2012
DOI: 10.1016/j.ajo.2012.03.047
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Intraocular Pharmacokinetics of Ranibizumab Following a Single Intravitreal Injection in Humans

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Cited by 213 publications
(146 citation statements)
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“…A similar difference between the ocular and systemic half-life was noted in a TMDD model of lampalizumab in humans (Le et al, 2015), in which the vitreous half-life was 5.9 days compared with a systemic half-life of 9 hours. The shorter ocular half-life in monkeys (3 days) compared with humans (7-9 days) was also reported for ranibizumab (Gaudreault et al, 2005;Krohne et al, 2012;Xu et al, 2013). Similar to the clinical results, lampalizumab in the cynomolgus monkey also exhibits flipflop pharmacokinetics, a phenomenon in which the rate of drug egressing out of the vitreous humor is much slower than …”
Section: Discussionsupporting
confidence: 69%
See 1 more Smart Citation
“…A similar difference between the ocular and systemic half-life was noted in a TMDD model of lampalizumab in humans (Le et al, 2015), in which the vitreous half-life was 5.9 days compared with a systemic half-life of 9 hours. The shorter ocular half-life in monkeys (3 days) compared with humans (7-9 days) was also reported for ranibizumab (Gaudreault et al, 2005;Krohne et al, 2012;Xu et al, 2013). Similar to the clinical results, lampalizumab in the cynomolgus monkey also exhibits flipflop pharmacokinetics, a phenomenon in which the rate of drug egressing out of the vitreous humor is much slower than …”
Section: Discussionsupporting
confidence: 69%
“…The relationship between the ocular half-life and molecular size is unknown beyond this range. However, literature on ITV administration of anti-vascular endothelial growth factor therapy suggested that the half-life of ranibizumab (7-9 days) (Krohne et al, 2012;Xu et al, 2013) was only slightly shorter than that for bevacizumab (9.8 days) (Krohne et al, 2012) in humans. Notably, the quasi-steady state equilibrium constant K ss was fixed to the in vitro measured value of the dissociation equilibrium constant (K D ) of 11.7 pM (Loyet et al, 2014) and was able to describe the data quite well.…”
Section: Tmdd Model Of Lampalizumab In Cynomolgus Monkeysmentioning
confidence: 99%
“…They reported that vitreous concentrations of ranibizumab declined in a monoexponential fashion with a half-life of 2.88 days; concentrations of >0.1 μg/ml ranibizumab were maintained in the vitreous humor for 29 days [18]. Krohne et al found that the aqueous halflife of 0.5 mg of intravitreal injected ranibizunab was 7.19 days in nonvitrectomized human eyes [19]. Xu et al demonstrated that due to the slow release of ranibizumab from the stagnant vitreous, the apparent serum half-life following intravitreal ranibizumab administration was 9 days in adult patients.…”
Section: Discussionmentioning
confidence: 96%
“…18 Relative to bevacizumab, ranibizumab has been reported to have a somewhat shorter vitreous half-life, but has 5-to 20-fold higher biologic activity. 19,20 This increased activity, coupled with the smaller molecular size of ranibizumab, may further benefit eyes with DME. The US Food and Drug Administration approval for ranibizumab 0.3-mg for the treatment of DME was granted in August 2012.…”
Section: Introductionmentioning
confidence: 99%