PAN-90806 / PanOptica - LARVOL DELTA

Discovery of novel thiophene-3-carboxamide derivatives as potential VEGFR-2 inhibitors with anti-angiogenic properties. (PubMed, Bioorg Chem) - "This study reports a series of novel thiophene-3-carboxamide derivatives based on PAN-90806 as VEGFR-2 inhibitors, among which compound 14d exhibits excellent anti-proliferative activity against HCT116, MCF7, PC3, and A549 cell lines, and has effective VEGFR-2 inhibitory activity with an IC50 value of 191.1 nM...Molecular docking and molecular dynamics simulations had shown that compound 14d could stably bind to the active site of VEGFR-2. These results confirmed that compound 14d might be a promising lead compound for anti-angiogenesis."

Journal • Oncology

Vascular Endothelial Growth Factor Antagonists: Promising Players in the Treatment of Neovascular Age-Related Macular Degeneration. (PubMed, Drug Des Devel Ther) - "Abicipar pegol, a designed ankyrin repeat protein (DARPin), demonstrated the ability to maintain stable visual acuity with 12-week dosing, but was not approved by the FDA due to higher than usual rates of intraocular inflammation. Conbercept, a recombinant anti-VEGF fusion protein, has been approved in China, and is in Phase 3 trials globally. KSI-301 is an anti-VEGF antibody biopolymer conjugate that allowed 66% of nAMD patients to maintain at least a 6-month treatment-free interval in Phase 1b studies. OPT-302, an inhibitor of VEGF-C/D, will be tested in phase 3 studies that compare anti-VEGF-A monotherapy against combination therapy with OPT-302. Faricimab is a bispecific anti-VEGF/Ang-2 antibody that upregulates the Tie-2 signaling pathway and promotes vascular stability; it is undergoing phase 3 trials with potential for 12- or 16-week dosing. PAN-90806 is a topical anti-VEGF agent that showed the ability to reduce injection frequency by 79% compared to ranibizumab..."

Journal • Review • Age-related Macular Degeneration • Complement-mediated Rare Disorders • Gene Therapies • Immunology • Inflammation • Macular Degeneration • Ophthalmology • Retinal Disorders • Wet Age-related Macular Degeneration • VEGFC

Emerging Therapies in Neovascular Age-Related Macular Degeneration in 2020. (PubMed, Asia Pac J Ophthalmol (Phila)) - "For nAMD: Abicipar pegol, an intravitreal anti-vascular endothelial growth factor based on designed ankyrin repeat proteins (DARP) in protein, is currently pending approval. Conbercept and Faricimab, 2 intravitreal anti-growth factors, are currently in phase 3. Nine other upcoming agents have at least produced results in the 2A phase including intravitreal injections (KSI-301, OPT-302, RGX-314, ICON-1, and DE-122), depot (GB-102), drug reservoir (PDS), topical drops (PAN-90806), and oral formulations (AKST4290). We summarize all the newer molecules."

Journal • Age-related Macular Degeneration • Complement-mediated Rare Disorders • Gene Therapies • Ophthalmology • Retinal Disorders • Wet Age-related Macular Degeneration

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,..."

Journal

PanOptica anti-VEGF eye drop shows promise in treatment of neovascular (wet) AMD (Businesswire) - P1/2; N=51; "At the Ophthalmology Innovation Summit at the American Academy of Ophthalmology annual meeting (OIS@AAO) in San Francisco, the company presented topline results from a Phase 1/2 dose-ranging clinical trial in which PAN-90806...demonstrate both safety and biological response as monotherapy in treatment-naïve patients with neovascular age-related macular degeneration (wet AMD)...'The Phase 1/2 safety results and findings associated with anti-VEGF biological activity suggest that a topical eye drop may make anti-VEGF therapy safer, less burdensome, and more sustainable by helping patients avoid the frequent intravitreal injections that current regimens require,' commented Allen C. Ho, MD, FACS...'Once-daily topical ocular PAN-90806 creates the opportunity to change the wet AMD treatment paradigm by potentially improving patient adherence, reducing losses to follow-up, and maintaining early patient benefits obtained with initial injection...

Media quote • P1/2 data

Study of PAN-90806 Eye Drops, Suspension for Neovascular AMD (clinicaltrials.gov) - P1/2; N=51; Completed; Sponsor: PanOptica, Inc.; Enrolling by invitation ➔ Completed

Clinical • Trial completion