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

General Information of Drug (ID: DMYDTJ6)

• Drug Name: CEP-11981 Drug Info
• Synonyms: CEP-11981; UNII-J8AY0Z4CBP; 856691-93-5; J8AY0Z4CBP; CHEMBL2010872; BOL-303213X; compound 11b [PMID 22148921]; GTPL8189; SCHEMBL2439310; DTXSID80234942; CEP11981; BDBM50379186; CEP 11981; 4H-Indazolo(5,4-a)pyrrolo(3,4-C)carbazol-4-one, 2,5,6,11,12,13-hexahydro-2-methyl-11-(2-methylpropyl)-8-(2-pyrimidinylamino)-; Z-3152

Indication

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

• Cross-matching ID:
  PubChem CID: 11751922
  CAS Number: CAS 856691-93-5
  TTD Drug ID: DMYDTJ6

Molecule-Related Drug Atlas

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

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Tivozanib	DMUKC5L	Renal cell carcinoma	2C90	Approved	[5]
E-3810	DM42PFT	Solid tumour/cancer	2A00-2F9Z	Phase 3	[6]
Sulfatinib	DMPOTM4	Neuroendocrine cancer	2B72.1	Phase 3	[7]
Fruquintinib	DMHOSCQ	Solid tumour/cancer	2A00-2F9Z	Phase 3	[8]
Famitinib	DMSFWT7	Solid tumour/cancer	2A00-2F9Z	Phase 2	[9]
X-82	DMW1NKO	Age-related macular degeneration	9B75.0	Phase 2	[10]
OCV-101	DMT9QI2	Pancreatic cancer	2C10	Phase 2	[11]
LY3012212	DMRVEHY	Arteriosclerosis	BD40	Phase 2	[12]
OTSGC-A24	DMN0ZQ5	Colorectal cancer	2B91.Z	Phase 1/2	[13]
EW-A-401	DM3VC6T	Peripheral vascular disease	BD4Z	Phase 1	[14]

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	[15]
Romiplostim	DM3U7SZ	Thrombocytopenia	3B64	Approved	[16]
Regorafenib	DMHSY1I	Metastatic colorectal cancer	2B91	Approved	[17]
Sunitinib	DMCBJSR	Gastrointestinal cancer	2C11	Approved	[18]
Axitinib	DMGVH6N	Renal cell carcinoma	2C90	Approved	[19]
Vandetanib	DMRICNP	Solid tumour/cancer	2A00-2F9Z	Approved	[4]
Pazopanib HCl	DM6U9CQ	Renal cell carcinoma	2C90	Approved	[20]
Cabozantinib	DMIYDT4	Thyroid cancer	2D10	Approved	[21]
Tivozanib	DMUKC5L	Renal cell carcinoma	2C90	Approved	[5]
Lenvatinib	DMB1IU4	Thyroid cancer	2D10	Approved	[22]

Drug(s) Targeting Angiopoietin 1 receptor (TEK)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
AKB-9778	DMKNRYH	Diabetic macular edema	9B71.02	Phase 2	[23]
DCC-2036	DMJKFNU	Chronic myeloid leukaemia	2A20	Phase 1/2	[24]
Altiratinib	DMUJCBT	Solid tumour/cancer	2A00-2F9Z	Phase 1	[25]
ARRY-614	DMXD93K	Arthritis	FA20	Discontinued in Phase 1	[26]
3,4-di-(4-methoxyphenyl)-1H-pyrrole-2,5-dione	DMDO175	Discovery agent	N.A.	Investigative	[27]
3,4-diphenyl-1H-pyrrole-2,5-dione	DMPK6YT	Discovery agent	N.A.	Investigative	[27]
3-(4-methoxyphenyl)-4-phenyl-1H-pyrrole-2,5-dione	DMGC7RY	Discovery agent	N.A.	Investigative	[27]
3-(indole-3-yl)-4-phenyl-1H-pyrrole-2,5-dione	DM3EV9N	Discovery agent	N.A.	Investigative	[27]
PMID21561767C8h	DMABZH6	Discovery agent	N.A.	Investigative	[28]
(4-Phenoxy-phenyl)-quinazolin-4-yl-amine	DMFO8DR	Discovery agent	N.A.	Investigative	[29]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Angiopoietin 1 receptor (TEK)	TT9VGXW	TIE2_HUMAN	Modulator	[3]
Vascular endothelial growth factor receptor 1 (FLT-1)	TT2Q6G1	VGFR1_HUMAN	Modulator	[1]
Vascular endothelial growth factor receptor 2 (KDR)	TTUTJGQ	VGFR2_HUMAN	Inhibitor	[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: 8189).
• [2] ClinicalTrials.gov (NCT00875264) Open-Label Study to Determine the Maximum Tolerated Oral Dose of the Kinase Inhibitor CEP-11981 in Patients With Advanced Cancer. U.S. National Institutes of Health.
• [3] 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: 1842).
• [4] 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.
• [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] Clinical pipeline report, company report or official report of Hutchison Medi Pharma.
• [8] 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.
• [9] Metabolism and bioactivation of famitinib, a novel inhibitor of receptor tyrosine kinase, in cancer patients. Br J Pharmacol. 2013 Apr;168(7):1687-706.
• [10] National Cancer Institute Drug Dictionary (drug id 695817).
• [11] 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.
• [12] 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.
• [13] J Clin Oncol 33, 2015 (suppl 3; abstr 65).
• [14] DOI: http://dx.doi.org/10.1016/j.tips.2014.09.007
• [15] 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.
• [16] Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. J Med Chem. 2002 Dec 19;45(26):5687-93.
• [17] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
• [18] 2006 drug approvals: finding the niche. Nat Rev Drug Discov. 2007 Feb;6(2):99-101.
• [19] Nat Rev Drug Discov. 2013 Feb;12(2):87-90.
• [20] Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
• [21] Clinical pipeline report, company report or official report of Exelixis (2011).
• [22] Emerging drugs for ovarian cancer. Expert Opin Emerg Drugs. 2008 Sep;13(3):523-36.
• [23] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [24] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [25] Clinical pipeline report, company report or official report of Deciphera Pharmaceuticals.
• [26] Cmpany report (Arraybiopharma)
• [27] Design, synthesis, and biological evaluation of 3,4-diarylmaleimides as angiogenesis inhibitors. J Med Chem. 2006 Feb 23;49(4):1271-81.
• [28] Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant. Bioorg Med Chem Lett. 2011 Jun 15;21(12):3743-8.
• [29] Pyrrolo[2,3-d]pyrimidines containing an extended 5-substituent as potent and selective inhibitors of lck I. Bioorg Med Chem Lett. 2000 Oct 2;10(19):2167-70.