Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DMPOTM4)

• Drug Name: Sulfatinib Drug Info
• Synonyms: Anticancer agents, Hutchison; HMPL-012; Kinase inhibitors (cancer), Hutchison; VEGFR-1, 2, 3 and FGFR 1 inhibitor (oral, cancer), Hutchison

Indication

Disease Entry	ICD 11	Status	REF
Neuroendocrine cancer	2B72.1	Phase 3	[1]
Solid tumour/cancer	2A00-2F9Z	Phase 1	[2]

• Cross-matching ID:
  PubChem CID: 52920501
  CAS Number: CAS 1308672-74-3
  TTD Drug ID: DMPOTM4

Molecule-Related Drug Atlas

Drug(s) Targeting Vascular endothelial growth factor receptor 3 (FLT-4)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Fruquintinib	DMHOSCQ	Colorectal cancer	2B91.Z	Approved	[5]
Tivozanib	DMUKC5L	Renal cell carcinoma	2C90	Approved	[6]
E-3810	DM42PFT	Solid tumour/cancer	2A00-2F9Z	Phase 3	[7]
PI-88	DMGZPX6	Hepatocellular carcinoma	2C12.02	Phase 3	[8]
Taberminogene vadenovec	DMW5PHL	Vascular restinosis	BE2Z	Phase 3	[9]
ABT-869	DMREDYP	Solid tumour/cancer	2A00-2F9Z	Phase 3	[10]
MGCD516	DM752PU	Solid tumour/cancer	2A00-2F9Z	Phase 2/3	[11]
Famitinib	DMSFWT7	Solid tumour/cancer	2A00-2F9Z	Phase 2	[12]
VATALANIB	DMY0UEQ	Solid tumour/cancer	2A00-2F9Z	Phase 2	[13]
MK-2461	DM21WBH	Alzheimer disease	8A20	Phase 1/2	[14]

Drug(s) Targeting Macrophage colony-stimulating factor 1 receptor (CSF1R)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Pexidartinib	DMS2J0Z	Tenosynovial giant cell tumour	2F7B	Approved	[15]
ARRY-382	DM0VGDC	Solid tumour/cancer	2A00-2F9Z	Phase 2	[4]
BLZ-945	DMG1LVA	Amyotrophic lateral sclerosis	8B60.0	Phase 2	[4]
Cabiralizumab	DMGE058	Pancreatic cancer	2C10	Phase 2	[16]
AMB-05X	DM958C5	Idiopathic pulmonary fibrosis	CB03.4	Phase 2	[17]
FPA-008	DM3ZN6Y	Autoimmune diabetes	5A10	Phase 1/2	[18]
DCC-3014	DMHW289	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[4]
DCC-3014	DMHW289	Solid tumour/cancer	2A00-2F9Z	Phase 1/2	[19]
PLX7486	DM0IVGU	Pancreatic cancer	2C10	Phase 1	[4]
TPX-0022	DMC2IJN	Solid tumour/cancer	2A00-2F9Z	Phase 1	[20]

Drug(s) Targeting Vascular endothelial growth factor receptor (VEGFR)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Intedanib	DMSTA36	Colorectal cancer	2B91.Z	Approved	[21]
Fruquintinib	DMHOSCQ	Colorectal cancer	2B91.Z	Approved	[4]
KH-902	DM8VO16	Diabetic macular edema	9B71.02	Phase 3	[22]
ABP 938	DM00ACQ	Neovascular age-related macular degeneration	9B78.3Z	Phase 3	[23]
XL-820	DMMHX9K	Solid tumour/cancer	2A00-2F9Z	Phase 2	[24]
BAY-57-9352	DMVA5NS	Gastric adenocarcinoma	2B72	Phase 2	[18]
X-82	DMW1NKO	Age-related macular degeneration	9B75.0	Phase 2	[4]
Vorolanib	DMIM1U9	Non-small-cell lung cancer	2C25	Phase 2	[25]
BFH-772	DMVUX1C	Psoriasis vulgaris	EA90	Phase 2	[26]
ASP-8477	DMBZQS7	Neuropathic pain	8E43.0	Phase 2	[27]

Drug(s) Targeting Fibroblast growth factor receptor 1 (FGFR1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Romiplostim	DM3U7SZ	Thrombocytopenia	3B64	Approved	[28]
Intedanib	DMSTA36	Colorectal cancer	2B91.Z	Approved	[21]
Pemigatinib	DM819JF	Cholangiocarcinoma	2C12.10	Approved	[29]
Infigratinib	DMNKBEC	Cholangiocarcinoma	2C12.10	Approved	[30]
E-3810	DM42PFT	Solid tumour/cancer	2A00-2F9Z	Phase 3	[7]
ARQ-087	DM02BVQ	Intrahepatic cholangiocarcinoma	2C12.10	Phase 3	[31]
AZD4547	DM3827C	Solid tumour/cancer	2A00-2F9Z	Phase 2/3	[32]
Debio 1347	DMZW50O	Solid tumour/cancer	2A00-2F9Z	Phase 2	[4]
AM-001	DMGVQI8	Actinic keratosis	EK90.0	Phase 2	[33]
FGF-1	DMXMC8I	Coronary heart disease	BA80.Z	Phase 2	[34]

Drug(s) Targeting Vascular endothelial growth factor receptor 1 (FLT-1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Fruquintinib	DMHOSCQ	Colorectal cancer	2B91.Z	Approved	[5]
Tivozanib	DMUKC5L	Renal cell carcinoma	2C90	Approved	[6]
E-3810	DM42PFT	Solid tumour/cancer	2A00-2F9Z	Phase 3	[7]
Famitinib	DMSFWT7	Solid tumour/cancer	2A00-2F9Z	Phase 2	[12]
X-82	DMW1NKO	Age-related macular degeneration	9B75.0	Phase 2	[35]
OCV-101	DMT9QI2	Pancreatic cancer	2C10	Phase 2	[36]
LY3012212	DMRVEHY	Arteriosclerosis	BD40	Phase 2	[37]
OTSGC-A24	DMN0ZQ5	Colorectal cancer	2B91.Z	Phase 1/2	[38]
CEP-11981	DMYDTJ6	Solid tumour/cancer	2A00-2F9Z	Phase 1	[39]
EW-A-401	DM3VC6T	Peripheral vascular disease	BD4Z	Phase 1	[40]

Drug(s) Targeting Vascular endothelial growth factor receptor 2 (KDR)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Sorafenib	DMS8IFC	Adenocarcinoma	2D40	Approved	[41]
Romiplostim	DM3U7SZ	Thrombocytopenia	3B64	Approved	[28]
Regorafenib	DMHSY1I	Gastrointestinal stromal tumour	2B5B	Approved	[42]
Sunitinib	DMCBJSR	Acute undifferentiated leukemia		Approved	[43]
Axitinib	DMGVH6N	Renal cell carcinoma	2C90	Approved	[44]
Vandetanib	DMRICNP	Solid tumour/cancer	2A00-2F9Z	Approved	[45]
Pazopanib HCl	DM6U9CQ	Renal cell carcinoma	2C90	Approved	[46]
Fruquintinib	DMHOSCQ	Colorectal cancer	2B91.Z	Approved	[5]
Cabozantinib	DMIYDT4	Medullary thyroid gland carcinoma		Approved	[47]
Tivozanib	DMUKC5L	Renal cell carcinoma	2C90	Approved	[6]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Fibroblast growth factor receptor 1 (FGFR1)	TTRLW2X	FGFR1_HUMAN	Inhibitor	[3]
Macrophage colony-stimulating factor 1 receptor (CSF1R)	TT7MRDV	CSF1R_HUMAN	Inhibitor	[4]
Vascular endothelial growth factor receptor (VEGFR)	TTVJ1D8	NOUNIPROTAC	Inhibitor	[4]
Vascular endothelial growth factor receptor 1 (FLT-1)	TT2Q6G1	VGFR1_HUMAN	Inhibitor	[3]
Vascular endothelial growth factor receptor 2 (KDR)	TTUTJGQ	VGFR2_HUMAN	Inhibitor	[3]
Vascular endothelial growth factor receptor 3 (FLT-4)	TTDCBX5	VGFR3_HUMAN	Inhibitor	[3]

References

• [1] ClinicalTrials.gov (NCT02589821) Phase III Study of Surufatinib in Treating Advanced Pancreatic Neuroendocrine Tumors. U.S. National Institutes of Health.
• [2] ClinicalTrials.gov (NCT02133157) Phase I Study of Sulfatinib(HMPL-012) in Patients With Advanced Solid Tumors. U.S. National Institutes of Health.
• [3] Clinical pipeline report, company report or official report of Hutchison Medi Pharma.
• [4] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [5] Discovery of fruquintinib, a potent and highly selective small molecule inhibitor of VEGFR 1, 2, 3 tyrosine kinases for cancer therapy. Cancer Biol Ther. 2014;15(12):1635-45.
• [6] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services
• [7] E-3810 is a potent dual inhibitor of VEGFR and FGFR that exerts antitumor activity in multiple preclinical models. Cancer Res. 2011 Feb 15;71(4):1396-405.
• [8] Company report (Medigen)
• [9] Advances in kinase targeting: current clinical use and clinical trials. Trends Pharmacol Sci. 2014 Nov;35(11):604-20.
• [10] Preclinical activity of ABT-869, a multitargeted receptor tyrosine kinase inhibitor. Mol Cancer Ther. 2006 Apr;5(4):995-1006.
• [11] URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 1814).
• [12] Metabolism and bioactivation of famitinib, a novel inhibitor of receptor tyrosine kinase, in cancer patients. Br J Pharmacol. 2013 Apr;168(7):1687-706.
• [13] Discovery and evaluation of 2-anilino-5-aryloxazoles as a novel class of VEGFR2 kinase inhibitors. J Med Chem. 2005 Mar 10;48(5):1610-9.
• [14] MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor. Cancer Res. 2010 Feb 15;70(4):1524-33.
• [15] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
• [16] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [17] Clinical pipeline report, company report or official report of AmMax Bio
• [18] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [19] Clinical pipeline report, company report or official report of Deciphera Pharmaceuticals.
• [20] Clinical pipeline report, company report or official report of Turning Point Therapeutics.
• [21] 2014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
• [22] Effects of intravitreal injection of KH902, a vascular endothelial growth factor receptor decoy, on the retinas of streptozotocin-induced diabetic rats. Diabetes Obes Metab. 2012 Jul;14(7):644-53.
• [23] Clinical pipeline report, company report or official report of Amgen
• [24] National Cancer Institute Drug Dictionary (drug id 452042).
• [25] Vorolanib, an oral VEGFR/PDGFR dual tyrosine kinase inhibitor for treatment of patients with advanced solid tumors: An open-label, phase I dose escalation and dose expansion trial. Chin J Cancer Res. 2021 Feb 28;33(1):103-114.
• [26] CA patent application no. 841416, Method of selecting therapeutic indications.
• [27] ClinicalTrials.gov (NCT02065349) A Study Into Pain Relief Given by ASP8477 for Peripheral Neuropathic Pain (Either Post-herpetic Neuralgia or Painful Diabetic Peripheral Neuropathy) and Its Safety. U.S. National Institutes of Health.
• [28] Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. J Med Chem. 2002 Dec 19;45(26):5687-93.
• [29] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
• [30] Pharmacological inhibition of fibroblast growth factor (FGF) receptor signaling ameliorates FGF23-mediated hypophosphatemic rickets. J Bone Miner Res. 2013 Apr;28(4):899-911.
• [31] URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 1808).
• [32] AZD4547: an orally bioavailable, potent, and selective inhibitor of the fibroblast growth factor receptor tyrosine kinase family. Cancer Res. 2012 Apr 15;72(8):2045-56.
• [33] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800029917)
• [34] Marimastat as maintenance therapy for patients with advanced gastric cancer: a randomised trial. Br J Cancer. 2002 Jun 17;86(12):1864-70.
• [35] National Cancer Institute Drug Dictionary (drug id 695817).
• [36] Phase I trial of OTS11101, an anti-angiogenic vaccine targeting vascular endothelial growth factor receptor 1 in solid tumor.Cancer Sci.2013 Jan;104(1):98-104.
• [37] Icrucumab, a fully human monoclonal antibody against the vascular endothelial growth factor receptor-1, in the treatment of patients with advanced solid malignancies: a Phase 1 study. Invest New Drugs. 2014 Apr;32(2):303-11.
• [38] J Clin Oncol 33, 2015 (suppl 3; abstr 65).
• [39] URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 8189).
• [40] DOI: http://dx.doi.org/10.1016/j.tips.2014.09.007
• [41] Preclinical overview of sorafenib, a multikinase inhibitor that targets both Raf and VEGF and PDGF receptor tyrosine kinase signaling.Mol Cancer Ther.2008 Oct;7(10):3129-40.
• [42] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
• [43] 2006 drug approvals: finding the niche. Nat Rev Drug Discov. 2007 Feb;6(2):99-101.
• [44] Nat Rev Drug Discov. 2013 Feb;12(2):87-90.
• [45] A comparison of physicochemical property profiles of marketed oral drugs and orally bioavailable anti-cancer protein kinase inhibitors in clinical development. Curr Top Med Chem. 2007;7(14):1408-22.
• [46] Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
• [47] Clinical pipeline report, company report or official report of Exelixis (2011).