Cilengitide

• CAS Number: 188968-51-6

Cilengitide (EMD 121974, Brand Name: Impetreve, in the one-letter code: cyclo - [ RGDfN (Me) V] ) is the international non-proprietary name for a cyclic pentapeptide. It is currently being tested in oncology for its applicability as an angiogenesis inhibitor for treating glioblastoma, a particularly malignant form of brain tumor. It was developed by Merck KGaA in collaboration with Horst Kessler from the Technical University of Munich.

Mechanism of action

Cilengitide contains an RGD amino acid sequence. This sequence consisting of the three amino acids Arginine ( R), glycine ( G), and aspartic acid ( D), mediates the binding to specific receptors, known as integrins. Cilengitide inhibits integrins avb3 and αvβ5 and is thus the formation and growth of tumor's own blood vessels ( angiogenesis) and thus the growth and spread of tumor cells to bind. As a result, the blood supply is cut off, the tumor " starved " by downright and can no longer form metastases. Some cancer cells react to this substance even very directly and die (apoptosis).

Clinical Trials

Cilengitide is not currently approved for use in humans. The substance is still in clinical testing.

• The results of a multicenter dose-finding study to determine the maximum tolerated dose of Cilengitide in glioma patients have been published on the ninth annual meeting of the American Society for Neuro- Oncology ( SNO ) in Toronto: In two of the 51 recruited patients with complete remission was achieved in three patients a partial remission and four patients a stabilization of the disease state for more than six months.
• Currently (as of June 2007) run seven funded by the National Cancer Institute studies Cilengitide as monotherapy in various tumor types, including newly diagnosed glioblastoma, recurrent glioblastoma in adults and recurrent brain tumors in children. Another NCI study currently being investigated in phase II setting the combination of temozolomide with radiotherapy and Cilengitide in patients with newly diagnosed glioblastoma.
• At the last annual meeting of the American Cancer Society, American Society of Clinical Oncology (ASCO ), the results of two other phase I / II studies with investigated for the treatment of patients with glioblastoma were presented.
• In addition Cilengitide currently against various other tumors, such as metastatic prostate cancer (Phase II), advanced non- small cell lung cancer (Phase II) will be tested and advanced squamous cell carcinoma of the head and neck ( Phase I / II).