acrizanib (LHA510) / Novartis - LARVOL DELTA

Acrizanib as a Novel Therapeutic Agent for Fundus Neovascularization via Inhibitory Phosphorylation of VEGFR2. (PubMed, Transl Vis Sci Technol) - "Acrizanib functioned through inhibiting multiple phosphorylation sites of VEGFR2 in endothelial cells to different degrees. These results indicated that acrizanib might hold promise as a potential candidate for the treatment of ocular vascular diseases."

Journal • Inflammation • Retinal Disorders

Safety and Efficacy of Acrizanib in Suppressing Fundus Neovascularization via Inhibitory Phosphorylation of VEGFR2 (ARVO 2023) - "Layman Abstract (optional): Provide a 50-200 word description of your work that non-scientists can understand. Describe the big picture and the implications of your findings, not the study itself and the associated details."

Clinical • Ophthalmology • Retinal Disorders

A randomized, double-masked, multicenter trial of topical acrizanib (LHA510), a tyrosine kinase VEGF-receptor inhibitor, in treatment-experienced subjects with neovascular age-related macular degeneration. (PubMed, Am J Ophthalmol) - "All patients received an intravitreal injection of ranibizumab at baseline and were re-treated when there was evidence of disease recurrence (rescue). Secondary and subgroup analysis did not support evidence of efficacy. Twenty-one of 46 patients administered LHA510 developed a reversible corneal haze that resolved with cessation of treatment and did not recur in patients restarted at once daily frequency In spite of extensive optimization for topical efficacy, LHA510 failed to demonstrate clinical efficacy."

Journal • Age-related Macular Degeneration • Macular Degeneration • Ophthalmology • Retinal Disorders • Wet Age-related Macular Degeneration

"Novartis’s VEGF inhibitor LHA510 shows topical efficacy in vivo. Live from #ARVO20" - Cortellis

Clinical • Preclinical • Biosimilar

Innovative therapies for neovascular age-related macular degeneration. (PubMed, Expert Opin Pharmacother) - "Expert opinion: Long-acting anti-VEGF agents have demonstrated promising results in phase 3 studies, and include Brolucizumab, a single-chain antibody fragment, and Abicipar, a designed ankyrin repeat protein (DARPin). Other unique anti-VEGF agents in current trials include Conbercept - a fusion protein of the VEGF receptor domains, KSI-301 - an anti-VEGF antibody biopolymer conjugate, and OPT-302 - an inhibitor of VEGF-C/D. Strategies to activate the Tie-2 receptor, some in combination with VEGF inhibition, are of interest, with recent trials of Faricimab, ARP-1536, and nesvacumab. Topical anti-VEGF ± anti-PDGF agents, such as pazopanib, squalamine lactate, regorafenib, and LHA510 have shown limited efficacy and/or have not been advanced, although PAN-90806 continues to advance with promising initial results. Sustained-release anti-VEGF treatments, to address treatment burden, include the ranibizumab Port Delivery System, GB-102, NT-503, hydrogel depot,..."

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