Amlexanox

Overall Health Benefits of Amlexanox

• Promotes weight loss [1-4]
• Improves blood sugar levels [1-3] [5]
• Prevents bone loss [6]
• Improves liver health [5] [7-10]
• Treats asthma [11-19]
• Treats mouth ulcers [20-27]

What is Amlexanox?

Amlexanox is a medication with fat-burning properties. It promotes fat loss by inhibiting the production of a specific enzyme in the body that is responsible for fat storage and inflammation. Amlexanox is known to protect against bone disorders and liver disease. It can also help treat certain medical conditions like asthma and mouth ulcers.

How Does Amlexanox Work?

Amlexanox works by inhibiting the release of histamine and leukotrienes – both of which are involved in inflammation and allergic reaction. This medication also helps reduce weight loss by inhibiting TBK1 (TANK-binding kinase 1), an enzyme involved in fat storage and inflammation.

Chemical Structure of Amlexanox

Research on Amlexanox

A. Promotes Weight Loss

The primary benefit of amlexanox is supported by a number of high-quality studies:

1. 1. A study found that amlexanox can help induce fat loss by increasing the energy expenditure of fat cells. [1]
   2. In obese mice, amlexanox improved obesity-related metabolic dysfunctions by increasing thermogenesis (dissipation of energy through the production of heat), improving insulin sensitivity, and decreasing steatosis (fat build-up in the liver). [2]
   3. A study found a reduction in both percent total body fat and percent truncal fat in a group of patients treated with amlexanox compared to the non-treated subjects. [3]
   4. A study reported that amlexanox can help promote weight loss by inhibiting TBK1 (TANK-binding kinase 1), an enzyme involved in fat storage. [4]

B. Improves Blood Sugar Levels

Amlexanox has also been found to exert beneficial effects on blood sugar levels:

1. 1. In obese mice, acute amlexanox treatment suppressed blood sugar production in the liver. [1]
   2. In obese mice, amlexanox decreased blood sugar levels by improving insulin sensitivity. [2]
   3. In obese patients with type 2 diabetes and nonalcoholic fatty liver disease, treatment with amlexanox produced a statistically significant reduction in Hemoglobin A1c, a measure of blood sugar. [3]
   4. In mice fed with a high-fat diet, amlexanox administration for 18 weeks reversed blood sugar and lipid metabolic disturbance. [5]

C. Prevents Bone Loss

Amlexanox may be used for the treatment of bone disorders due to its anti-inflammatory effects.

In one study, researchers investigated the effects of amlexanox on mice with bone loss caused by surgical removal of the ovaries. [6] Results showed that amlexanox inhibited the formation of osteoclasts, which are specialized cells that absorb and remove bone to allow the development of new bones and maintenance of bone strength. Moreover, amlexanox enhanced the production of bone-forming cells known as osteoblasts. These results suggest that amlexanox may be considered a new therapeutic candidate for bone disorders like osteoporosis and rheumatoid arthritis.

D. Improves Liver Health

A number of studies suggest that amlexanox can protect against various types of liver disease:

1. 1. In mice fed with a high-fat diet, amlexanox reversed fat build-up in the liver. [5]
   2. In mice, amlexanox ameliorated acetaminophen-induced acute liver injury by reducing oxidative stress. [7]
   3. In male mice fed with a high-fat diet, amlexanox alleviated steatohepatitis (liver inflammation caused by fat build-up). [8]
   4. In mouse models with obesity-related metabolic dysfunctions, amlexanox mitigated palmitic acid-induced liver toxicity. [9]
   5. In mice, oral administration with amlexanox (25, 50, and 100 mg/kg) attenuated liver scarring caused by the liver toxin carbon tetrachloride. [10]

E. Treats Asthma

Evidence shows that the anti-inflammatory properties of amlexanox can help treat symptoms of asthma:

1. 1. In patients with aspirin-induced asthma, amlexanox significantly improved measures of lung function. [11-12]
   2. Studies found that amlexanox can effectively treat allergic asthma and rhinitis by reducing the levels of inflammatory substances such as histamine, LTB4, LTC4, LTD4, and LTE4. [13-14]
   3. In mice, intranasal and oral administration of amlexanox decreased lung allergic inflammation. [15]
   4. In rats and guinea pigs, amlexanox inhibited experimental asthma by decreasing airway constriction. [16-17]
   5. In mice with lung inflammation, amlexanox improved lung function and structure. [18-19]

F. Treats Mouth Ulcers

Studies also show that amlexanox can safely and effectively treat different types of mouth ulcers:

1. 1. In patients with canker sores, the application of 5% amlexanox topical paste was shown to consistently and significantly speed up complete ulcer healing and the time to pain resolution. [20]
   2. In patients diagnosed with canker sores, application of 5% amlexanox oral paste directly on the ulcer 4 times a day for 6 days resulted in a marked reduction in ulcer size and pain scores. [21]
   3. The administration of OraDisc (active component 2 mg amlexanox) in patients with canker sores resulted in significant improvement in erythema (skin rash caused by inflamed blood capillaries) score, ulcer size, and pain scores. [22]
   4. In patients with recurrent aphthous stomatitis (mouth sores), amlexanox oral adhesive pellicles significantly reduced ulcer size and alleviated ulcer pain. [23]
   5. A clinical trial conducted on 100 patients with canker sores found that amlexanox 5% can reduce the frequency, duration, and symptoms of the condition with no adverse side effects. [24]
   6. In patients with recurrent oral ulcerations, the application of 5% amlexanox paste on the ulcers was found to be superior to placebo with regards to speeding up the rate of healing. [25]
   7. When applied directly to the lesion, 5% amlexanox topical paste at a dose of 100 mg was found to be safe, effective, and well-tolerated. [26]
   8. In immunocompetent patients with mild to moderate canker sores, the application of amlexanox oral paste (Aphthasol) was shown to achieve complete healing of ulcers and resolution of pain in just 3 days. [27]

Associated Side Effects of Amlexanox

Amlexanox side effects are very uncommon. There have been some side effects associated with the use of this drug wherein the patient had one of the issues listed below at some point while being on amlexanox. However, these side effects weren’t confirmed to be associated with the treatment and could have been a coincidence and not related to the use of amlexanox. Despite this, it was listed as a side effect associated with amlexanox even though these associated side effects are very uncommon.

Side effects associated with amlexanox may include the following:

• Rashes
• Itching
• Difficulty breathing
• Tightness in the chest
• Swelling of the mouth, face, lips, or tongue
• Inflammation of the lining of the mouth
• Slight pain, stinging, or burning of the skin
• Nausea
• Diarrhea

References

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2. Reilly SM, Chiang SH, Decker SJ, et al. An inhibitor of the protein kinases TBK1 and IKK-ɛ improves obesity-related metabolic dysfunctions in mice. Nat Med. 2013;19(3):313-321. doi:10.1038/nm.3082.
3. Oral EA, Reilly SM, Gomez AV, et al. Inhibition of IKKɛ and TBK1 Improves Glucose Control in a Subset of Patients with Type 2 Diabetes. Cell Metab. 2017;26(1):157-170.e7. doi:10.1016/j.cmet.2017.06.006.
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