Benfotiamine (rINN, or S-benzoylthiamine O-monophosphate) is a synthetic S-acyl derivative of thiamine (vitamin B1).
It is marketed as a dietary supplement in most of the developed world, and as a pharmaceutical drug in some countries for treating diabetic neuropathy under the trade name Milgamma
and others. Combination drugs with pyridoxine or cyanocobalamin are also marketed in a few countries.
Benfotiamine is primarily marketed as an antioxidant dietary supplement.
In some countries it is marketed as a drug to treat diabetic neuropathy; clinical trials results are mixed, finding it mildly useful or no different from placebo.
There is little published data on adverse effects; in one study of a combination drug of benfotiamine, pyridoxine, and cyanocobalamin, around 8% of people taking the drug experienced nausea, dizziness, stomach ache and weight gain.
Benfotiamine is more bioavailable than thiamine salts, providing higher levels of thiamine in muscle, brain, liver, and kidney.
Benfotiamine is dephosphorylated to S-benzoylthiamine by ecto-alkaline phosphatases present in the intestinal mucosa, and is then hydrolyzed to thiamine by thioesterases in the liver.
Benfotiamine mainly acts on peripheral tissues through an increase in transketolase activity.
Benfotiamine is a synthetic S-acyl Vitamin B1 analogue; its chemical name is S-benzoylthiamine O-monophoshate. Benfotiamin is a lipid derivative of thiamine vitamin. It has very low solubility in water or other aqueous solvents. .
As of 2017, benfotiamine was marketed as a pharmaceutical drug in Argentina, Bosnia & Herzegowina, Bulgaria, Colombia, Czech Republic, Estonia, Georgia, Germany, Hong Kong, Hungary, India, Indonesia, Japan, Latvia, Lithuania, Poland, Portugal, Romania, Serbia, Slovakia, Slovenia, Russian Federation, Taiwan, and Vietnam under the following brand names: Benalgis, Benfogamma, Benforce, Benfotiamina, Biotamin, Biotowa, Milgamma
, and Vilotram.
It was also marketed in some jurisdictions as a combination drug with cyanocobalamin as Milgamma
, in combination with pyridoxine as Milgamma
, in combination with metformin as Benforce-M, and with thiamine as Vitafos.
Benfotiamine has been studied in laboratory models of diabetic retinopathy, neuropathy, and nephropathy, As of 2015 there had been one clinical study of benfotiamine in diabetic nephropathy.
Administration of benfotiamine may increase intracellular levels of thiamine diphosphate, a cofactor of transketolase, and based on metabolic theories of Alzheimers, it has been studied in preclinical models of Alzheimers disease.