Clinical data | |
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Trade names | Aphthasol |
AHFS/ Drugs.com | Monograph |
MedlinePlus | a601017 |
Routes of administration | Topical |
ATC code | |
Pharmacokinetic data | |
Elimination half-life | 3.5 hours |
Excretion | Renal (17%) |
Identifiers | |
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CAS Number | |
PubChem CID | |
IUPHAR/BPS | |
DrugBank | |
ChemSpider | |
UNII | |
KEGG | |
ChEBI | |
ChEMBL | |
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 name Aphthasol) is an anti-inflammatory antiallergic immunomodulator used to treat recurrent aphthous ulcers (canker sores), and (in Japan) several inflammatory conditions. This drug has been discontinued in the U.S. [1]
Amlexanox is the active ingredient in a common topical treatment for recurrent aphthous 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 with Behçet disease. [7]
In Japan, it is used to treat bronchial asthma, allergic rhinitis and conjunctivitis. [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 of histamine and leukotrienes. [8] It has been shown to selectively inhibit TBK1 and IKK-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 in glycated hemoglobin and fructosamine in obese patients with type 2 diabetes and nonalcoholic 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 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. [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 an inhibitor of the protein kinases TBK1 and IKK-ε, [9] which are implicated in the etiology of type II diabetes and obesity, [13] amlexanox may be a candidate for human clinical trials testing in relation to these diseases. [9]