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

General Information of Drug (ID: DMX054A)

• Drug Name: CP-547632 Drug Info
• Synonyms: BFF; CP 547632; CP-547,632; 3-(4-Bromo-2,6-difluorobenzyloxy)-5-(3-(4-pyrrolidin-1-ylbutyl)ureido)isothiazole-4-carboxylic acid amide

Indication

Disease Entry	ICD 11	Status	REF
Non-small-cell lung cancer	2C25.Y	Phase 2	[1] , [2]
Ovarian cancer	2C73	Phase 2	[1] , [2]
Solid tumour/cancer	2A00-2F9Z	Phase 2	[1] , [2]

• Therapeutic Class: Anticancer Agents
• Cross-matching ID:
  PubChem CID: 9811611
  CAS Number: CAS 252003-65-9
  TTD Drug ID: DMX054A

Molecule-Related Drug Atlas

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

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Sorafenib	DMS8IFC	Hepatocellular carcinoma	2C12.02	Approved	[5]
Romiplostim	DM3U7SZ	Thrombocytopenia	3B64	Approved	[6]
Regorafenib	DMHSY1I	Metastatic colorectal cancer	2B91	Approved	[7]
Sunitinib	DMCBJSR	Gastrointestinal cancer	2C11	Approved	[8]
Axitinib	DMGVH6N	Renal cell carcinoma	2C90	Approved	[9]
Vandetanib	DMRICNP	Solid tumour/cancer	2A00-2F9Z	Approved	[3]
Pazopanib HCl	DM6U9CQ	Renal cell carcinoma	2C90	Approved	[10]
Cabozantinib	DMIYDT4	Thyroid cancer	2D10	Approved	[11]
Tivozanib	DMUKC5L	Renal cell carcinoma	2C90	Approved	[12]
Lenvatinib	DMB1IU4	Thyroid cancer	2D10	Approved	[13]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Vascular endothelial growth factor receptor 2 (KDR)	TTUTJGQ	VGFR2_HUMAN	Inhibitor	[3] , [4]

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: 7881).
• [2] ClinicalTrials.gov (NCT00096239) CP-547,632 in Treating Patients With Recurrent or Persistent Ovarian Cancer, Primary Peritoneal Cancer, or Fallopian Tube Cancer. U.S. National Institutes of Health.
• [3] 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.
• [4] YM-359445, an orally bioavailable vascular endothelial growth factor receptor-2 tyrosine kinase inhibitor, has highly potent antitumor activity against established tumors. Clin Cancer Res. 2006 Mar 1;12(5):1630-8.
• [5] 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.
• [6] Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. J Med Chem. 2002 Dec 19;45(26):5687-93.
• [7] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
• [8] 2006 drug approvals: finding the niche. Nat Rev Drug Discov. 2007 Feb;6(2):99-101.
• [9] Nat Rev Drug Discov. 2013 Feb;12(2):87-90.
• [10] Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
• [11] Clinical pipeline report, company report or official report of Exelixis (2011).
• [12] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services
• [13] Emerging drugs for ovarian cancer. Expert Opin Emerg Drugs. 2008 Sep;13(3):523-36.