Drug intelligence / Profile preview

benfotiamine

Development stage
Phase 4
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Benfotiamine is a synthetic fat-soluble derivative of thiamine (vitamin B1), specifically an S-acyl derivative known as S-benzoylthiamine O-monophosphate. It is more bioavailable than standard thiamine salts and is primarily used to increase thiamine levels in the body. After oral administration and dephosphorylation in the intestine and liver, it is converted to active thiamine. Its main mechanism involves increasing transketolase activity in peripheral tissues via the pentose phosphate pathway. This action helps reduce hyperglycemic damage by blocking pathways such as hexosamine formation, advanced glycation end product (AGE) formation, and diacylglycerol-protein kinase C activation. Clinically, benfotiamine has been investigated for diabetic neuropathy and other diabetes-related complications; it may improve symptoms of diabetic polyneuropathy but evidence for other indications remains limited[1][3][5][6].

Brand names
BenalgisBenfogammaBenforceBenfotiaminaBiotaminBiotowaMilgammaVilotram
Other names
S-benzoylthiamine O-monophosphate
02

Targets

TKT (Transketolase)

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