Pharmacokinetics of Intravitreally Applied VEGF Inhibitors

Abstract

In addition to topical, periocular, and systemic administration, intravitreal injection has been established in recent years as an additional standard procedure for ophthalmological drug delivery. This route of administration is now most frequently used for the therapy of retinal diseases with inhibitors of the vascular endothelial growth factor (VEGF). Intravitreal administration allows for high drug concentrations in the target tissue while minimizing systemic drug exposure. Depending on properties such as molecular weight and binding capacity to the neonatal Fc receptor, intravitreally applied VEGF inhibitors can exhibit relevant differences in intraocular and systemic pharmacokinetics. Moreover, their pharmacokinetics can be affected by properties of the individual eye such as ocular volume, vitreous liquefaction, and prior vitrectomy. Pharmacokinetics of intravitreally administered drugs determines both duration of ocular effect and degree of systemic exposure and are thus of clinical relevance with regard to reinjection strategy and systemic safety.

Original Publication (in German):

Tim U. Krohne, Frank G. Holz, Carsten H. Meyer. Pharmakokinetik intravitreal applizierter VEGF-Inhibitoren. Der Ophthalmologe. February 2014, Volume 111, Issue 2, pp 113-120. doi: 10.1007/s00347-013-2932-9. © Springer-Verlag Berlin Heidelberg 2013. Republication with kind permission of Springer Science+Business Media