Intraocular pharmacokinetics of ranibizumab following a single intravitreal injection in humans.

Abstract:

PURPOSE:To investigate intraocular concentrations and pharmacokinetics of ranibizumab after a single intravitreal injection in humans. DESIGN:Prospective, noncomparative, interventional case series. METHODS:We included 18 nonvitrectomized eyes of 18 patients (age range, 61-85 years) that were diagnosed with both clinically significant cataract and macular edema secondary to either exudative age-related macular degeneration, diabetic maculopathy, or retinal vein occlusion. Each eye received a single intravitreal injection of 0.5 mg ranibizumab. An aqueous humor sample was obtained during cataract surgery between 1 and 37 days after injection. Concentrations of unbound ranibizumab in these samples were quantified by enzyme-linked immunosorbent assay. RESULTS:Ranibizumab concentration in aqueous humor peaked the first day after injection (range, 36.9-66.1 μg/mL) and subsequently declined in a mono-exponential fashion. Nonlinear regression analysis determined an initial peak concentration (c(max)) of 56.1 μg/mL and an elimination half-life (t(1/2)) of 7.19 days with a coefficient of determination (R(2)) of 0.90. Correction of ranibizumab concentrations for ocular volume as calculated from axial length measurements did not alter regression analysis results significantly (t(1/2), 7.15 days; R(2), 0.89). CONCLUSIONS:In human nonvitrectomized eyes, the aqueous half-life of 0.5 mg intravitreally injected ranibizumab is 7.19 days, slightly shorter than the half-life of 9.82 days previously determined for bevacizumab by comparable methods.

journal_name

Am J Ophthalmol

authors

Krohne TU,Liu Z,Holz FG,Meyer CH

doi

10.1016/j.ajo.2012.03.047

subject

Has Abstract

pub_date

2012-10-01 00:00:00

pages

682-686.e2

issue

4

eissn

0002-9394

issn

1879-1891

pii

S0002-9394(12)00261-9

journal_volume

154

pub_type

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