Amlexanox is the active ingredient in a common topical treatment for recurrent aphthous ulcers of the mouth (canker sores), reducing both healing time and pain. Amlexanox 5% paste is well tolerated, and is typically applied four times per day directly on the ulcers. A 2011 review found it to be the most effective treatment of the eight treatments investigated for recurrent canker sores. It is also used to treat ulcers associated with Behçet disease.
The chemical itself is an odorless, white to yellowish-white powder.
The 5% preparation for patient use is an adherent beige paste, and it is also available in some countries as a tablet that adheres to the ulcer in the mouth.
Amlexanox applied to an aphthous ulcer is largely absorbed through the gastrointestinal tract; an insignificant amount enters the bloodstream through the ulcer itself. After a single 100 mg dose, mean maximum serum concentration occurs 2.4 +/- 0.9 hours after application, with a half-life of elimination (through urine) of 3.5 +/- 1.1 hours. With multiple daily applications (four doses per day), steady state serum levels occur after one week, with no accumulation occurring after four weeks.
The patent for its use as a treatment for aphthous ulcers was issued in November 1994 to inventors Kakubhai R. Vora, Atul Khandwala and Charles G. Smith, and assigned to Chemex Pharmaceuticals, Inc.
^Oral, E. A., Reilly, S. M., Gomez, A. V., Meral, R., Butz, L., Ajluni, N., ... & Rus, D. (2017). Inhibition of IKKɛ and TBK1 improves glucose control in a subset of patients with type 2 diabetes. Cell Metabolism, 26(1), 157-170. doi:10.1016/j.cmet.2017.06.006
^US patent 5362737, Kakubhai R. Vora, Atul Khandwala, Charles G. Smith, "Methods of treating aphthous ulcers and other mucocutaneous disorders with amlexanox", assigned to Chemex Pharmaceuticals, Inc.
^Burgess JA, van der Ven PF, Martin M, Sherman J, Haley J (2008). "Review of over-the-counter treatments for aphthous ulceration and results from use of a dissolving oral patch containing glycyrrhiza complex herbal extract". J Contemp Dent Pract. 9 (3): 88–98. doi:10.5005/jcdp-9-3-88. PMID18335124.