Benfotiamine (BFT)

Benfotiamine is a synthetic, lipid-soluble S-acyl derivative of thiamine (vitamin B1) that serves as a highly bioavailable prodrug [3, 9]. Upon oral administration, it is dephosphorylated by alkaline phosphatases in the intestinal tract and absorbed via passive diffusion, leading to significantly higher intracellular levels of thiamine pyrophosphate (TPP) compared to water-soluble thiamine [1, 5, 12]. TPP is a critical cofactor for enzymes such as transketolase, pyruvate dehydrogenase, and alpha-ketoglutarate dehydrogenase, which are essential for glucose metabolism [2, 8, 15]. By activating transketolase, benfotiamine helps reduce the accumulation of toxic glucose metabolites and advanced glycation end-products (AGEs), which are primary drivers of microvascular damage in diabetes [4, 10, 11]. Consequently, it is widely used to treat diabetic complications, including neuropathy, retinopathy, and nephropathy, and is under investigation for neuroprotective effects in Alzheimer's disease [6, 7, 13]. Although it is a therapeutic agent rather than a biological target, its ability to modulate metabolic flux and suppress oxidative stress makes it a significant tool in managing metabolic and degenerative disorders [1, 10].

Other names

S-benzoylthiamine O-monophosphateBenzoylthiamine monophosphateBTMPBenphothiamineS-benzoylthiamine-O-monophosphateBiotamin

Benfotiamine is a lipid-soluble prodrug that is converted into thiamine and subsequently into its active coenzyme form, thiamine pyrophosphate (TPP) [1, 3]. TPP acts as a cofactor for the enzyme transketolase, which diverts excess glucose metabolites from the glycolytic pathway into the pentose phosphate pathway [2, 8]. This action reduces the formation of advanced glycation end-products (AGEs) and inhibits several pathways of hyperglycemic damage, including the polyol pathway, the protein kinase C (PKC) pathway, and the hexosamine pathway [4, 10, 11].