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loteprednol etabonate
- Development stage
- Approved
- Lead developer
- Bausch + Lomb
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
- Administration
- Ophthalmic, Intranasal
01
Overview
Loteprednol etabonate is a synthetic corticosteroid used primarily as an ophthalmic agent to treat inflammation and pain following ocular surgery and to manage steroid-responsive inflammatory conditions of the eye such as allergic conjunctivitis, uveitis, acne rosacea, superficial punctate keratitis, herpes zoster keratitis, iritis, cyclitis, and selected infective conjunctivitides. It is also available as a nasal spray for seasonal allergic rhinitis. Loteprednol etabonate was developed using retrometabolic drug design as a "soft" steroid—its structure allows it to be predictably metabolized into inactive substances after exerting its effect. The drug acts by binding with high affinity to the cytosolic glucocorticoid receptor (GR), modulating gene expression to upregulate anti-inflammatory proteins and repress proinflammatory proteins. This results in inhibition of inflammatory cytokines and mediators while stabilizing cell membranes and reducing leukocyte migration[4][5][6][8]. Its design minimizes systemic absorption and side effects compared with other corticosteroids.
- Brand names
- AlrexEysuvisInveltysLotemaxZyletLoterex
- Other names
- loteprednol
02
Targets
GR (Glucocorticoid receptor)
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