X-82 is an oral tyrosine kinase inhibitor that blocks the action of vascular endothelial growth factor and platelet-derived growth factor; might it treat neovascular age-related macular degeneration?
Findings In this phase 1 dose-escalation study of 35 participants, the most common adverse events attributed to oral X-82 were diarrhea (n = 6), nausea (n = 5), fatigue (n = 5), and transaminase elevation (n = 4). The 71% of participants who tolerated X-82 and completed 6 months of treatment averaged 0.68 intravitreous anti–vascular endothelial growth factor rescue injections, with 60% requiring none.
Meaning These results justify further study, and a phase 2 trial has completed recruitment.
Importance An oral treatment for neovascular age-related macular degeneration would be less burdensome than repeated intravitreous injections. X-82 is an oral tyrosine kinase inhibitor active against vascular endothelial growth factor (VEGF) and platelet-derived growth factor.
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