Intraocular Pharmacokinetics of Bevacizumab After a Single Intravitreal Injection in Humans

• Published in: American journal of ophthalmology Vol. 146; no. 4; pp. 508 - 512
• Main Authors: Krohne, Tim U, Eter, Nicole, Holz, Frank G, Meyer, Carsten H
• Format: Journal Article
• Language: English
• Published: New York, NY Elsevier Inc 01.10.2008; Elsevier; Elsevier Limited
• Subjects: Adult; Aged; Aged, 80 and over; Angiogenesis Inhibitors - pharmacokinetics; Antibodies, Monoclonal - pharmacokinetics; Antibodies, Monoclonal, Humanized; Aqueous Humor - metabolism; Bevacizumab; Biological and medical sciences; Cataract - complications; Cataract Extraction; Cataracts; Colleges & universities; Diabetes; Diabetic retinopathy; Diabetic Retinopathy - complications; Enzyme-Linked Immunosorbent Assay; Enzymes; Eye surgery; Female; Half-Life; Humans; Injections; Macular degeneration; Macular Degeneration - complications; Macular Edema - etiology; Male; Medical sciences; Middle Aged; Miscellaneous; Molecular weight; Ophthalmology; Patients; Prospective Studies; Regression analysis; Retinal Vein Occlusion - complications; Statistical analysis; Surgery; Vascular endothelial growth factor; Vascular Endothelial Growth Factor A - antagonists & inhibitors; Vitreous Body; South San Francisco California; California; Antineoplastic agent; Human; Immunomodulator; Vascular endothelium growth factor; Intraocular; Single dose; Vitreous body; Monoclonal antibody; Ophthalmology; Antiangiogenic agent; Pharmacokinetics; Bevacizumab
• ISSN: 0002-9394; 1879-1891
• DOI: 10.1016/j.ajo.2008.05.036

Purpose To investigate intraocular concentrations and pharmacokinetics of bevacizumab after a single intravitreal injection in humans. Design Prospective, noncomparative, interventional case series. Methods We included 30 nonvitrectomized eyes of 30 patients (age range, 43 to 93 years) diagnosed with clinically significant cataract and concurrent macular edema secondary to neovascular age-related macular degeneration, diabetic retinopathy, or retinal venous occlusion in the same eye. All patients received an intravitreal injection of 1.5 mg bevacizumab. Between one and 53 days after injection, an aqueous humor sample was obtained during elective cataract surgery. Concentrations of unbound bevacizumab in these samples were quantified by enzyme-linked immunosorbent assay. Results Concentration of bevacizumab in aqueous humor peaked on the first day after injection with a mean concentration (cmax ) of 33.3 μg/ml (range, 16.6 to 42.5 μg/ml) and subsequently declined in a monoexponential fashion. Nonlinear regression analysis determined an elimination half-time (t1/2 ) of 9.82 days ( R2 = 0.81). No significant differences between diagnosis subgroups were noted. Conclusions In human nonvitrectomized eyes, the aqueous half-life of 1.5 mg intravitreally injected bevacizumab is 9.82 days.