The first and only EU-approved ciclosporin eyedrop has arrived – what does this mean for patients with severe keratitis in dry eye disease?
sponsored by Santen Pharmaceuticals
There’s currently a considerable unmet need amongst people with severe dry eye disease (DED): obtaining effective treatment (1). Diagnosis can be challenging when a significant proportion of patients with DED present with discordance between signs and symptoms (2) although thankfully, improved diagnostic algorithms and questionnaires are helping to identify more of those patients with the severe forms of the disease who are in need of an intervention (3).
But what are those interventions? Unlike milder forms of DED that can be managed with tear substitutes, lubricant drops or gels for symptom relief, more severe forms of DED are driven by a vicious circle of inflammatory processes that need something more than artificial tears to dampen the disease (4). Without causal treatment, this vicious circle can lead to severe damage to the corneal epithelium (5). Corticosteroids can perform that function, but have a poor side effect profile (especially with chronic use), and risk raising patients’ intraocular pressure or inducing cataract formation (6).
The other way to dampen inflammation is to use ciclosporin-containing eyedrops (7), but this has been a challenge in the EU so far due to the absence of an approved, commercially available product.
That was yesterday’s challenge. Ikervis, 1 mg/mL ciclosporin (Santen) has recently received marketing approval in the EU for the “treatment of severe keratitis in adult patients with dry eye disease, which has not improved despite treatment with tear substitutes” (8–10). The posology is simple: a single drop into each affected eye once daily at bedtime (8). Ikervis has a three-year shelf-life, is supplied in single-dose containers (8), and Ikervis is now approved for use in the EU.
The formulation is worth a closer look. Ikervis is a cationic oil-in-water emulsion of ciclosporin, based on Santen’s Novasorb technology (11). The positively charged nano-sized droplets of the emulsion electrostatically adhere to the negatively charged mucins on the ocular surface, thereby improving ocular retention and absorption (Figure 1), and the lipids in the formulation support the stabilization of the tear film, too (11). The fact that the droplets are nano-sized is important: as droplet size reduces, the surface area to volume ratio increases, meaning a greater total surface area of the emulsion is exposed to the ocular surface – in essence, the eye “sees” more of the eyedrop. This has been demonstrated in rabbits (12) – Ikervis (1 mg/mL ciclosporin) administration results in corneal ciclosporin concentrations around four times greater than that of an anionic emulsion of 0.5 mg/mL ciclosporin. That is why the innovative cationic formulation of Ikervis makes once-a-day dosing possible (8).
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