期刊
EXPERT REVIEW OF NEUROTHERAPEUTICS
卷 16, 期 3, 页码 259-277出版社
TAYLOR & FRANCIS LTD
DOI: 10.1586/14737175.2016.1140039
关键词
tau phosphorylation inhibitors; tau aggregation inhibitors; dementia; immunotherapy; TRx0237; microtubule-stabilizing agents; leuco-methylthioninium; tau protein; Alzheimer's disease; methylthioninium
资金
- Ministero della Salute
- I.R.C.C.S. Research Program
- Ricerca Corrente
- Linea Malattie complesse e terapie innovative [2]
- Programmi di Ricerca Scientifica di Rilevante Interesse Nazionale (PRIN) [2009E4RM4Z]
Small molecular weight compounds able to inhibit formation of tau oligomers and fibrils have already been tested for Alzheimer's 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.
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