Drug intelligence / Profile preview

fursultiamine

Development stage
Phase 1
Lead developer
Takeda
Modality
Small Molecules
Administration
Oral, Intramuscular, Intravenous
01

Overview

Fursultiamine is a synthetic derivative of vitamin B1 (thiamine), specifically a disulfide derivative known as thiamine tetrahydrofurfuryl disulfide (TTFD). It was developed to improve the lipophilicity and bioavailability of thiamine for the treatment of vitamin B1 deficiency, such as beriberi. Fursultiamine is rapidly metabolized into active thiamine after oral administration. Beyond its use in deficiency states, it has been investigated for potential benefits in non-deficiency disorders, including Alzheimer's disease and autism spectrum disorder, with some evidence suggesting mild cognitive improvement and beneficial effects on emotional or mental symptoms in mildly impaired subjects. Mechanistically, it may act as an antioxidant and anti-apoptotic agent by reducing mitochondrial oxidative stress and suppressing apoptosis in cochlear hair cells. Additionally, preclinical studies suggest that it can inhibit cancer stem cell proliferation by downregulating key transcription factors (OCT4, SOX2, NANOG) and ABC transporters involved in chemoresistance. Fursultiamine also shows anti-inflammatory properties by modulating cytokines such as IL‑1β, IL‑6, IL‑8, TNF‑α via inhibition of NF-kB signaling pathways[1][2][3][4][5][6].

Brand names
AdventanAlinamin FBenlipoidBevitol LipophilJudolorLipothiamineDiteftinLinamin
Other names
fursultiamine hydrochloridethiamine tetrahydrofurfuryl disulfidethiamin tetrahydrofurfuryl disulfidefursultiaminafursultiaminum
02

Targets

THTR (Thiamine transporter 1)

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