Intraocular pharmacokinetics of bevacizumab after a single intravitreal injection in humans.
OBJECTIVE
To investigate intraocular concentrations and pharmacokinetics of bevacizumab after a single intravitreal injection in humans.


METHODS
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 (c(max)) of 33.3 microg/ml (range, 16.6 to 42.5 microg/ml) and subsequently declined in a monoexponential fashion. Nonlinear regression analysis determined an elimination half-time (t(1/2)) of 9.82 days (R(2) = 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.
Krohne
Tim U
TU
Department of Ophthalmology, University of Bonn, Bonn, Germany.
Eter
Nicole
N
Holz
Frank G
FG
Meyer
Carsten H
CH
D000328:Adult; D000368:Aged; D000369:Aged, 80 and over; D020533:Angiogenesis Inhibitors / Q000493:pharmacokinetics*; D000911:Antibodies, Monoclonal / Q000493:pharmacokinetics*; D061067:Antibodies, Monoclonal, Humanized; D001082:Aqueous Humor / Q000378:metabolism*; D000068258:Bevacizumab; D002386:Cataract / Q000150:complications; D002387:Cataract Extraction; D003930:Diabetic Retinopathy / Q000150:complications; D004797:Enzyme-Linked Immunosorbent Assay; D005260:Female; D006207:Half-Life; D006801:Humans; D007267:Injections; D008268:Macular Degeneration / Q000150:complications; D008269:Macular Edema / Q000209:etiology; D008297:Male; D008875:Middle Aged; D011446:Prospective Studies; D012170:Retinal Vein Occlusion / Q000150:complications; D042461:Vascular Endothelial Growth Factor A / Q000037:antagonists & inhibitors; D014822:Vitreous Body
D020533:Angiogenesis Inhibitors; D000911:Antibodies, Monoclonal; D061067:Antibodies, Monoclonal, Humanized; D042461:Vascular Endothelial Growth Factor A; D000068258:Bevacizumab