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| Clinical data | |
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| Trade names | Aphthasol |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a601017 |
| Routes of administration | Topical |
| ATC code | |
| Pharmacokinetic data | |
| Eliminationhalf-life | 3.5 hours |
| Excretion | Renal (17%) |
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| CompTox Dashboard(EPA) | |
| ECHA InfoCard | 100.230.878 |
| Chemical and physical data | |
| Formula | C16H14N2O4 |
| Molar mass | 298.298 g·mol−1 |
| 3D model (JSmol) | |
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Amlexanox (trade nameAphthasol) is ananti-inflammatoryantiallergicimmunomodulator used to treat recurrentaphthous ulcers (canker sores), and (in Japan) severalinflammatory conditions. This drug has been discontinued in the U.S.[1]
Amlexanox is the active ingredient in a common topical treatment for recurrentaphthous ulcers of the mouth (canker sores),[2] reducing both healing time[3] and pain.[4] Amlexanox 5% paste is well tolerated,[5] and is typically applied four times per day directly on the ulcers.[3] A 2011 review found it to be the most effective treatment of the eight treatments investigated for recurrent canker sores.[6] It is also used to treat ulcers associated withBehçet disease.[7]
In Japan, it is used to treatbronchial asthma, allergicrhinitis andconjunctivitis.[8]
The drug is contraindicated in those with known allergies to it.[3]
Amlexanox may cause a slightly painful stinging or burning sensation, nausea or diarrhea.[3]
Its mechanism of action is not well-determined, but it might inhibit inflammation by inhibiting the release ofhistamine andleukotrienes.[8] It has been shown to selectively inhibitTBK1 andIKK-ε, producing reversible weight loss and improved insulin sensitivity, reduced inflammation and attenuated hepatic steatosis without affecting food intake in obese mice.[9] It produced a statistically significant reduction inglycated hemoglobin andfructosamine in obese patients withtype 2 diabetes andnonalcoholic fatty liver disease[10]
The chemical itself is an odorless, white to yellowish-white powder.[8]
The 5% preparation for patient use is an adherent beige paste,[3][8] and it is also available in some countries as a tablet that adheres to the ulcer in the mouth.[4]
Amlexanox applied to an aphthous ulcer is largely absorbed through thegastrointestinal tract; an insignificant amount enters thebloodstream through the ulcer itself. After a single 100 mg dose, mean maximumserum 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.[8]
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.[11]
A 2011 review found a one-week supply of amlexanox 5% paste to cost $30.[6]
A review found that, as of July 2011[update], robust studies investigating its effectiveness alongside other canker sore treatments were still needed.[12]
Because it is aninhibitor of theprotein kinasesTBK1 andIKK-ε,[9] which are implicated in theetiology oftype II diabetes andobesity,[13] amlexanox may be a candidate for human clinical trials testing in relation to these diseases.[9]
