Amlexanox #98190

Amlexanox is an anti-allergic and anti-inflammatory drug that was once commonly used to treat recurrent aphthous ulcers (canker sores). It has also been effective in treating asthma, hay fever, and conjunctivitis, possibly through reducing the release of histamine and leukotriene from leukocytes and mast cells (1). Amlexanox binds (IC₅₀ of approximately 1-2 μM) and inhibits the non-canonical IκB kinases IKK-ε and TANK-binding kinase 1 (TBK1), inhibiting inflammation. Studies in obese mice treated with Amlexanox show that mice develop increased thermogenesis, producing increased insulin sensitivity and weight loss. These findings suggest a potential role for Amlexanox in the treatment of diabetes, obesity, and related disorders (2). Further, Amlexanox has demonstrated anti-cancer properties in numerous mouse models and appears to bind to at least 12 different enzyme and non-enzyme proteins (3). Binding of Amlexanox to the molecular chaperone HSP90 inhibits C-terminal chaperone activity and disrupts the multichaperone complex (4), while interaction with the calcium-binding proteins S100A12 and S100A13 is associated with an inhibition of FGF1 release and reduced cell migration and proliferation (5).