Drug intelligence / Profile preview

citicoline

Development stage
Phase 4
Lead developer
Takeda
Modality
Small Molecules
Administration
Oral, Intravenous, Intramuscular, Ophthalmic
01

Overview

Citicoline (cytidine 5'-diphosphocholine) is a naturally occurring endogenous nucleoside that serves as a critical intermediate in the biosynthesis of structural phospholipids in cell membranes, particularly phosphatidylcholine. Upon administration, citicoline is hydrolyzed into cytidine and choline, which cross the blood-brain barrier and are resynthesized into citicoline in the brain. Its neuroprotective mechanism involves the preservation of sphingomyelin and cardiolipin, the restoration of Na+/K+-ATPase activity, and the inhibition of phospholipase A2, which reduces the release of arachidonic acid and subsequent inflammatory mediators. Clinically, it is utilized for the treatment of acute stroke, traumatic brain injury, and cognitive impairment associated with neurodegenerative diseases like Alzheimer's. In many jurisdictions, it is regulated as a pharmaceutical drug, while in others, such as the United States, it is primarily marketed as a dietary supplement for cognitive enhancement.

Brand names
SomazinaCeraxonCognizinNicholinNeuraxionCebrotonCebrol
Other names
Cytidine 5'-diphosphocholineCytidine diphosphate-choline
02

Targets

SLC1A2 (Glutamate Transporter 1)

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