VEGF Receptor-2 Antagonist

Ramucirumab

VEGF-Receptor-2-Antagonist

Adams RH and Alitalo K1; Hicklin DJ and Ellis LM2

Target
Angiogenesis is a tightly regulated, multiple-step process, which results in the formation of new blood vessels from preexisting vasculature and is an important component in the development and progression of malignant disease. Signaling by vascular endothelial growth factor (VEGF) receptor-2 in endothelial cells plays a role in inducing normal and pathologic angiogenesis and is activated by binding of ligands VEGF-A, VEGF-C, and VEGF-D.1-3
Molecule
Ramucirumab is a human IgG1 monoclonal antibody receptor antagonist that has been shown in vitro to bind to and block the activation of VEGF receptor-2 by preventing the binding of VEGF receptor ligands VEGF-A, VEGF-C, and VEGF-D.4,5
Clinical Development
Ramucirumab is being investigated in clinical trials in patients with non-small cell lung cancer or pediatric sarcoma.

References

  1. Adams RH, Alitalo K. Nat Rev Mol Cell Biol. 2007;8(6):464-478.
  2. Hicklin DJ, Ellis LM. J Clin Oncol. 2005;23(5):1011-1027.
  3. Olsson AK, et al. Nat Rev Mol Cell Biol. 2006;7(5):359-371.
  4. Lu D, et al. J Biol Chem. 2003;278(44):43496-43507.
  5. Zhu Z, et al. Leukemia. 2003;17(3):604-611.
Ramucirumab Mechanism of Action
Clinical Development
Ramucirumab is being investigated in clinical trials in patients with non-small cell lung cancer or pediatric sarcoma.

References

  1. Adams RH, Alitalo K. Nat Rev Mol Cell Biol. 2007;8(6):464-478.
  2. Hicklin DJ, Ellis LM. J Clin Oncol. 2005;23(5):1011-1027.
  3. Olsson AK, et al. Nat Rev Mol Cell Biol. 2006;7(5):359-371.
  4. Lu D, et al. J Biol Chem. 2003;278(44):43496-43507.
  5. Zhu Z, et al. Leukemia. 2003;17(3):604-611.

The safety and efficacy of the agents under investigation have not been established. There is no guarantee that the agents will receive regulatory approval and become commercially available for the uses being investigated.

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