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Methylene blue is an oxidation-reduction agent used for the treatment of pediatric and adult patients with acquired methemoglobinemia. Historically, it has been widely used in Africa to treat malaria, but now it disappeared when chloroquine (CQ) and other drugs entered the market.
- Mechanism
- Curator reviewed · 2 references
Main mechanism of action involves the inhibition of nitric oxide synthase and guanylate cyclase. In Alzheimers Disease: a mechanistic study found that methylene blue oxidizes cysteine sulfhydryl groups on tau to keep tau monomeric. One preclinical treatment study in tauopathy mice reported anti-inflammatory or neuroprotective effects mediated by the Nrf2/antioxidant response element (ARE); another reported insoluble tau reduction and a learning and memory benefit when given early. In Methemoglobinemia: Methylene Blue acts by reacting within RBC to form leukomethylene blue, which is a reducing agent of oxidized hemoglobin converting the ferric ion (fe+++) back to its oxygen-carrying ferrous state(fe++). As antimalarial agent: Methylene Blue, a specific inhibitor of P.falciparum glutathione reductase has the potential to reverse CQ resistance and it prevents the polymerization of haem into haemozoin similar to 4-amino-quinoline antimalarials. For ifosfamide induced neurotoxicity: Methylene blue functions as an alternate electron acceptor. It acts to reverse the NADH inhibition caused by gluconeogenesis in the liver while blocking the transformation of chloroethylamine into chloroacetaldehyde. In addition, it inhibits various amine oxidase activities, which also prevents the formation of chloroacetaldehyde. Methylene blue is a reversible inhibitor of monoamine oxidase A.
- Primary indication
- Indicated for the treatment of pediatric and adult patients with acquired methemoglobinemia.Curator reviewed · 7 structured indications
- Formula / weight
- C16H18ClN3S · 319.85 g/mol (avg)
- First approval
- Canada, 2000 · United States, 2016 · European Union, 2016
- Also known as
- Basic Blue 9 · C.I. basic blue 9 · Methylthioninium chloride
- Code names
- CI-52015 · NSC-617593 · TRX-0014
- Brand names
- Hyophen
- Phosphasal
- Provayblue
- Proveblue
- Urelle
- Uribel
- Urimar Reformulated Oct 2013
- Urin DS
- Urogesic Blue Reformulated Apr 2012
- Ustell
Resolves to
CXKWCBBOMKCUKX-UHFFFAOYSA-MSMILES[Cl-].CN(C)C1=CC2=[S+]C3=C(C=CC(=C3)N(C)C)N=C2C=C1What you can answer from here — as of September 23, 2026
Which drugs share a target with Methylene blue, and which of those have an active Phase 3 trial?