Cilengitide: An integrin-targeting arginine-glycine-aspartic acid peptide with promising activity for glioblastoma multiforme

David A. Reardon*, L. Burt Nabors, Roger Stupp, Tom Mikkelsen

*Corresponding author for this work

Research output: Contribution to journalReview article

150 Scopus citations


Background: Glioblastoma multiforme (GBM), a highly invasive and vascular cancer, responds poorly to conventional cytotoxic therapy. Integrins, widely expressed in GBM and tumor vasculature, mediate cell survival, migration and angiogenesis. Cilengitide is a potent αvβ3 and αvβ5 integrin inhibitor. Objective: To summarize the preclinical and clinical experience with cilengitide for GBM. Methods: Preclinical studies and clinical trials evaluating cilengitide for GBM were reviewed. Results/conclusions: Cilengitide is active and synergizes with external beam radiotherapy in preclinical GBM models. In clinical trials for recurrent GBM, single-agent cilengitide has antitumor benefits and minimal toxicity. Among newly diagnosed GBM patients, single-arm studies incorporating cilengitide into standard external beam radiotherapy/ temozolomide have shown encouraging activity with no increased toxicity and have led to a planned randomized Phase III trial.

Original languageEnglish (US)
Pages (from-to)1225-1235
Number of pages11
JournalExpert Opinion on Investigational Drugs
Issue number8
Publication statusPublished - Aug 1 2008



  • Angiogenesis
  • Glioblastoma multiforme
  • Integrins
  • Malignant glioma
  • Vascular endothelial growth factor

ASJC Scopus subject areas

  • Pharmacology
  • Pharmacology (medical)

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