Intraocular pharmacokinetics of intravitreal vascular endothelial growth factor-Trap in a rabbit model

Intraocular Pharmacokinetics of Intravitreal Aflibercept (Eylea) in a Rabbit Model

“…[6][7][8][9][10][11][12] This resulted in our recent study investigating the detailed intraocular PK properties of intravitreally administrated VEGF-Trap, a prototype of VEGF Trap-Eye, by the use of a conventional immunoassaybased rabbit model. 3 However, although the sequences of VEGF-Trap and VEGF Trap-Eye are similar and show differences in only 5.3% (25 of 476) of the amino acids, these differences iovs.arvojournals.org j ISSN: 1552-5783 might result in differences in their intraocular PK properties. 1,3 Moreover, the commercially available VEGF Trap-Eye, Eylea, (which is widely used in clinical practice) passes through several manufacturing processes, which also might affect its intraocular PK properties.…”

“…3 However, although the sequences of VEGF-Trap and VEGF Trap-Eye are similar and show differences in only 5.3% (25 of 476) of the amino acids, these differences iovs.arvojournals.org j ISSN: 1552-5783 might result in differences in their intraocular PK properties. 1,3 Moreover, the commercially available VEGF Trap-Eye, Eylea, (which is widely used in clinical practice) passes through several manufacturing processes, which also might affect its intraocular PK properties. Hence, in this study, we investigated the intraocular PK properties of aflibercept (Eylea) in the same experimental setting described in our previous PK studies for bevacizumab, ranibizumab, and VEGF-Trap to provide comparable PK data of aflibercept with that of bevacizumab, ranibizumab, and VEGF-Trap.…”

“…Aflibercept has greater binding affinity to VEGF than does ranibizumab or bevacizumab, which indicates longer duration of action for aflibercept in the eyes. [1][2][3] However, unlike that for ranibizumab and bevacizumab, data for the intraocular pharmacokinetics (PK) of aflibercept are scarce. A rabbit model-based PK study reported intravitreal PK properties of intravitreally administrated I-124-labeled aflibercept by the use of positron emission tomography/computed tomography (PET/CT) imaging; the intravitreal half-life of I-124-aflibercept was 4.58 days, which was similar to the manufacturer data of 4.79 days.…”

“…Hence, in this study, we investigated the intraocular PK properties of aflibercept (Eylea) in the same experimental setting described in our previous PK studies for bevacizumab, ranibizumab, and VEGF-Trap to provide comparable PK data of aflibercept with that of bevacizumab, ranibizumab, and VEGF-Trap. 3,6,7 …”

Diabetic macular oedema: pathophysiology, management challenges and treatment resistance

“…These drugs may also be more effective earlier in the natural history of DMO. When the sham arm in RISE/RIDE was switched to a From rabbit animal model data [108] ranibizumab after 24 months, the gains in vision were less than in those started on ranibizumab earlier [88]. Previous studies of treatment-resistant neovascular age-related macular degeneration (nAMD) have shown benefit in switching therapy from one anti-VEGF drug to another, prompting others to investigate this approach in DMO [93].…”