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Bucillamine is an orally bioavailable small molecule derivative of the amino acid cysteine, containing two donatable thiol groups. It acts as a potent antioxidant and anti-inflammatory agent, primarily by replenishing intracellular glutathione (GSH) levels and increasing GSH activity, which protects against oxidative stress and injury. Bucillamine also inhibits Nuclear factor kappa-light-chain-enhancer of activated B cells (NF-kappaB) to reduce inflammatory mediator expression and has immunomodulatory effects on T cells and macrophages. Originally developed in Japan from tiopronin, it has been used for over 30 years in Japan and South Korea for the treatment of rheumatoid arthritis. It is significantly more potent than N-acetylcysteine as a thiol donor. Clinical applications include rheumatoid arthritis, gout, organ transplantation preservation, acute lung injury prevention (including during influenza infection), myocardial infarction protection, seizure activity reduction, and investigational use in COVID-19[1][2][3][4][5][6][7][8].
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