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

General Information of Drug (ID: DMGQXN7)

• Drug Name: SU-11652 Drug Info
• Synonyms: SU11652; SU-11652; 5-[(Z)-(5-chloro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]-N-[2-(diethylamino)ethyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide; UNII-1C7AZL970U; CHEMBL13485; 1C7AZL970U; 326914-10-7; 5-[(E)-(5-Chloro-2-Oxo-1,2-Dihydro-3h-Indol-3-Ylidene)methyl]-N-[2-(Diethylamino)ethyl]-2,4-Dimethyl-1h-Pyrrole-3-Carboxamide; 5-{[(3Z)-5-chloro-2-oxo-2,3-dihydro-1H-indol-3-ylidene]methyl}-N-[2-(diethylamino)ethyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide; AC1NS62M; SU11248 analog 12c; GTPL6043; BDBM4815; SCHEMBL2114096

Indication

Disease Entry	ICD 11	Status	REF
Discovery agent	N.A.	Investigative	[1]

• Cross-matching ID:
  PubChem CID: 5329103
  ChEBI ID: CHEBI:94073
  CAS Number: CAS 326914-10-7
  TTD Drug ID: DMGQXN7

Molecule-Related Drug Atlas

Drug(s) Targeting Platelet-derived growth factor receptor alpha (PDGFRA)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Romiplostim	DM3U7SZ	Thrombocytopenia	3B64	Approved	[2]
Ripretinib	DM958QB	Gastrointestinal stromal tumour	2B5B	Approved	[3]
Olaratumab	DMNYOIX	Soft tissue sarcoma	2B57	Approved	[4]
Avapritinib	DMK2GZX	Gastrointestinal stromal tumour	2B5B	Approved	[5]
E-3810	DM42PFT	Solid tumour/cancer	2A00-2F9Z	Phase 3	[6]
CP-868596	DMZIM37	Gastrointestinal cancer	2C11	Phase 3	[7]
Famitinib	DMSFWT7	Solid tumour/cancer	2A00-2F9Z	Phase 2	[8]
XL-820	DMMHX9K	Solid tumour/cancer	2A00-2F9Z	Phase 2	[9]
MP470	DMELUAK	Solid tumour/cancer	2A00-2F9Z	Phase 2	[10]
MEDI-575	DMI9WVM	Glioblastoma multiforme	2A00.0	Phase 2	[11]

Drug(s) Targeting Platelet-derived growth factor receptor beta (PDGFRB)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Sorafenib	DMS8IFC	Adenocarcinoma	2D40	Approved	[12]
Romiplostim	DM3U7SZ	Thrombocytopenia	3B64	Approved	[2]
Becaplermin	DM1R5X4	Diabetic complication	5A2Y	Approved	[13]
E-3810	DM42PFT	Solid tumour/cancer	2A00-2F9Z	Phase 3	[6]
Famitinib	DMSFWT7	Solid tumour/cancer	2A00-2F9Z	Phase 2	[8]
XL-820	DMMHX9K	Solid tumour/cancer	2A00-2F9Z	Phase 2	[9]
MK-2461	DM21WBH	Alzheimer disease	8A20	Phase 1/2	[14]
SNN-0031	DM2X3BR	Brain injury	NA07.Z	Phase 1/2	[15]
TAK-593	DMNFZOT	Solid tumour/cancer	2A00-2F9Z	Phase 1	[16]
Pyridine derivative 18	DMBZMYT	N. A.	N. A.	Patented	[17]

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	[18]
Tivozanib	DMUKC5L	Renal cell carcinoma	2C90	Approved	[19]
E-3810	DM42PFT	Solid tumour/cancer	2A00-2F9Z	Phase 3	[6]
Sulfatinib	DMPOTM4	Neuroendocrine cancer	2B72.1	Phase 3	[20]
Famitinib	DMSFWT7	Solid tumour/cancer	2A00-2F9Z	Phase 2	[8]
X-82	DMW1NKO	Age-related macular degeneration	9B75.0	Phase 2	[21]
OCV-101	DMT9QI2	Pancreatic cancer	2C10	Phase 2	[22]
LY3012212	DMRVEHY	Arteriosclerosis	BD40	Phase 2	[23]
OTSGC-A24	DMN0ZQ5	Colorectal cancer	2B91.Z	Phase 1/2	[24]
CEP-11981	DMYDTJ6	Solid tumour/cancer	2A00-2F9Z	Phase 1	[25]

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	[12]
Romiplostim	DM3U7SZ	Thrombocytopenia	3B64	Approved	[26]
Regorafenib	DMHSY1I	Gastrointestinal stromal tumour	2B5B	Approved	[27]
Sunitinib	DMCBJSR	Acute undifferentiated leukemia		Approved	[28]
Axitinib	DMGVH6N	Renal cell carcinoma	2C90	Approved	[29]
Vandetanib	DMRICNP	Solid tumour/cancer	2A00-2F9Z	Approved	[30]
Pazopanib HCl	DM6U9CQ	Renal cell carcinoma	2C90	Approved	[31]
Fruquintinib	DMHOSCQ	Colorectal cancer	2B91.Z	Approved	[18]
Cabozantinib	DMIYDT4	Medullary thyroid gland carcinoma		Approved	[32]
Tivozanib	DMUKC5L	Renal cell carcinoma	2C90	Approved	[19]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Platelet-derived growth factor receptor alpha (PDGFRA)	TT8FYO9	PGFRA_HUMAN	Inhibitor	[2]
Platelet-derived growth factor receptor beta (PDGFRB)	TTI7421	PGFRB_HUMAN	Inhibitor	[2]
Vascular endothelial growth factor receptor 1 (FLT-1)	TT2Q6G1	VGFR1_HUMAN	Inhibitor	[2]
Vascular endothelial growth factor receptor 2 (KDR)	TTUTJGQ	VGFR2_HUMAN	Inhibitor	[2]

References

• [1] 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: 6043).
• [2] Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel... J Med Chem. 2003 Mar 27;46(7):1116-9.
• [3] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
• [4] A phase I study of olaratumab, an anti-platelet-derived growth factor receptor alpha (PDGFRalpha) monoclonal antibody, in patients with advanced solid tumors. Cancer Chemother Pharmacol. 2014 Mar;73(3):595-604.
• [5] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
• [6] 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.
• [7] The FLT3 and PDGFR inhibitor crenolanib is a substrate of the multidrug resistance protein ABCB1 but does not inhibit transport function at pharmacologically relevant concentrations.Invest New Drugs.2015 Apr;33(2):300-9.
• [8] Metabolism and bioactivation of famitinib, a novel inhibitor of receptor tyrosine kinase, in cancer patients. Br J Pharmacol. 2013 Apr;168(7):1687-706.
• [9] National Cancer Institute Drug Dictionary (drug id 452042).
• [10] Phase 1B study of amuvatinib in combination with five standard cancer therapies in adults with advanced solid tumors. Cancer Chemother Pharmacol. 2014 Jul;74(1):195-204.
• [11] Clinical pipeline report, company report or official report of MedImmune (2011).
• [12] 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.
• [13] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
• [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] Company report (Neuronova)
• [16] Biochemical characterization of TAK-593, a novel VEGFR/PDGFR inhibitor with a two-step slow binding mechanism. Biochemistry. 2011 Feb 8;50(5):738-51.
• [17] RET kinase inhibitors: a review of recent patents (2012-2015).Expert Opin Ther Pat. 2017 Jan;27(1):91-99.
• [18] 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.
• [19] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services
• [20] Clinical pipeline report, company report or official report of Hutchison Medi Pharma.
• [21] National Cancer Institute Drug Dictionary (drug id 695817).
• [22] 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.
• [23] 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.
• [24] J Clin Oncol 33, 2015 (suppl 3; abstr 65).
• [25] 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).
• [26] Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. J Med Chem. 2002 Dec 19;45(26):5687-93.
• [27] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
• [28] 2006 drug approvals: finding the niche. Nat Rev Drug Discov. 2007 Feb;6(2):99-101.
• [29] Nat Rev Drug Discov. 2013 Feb;12(2):87-90.
• [30] 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.
• [31] Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
• [32] Clinical pipeline report, company report or official report of Exelixis (2011).