
Comment: This VEGFR2 (KDR) inhibitor is claimed in patent WO2011060746 as a potential anti-angiogenic agent [1]. In this patent it is referred to as 'Compound of Formula A'.
Click here for help
2D Structure
Click here for help
Click here for structure editor
Physico-chemical Properties
Click here for help
Hydrogen bond acceptors 7
Hydrogen bond donors 3
Rotatable bonds 10
Topological polar surface area 120.62
Molecular weight 480.19
XLogP 2.96
No. Lipinski's rules broken 0
SMILES / InChI / InChIKey
Click here for help
Canonical SMILES CN(CCNS(=O)(=O)Cc1cccc(c1)Nc1nccc(n1)Oc1ccc2c(c1)cc([nH]2)C)C
Isomeric SMILES CN(CCNS(=O)(=O)Cc1cccc(c1)Nc1nccc(n1)Oc1ccc2c(c1)cc([nH]2)C)C
InChI 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)
InChI Key TTZSNFLLYPYKIL-UHFFFAOYSA-N
No information available.
Summary of Clinical Use Click here for help
Surufatinib has progressed to Phase 3 evaluations in neuroendocrine tumours (NET), and it is being advanced for other solid tumours. In April 2020 the FDA granted Fast Track Designation for surufatinib for the treatment of pancreatic and extra-pancreatic NET. As of June 2020 Hutchison China MediTech (Chi-Med) were in the process of submitting a FDA New Drug Application for surufatinib as a therapy for NET.
Clinical Trials
Clinical Trial ID Title Type Source Comment References
NCT02589821 Phase III Study of Surufatinib in Treating Advanced Pancreatic Neuroendocrine Tumors Phase 3 Interventional Hutchison Medipharma Limited
NCT02588170 Phase III Study of Surufatinib in Treating Advanced Extrapancreatic Neuroendocrine Tumors Phase 3 Interventional Hutchison Medipharma Limited
NCT02549937 A Multi-Center, Open-Label Study of Surufatinib (HMPL-012) in Patients With Advanced Solid Tumors Phase 1/Phase 2 Interventional Hutchison Medipharma Limited
NCT03873532 A Trial Evaluating Surufatinib Efficacy and Safety in Biliary Tract Carcinoma Patients Phase 2/Phase 3 Interventional Hutchison Medipharma Limited