A proprietary formulation of laquinimod for corneal application was developed, taking the specific physico-chemical characteristics of this agent into account, to facilitate that a clinically relevant intraocular therapeutic concentration of laquinimod can be obtained.

The study, which is being conducted by principal investigator Professor Dr Nguyen at the Byers Eye Institute, Stanford University, Palo Alto, CA, US, aims to evaluate if laquinimod when administered as eye drops reaches the anterior and the posterior chambers of the eye, to support further development in patients with Uveitis.

During a 14-day preoperative administration of laquinimod as eye drops, all the three subjects in the first dose group received 0.6mg laquinimod once daily. All subjects, had significant concentrations of laquinimod in vitreous as well as in the anterior chamber fluid when sampled during surgery. This supports distribution of laquinimod from the cornea and sclera into the anterior chamber and onwards to the posterior parts of the eye. These data are also consistent with results previously obtained in rabbits and in an in vitro bovine corneal model of laquinimod penetration into the eye.

The bioanalytical results also show that administration of laquinimod eye drops leads to quantities of laquinimod in vitreous humour at therapeutically relevant concentrations, as determined from prior studies in multiple sclerosis patients. Anecdotally, a potent anti-inflammatory ocular effect of laquinimod was noted in the anterior chamber of one patient following 14-days of application as per the protocol, in absence of any concomitant corticosteroid treatment.

These initial findings are important to the further development of laquinimod for ocular disorders, as they unequivocally establish trans-corneal-scleral passage of laquinimod. The current study design involves enrolling additional patients at different dose-levels with top-line results expected in late 2024/early 2025.

"It is tremendously satisfying to learn that topical laquinimod, even at a low dose, can have the ability to penetrate into the anterior chamber, and more importantly, the vitreous of human eyes," said Quan Đông Nguyen, MD, Professor of Ophthalmology, Medicine and Pediatrics at the Byers Eye Institute and the Stanford University School of Medicine. "The potential applications of a topical formulation and delivery that reaches the vitreous and possibly posterior segment are quite significant and can lead to very important and novel therapeutic implications. Our talented team at Byers and Stanford is very excited to proceed to complete the Study."