Loteprednol Etabonate for the Treatment of Dry Eye Disease

Abstract

Dry eye disease (DED) is a common ocular condition that can impair vision and may adversely impact quality of life. Due to the inflammatory nature of this disorder, topical corticosteroids are an effective treatment option, particularly for moderate-to-severe DED when first-line treatments, such as ocular lubricants, are insufficient. Loteprednol etabonate (LE) is a retrometabolically designed corticosteroid with a low propensity to cause corticosteroid-related adverse effects, such as elevated intraocular pressure (IOP). This review was conducted to provide an assessment of published studies on the use of LE for treatment of inflammation associated with DED. Twelve prospective and 2 retrospective studies evaluating LE ophthalmic suspension 0.5% and 2 prospective studies evaluating LE ophthalmic gel 0.5% were identified. LE given as monotherapy or with artificial tears (AT) improved signs of DED, especially among patients with a more pronounced inflammatory component, and also improved DED symptoms compared to baseline and/or control. Treatment with LE before cyclosporine A (CsA) therapy reduced stinging upon CsA initiation and provided more rapid relief of DED signs and symptoms than CsA plus AT alone. In patients with meibomian gland dysfunction, LE alone, or in addition to eyelid scrubs/warm compresses, reduced clinical signs and symptoms, and tear proinflammatory cytokine levels. Overall, LE was safe and well tolerated, with minimal effects on IOP. While larger and longerterm studies are warranted, these data support the use of LE as a safe and effective treatment option for DED.

Current Advances in Mechanisms and Treatment of Dry Eye Disease: Toward Anti-inflammatory and Immunomodulatory Therapy and Traditional Chinese Medicine

“…Fluorometholone eye drops (0.1%) is safe and has low incidence of adverse effects ( 136 ). Loteprednol is a new type of glucocorticoid drug ( 137 ) that has recently been approved by the FDA for the treatment of short-term DED ( 138 ). Loteprednol can fully exert therapeutic effects in DED by inducing the inhibition of phospholipase A. Loteprednol has low toxicity with high fat-solubility and good corneal permeability.…”

Potential Therapeutic Role of Pituitary Adenylate Cyclase-Activating Polypeptide for Dry Eye Disease

“…Loteprednol etabonate (LE) is an ocular corticosteroid with improved safety compared with other corticosteroids. LE was synthesized from the modification of an inactive metabolite of prednisolone acetate [ 33 ]. LE undergoes deesterification of an inactive carboxylic acid metabolite after exerting its effect, thus reducing the potential for adverse reactions [ 34 ].…”

Practical Guidance for the Use of Loteprednol Etabonate Ophthalmic Suspension 0.25% in the Management of Dry Eye Disease

“…4 After exerting its therapeutic effects, it is rapidly de-esterified to inactive metabolites reducing risk of adverse reactions. 16 Accordingly, it has been shown to have lower side effect risk of clinically significant intraocular pressure (IOP) elevations with both short-term and long-term use. 17 There have been several studies on the utility of loteprednol etabonate for the treatment of DED.…”