Cilengitide
An integrin-blocking peptide that failed in glioblastoma
Cilengitide is an arginine-glycine-aspartic acid (RGD) peptide that blocks alphavbeta3 and alphavbeta5 integrins, which help tumours grow blood vessels and invade. Promising early trials in glioblastoma led to the phase 3 CENTRIC trial, where median survival was 26.3 months with and without it.
What is it?
Integrins alphavbeta3 and alphavbeta5 regulate angiogenesis and invasiveness in cancer, and cilengitide was designed as an integrin-targeting arginine-glycine-aspartic acid (RGD) peptide to block them. In preclinical glioblastoma models it was active and worked with radiotherapy, and early clinical trials found it well tolerated with signs of activity, which led to a planned phase 3 trial.
In recurrent glioblastoma, a randomised phase 2 trial of 81 patients found an excellent safety profile and more activity at the higher dose (6-month progression-free survival 15%, median survival 9.9 months). In newly diagnosed disease, a phase 2 trial in patients without MGMT promoter methylation reported median survival of 16.3 months with the standard cilengitide regimen against 13.4 months for controls.
The decisive test was CENTRIC: 545 patients with methylated MGMT promoter tumours were randomised to standard treatment with or without cilengitide. Median overall survival was 26.3 months in both groups (hazard ratio 1.02), and no subgroup benefited. Later biomarker work confirmed that both CENTRIC and CORE missed their primary endpoints. Cilengitide was not approved.
At a Glance
Every value in this table is printed from the Grey Peptides dataset, the same record the compound explorer and comparison tool read, so the three can never disagree.
Educational information, not medical advice. The doses on this page come from approved labels, published studies and, where no study exists, amounts reported by users. None is a recommendation for you. An unapproved compound has no established safe or effective human dose, and products sold for “research use only” are not made or tested for people. Talk to a doctor before acting on anything on this site, including before you start, stop or change any medicine or dose. Full medical disclaimer.
Published Research
Studies of cilengitide, from their PubMed abstracts.
CENTRIC phase 3
In 545 patients with MGMT-methylated glioblastoma, median overall survival was 26.3 months with cilengitide and 26.3 months without (hazard ratio 1.02, p = 0.86); no subgroup benefited and no additional toxicity was seen.
CORE: unmethylated tumours
Median overall survival was 16.3 months with standard cilengitide (HR 0.686, p = 0.032) and 14.5 months with intensive cilengitide against 13.4 months for controls; cilengitide was well tolerated.
Recurrent glioblastoma phase 2
In 81 patients, cilengitide had an excellent safety profile; activity trended better at 2,000 mg, with 6-month progression-free survival of 15% and median survival of 9.9 months.
Biomarkers after CENTRIC and CORE
Both trials of cilengitide in newly diagnosed glioblastoma failed their primary endpoints; this analysis examined whether levels of its integrin targets predicted outcome.
Why it looked promising
Cilengitide was active and synergised with radiotherapy in preclinical glioblastoma models, showed antitumour benefit with minimal toxicity in recurrent disease, and encouraging single-arm results led to a phase 3 trial.
Side Effects & Contraindications
Reported Side Effects
From the trials above.
Contraindications & Cautions
No label; it is investigational.
Legal Status
Cilengitide is investigational and not approved.
Frequently Asked Questions
?What is cilengitide?
An investigational RGD peptide that blocks alphavbeta3 and alphavbeta5 integrins, developed as a treatment for glioblastoma.
?Why did cilengitide fail?
In the phase 3 CENTRIC trial, median survival was 26.3 months with or without it, and no subgroup benefited, despite encouraging earlier phase 2 results.
?Is cilengitide available?
No. It was never approved, and anything sold under its name is an unverified research chemical.
?Was cilengitide safe?
Yes, in the trials: the recurrent glioblastoma phase 2 study reported no significant reproducible toxicities, and CENTRIC found no overall additional toxic effects over standard treatment; lymphopenia and thrombocytopenia occurred in both arms.
?Did any trial show a survival benefit?
The phase 2 CORE trial in unmethylated tumours reported 16.3 months with the standard cilengitide regimen against 13.4 months for controls, but the trial missed its primary endpoint and the larger CENTRIC trial found no benefit.
?Which patients were in CENTRIC?
Of 3,471 patients screened, 926 had a methylated MGMT promoter and 545 were randomised to standard radiotherapy and temozolomide with or without cilengitide.
References
- [clinical-trial] Stupp R, et al. "Cilengitide combined with standard treatment for patients with newly diagnosed glioblastoma with methylated MGMT promoter (CENTRIC EORTC 26071-22072 study): a multicentre, randomised, open-label, phase 3 trial." Lancet Oncol, 2014;15(10):1100-8. PMID: 25163906.
- [clinical-trial] Nabors LB, et al. "Two cilengitide regimens in combination with standard treatment for patients with newly diagnosed glioblastoma and unmethylated MGMT gene promoter: results of the open-label, controlled, randomized phase II CORE study." Neuro Oncol, 2015;17(5):708-17. PMID: 25762461.
- [clinical-trial] Reardon DA, et al. "Randomized phase II study of cilengitide, an integrin-targeting arginine-glycine-aspartic acid peptide, in recurrent glioblastoma multiforme." J Clin Oncol, 2008;26(34):5610-7. PMID: 18981465.
- [pubmed] Weller M, et al. "Cilengitide in newly diagnosed glioblastoma: biomarker expression and outcome." Oncotarget, 2016;7(12):15018-32. PMID: 26918452.
- [pubmed] Reardon DA, et al. "Cilengitide: an integrin-targeting arginine-glycine-aspartic acid peptide with promising activity for glioblastoma multiforme." Expert Opin Investig Drugs, 2008;17(8):1225-35. PMID: 18616418.
Sources & Citations
Studies were read from their PubMed records, October 3, 2026.
Medical Disclaimer: This content is for educational and informational purposes only. It is not medical advice, and nothing here is an instruction to obtain or use any compound. Consult a licensed healthcare provider before making health decisions.