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

General Information of Drug (ID: DMEAOZ0)

• Drug Name: Cilengitide Drug Info
• Synonyms: Cilengitide; 188968-51-6; EMD-121974; Cilengitide [USAN:INN]; UNII-4EDF46E4GI; EMD121974; EMD-12192; EMD 121974; 4EDF46E4GI; CHEMBL429876; 2-[(2S,5R,8S,11S)-5-benzyl-11-[3-(diaminomethylideneamino)propyl]-7-methyl-3,6,9,12,15-pentaoxo-8-propan-2-yl-1,4,7,10,13-pentazacyclopentadec-2-yl]acetic acid; Cyclo(L-arginylglycyl-L-aspartyl-D-phenylalanyl-N-methyl-L-valyl); Cyclo(L-arginylglycyl-L-alpha-aspartyl-D-phenylalanyl-N-methyl-L-valyl); Cilengitide (TFA salt)

Indication

Disease Entry	ICD 11	Status	REF
Rheumatoid arthritis	FA20	Phase 3	[1] , [2]

• Cross-matching ID:
  PubChem CID: 176873
  CAS Number: CAS 188968-51-6
  TTD Drug ID: DMEAOZ0

Molecule-Related Drug Atlas

Drug(s) Targeting Integrin alpha-V/beta-3 (ITGAV/B3)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
ATN-161	DM4T9RS	Renal cell carcinoma	2C90	Phase 2	[5]
Intetumumab	DMBXEG9	Prostate cancer	2C82.0	Phase 2	[6]
VLTS-589	DM4O17U	Peripheral vascular disease	BD4Z	Phase 2	[7]
Fluciclatide F-18	DME01HT	Solid tumour/cancer	2A00-2F9Z	Phase 2	[8]
SF0166	DM4NK3J	Diabetic macular edema	9B71.02	Phase 1/2	[9]
AMEP	DMFELMQ	Melanoma	2C30	Phase 1	[10]
Vitaxin	DMHCLVQ	Solid tumour/cancer	2A00-2F9Z	Discontinued in Phase 2	[11]
SB-267268	DMIBFAV	Osteoporosis	FB83.0	Discontinued in Phase 1	[12]
SB-273005	DMV7M1H	Osteoporosis	FB83.0	Discontinued in Phase 1	[13]
PS-388023	DM8P05S	Ocular disease	1F00.1Z	Terminated	[14]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Integrin alpha-V/beta-3 (ITGAV/B3)	TT69TQN	ITAV_HUMAN-ITB3_HUMAN	Modulator	[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: 6597).
• [2] ClinicalTrials.gov (NCT00689221) Cilengitide, Temozolomide, and Radiation Therapy in Treating Patients With Newly Diagnosed Glioblastoma and Methylated Gene Promoter Status. U.S. National Institutes of Health.
• [3] The integrin antagonist cilengitide activates alphaVbeta3, disrupts VE-cadherin localization at cell junctions and enhances permeability in endothelial cells.PLoS One.2009;4(2):e4449.
• [4] Pharmacological inhibition of integrin alphavbeta3 aggravates experimental liver fibrosis and suppresses hepatic angiogenesis.Hepatology.2009 Nov;50(5):1501-11.
• [5] A non-RGD-based integrin binding peptide (ATN-161) blocks breast cancer growth and metastasis in vivo. Mol Cancer Ther. 2006 Sep;5(9):2271-80.
• [6] A randomised, phase II study of intetumumab, an anti-alphav-integrin mAb, alone and with dacarbazine in stage IV melanoma. Br J Cancer. 2011 Jul 26;105(3):346-52.
• [7] AbbVie Licenses Phase II-Ready Antibody Programme to Receptos for Development in Eosinophilic Oesophagitis. 2013(4), Page 35.
• [8] Use of a novel Arg-Gly-Asp radioligand, 18F-AH111585, to determine changes in tumor vascularity after antitumor therapy.J Nucl Med.2009 Jan;50(1):116-22.
• [9] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [10] Gene electrotransfer of plasmid AMEP, an integrin-targeted therapy, has antitumor and antiangiogenic action in murine B16 melanoma.Gene Ther.2015 Jul;22(7):578-90.
• [11] Monoclonal antibodies to alphaVbeta3 (7E3 and LM609) inhibit sickle red blood cell-endothelium interactions induced by platelet-activating factor. Blood. 2000 Jan 15;95(2):368-74.
• [12] SB-267268, a nonpeptidic antagonist of alpha(v)beta3 and alpha(v)beta5 integrins, reduces angiogenesis and VEGF expression in a mouse model of retinopathy of prematurity. Invest Ophthalmol Vis Sci. 2006 Apr;47(4):1600-5.
• [13] Disease-modifying activity of SB 273005, an orally active, nonpeptide alphavbeta3 (vitronectin receptor) antagonist, in rat adjuvant-induced arthri... Arthritis Rheum. 2001 Jan;44(1):128-37.
• [14] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.