An evaluation of hydromethylthionine as a treatment option for Alzheimer's disease.

Abstract

INTRODUCTION:

Alzheimer's disease (AD) is a major cause of morbidity worldwide and its prevalence is expected to rise. Previous studies involving compounds that target the accumulation of amyloid β protein have been unsuccessful, renewing interest in therapies directed against intracellular deposits of tau proteins. Derived from methylene blue, hydromethylthionine is a tau aggregation inhibitor that recently emerged as a promising disease-modifying treatment for AD.

AREAS COVERED:

Herein, the authors cover the chemistry, pharmacodynamics and pharmacokinetics of hydromethylthionine and its oxidized form methylthionine chloride (MTC) that was first studied, as well as clinical efficacy and safety of hydromethylthionine in the treatment of mild to moderate AD.

EXPERT OPINION:

Randomized clinical trials with hydromethylthionine failed to show any impact of the doses used on the disease course. Data analysis from a non-randomized cohort showed that a smaller dose of the drug previously thought to be ineffective and used as placebo, prescribed as monotherapy rather than as add-on to AD approved symptomatic therapies may slow cognitive decline. This finding was further confirmed by a pharmacokinetic analysis study showing a dose/response relationship with doses around 16 mg daily. Future trials need to study the pharmacological properties of hydromethylthionine and ascertain the optimal safe and effective dose to be used.

• Authors: Nader Nael Hashweh, Zachary Bartochowski, Rita Khoury, George T Grossberg
• Journal: Expert opinion on pharmacotherapy (Expert Opin Pharmacother) Vol. 21 Issue 6 Pg. 619-627 (Apr 2020) ISSN: 1744-7666 [Electronic] England
• PMID: 32037892 (Publication Type: Journal Article, Review)

Chemical References

• Amyloid beta-Peptides
• Protein Aggregates
• tau Proteins
• hydromethylthionine
• Methylene Blue

Topics

• Alzheimer Disease (drug therapy, metabolism)
• Amyloid beta-Peptides (metabolism)
• Animals
• Cognitive Dysfunction (prevention & control)
• Cohort Studies
• Disease Progression
• Dose-Response Relationship, Drug
• Humans
• Methylene Blue (adverse effects, analogs & derivatives, pharmacokinetics, therapeutic use)
• Protein Aggregates (drug effects)
• Randomized Controlled Trials as Topic
• Treatment Outcome
• tau Proteins (metabolism)