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Amlexanox, a potential new metabolic agent

amlexanox aphthtab lexanox obesity diabetes

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#1 8bitmore

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Posted 11 February 2013 - 02:27 PM


Seems a new pathway have been found to combat diabetes and obesity, from article: "Amlexanox appears to work in mice by inhibiting two genes -- IKKE and TBK1 -- that we think together act as a sort of brake on metabolism,".

I wonder whether these two genes have other implications when it comes to efficiency of metabolism. Does anyone here have experience with taking Amlexanox or any of the variants and if so.. what were/are the results/side-effects/etc.?!

Sources:
http://www.scienceda...30210143250.htm
http://en.wikipedia.org/wiki/Amlexanox
http://www.nature.co...ll/nm.3082.html
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#2 Turnbuckle

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Posted 11 February 2013 - 04:40 PM

I see nothing but a 5% paste available in the US. I suppose it won't take long before someone begins selling it in capsules.

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#3 8bitmore

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Posted 11 February 2013 - 05:43 PM

I see nothing but a 5% paste available in the US. I suppose it won't take long before someone begins selling it in capsules.


Same-same for Europe; I guess someone with access (mostly past language barrier) to Japanese market could buy the Solfa brand tablets which consist of 25mg Amlexanox according to search engines. Also, on the subject of searching; while I was looking for oral formulations of AMLX (just curiosity at this stage) I found this study on guinea pigs which seems to suggest that oral use is safer than topical use and might help to avoid sensitization issues with the topical agent if pre-administered.

#4 Logic

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Posted 12 February 2013 - 07:57 AM

Good find!
From Wiki; it seems to already be available in pill form:

Amlexanox (trade name Aphthasol) is a medication with antiallergic and anti-inflammatory effects used in the treatment of aphthous ulcers (canker sores). Amlexanox is also available in Japan as oral tablets (trade name Solfa) for treatment of bronchial asthma, where it has been marketed by the Takeda Pharmaceutical Company since 1987, though Aphthtab by Egyptian Eva pharma also exist. In India it is available as Lexanox by Macleods Pharmaceuticals Ltd. In Bangladesh it is marketed by Square Pharmaceuticals as Apsol.

Dosage??

Edited by Logic, 12 February 2013 - 08:05 AM.


#5 Lufega

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Posted 12 February 2013 - 01:44 PM

I read about it yesterday. Very interested. Any online Japanese pharmacies sell this stuff? (doubt it).

#6 8bitmore

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Posted 12 February 2013 - 02:42 PM

I read about it yesterday. Very interested. Any online Japanese pharmacies sell this stuff? (doubt it).


Ah yes, I would really like to see Takeda Pharmaceutical Company's original Solfa tablets sold online as well.. feeling more than iffy about this option: http://top-biochem.e...x_TOP_PURE.html -- but then again.. it is TOP PURE ;)

Edited by 8bitmore, 12 February 2013 - 02:43 PM.


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#7 Turnbuckle

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Posted 14 February 2013 - 03:50 PM

I read about it yesterday. Very interested. Any online Japanese pharmacies sell this stuff? (doubt it).


Ah yes, I would really like to see Takeda Pharmaceutical Company's original Solfa tablets sold online as well.. feeling more than iffy about this option: http://top-biochem.e...x_TOP_PURE.html -- but then again.. it is TOP PURE ;)


Since the page says the minimum order is 100 g, I asked for a quote on that, but there was no response.

#8 8bitmore

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Posted 16 February 2013 - 09:06 PM

I read about it yesterday. Very interested. Any online Japanese pharmacies sell this stuff? (doubt it).


Ah yes, I would really like to see Takeda Pharmaceutical Company's original Solfa tablets sold online as well.. feeling more than iffy about this option: http://top-biochem.e...x_TOP_PURE.html -- but then again.. it is TOP PURE ;)


Since the page says the minimum order is 100 g, I asked for a quote on that, but there was no response.


Hmm, odd, the few times I have used Alibaba the responses have been very immediate (although hard to understand at times, still big language barrier between china/west): all the same; I did a search on the overall Alibaba site and the following popped up too (also min. of 100g): http://www.alibaba.c...68302_57_8.html
Overall I am really impressed with the capacity and width of expertise (synthesizing-wise) with these Chinese companies, I would really like to have access to good independent lab to do tests for reasonable fees before really getting into using them - I think a company with the right expertise would have a hell of niche open to them if they chose to pursue "independent transparent testing for end-users".

#9 Turnbuckle

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Posted 18 February 2013 - 11:47 AM

This is the response from Shaanxi TOP Pharm Chemical Co., Ltd.--

1)Conmmodity: Amlexanox

2)CAS NO. :68302-57-8

3)MOQ: 100g

4)specification: Enterprise Standard

5)unit price: US$ 1.50/g FOB Shanghai.
US$ 1.93/g CIF USA by EMS (door to door )

6)Packaging Details: 100g/bag

7)Delivery Time: within 3 days after your payment

8)price vailded time : 7 days

9)Payment Terms: T/T

10)COA,enclosed.



If anyone wants the full contact info, send me a message.
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#10 MrHappy

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Posted 20 February 2013 - 09:17 PM

I would like to see a human study on amlexanox treating alzheimer's disease. Could be a panacea.

#11 fubarama

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Posted 25 April 2013 - 05:40 AM

I'm overweight even though I keep calories low, eat a healthy diet and exercise more than most people, and I have type-2 diabetes. I also get canker sores now and then. I asked my endocrinologist to prescribe apthasol paste for the canker sores and told her I hoped it would help me lose weight and alleviate diabetes. She had never heard of it, but she was cautiously sympathetic. It's off the formulary for my health insurance plan, so I have to pay for it. $40 for a five gram tube, 5% active ingredient. They said they would have to order it from their wholesaler and they weren't sure they would be able to get it at all.

I paid the $32 for the full text of the article in Nature Medicine, learned that the mice got either 100 mg./kg./day or 25 mg./kg./day. The lower dose seemed to work just as well.

Sad to say, at 25 mg./kg./day, I'd need about 2.5 grams per day of the active ingredient. A 5 gram tube of 5% contains 250 mg. and it's a twelve day supply if you use it every day, so I'll be getting about 20 mg./day or 0.2 mg./kg./day.

Nevertheless... The active ingredient works systemically, not locally, even though it's applied to the gums as a paste. If it's potent enough to rapidly heal canker sores, maybe it's potent enough to partly remedy metabolic syndrome, even at low doses. Time will tell. I'll report back.

#12 MrHappy

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Posted 25 April 2013 - 08:16 AM

I'm overweight even though I keep calories low, eat a healthy diet and exercise more than most people, and I have type-2 diabetes. I also get canker sores now and then. I asked my endocrinologist to prescribe apthasol paste for the canker sores and told her I hoped it would help me lose weight and alleviate diabetes. She had never heard of it, but she was cautiously sympathetic. It's off the formulary for my health insurance plan, so I have to pay for it. $40 for a five gram tube, 5% active ingredient. They said they would have to order it from their wholesaler and they weren't sure they would be able to get it at all.

I paid the $32 for the full text of the article in Nature Medicine, learned that the mice got either 100 mg./kg./day or 25 mg./kg./day. The lower dose seemed to work just as well.

Sad to say, at 25 mg./kg./day, I'd need about 2.5 grams per day of the active ingredient. A 5 gram tube of 5% contains 250 mg. and it's a twelve day supply if you use it every day, so I'll be getting about 20 mg./day or 0.2 mg./kg./day.

Nevertheless... The active ingredient works systemically, not locally, even though it's applied to the gums as a paste. If it's potent enough to rapidly heal canker sores, maybe it's potent enough to partly remedy metabolic syndrome, even at low doses. Time will tell. I'll report back.


Thanks! Please keep us updated.

Also, have you explored a ketogenic diet as an option?

#13 fubarama

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Posted 25 April 2013 - 03:33 PM

Also, have you explored a ketogenic diet as an option?


Yes of course. Every time I discuss this topic on the internet, I encounter half a dozen highly enthusiastic advocates for low carb diets.

I went way low on carbs for about a year. 25 to 35 grams per day. I was able to have more or less normal blood glucose readings without insulin or other meds. I lost about 30 lbs in six months, couldn't lose any more after that, though I was still too fat. I was eating too much red meat. I was often nauseated and light-headed, and otherwise felt vaguely ill much of the time. I was always vaguely hungry and vaguely nauseated. I was somewhat irritable and dysphoric much of the time. Being around tempting carbs, like maybe in a grocery store, made me insane. I had to run away. I was lass active, physically and mentally, less productive in my work. After about a year, I couldn't stand to live that way any more. I decided to return very cautiously to normal eating, keeping the calories low, eating as healthily as possible. I did all that, but my blood sugar shot up almost immediately, and I regained the lost weight within six months or less, despite my best efforts.

In my work, I often talk with people who desperately need to lose weight. About half of them have tried a low-carb diet at one time or another. My story is typical, almost universal. I can't understand how the enthusiasm for low carb diets persists on the internet year after year. It's been going on for twenty years now.

But let's not start that debate. I'm here to talk about Apthasol.

fubarama
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#14 revenant

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Posted 26 April 2013 - 04:12 AM

Thanks 8bit, this is very interesting. I am thinking this drug could possibly defang senescent cells to some degree. Here is another link: http://www.rxlist.co...harmacology.htm

#15 Gerd

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Posted 26 June 2013 - 10:33 PM

@fubarama,

Would you mind sharing this article from Nature Medicine?

#16 nbourbaki

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Posted 04 September 2013 - 05:20 PM

Has anyone tried a therapeutic dose and what were the results?

#17 soupishness

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Posted 21 October 2013 - 01:57 AM

Has anyone tried a therapeutic dose and what were the results?


I ordered 100x50mg Sol-fa tablets, I've been taking it for the last 5 days. I initially planned on taking 200 mg per day, but I found out it is also extremely effective at eliminating the itching and inflamation of my psoriasis, and greatly reduces the plaque build-up.This only lasts for about 2 hours per 100mg dose. So I've been taking 800 mg per day. Unfortunately, I'm afraid it's too effective for weight loss at this dose. I've lost 9 lbs so far, 241-232. I ate heavily on the first day, normally for 2, fasted for one, and normally again today. Yesterday, I lost 4 lbs, measured after eating 2 meals today. Anywhere I have a good deal of adipose tissue, my upper arms, stomach, thighs, butt, is warm, and has a dull ache. I've also developed petechiae on the skin over those areas. So I'm not going to try using it for psoriasis anymore, and will cut it back to 200mg. Hopefully these petechiae will clear up. I also had diarrhea for the first two days but that has stopped.

Edited by soupishness, 21 October 2013 - 02:09 AM.

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#18 blood

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Posted 21 October 2013 - 08:30 AM

Has anyone tried a therapeutic dose and what were the results?


I ordered 100x50mg Sol-fa tablets, I've been taking it for the last 5 days. I initially planned on taking 200 mg per day, but I found out it is also extremely effective at eliminating the itching and inflamation of my psoriasis, and greatly reduces the plaque build-up.This only lasts for about 2 hours per 100mg dose. So I've been taking 800 mg per day. Unfortunately, I'm afraid it's too effective for weight loss at this dose. I've lost 9 lbs so far, 241-232. I ate heavily on the first day, normally for 2, fasted for one, and normally again today. Yesterday, I lost 4 lbs, measured after eating 2 meals today. Anywhere I have a good deal of adipose tissue, my upper arms, stomach, thighs, butt, is warm, and has a dull ache. I've also developed petechiae on the skin over those areas. So I'm not going to try using it for psoriasis anymore, and will cut it back to 200mg. Hopefully these petechiae will clear up. I also had diarrhea for the first two days but that has stopped.


Fascinating.

How did you decide on a dose of 200 mg/ day?

Please continue to update us with your progress!

#19 soupishness

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Posted 21 October 2013 - 01:02 PM

Fascinating.

How did you decide on a dose of 200 mg/ day?

Please continue to update us with your progress!


200 mg = ~100 kg * 25 mg/kg * 3/37(mouse to human body surface area normalization factor)

Though in the study, the mice were injected with amlexanox, rather than taking orally, so I expected I would need a few times more. Perhaps I wont. I'll see how I progress at 200mg.

#20 Gerd

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Posted 21 October 2013 - 02:59 PM

Hi,

Wouldn't one calculate the normalization factor on body weight instead of body surface area?
But 1000 mg would also have been my estimation because in mice there was no big drop in effect when the smaller dose was used.

Regards,
Gerd
P.S.:
And KUDOS on trying that stuff in such a dose.

#21 soupishness

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Posted 21 October 2013 - 05:48 PM

Hi,

Wouldn't one calculate the normalization factor on body weight instead of body surface area?
But 1000 mg would also have been my estimation because in mice there was no big drop in effect when the smaller dose was used.

Regards,
Gerd
P.S.:
And KUDOS on trying that stuff in such a dose.



It's a normalization of the weight(where the 100kg came in) with the body surface area. I havent posted enough to include links, but you can google "Dose translation from animal to human studies revisited.", for a more detailed explanation of how this relates to metabolic rates. You'll get way too high a dose doing a straight bodyweight to bodyweight conversion.


#22 Gerd

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Posted 21 October 2013 - 06:31 PM

Hi,

The metabolic rate does not necessarily correlate with surface ares. Ok, also not necessarily with body weight.
I assume one would have to look for similar plasma or tissue levels.

Actually those values (plasma level vs. daily dose) should be known for humans due to amlexanox being approved in Japan.
Don't know if those levels were measured in the mouse studies...

Regards,
Gerd

#23 soupishness

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Posted 21 October 2013 - 08:26 PM

"The animal dose should not be extrapolated to a human equivalent dose (HED) by a simple conversion based on body weight, as was reported. For the more appropriate conversion of drug doses from animal studies to human studies, we suggest using the body surface area (BSA) normalization method. BSA correlates well across several mammalian species with several parameters of biology, including oxygen utilization, caloric expenditure, basal metabolism, blood volume, circulating plasma proteins, and renal function."

#24 Gerd

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Posted 21 October 2013 - 08:52 PM

How about hepatic function?
Excretion rate of thousands of different API?

IMO the importatn thing is the level of the drug in the target tissue.
If you can not measure this, you might go with rude assumptions. If you can measure it, forget normalization factors.

IIRC, the approved dose in Japan is up to 300mg. If 200mg would suffice for weight loss, wouldn't someone have appreciated this effect while about to treat allergic rhihitis?
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#25 soupishness

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Posted 21 October 2013 - 09:22 PM

Anorexia 食欲不振 is listed as a side effect of Sol-faソルファ tablets at 1-5%.

edit: looks like this forum doesn't support Japanese text.

Edited by soupishness, 21 October 2013 - 09:26 PM.


#26 blood

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Posted 21 October 2013 - 11:39 PM

IIRC, the approved dose in Japan is up to 300mg. If 200mg would suffice for weight loss, wouldn't someone have appreciated this effect while about to treat allergic rhihitis?


How do you know people in Japan haven't noticed it has a weight loss side effect at those doses? What prompted researchers to test the compound on obese mice?

#27 soupishness

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Posted 22 October 2013 - 12:30 AM

IIRC, the approved dose in Japan is up to 300mg. If 200mg would suffice for weight loss, wouldn't someone have appreciated this effect while about to treat allergic rhihitis?


How do you know people in Japan haven't noticed it has a weight loss side effect at those doses? What prompted researchers to test the compound on obese mice?


And they weren't just obese mice, ob/ob mice cannot lose their appetite, as they produce no leptin to tell them that they are full. So using them, it's easier to distinguish between weight loss caused by reduced appetite and weight loss through other metabolic processes.
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#28 blood

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Posted 27 October 2013 - 11:51 AM

IIRC, the approved dose in Japan is up to 300mg. If 200mg would suffice for weight loss, wouldn't someone have appreciated this effect while about to treat allergic rhihitis?


How do you know people in Japan haven't noticed it has a weight loss side effect at those doses? What prompted researchers to test the compound on obese mice?


And they weren't just obese mice, ob/ob mice cannot lose their appetite, as they produce no leptin to tell them that they are full. So using them, it's easier to distinguish between weight loss caused by reduced appetite and weight loss through other metabolic processes.


Hi Soupishness,

Did your petechiae clear up?

Are you still on 200 mg/day?

Are you still losing weight at a rapid clip?

#29 soupishness

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Posted 28 October 2013 - 09:30 PM

I got some blood work done. My ALT and AST were both significantly elevated, so it seems liver toxicity was behind the petechiae. They cleared up after 3-4 days after I stopped. I also take Adderall, which I found raises ALT and AST, so combining them probably isn't a good Idea. The liver toxicity wasn't observed in rats until 300 mg/kg, but it was quickly reversible. I'm going to take a few weeks break from both meds, and get an all clear on my liver enzymes, before trying again. Maybe take some vitamin K supplements. I ordered my second set of 100 x 50 mg pills. I'm also going to try ordering 100g of the raw API from China, as at 200 mg a day, $180 a month for the tablets is a bit expensive to sustain for long.

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#30 Nattzor

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Posted 12 November 2013 - 01:03 PM

I got some blood work done. My ALT and AST were both significantly elevated, so it seems liver toxicity was behind the petechiae. They cleared up after 3-4 days after I stopped. I also take Adderall, which I found raises ALT and AST, so combining them probably isn't a good Idea. The liver toxicity wasn't observed in rats until 300 mg/kg, but it was quickly reversible. I'm going to take a few weeks break from both meds, and get an all clear on my liver enzymes, before trying again. Maybe take some vitamin K supplements. I ordered my second set of 100 x 50 mg pills. I'm also going to try ordering 100g of the raw API from China, as at 200 mg a day, $180 a month for the tablets is a bit expensive to sustain for long.


Any updates?

Would also be probably smart to take with some liver protectant if you get elevated enzyme levels.





Also tagged with one or more of these keywords: amlexanox, aphthtab, lexanox, obesity, diabetes

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