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Laquinimod Eye Drops Show Safety and Penetration in Phase I LION Trial

Topical laquinimod reaches posterior eye tissues with dose-related distribution and good tolerability in patients preparing for vitrectomy

Active Biotech has just released encouraging topline results from its LION Phase I trial, marking a step forward for treating non-infectious inflammatory eye disease with topical therapy. The study asked whether laquinimod in eye drop form could safely reach both front and back parts of the eye and at levels likely to be therapeutically useful.

The trial involved patients who were already scheduled to undergo pars plana vitrectomy for various elective reasons. Over a two-week preoperative period, they received daily doses of laquinimod eye drops at three different strengths: low, medium, and high. The primary goals were safety, tolerability, and measurement of drug concentrations in different intraocular compartments.

The findings were promising. The higher dose levels delivered dose-related concentrations of laquinimod not only in the anterior chamber but also in the vitreous humor, the part of the eye toward the back that is often harder for topical treatments to reach. That means the drug is able to penetrate far enough to potentially influence disease processes in the posterior segment. The treatment was well tolerated: there were no dose-limiting toxicities in any group, and adverse events were mild or moderate.

These results are important because many inflammatory eye diseases affect the posterior segment, and delivering medication there usually requires injections or systemic administration. Topical therapy that is safe and effective could improve patient comfort, reduce risks tied to more invasive routes, and simplify treatment protocols.

Moving forward, Active Biotech is now seeking partners to continue development of laquinimod eye drops for inflammatory eye disorders. Key next steps will include defining optimal dosing, confirming efficacy in disease settings (not just preoperative situations), and demonstrating long-term safety, especially in the posterior segments of the eye where the tissue is more fragile.

For clinical researchers the LION trial reinforces a few themes: first, that topical formulations are increasingly being explored for eye disease beyond mild anterior inflammation. Second, that measuring intraocular drug levels is essential to understanding whether a therapy has true potential in posterior inflammation. Third, safety remains a critical hurdle, especially when delivering drugs to sensitive tissues inside the eye.

All in all, the LION results offer tangible reason for optimism. If further trials confirm efficacy and long-term safety, laquinimod eye drops might become a less invasive option for patients with posterior eye inflammation.

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