[Aflibercept. An approach to pharmacology].
Aflibercept is a fusion protein whose chemical structure combines the constant fraction of any IgG with a variable fraction constructed with fundamental parts of VEGF receptors. Consequently, it is able to bind to various VEGF as well as to placental growth factor (PIGF), which has been related to a possible synergistic effect in efficacy. The affinity of this drug is higher than that of ranibizumab and bevacizumab. Moreover, it has an intraocular antiinflammatory effect. Intravitreal administration leads to the presence of traces of the drug in plasma but the concentrations are so reduced that the presence of systemic adverse effects, including arterial hypertension, is practically nil. Because of its prolonged intraocular elimination half-life and high affinity, the drug can be administered in convenient regimens, since, after an initial monthly injection for the first three doses, the interval between injections is increased to one every two months and, after the first 12 months, the dosing will depend on the visual and anatomical results.
Servicio de Farmacología Clínica, Clínica Universidad de Navarra, Pamplona, España; Sociedad Española de la Retina y Vítreo, Instituto de Salud Carlos III, Madrid, España; Red Temática de Investigación Cooperativa OFTARED, Instituto de Salud Carlos III, Madrid, España. Electronic address: jrazanza@unav.es.
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JR
Azanza Perea
Servicio de Farmacología Clínica, Clínica Universidad de Navarra, Pamplona, España; Sociedad Española de la Retina y Vítreo, Instituto de Salud Carlos III, Madrid, España; Red Temática de Investigación Cooperativa OFTARED, Instituto de Salud Carlos III, Madrid, España.
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B
Sádaba
D020533:Angiogenesis Inhibitors / Q000009:adverse effects / Q000494:pharmacology* / Q000627:therapeutic use; D000818:Animals; D020256:Choroidal Neovascularization / Q000188:drug therapy; D002986:Clinical Trials as Topic; D004334:Drug Administration Schedule; D004353:Drug Evaluation, Preclinical; D006207:Half-Life; D006801:Humans; D007141:Immunoglobulin Fc Fragments / Q000009:adverse effects / Q000494:pharmacology* / Q000627:therapeutic use; D056965:Injections, Intraocular; D015394:Molecular Structure; D040262:Receptors, Vascular Endothelial Growth Factor / Q000627:therapeutic use; D011993:Recombinant Fusion Proteins / Q000009:adverse effects / Q000494:pharmacology* / Q000627:therapeutic use; D015861:Retinal Neovascularization / Q000188:drug therapy* / Q000209:etiology; D014018:Tissue Distribution
D020533:Angiogenesis Inhibitors; D007141:Immunoglobulin Fc Fragments; D011993:Recombinant Fusion Proteins; C533178:aflibercept; D040262:Receptors, Vascular Endothelial Growth Factor
Aflibercept; Anti-VEFG; Anti-VEGF; Farmacocinética; Farmacología; Pharmacokinetics; Pharmacology