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Keywords:

  • platelet-derived growth factor receptor α;
  • platelet-derived growth factor;
  • vascular endothelial growth factors;
  • neoplasms;
  • monoclonal antibodies;
  • antineoplastic agents;
  • malignant stroma;
  • cancer-associated stroma;
  • tumor-associated stroma

Abstract

A large body of evidence suggests that the platelet-derived growth factor (PDGF) family and associated receptors are potential targets in oncology therapeutic development because of their critical roles in the proliferation and survival of various cancers and in the regulation and growth of the tumor stroma and blood vessels. Several small molecules that nonspecifically target the PDGF signaling axis are in current use or development as anticancer therapies. However, for the majority of these agents, PDGF and its receptors are neither the primary targets nor the principal mediators of anticancer activity. IMC-3G3, a fully human monoclonal antibody of the immunoglobulin G subclass 1, specifically binds to the human PDGF receptor α (PDGFRα) with high affinity and blocks PDGF ligand binding and PDGFRα activation. The results of preclinical studies and the frequent expression of PDGFRα in many types of cancer and in cancer-associated stroma support a rationale for the clinical development of IMC-3G3. Currently, IMC-3G3 is being evaluated in early clinical development for patients with several types of solid malignancies. Cancer 2010;116(4 suppl):1018–26. © 2010 American Cancer Society.