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The development of new, abnormal and leaky blood vessels, termed choroidal neovascularization, causes loss of vision and quality of life as a result of many ocular diseases. A current therapy for a leading cause of irreversible blindness in older people in the United States, age-related macular degeneration, is intravitreal injection of ranibizumab. However, ranibizumab has also been used off-label to successfully treat a number of other ocular diseases causing significant ocular morbidity, including retinal vascular occlusion and diabetic macular edema. Despite its efficacy, the association of detectable serum levels of ranibizumab and arterial thromboembolic events in major follow-up studies since its approval by the United States Food and Drug Administration as well as its high cost relative to the possible existence of cheaper, equally efficacious alternatives has underscored the importance of understanding the mode of action and clinical utility of this novel pharmacotherapy.