Cilengitide (TFA salt) - CAS 188968-51-6
Not Intended for Therapeutic Use. For research use only.
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Certificate of Analysis-Cilengitide (TFA salt) 188968-51-6 B17LM09012  
Cilengitide is a cyclic Arg-Gly-Asp peptide with potential antineoplastic activity. Cilengitide binds to and inhibits the activities of the alpha(v)beta(3) and alpha(v)beta(5) integrins, thereby inhibiting endothelial cell-cell interactions, endothelial cell-matrix interactions, and angiogenesis. It is being studied for the treatment of glioblastoma.
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Brife Description:
cyclic Arg-Gly-Asp peptide, potential antineoplastic activity
Lyophilized material
Cilengitide TFA salt; EMD-121974; Cilengitide [USAN:INN]; UNII-4EDF46E4GI; EMD-12192
the potential treatment of glioblastoma
Shelf Life:
2 years
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Technical University Munich / Merck KGaA
1.Tumor Microenvironment-Mediated Construction and Deconstruction of Extracellular Drug-Delivery Depots.
Hu Q1,2, Sun W1,2, Lu Y1,2, Bomba HN1,2, Ye Y1,2, Jiang T3, Isaacson AJ4, Gu Z1,2,5. Nano Lett. 2016 Feb 10;16(2):1118-26. doi: 10.1021/acs.nanolett.5b04343. Epub 2016 Jan 19.
Protein therapy has been considered the most direct and safe approach to treat cancer. Targeting delivery of extracellularly active protein without internalization barriers, such as membrane permeation and endosome escape, is efficient and holds vast promise for anticancer treatment. Herein, we describe a "transformable" core-shell based nanocarrier (designated CS-NG), which can enzymatically assemble into microsized extracellular depots at the tumor site with assistance of hyaluronidase (HAase), an overexpressed enzyme at the tumor microenvironment. Equipped with an acid-degradable modality, the resulting CS-NG can substantially release combinational anticancer drugs-tumor necrosis factor (TNF)-related apoptosis inducing ligand (TRAIL) and antiangiogenic cilengitide toward the membrane of cancer cells and endothelial cells at the acidic tumor microenvironment, respectively. Enhanced cytotoxicity on MDA-MB-231 cells and improved antitumor efficacy were observed using CS-NG, which was attributed to the inhibition of cellular internalization and prolonged retention time in vivo.
2.Pharmacotherapies for the treatment of glioblastoma - current evidence and perspectives.
Seystahl K1, Gramatzki D1, Roth P1, Weller M1. Expert Opin Pharmacother. 2016 Apr 7. [Epub ahead of print]
Introduction Glioblastoma, the most common malignant brain tumor, exhibits a poor prognosis with little therapeutic progress in the last decade. Novel treatment strategies beyond the established standard of care with temozolomide-based radiotherapy are urgently needed. Areas covered We reviewed the literature on glioblastoma with a focus on phase III trials for pharmacotherapies and/or innovative concepts until December 2015. Expert opinion In the last decade, phase III trials on novel compounds largely failed to introduce efficacious pharmacotherapies beyond temozolomide in glioblastoma. So far, inhibition of angiogenesis by compounds such as bevacizumab, cediranib, enzastaurin or cilengitide as well as alternative dosing schedules of temozolomide did not prolong survival, neither at primary diagnosis nor at recurrent disease. Promising strategies of pharmacotherapy currently under evaluation represent targeting epidermal growth factor receptor (EGFR) with biomarker-stratified patient populations and immunotherapeutic concepts including checkpoint inhibition and vaccination.
3.Glioma-targeted therapy using Cilengitide nanoparticles combined with UTMD enhanced delivery.
Zhao YZ1, Lin Q2, Wong HL3, Shen XT4, Yang W2, Xu HL2, Mao KL2, Tian FR2, Yang JJ2, Xu J2, Xiao J2, Lu CT5. J Control Release. 2016 Feb 28;224:112-25. doi: 10.1016/j.jconrel.2016.01.015. Epub 2016 Jan 11.
Malignant gliomas especially glioblastoma (GBM) are poorly responsive to the current treatments. Cilengitide (CGT) is a cyclic pentapeptide that demonstrated efficacy for GBM treatment by targeting the integrins avβ3 and avβ5 over-expressed on GBM cells. However, clinical translation of this therapy has been limited by issues including fast blood clearance, high kidney and liver uptake, poor blood-brain barrier (BBB) penetration, low tumor specificity and rapid washout from tumors. In this study, these issues were tackled in an integrated manner using a multi-stage strategy combining ultrasound-targeted microbubble destruction (UTMD) with CGT nanotherapy. CGT nanoparticles (CGT-NP) prepared using gelatin and Poloxamer 188-grafted heparin copolymer demonstrated significant apoptotic and cytotoxic effects in C6 GBM cells. Biodistribution study in a rat GBM model demonstrated buildup of high CGT level in tumors subjected to CGT-NP+UTMD combined therapy.
4.Cilengitide in newly diagnosed glioblastoma: biomarker expression and outcome.
Weller M1, Nabors LB2, Gorlia T3, Leske H4, Rushing E4, Bady P5,6,7, Hicking C8, Perry J9, Hong YK10, Roth P1, Wick W11,12, Goodman SL8, Hegi ME7, Picard M8, Moch H13, Straub J8, Stupp R14. Oncotarget. 2016 Feb 22. doi: 10.18632/oncotarget.7588. [Epub ahead of print]
Integrins αvβ3 and αvβ5 regulate angiogenesis and invasiveness in cancer, potentially by modulating activation of the transforming growth factor (TGF)-β pathway. The randomized phase III CENTRIC and phase II CORE trials explored the integrin inhibitor cilengitide in patients with newly diagnosed glioblastoma with versus without O6-methylguanine DNA methyltransferase (MGMT) promoter methylation. These trials failed to meet their primary endpoints. Immunohistochemistry was used to assess the levels of the target integrins of cilengitide, αvβ3 and αvβ5 integrins, of αvβ8 and of their putative target, phosphorylation of SMAD2, in tumor tissues from CENTRIC (n=274) and CORE (n=224). αvβ3 and αvβ5 expression correlated well in tumor and endothelial cells, but showed little association with αvβ8 or pSMAD2 levels. In CENTRIC, there was no interaction between the biomarkers and treatment for prediction of outcome. In CORE, higher αvβ3 levels in tumor cells were associated with improved progression-free survival by central review and with improved overall survival in patients treated with cilengitide.
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CAS 188968-51-6 Cilengitide (TFA salt)

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