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

Expert Opin Investig Drugs. 2008 Aug;17(8):1225-35. doi: 10.1517/13543784.17.8.1225.


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 alphavbeta3 and alphavbeta5 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.

Publication types

  • Research Support, N.I.H., Extramural
  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / administration & dosage
  • Antineoplastic Agents / adverse effects
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / therapeutic use*
  • Central Nervous System Neoplasms / diagnosis
  • Central Nervous System Neoplasms / drug therapy*
  • Clinical Trials as Topic
  • Drug Evaluation, Preclinical
  • Glioblastoma / diagnosis
  • Glioblastoma / drug therapy*
  • Humans
  • Integrins / metabolism*
  • Models, Molecular
  • Oligopeptides / administration & dosage
  • Oligopeptides / adverse effects
  • Oligopeptides / chemistry
  • Oligopeptides / therapeutic use*
  • Protein Binding
  • Snake Venoms / administration & dosage
  • Snake Venoms / adverse effects
  • Snake Venoms / chemistry
  • Snake Venoms / therapeutic use*
  • Treatment Outcome


  • Antineoplastic Agents
  • Integrins
  • Oligopeptides
  • Snake Venoms
  • Cilengitide
  • arginyl-glycyl-aspartic acid