Drug intelligence / Profile preview

cyclosporine + loteprednol

Development stage
Phase 3
Lead developer
ImprimisRx
Modality
Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Ophthalmic, Topical
01

Overview

Cyclosporine + loteprednol is a fixed-dose combination ophthalmic suspension containing cyclosporine (an immunosuppressant calcineurin inhibitor) and loteprednol etabonate (a corticosteroid). This preservative-free formulation is designed for topical use in the eye, primarily to manage dry eye disease and ocular surface inflammation. Cyclosporine acts by inhibiting T-cell activation and reducing inflammatory cytokines on the ocular surface, thereby improving tear production and reducing chronic inflammation. Loteprednol etabonate provides rapid anti-inflammatory effects by suppressing multiple inflammatory pathways, including inhibition of phospholipase A2 activity, which reduces prostaglandin and leukotriene synthesis; it is metabolized quickly in ocular tissues to minimize steroid-related side effects such as increased intraocular pressure or cataract formation[1][2][3]. The combination aims to provide both immediate symptom relief (from the steroid) and long-term disease control (from the immunomodulator), with clinical studies showing faster improvement in dry eye symptoms compared to cyclosporine alone[1][2][5]. This product has not been reviewed or approved by the FDA as a fixed-dose combination but is available as a compounded medication.

Brand names
Klarity CL
Other names
cyclosporine 0.1% + loteprednol etabonate 0.2%cyclosporine-loteprednol ophthalmic suspension
02

Targets

PPIA (Peptidyl-prolyl cis-trans isomerase A)CN (Calcineurin)GR (Glucocorticoid receptor)

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