Drug intelligence / Profile preview

sulbutiamine

Development stage
Unknown
Lead developer
Servier
Modality
Small Molecules
Administration
Oral
01

Overview

Sulbutiamine is a synthetic derivative of thiamine (vitamin B1) developed in Japan in the mid-1960s as a treatment for asthenia and beriberi[4][7]. It consists of two modified thiamine molecules joined to form a dimer, making it highly lipophilic and able to cross the blood-brain barrier more efficiently than standard thiamine[3][7]. Once inside the body, sulbutiamine is hydrolyzed to release thiamine, which increases levels of thiamine and its phosphate esters (such as ThMP and ThTP) in the brain[4][8]. This action supports energy metabolism by facilitating pyruvate decarboxylation to acetyl-CoA within the citric acid cycle, thus enhancing ATP production[6][8]. Sulbutiamine has been shown to modulate dopaminergic and glutamatergic neurotransmission, potentially improving memory formation, neuromuscular efficiency, learning capacity, and resistance to fatigue[3][5][6]. Its primary clinical use is for treating asthenia (fatigue/weakness), though it has also been explored for cognitive enhancement and other off-label uses. The drug is marketed under brand names such as Arcalion.

Brand names
ArcalionVitaberin
Other names
sulbutiaminebisibutiaminvitaberin
02

Targets

Kainate-type ionotropic glutamate receptorTHTR (Thiamine transporter 1)DRD1 (Dopamine D1 Receptor)

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