Benfotiamine ( rINN, or ''S''-benzoylthiamine ''O''-monophosphate) is a synthetic, fat-soluble, ''S''-acyl derivative of

thiamine Thiamine, also known as thiamin and vitamin B1, is a vitamin – an Nutrient#Micronutrients, essential micronutrient for humans and animals. It is found in food and commercially synthesized to be a dietary supplement or medication. Phosp ...

(vitamin B1) that is approved in some countries as a medication or

dietary supplement A dietary supplement is a manufactured product intended to supplement a person's diet by taking a pill (pharmacy), pill, capsule (pharmacy), capsule, tablet (pharmacy), tablet, powder, or liquid. A supplement can provide nutrients eithe ...

to treat diabetic sensorimotor polyneuropathy. Benfotiamine was developed in late 1950s in Japan.

Uses

Benfotiamine is primarily marketed as an

over-the-counter drug Over-the-counter (OTC) drugs are medicines sold directly to a consumer without a requirement for a prescription from a healthcare professional, as opposed to prescription drugs, which may be supplied only to consumers possessing a valid pres ...

to treat diabetic polyneuropathy. A 2021 review described two clinical trials with positive results for diabetic polyneuropathy and concluded that more research is needed. As of 2017, benfotiamine was marketed as a

pharmaceutical drug Medication (also called medicament, medicine, pharmaceutical drug, medicinal product, medicinal drug or simply drug) is a drug used to diagnose, cure, treat, or prevent disease. Drug therapy ( pharmacotherapy) is an important part of the ...

in many countries 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 A combination drug is a combination of two or more pharmaceutical drugs as active ingredients combined into a single dosage form, typically as a ''fixed-dose combination'', with each constituent standardized to specifications of a fixed dose. Fix ...

with

cyanocobalamin Cyanocobalamin is a form of Vitamin B12, vitamin used to treat and prevent vitamin B12 deficiency, vitamin deficiency except in the presence of cyanide toxicity. The deficiency may occur in pernicious anemia, following gastrectomy, surgical r ...

as Milgamma, in combination with

pyridoxine Pyridoxine (PN) is a form of vitamin B6 found commonly in food and used as a dietary supplement. As a supplement it is used to treat and prevent pyridoxine deficiency, sideroblastic anaemia, pyridoxine-dependent epilepsy, certain metaboli ...

as Milgamma, in combination with metformin as Benforce-M, and with

as Vitafos.

Adverse effects

There is little published data on adverse effects. In one study of a combination of benfotiamine, pyridoxine, and cyanocobalamin, around 8% of people taking the drug experienced nausea, dizziness, stomach ache and weight gain.

Pharmacology

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 is more bioavailable than thiamine salts, providing higher levels of thiamine in muscle, brain, liver, and kidney. Benfotiamine mainly acts on peripheral tissues through an increase in transketolase activity.

Chemistry

Benfotiamine is a lipid derivative of thiamine, specifically a synthetic S-acyl Vitamin B₁ analogue; its chemical name is S-benzoylthiamine O-monophosphate. It has very low solubility in water or other aqueous solvents.

Research

Benfotiamine has been studied in laboratory models of

diabetic retinopathy Diabetic retinopathy (also known as diabetic eye disease) is a medical condition in which damage occurs to the retina due to diabetes. It is a leading cause of blindness in developed countries and one of the lead causes of sight loss in the wor ...

neuropathy Peripheral neuropathy, often shortened to neuropathy, refers to damage or disease affecting the nerves. Damage to nerves may impair sensation, movement, gland function, and/or organ function depending on which nerve fibers are affected. Neuropa ...

, and nephropathy. A 2021 review of its use for diabetic polyneuropathy described two clinical trials which showed improvements in neuropathic pain and neuropathic symptoms scores, the latter of which showed a dose-response effect. The authors concluded that it could potentially serve as an economical supplement to enhance neuropathy treatment and that more research is needed. Administration of benfotiamine may increase intracellular levels of thiamine diphosphate, a cofactor of

transketolase Transketolase (abbreviated as TK) is an enzyme that, in humans, is encoded by the ''TKT'' gene. It participates in both the pentose phosphate pathway in all organisms and the Calvin cycle of photosynthesis. Transketolase catalyzes two important r ...

. Based on metabolic theories of

Alzheimer's disease Alzheimer's disease (AD) is a neurodegenerative disease and the cause of 60–70% of cases of dementia. The most common early symptom is difficulty in remembering recent events. As the disease advances, symptoms can include problems wit ...

, since thiamine-dependent processes are critical in glucose metabolism and are diminished in brains of Alzheimer's disease patients at autopsy, and since treatment of mouse models of Alzheimer's disease with benfotiamine diminishes plaques, decreases phosphorylation of tau and reverses memory deficits, benfotiamine administration has been proposed as a possible intervention to reverse biological and clinical processes of Alzheimer's disease.

References