Surufatinib

Surufatinib
Clinical data
Trade names	Sulanda
Other names	Sulfatinib; HMPL-012
ATC code	L01EX24 (WHO) ;
Legal status
Legal status	In general: ℞ (Prescription only);
Identifiers
	IUPAC name N-[2-(Dimethylamino)ethyl]-1-[3-[[4-[(2-methyl-1H-indol-5-yl)oxy]pyrimidin-2-yl]amino]phenyl]methanesulfonamide;
CAS Number	1308672-74-3;
PubChem CID	52920501;
IUPHAR/BPS	9769;
DrugBank	DB15106;
ChemSpider	57583328;
UNII	B2K5L1L8S9;
ChEMBL	ChEMBL4297190;
Chemical and physical data
Formula	C24H28N6O3S
Molar mass	480.59 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CC1=CC2=C(N1)C=CC(=C2)OC3=NC(=NC=C3)NC4=CC=CC(=C4)CS(=O)(=O)NCCN(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); Key:TTZSNFLLYPYKIL-UHFFFAOYSA-N;

Surufatinib (trade name Sulanda) is pharmaceutical drug for the treatment of cancer. In China, it is approved for late-stage, well-differentiated, extrapancreatic neuroendocrine tumors.^[1]

It is also under investigation for the treatment of other types of solid tumors.^[2]^[3]

Surufatinib targets fibroblast growth factor receptor 1 (FGFR1).^[4]

References

^ Syed YY (April 2021). "Surufatinib: First Approval". Drugs. 81 (6): 727–732. doi:10.1007/s40265-021-01489-y. PMID 33788183.
^ Liao S, Li J, Gao S, Han Y, Han X, Wu Y, et al. (2023). "Sulfatinib, a novel multi-targeted tyrosine kinase inhibitor of FGFR1, CSF1R, and VEGFR1-3, suppresses osteosarcoma proliferation and invasion via dual role in tumor cells and tumor microenvironment". Frontiers in Oncology. 13: 1158857. doi:10.3389/fonc.2023.1158857. PMC 10286821. PMID 37361567.
^ Xu JM, Wang Y, Chen YL, Jia R, Shen L, Wang J, et al. (2014). "First-in-human (FIH) phase I study of a selective VEGFR/FGFR dual inhibitor sulfatinib with milled formulation in patients with advanced solid tumors". Journal of Clinical Oncology. 32 (15_suppl): 2615. doi:10.1200/jco.2014.32.15_suppl.2615.
^ Lin Q, Dai S, Qu L, Lin H, Guo M, Wei H, et al. (January 2024). "Structural basis and selectivity of sulfatinib binding to FGFR and CSF-1R". Communications Chemistry. 7 (1): 3. doi:10.1038/s42004-023-01084-0. PMC 10764862. PMID 38172256.

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[1] Syed YY (April 2021). "Surufatinib: First Approval". Drugs. 81 (6): 727–732. doi:10.1007/s40265-021-01489-y. PMID 33788183.

[2] Liao S, Li J, Gao S, Han Y, Han X, Wu Y, et al. (2023). "Sulfatinib, a novel multi-targeted tyrosine kinase inhibitor of FGFR1, CSF1R, and VEGFR1-3, suppresses osteosarcoma proliferation and invasion via dual role in tumor cells and tumor microenvironment". Frontiers in Oncology. 13: 1158857. doi:10.3389/fonc.2023.1158857. PMC 10286821. PMID 37361567.

[3] Xu JM, Wang Y, Chen YL, Jia R, Shen L, Wang J, et al. (2014). "First-in-human (FIH) phase I study of a selective VEGFR/FGFR dual inhibitor sulfatinib with milled formulation in patients with advanced solid tumors". Journal of Clinical Oncology. 32 (15_suppl): 2615. doi:10.1200/jco.2014.32.15_suppl.2615.

[4] Lin Q, Dai S, Qu L, Lin H, Guo M, Wei H, et al. (January 2024). "Structural basis and selectivity of sulfatinib binding to FGFR and CSF-1R". Communications Chemistry. 7 (1): 3. doi:10.1038/s42004-023-01084-0. PMC 10764862. PMID 38172256.

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