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

General Information of Drug (ID: DMNFZOT)

• Drug Name: TAK-593 Drug Info
• Synonyms: TAK-593; 1005780-62-0; UNII-H3I42X8XX7; H3I42X8XX7; CHEMBL2180604; 1H-Pyrazole-5-carboxamide, N-[5-[[2-[(cyclopropylcarbonyl)amino]imidazo[1,2-b]pyridazin-6-yl]oxy]-2-methylphenyl]-1,3-dimethyl-;1H-Pyrazole-5-carboxamide, N-[5-[[2-[(cyclopropylcarbonyl)amino]imidazo[1,2-b]pyridazin-6-yl]oxy]-2-methylphenyl]-1,3-dimethyl-; TAK 593; SCHEMBL2515478; DZFZXPPHBWCXPQ-UHFFFAOYSA-N; ZINC95579919; BDBM50399537; AKOS030526192; CS-2403; DB13093; NCGC00485933-01; 1H-Pyrazole-5-carboxamide, N-(5-((2-((cyclopropylcarbonyl)amino)imidazo

Indication

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

• Cross-matching ID:
  PubChem CID: 24767976
  CAS Number: CAS 1005780-62-0
  TTD Drug ID: DMNFZOT

Molecule-Related Drug Atlas

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	[3]
Romiplostim	DM3U7SZ	Thrombocytopenia	3B64	Approved	[4]
Becaplermin	DM1R5X4	Diabetic complication	5A2Y	Approved	[5]
E-3810	DM42PFT	Solid tumour/cancer	2A00-2F9Z	Phase 3	[6]
Famitinib	DMSFWT7	Solid tumour/cancer	2A00-2F9Z	Phase 2	[7]
XL-820	DMMHX9K	Solid tumour/cancer	2A00-2F9Z	Phase 2	[8]
MK-2461	DM21WBH	Alzheimer disease	8A20	Phase 1/2	[9]
SNN-0031	DM2X3BR	Brain injury	NA07.Z	Phase 1/2	[10]
Pyridine derivative 18	DMBZMYT	N. A.	N. A.	Patented	[11]
PMID25656651-Compound-21a	DMCKAON	N. A.	N. A.	Patented	[12]

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	[3]
Romiplostim	DM3U7SZ	Thrombocytopenia	3B64	Approved	[13]
Regorafenib	DMHSY1I	Gastrointestinal stromal tumour	2B5B	Approved	[14]
Sunitinib	DMCBJSR	Acute undifferentiated leukemia		Approved	[15]
Axitinib	DMGVH6N	Renal cell carcinoma	2C90	Approved	[16]
Vandetanib	DMRICNP	Solid tumour/cancer	2A00-2F9Z	Approved	[17]
Pazopanib HCl	DM6U9CQ	Renal cell carcinoma	2C90	Approved	[18]
Fruquintinib	DMHOSCQ	Colorectal cancer	2B91.Z	Approved	[19]
Cabozantinib	DMIYDT4	Medullary thyroid gland carcinoma		Approved	[20]
Tivozanib	DMUKC5L	Renal cell carcinoma	2C90	Approved	[21]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Platelet-derived growth factor receptor beta (PDGFRB)	TTI7421	PGFRB_HUMAN	Modulator	[2]
Vascular endothelial growth factor receptor 2 (KDR)	TTUTJGQ	VGFR2_HUMAN	Modulator	[2]

References

• [1] Anti-angiogenic and anti-tumor effects of TAK-593, a potent and selective inhibitor of vascular endothelial growth factor and platelet-derived growth factor receptor tyrosine kinase. Cancer Sci. 2013Apr;104(4):486-94.
• [2] 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.
• [3] 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.
• [4] 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.
• [5] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
• [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] Metabolism and bioactivation of famitinib, a novel inhibitor of receptor tyrosine kinase, in cancer patients. Br J Pharmacol. 2013 Apr;168(7):1687-706.
• [8] National Cancer Institute Drug Dictionary (drug id 452042).
• [9] MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor. Cancer Res. 2010 Feb 15;70(4):1524-33.
• [10] Company report (Neuronova)
• [11] RET kinase inhibitors: a review of recent patents (2012-2015).Expert Opin Ther Pat. 2017 Jan;27(1):91-99.
• [12] Bcr-Abl tyrosine kinase inhibitors: a patent review.Expert Opin Ther Pat. 2015 Apr;25(4):397-412.
• [13] Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. J Med Chem. 2002 Dec 19;45(26):5687-93.
• [14] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
• [15] 2006 drug approvals: finding the niche. Nat Rev Drug Discov. 2007 Feb;6(2):99-101.
• [16] Nat Rev Drug Discov. 2013 Feb;12(2):87-90.
• [17] 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.
• [18] Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
• [19] 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.
• [20] Clinical pipeline report, company report or official report of Exelixis (2011).
• [21] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services