Figure 6: Efficacy of engineered variants of LAVA1 in the rabbit retinal vascular leakage model.
From: Long-acting protein drugs for the treatment of ocular diseases
Variants of LAVA1 that were engineered to be resistant to proteolysis (LAVA2, 3, 45 and 46) all potently inhibited fluorescein leakage and had terminal vitreal levels similar to LAVA1 when administered 20 days before fluorescein angiography. In contrast, non-glycosylated variants of LAVA1 (LAVA24 and LAVA25) minimally inhibited fluorescein leakage. The numbers in boxes above the datapoints are the mean terminal drug levels in the vitreous. LAVA24 and LAVA25 had terminal levels that were 39-fold lower than LAVA1. Terminal vitreal levels measured in ng ml−1 were converted to pmoles per eye using a molecular weight of 59 kDa for all LAVAs. Vitreal volume in rabbit was assumed to be 1.25 ml.
