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A recombinant fusion protein that suppresses neovascularization and decreases vascular permeability.
Used to treat forms of macular degeneration and edema and myopic choroidal neovascularization via intravitreal injection.
Following intravitreal administration, plasma concentrations at 1-3 days are low (0 to 0.05 microngram/mL) and undetectable at 2 weeks. This concentration is between 50 and 500 times lower than necessary to have some systemic effect. In addition, it binds to the vascular endothelial growth factor forming an inert complex that, like other proteins, is degraded by protein catabolism. It does not accumulate after repeated doses every 4 weeks (EMA 2017).
Its very high molecular weight explains the negligible passage to breast milk observed (Juncal 2020), since molecules of more than 800 - 1,000 Da do not pass into breast milk (Hale).
Due to its protein nature it is inactivated in the gastrointestinal tract, not being absorbed, so its oral bioavailability is practically nil, except in premature babies and the immediate neonatal period when there may be greater intestinal permeability.