Preclinical aspects of anti-VEGF agents for the treatment of wet AMD: ranibizumab and bevacizumab

Three anti-vascular endothelial growth factor (VEGF) therapies are currently used for the treatment of patients with wet age-related macular degeneration (AMD): pegaptanib, ranibizumab, and bevacizumab. Ranibizumab is an antibody fragment approved for the treatment of wet AMD. Bevacizumab is a full-...

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Veröffentlicht in:Eye (London) 2011-06, Vol.25 (6), p.661-672
Hauptverfasser: Meyer, C H, Holz, F G
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description Three anti-vascular endothelial growth factor (VEGF) therapies are currently used for the treatment of patients with wet age-related macular degeneration (AMD): pegaptanib, ranibizumab, and bevacizumab. Ranibizumab is an antibody fragment approved for the treatment of wet AMD. Bevacizumab is a full-length antibody registered for use in oncology but unlicensed for wet AMD. However, it is used off-label worldwide not only for wet AMD but also for various other ocular diseases associated with macular edema and abnormal vessel growth. We consider aspects of ranibizumab and bevacizumab in relation to their molecular characteristics, in vitro and in vivo properties, and preclinical safety data. Before 2009, most studies described the short-term toxicity of bevacizumab in multiple cell types of the eye. Since 2009, an increasing number of studies have compared the properties of ranibizumab and bevacizumab and investigated their impact on retinal cell functioning. Compared with bevacizumab, ranibizumab neutralizes VEGF better at low concentrations, maintains efficacy for longer, and has a higher retinal penetration and potency. Studies in animals demonstrate ranibizumab to be better localized to the injected eye, whereas bevacizumab appears to have a greater effect in the fellow eye. In humans, a localized and systemic effect has been reported for both molecules. In conclusion, overlapping yet distinct pharmacological properties of ranibizumab and bevacizumab indicate that safety or efficacy data from one cannot be extrapolated to the other.
doi_str_mv 10.1038/eye.2011.66
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subjects 631/378/1689/1626
631/92/436/2388
692/308/2778
Angiogenesis Inhibitors - pharmacokinetics
Angiogenesis Inhibitors - pharmacology
Angiogenesis Inhibitors - therapeutic use
Animals
Antibodies, Monoclonal - pharmacokinetics
Antibodies, Monoclonal - pharmacology
Antibodies, Monoclonal - therapeutic use
Antibodies, Monoclonal, Humanized
Bevacizumab
Biological and medical sciences
Disease Models, Animal
Drug Evaluation, Preclinical
Humans
Laboratory Medicine
Macular Degeneration - drug therapy
Macular Degeneration - metabolism
Medical sciences
Medicine
Medicine & Public Health
Miscellaneous
Off-Label Use
Ophthalmology
Pharmaceutical Sciences/Technology
Ranibizumab
Retinopathies
Review
Surgery
Surgical Oncology
Vascular Endothelial Growth Factor A - antagonists & inhibitors
Vascular Endothelial Growth Factor A - metabolism
title Preclinical aspects of anti-VEGF agents for the treatment of wet AMD: ranibizumab and bevacizumab
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