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lipoic acid choline ester
- Development stage
- Discontinued
- Lead developer
- Novartis
- Modality
- Small Molecules
- Administration
- Ophthalmic
01
Overview
Lipoic acid choline ester (EV06/UNR844) is a first-in-class, topically administered small molecule prodrug designed to treat presbyopia by restoring lens elasticity. Developed by Encore Vision and later acquired by Novartis, the drug penetrates the cornea and is hydrolyzed into lipoic acid and choline. Lipoic acid is then reduced to dihydrolipoic acid within the lens, where it acts to break chemically induced disulfide bonds between crystallin proteins. These disulfide cross-links are a primary cause of age-related lens stiffening; by reducing them, the drug aims to restore the lens's ability to change shape (accommodation), thereby improving near vision. Despite promising early results, Novartis terminated development in 2022 after the Phase 2 LUCID trial failed to meet its primary endpoint.
- Brand names
- Dioptin
- Other names
- lipoic acid choline ester chloridedi-lipoic acid choline ester
02
Targets
P-SH (Crystallin sulfhydryl group)
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