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LUIS JAVIER HERNANDEZ-PASTOR, PHARM D., is Resident, Pharmacy Department, University Clinic; ANA ORTEGA, PHARM.D., PH.D., is Consultant Pharmacist, Clinica Universitaria, and Assistant Professor, Faculty of Pharmacy; ALFREDO GARCIA-LAYANA, M.D., PH.D., is Consultant Ophthalmologist, Clinica Universitaria, and Professor, Faculty of Medicine; and JOAQUIN GIRALDEZ, PHARM D., PH.D., is Head of the Pharmacy Department, Clinica Universitaria, and Professor, Faculty of Pharmacy, University of Navarra, Pamplona, Spain.

Address correspondence to Dr. Hernandez-Pastor at the Pharmacy Department, Clinica Universitaria, University of Navarra, Av/Pio XII 36, PC, 31008 Pamplona, Spain (luisjaher{at}unav.es).

Purpose. The pharmacology, pharmacokinetics, clinical efficacy, safety, pharmacoeconomics, and place in therapy of ranibizumab are reviewed. Summary. Ranibizumab is the humanized fragment of the murine monoclonal antibody that binds all the active forms of the vascular endothelial growth factor, leading to the inhibition of the neovascular process underlying age-related macular degeneration (AMD). In animal studies, intravitreal administration of ranibizumab resulted in penetration of the drug into all layers of the retina and subsequent slow absorption into the systemic circulation. Improvement in visual acuity by 15 or more letters has been observed in 33.8–40.3% of patients treated with ranibizumab in pivotal clinical trials, compared with 5% of patients treated with sham injections and photodynamic therapy (PDT). The addition of PDT to ranibizumab has not been shown to offer any benefit in terms of efficacy and has been found to worsen ocular adverse reactions. The most common adverse ocular reactions reported in patients receiving ranibizumab during clinical trials include conjunctival hemorrhage, eye pain, vitreous floaters, increased intraocular pressure, and intraocular inflammation. Ranibizumab’s efficacy in the treatment of neovascular AMD is well established; however, questions remain regarding the drug’s optimal dosing strategy, duration of therapy, and combined therapy with other agents. While ranibizumab has been defined as the best available weapon against AMD, it is also the most expensive. Conclusion. The efficacy of ranibizumab in the treatment of AMD is well established, but more studies are needed to determine ranibizumab’s optimal dosage interval, duration of therapy, and combined use with other agents. Index terms: Antibodies; Macular degeneration; Mechanism of action; Pharmacoeconomics; Pharmacokinetics; Ranibizumab; Toxicity