Tau-directed approaches for the treatment of Alzheimers disease: Focus on leuco-methylthioninium

Davide Seripa, Vincenzo Solfrizzi, Bruno P. Imbimbo, Antonio Daniele, Andrea Santamato, Madia Lozupone, Giovanni Zuliani, Antonio Greco, Giancarlo Logroscino, Francesco Panza

Risultato della ricerca: Contributo in rivistaArticolo in rivista

24 Citazioni (Scopus)


Small molecular weight compounds able to inhibit formation of tau oligomers and fibrils have already been tested for Alzheimers disease (AD) treatment. The most advanced tau aggregation inhibitor (TAI) is methylthioninium (MT), a drug existing in equilibrium between a reduced (leuco-methylthioninium) and oxidized form (MT+). MT chloride (also known as methylene blue) was investigated in a 24-week Phase II study in 321 mild-to-moderate AD patients at the doses of 69, 138, and 228 mg/day. This trial failed to show significant positive effects of MT in the overall patient population. The dose of 138 mg/day showed potential benefits on cognitive performance of moderately affected patients and cerebral blood flow in mildly affected patients. A follow-up compound (TRx0237) claimed to be more bioavailable and less toxic than MT, is now being developed. Phase III clinical trials on this novel TAI in AD and in the behavioral variant of frontotemporal dementia are underway.
Lingua originaleEnglish
pagine (da-a)259-277
Numero di pagine19
RivistaExpert Review of Neurotherapeutics
Stato di pubblicazionePubblicato - 2016


  • Alzheimer Disease
  • Alzheimer's disease
  • Clinical Trials as Topic
  • Humans
  • Methylene Blue
  • Neurology (clinical)
  • Neuroscience (all)
  • Pharmacology (medical)
  • TRx0237
  • dementia
  • immunotherapy
  • leucomethylthioninium
  • methylthioninium
  • microtubule-stabilizing agents
  • tau Proteins
  • tau aggregation inhibitors
  • tau phosphorylation inhibitors
  • tau protein


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