Amlexanox

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.

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

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

Its mechanism of action is not well-determined, but it might inhibit inflammation by inhibiting the release of histamine and leukotrienes. 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. It produced a statistically significant reduction in glycated hemoglobin and fructosamine in obese patients with type 2 diabetes and nonalcoholic fatty liver disease{{cite journal | vauthors = Oral EA, Reilly SM, Gomez AV, Meral R, Butz L, Ajluni N, Chenevert TL, Korytnaya E, Neidert AH, Hench R, Rus D, Horowitz JF, Poirier B, Zhao P, Lehmann K, Jain M, Yu R, Liddle C, Ahmadian M, Downes M, Evans RM, Saltiel AR | display-authors = 6 | title = Inhibition of IKKɛ and TBK1 Improves Glucose Control in a Subset of Patients with Type 2 Diabetes | journal = Cell Metabolism | volume = 26 | issue = 1 | pages = 157–170.e7 | date = July 2017 | pmid = 28683283 | pmc = 5663294 | doi = 10.1016/j.cmet.2017.06.006 }}

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.

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

A review found that, {{asof|2011|7|lc=y}}, 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.

File:Amlexanoxsynthesis.png

{{reflist|35em|refs=

{{cite journal | vauthors = Bailey J, McCarthy C, Smith RF | title = Clinical inquiry. What is the most effective way to treat recurrent canker sores? | journal = The Journal of Family Practice | volume = 60 | issue = 10 | pages = 621–632 | date = October 2011 | pmid = 21977491 | url = http://www.jfponline.com/Pages.asp?AID=9930 }}

{{cite journal | vauthors = Bell J | title = Amlexanox for the treatment of recurrent aphthous ulcers | journal = Clinical Drug Investigation | volume = 25 | issue = 9 | pages = 555–566 | year = 2005 | pmid = 17532700 | doi = 10.2165/00044011-200525090-00001 | s2cid = 24492356 }}

{{cite journal | vauthors = Gonsalves WC, Chi AC, Neville BW | title = Common oral lesions: Part I. Superficial mucosal lesions | journal = American Family Physician | volume = 75 | issue = 4 | pages = 501–507 | date = February 2007 | pmid = 17323710 | url = http://www.aafp.org/afp/2007/0215/p501.html }}

{{cite journal | vauthors = Kuteyi T, Okwundu CI | title = Topical treatments for HIV-related oral ulcers | journal = The Cochrane Database of Systematic Reviews | volume = 1 | pages = CD007975 | date = January 2012 | pmid = 22258979 | doi = 10.1002/14651858.CD007975.pub2 | veditors = Kuteyi T }}

{{cite web |url=https://www.nlm.nih.gov/medlineplus/druginfo/meds/a601017.html |title=Amlexanox |date=February 2009 |work=MedlinePlus |publisher=U.S. National Library of Medicine |access-date=12 February 2013}}

{{cite web |vauthors=Yousefi M, Ferringer T, Lee S, Bang D | title=Dermatologic Aspects of Behcet Disease Treatment & Management |date=July 2012 |work=Medscape Reference|publisher=Medscape |access-date=14 February 2013 |url=http://emedicine.medscape.com/article/1122381-treatment}}

{{cite web | author = Plewa MC | title=Pediatric Aphthous Ulcers Treatment & Management |date=March 2012 |work=Medscape Reference|publisher=Medscape |access-date=14 February 2013 |url=http://emedicine.medscape.com/article/909213-treatment}}

{{cite patent |country=US |number=5362737 |status=patent |title=Methods of treating aphthous ulcers and other mucocutaneous disorders with amlexanox |pubdate=1994-11-08 |inventor= Vora KR, Khandwala A, Smith CG |assign1=Chemex Pharmaceuticals, Inc.}}

{{cite web |url=https://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?q=all&cid=2161#ec |title=Amlexanox |work=PubChem |publisher=U.S. National Library of Medicine |access-date=12 February 2013}}

{{cite journal | vauthors = Reilly SM, Chiang SH, Decker SJ, Chang L, Uhm M, Larsen MJ, Rubin JR, Mowers J, White NM, Hochberg I, Downes M, Yu RT, Liddle C, Evans RM, Oh D, Li P, Olefsky JM, Saltiel AR | display-authors = 6 | title = An inhibitor of the protein kinases TBK1 and IKK-ɛ improves obesity-related metabolic dysfunctions in mice | journal = Nature Medicine | volume = 19 | issue = 3 | pages = 313–321 | date = March 2013 | pmid = 23396211 | pmc = 3594079 | doi = 10.1038/nm.3082 }}

{{cite journal | vauthors = Chiang SH, Bazuine M, Lumeng CN, Geletka LM, Mowers J, White NM, Ma JT, Zhou J, Qi N, Westcott D, Delproposto JB, Blackwell TS, Yull FE, Saltiel AR | display-authors = 6 | title = The protein kinase IKKepsilon regulates energy balance in obese mice | journal = Cell | volume = 138 | issue = 5 | pages = 961–975 | date = September 2009 | pmid = 19737522 | pmc = 2756060 | doi = 10.1016/j.cell.2009.06.046 }}

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{{Stomatological preparations}}

{{Drugs for obstructive airway diseases}}

Category:Anti-inflammatory agents

Category:Leukotriene antagonists

Category:Carboxylic acids

Category:Isopropyl compounds