Amlexanox

Medical uses

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.

In Japan, it is used to treat bronchial asthma, allergic rhinitis and conjunctivitis.

Contraindications

The drug is contraindicated in those with known allergies to it.

Adverse effects

Amlexanox may cause a slightly painful stinging or burning sensation, nausea or diarrhea.

Mechanism of action

Its mechanism of action is not well-determined, but it might inhibit inflammation by inhibiting the release of histamine and leukotrienes.

Chemistry

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.

Pharmacokinetics

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.

History

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.

Society and culture

Economics

A 2011 review found a one-week supply of amlexanox 5% paste to cost $30.

Research

A review found that, , robust studies investigating its effectiveness alongside other canker sore treatments were still needed.

Because it is an inhibitor of the protein kinases TBK1 and IKK-ε, which are implicated in the etiology of type II diabetes and obesity, amlexanox may be a candidate for human clinical trials testing in relation to these diseases.

Synthesis

References

References

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5. (2005). "Amlexanox for the treatment of recurrent aphthous ulcers". Clinical Drug Investigation.
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9. (February 2009). "Amlexanox". U.S. National Library of Medicine.
10. (July 2012). "Dermatologic Aspects of Behcet Disease Treatment & Management". Medscape.
11. Plewa MC. (March 2012). "Pediatric Aphthous Ulcers Treatment & Management". Medscape.
12. (2009). "Amlexanox". U.S. National Library of Medicine.
13. "Methods of treating aphthous ulcers and other mucocutaneous disorders with amlexanox".
14. "Amlexanox". U.S. National Library of Medicine.
15. (March 2013). "An inhibitor of the protein kinases TBK1 and IKK-ɛ improves obesity-related metabolic dysfunctions in mice". Nature Medicine.
16. (September 2009). "The protein kinase IKKepsilon regulates energy balance in obese mice". Cell.