SciFluor Receives US Patent for KCNQ2/3 Activator to Treat Epilepsy and Neurological Disorders

Well, my tinnitus keeps decreasing over the months in which I take trobalt. I can very well believe the KV7 channels are important along with the KV3 channels. Remember I mix keppra with trobalt then again I take campral too.

 

IMPORTANT INFORMATION

As earlier indicated, I have been in contact with the CEO of SciFluor Life Sciences regarding SF0034. Dr. Amirana responded to my mail saying he would look into my query and get back to me. Unfortunately that did not happen (despite follow-up from my side). However, as I predicted earlier on in this thread, the researcher behind the compound (SF0034) is Prof. Tzounopolous (a very well known figure within the tinnitus research circles). This evening, I received the following e-mail from him:

The abstract of the above research paper (which was released just today) reads:

Why it has been possible to find pharmacological presentations on the compound already since a while is something I do not fully understand e.g. read the following post of mine from earlier on in this thread - and which has two pdf-attachments with detailed descriptions of the pharmacology of SF0034 (and which originate from SciFluor Life Sciences themselves):

www.tinnitustalk.com/threads/scifluor-receives-us-patent-for-kcnq2-3-activator-to-treat-epilepsy-and-neurological-disorders.7743/#post-113245

With the 30M dollars of capital recently raised by SciFluor it would be my opinion that a clinical trial of SF0034 is likely to be imminent. Given that SF0034 is a derivative of Trobalt, it may also mean that any upcoming clinical trial will be expedited and possibly accept patients (as opposed to only healthy volunteers) in a phase-I trial (indeed this was one of the questions for the CEO - but to which, I do not have the answer, of course). Below the full list of questions I asked (but did not receive a response to):

1) Will SF0034 head into a clinical trial in 2015?
2) Will a trial of SF0034 be conducted specifically in order to attempt to determine efficacy in relation to tinnitus (or just epilepsy)?
3) Is SF0034 expected to be geared as a treatment against tinnitus also (off-label) provided the clinical trial of epilepsy will be successful?
4) Assuming a trial will go ahead, will it start off as a phase-I trial, and will that be open to only healthy volunteers (or will it accept patients with conditions for which SF0034 is geared)?
5) As SF0034 is a derivative of an existing drug, will that allow the trial to become accelerated?
6) A fluorinated drug would have a better safety profile, correct?


attheedgeofscience
10/JUN/2015.

 

great work @attheedgeofscience!

 

A bit more information on SF0034 and clinical trial timelines (the following information is very recently released):

 

also, that bit about it hERG is cool. hERG is a cardiac Kv channel, so this will eliminate whatever heart issues people had, although from my understanding the threat to the heart was not too big an issue at the dosages we were taking.

 

Dont get that - for example @dan took it only twice - a 50mg pill of trobalt once and then again later in the day. He reported major heart palpitations. He has not taken it since due to his fear of what it may be doing to his heart.

 

this drug seems like you could take it and go about your day (hopefully with some appreciable effect on your T). trobalt made most tasks very difficult for me.

also, since we know the chemical structure of this drug, it may be possible to get a chinese synthesis of it. i wonder if it SciFlours flourination compound is essential for the synthesis of this drug.

 

If that were really possible then could we not raise the funds for this on TT and get it done in those chinese labs so that we members can try it rather than wait the years before it goes on trials and then gets hopefully approved? Or is that just as much a fantasy as getting it made in the chinese labs? hopefully not........is yours permanently lowered from the troblat locoyeti? @Danny Boy seems to have a permanent lowering as he has been off Troblalt for a few days now and his T has stayed down...he is still on Keppra though.......

 

Ok so they have deisgned SF0034 by incorporating a fluorine substituent in the 3-position of the tri-aminophenyl ring of retigabine. This appears to make it more selective in that it only affect K2/K3 channels and not K4/5 and furthermore is more potent and less toxic, reducing the excitability of CA1 hippocampal ( pyramid?)neurons that appear responsible for tinnitus. it appears that clinical trials will be necessary, from Ph 1 to Ph 3 given the profile of retigabine. There may be some flexibility on the Part of the FDA, that would need to agreed between the parties. As the market for tinnitus treatments is of the same order as epilepsy, it would make comercial sense for Sci Flour to evaluate it for both.

The timeline is never seamless for drug development, there will always be roadblocks, no matter how promising the drug.

 

Why SciFluor doesn't advertise it for tinnitus? Only epilepsy?

 

The original molecule from which their derivative is based of is advertised for epilepsy as well.

They do mention SF00034 for tinnitus.

http://www.scifluor.com/our-approach/our-approach-fluoro.php

 

guys


i ve think we ve discussed this somewhere but i don t find the thread so i m opening it here:

http://medicalxpress.com/news/2015-06-quiet-brain-drug-relief-epilepsy.html

A new drug may treat epilepsy and prevent tinnitus by selectively affecting potassium channels in the brain, UConn neurophysiologist Anastasios Tzingounis and colleagues report in the 10 June Journal of Neuroscience.


Epilepsy and tinnitus are both caused by overly excitable nerve cells. Healthy nerves have a built-in system that slams on the brakes when they get too excited. But in some people this braking system doesn't work, and the nerves run amok, signaling so much that the brain gets overloaded and has a seizure (epilepsy) or hears phantom ringing (tinnitus). About 65 million people worldwide are affected by epilepsy. The numbers on tinnitus are not as clearcut, but the American Tinnutus Association estimates 2 million people have tinnitus so disabling they have troubling functioning in daily life.

The existing drugs to treat epilepsy don't always work and can have serious side effects. One of the more effective, called retigabine, helps open KCNQ potassium channels, the "brakes" that shut down the signaling of overly excited nerves. Unfortunately, retigabine has awful side effects. Because of this, it's usually only given to adults who don't get relief from other epilepsy drugs.

Several years ago, doctors around the world began reporting infants with severe, brain-damaging seizures. Genetic testing showed that the children with this problem had genetic differences in their KCNQ potassium channels. Most existing anti-seizure drugs don't work for these children, and few want to give babies retigabine because of its side affects, which include sleepiness, dizziness, problems with urination and hearing, and an unnerving tendency to turn people's skin and eyes blue.

Tzingounis began working in 2013 with Thanos Tzounopoulos, a tinnitus expert at the University of Pittsburgh, on a new drug candidate. The drug, SF0034, was chemically identical to retigabine, except that it had an extra fluorine atom. A company called SciFluor had developed SF0034, and wanted to know whether the compound had promise against epilepsy and tinnitus. The two researchers thought the drug had the potential to be much better than retigabine.

The most important question to answer was whether SF0034 works on KCNQ potassium channels the same way retigabine does, and if so, was it better or worse that its parent compound? KCNQ potassium channels are found in the initial segment of axons, long nerve fibers that reach out and almost, but don't quite, touch other cells. The gap between the axon and the other cell is called a synapse. When the cell wants to signal to the axon, it floods the synapse with sodium ions to create an electrical potential. When that electrical potential goes on too long, or gets out of hand, the KCNQ potassium channel kicks in. It opens, potassium ions flood out, and the sodium-induced electrical potential shuts down. In some types of epilepsy, the KCNQ potassium channels have trouble opening and shutting down runaway electrical potentials in the nerve synapse. Retigabine helps them open.

There are five different kinds of KCNQ potassium channels in the body, but only two are important in epilepsy and tinnitus: KCNQ2 and KCNQ3. The problem with retigabine is that it acts on other KCNQ potassium channels as well. That's why it has so many unwanted side effects.

Tzingounis and Tzounopoulos first tested SF0034 in neurons, and found that it was more selective than retigabine. It seemed to open only KCNQ2 and KCNQ3 potassium channels, not affecting KCNQ 4 or 5. It was more effective than retigabine at preventing seizures in animals, and it was also less toxic.The results are promising, both for research and medicine. SciFluor now plans to start FDA trials with SF0034 and see if it is safe and effective in people. Treating epilepsy is the primary goal, but tinnitus can be similarly debilitating, and sufferers would be thrilled to have a decent treatment.

Tzingounis is pleased as well. "This [SF0034] gives me another tool, and a better tool, to dissect the function of these channels," Tzingounis says. "And we need to find solutions for kids—and adults—with this problem," he says.

 

http://medicalxpress.com/news/2015-06-quiet-brain-drug-relief-epilepsy.html\

 

...which proves that Retigabine has an effect lowering T.
Promising.

 

Haha...I think we all knew that. This sounds promising, although, how long will it take for this to come out? How long until Autifony or GSK lawsuit them?

 

I came to the point that Trobalt does not have any effect on tinnitus 0% but helps me sleep very vell

Is there a place to offer yourself to be guineapig ?

 

Hopefully they won't. We need that treatment/cure. So the more variants there are out there the better it is. It makes it easier to tailor suit treatments if you have more then one tool to treat patients.

 

I was just wondering more about the patents? Wouldn't this drug infringe on Autifony especially? Just wondering about the legality.

 

Well if they've managed to patent it then there shouldn't be any grounds for a lawsuit.

 

It might not have any effect on YOUR tinnitus. I don't think there will ever be a single ONE cure or treatment. Tinnitus is a complex ailment and can be caused by a number of reasons. And even if Autifony, Otonomy, Auris Medical and others manage to get their drugs on to the market they will not work for everyone. Or one of them might but not others. If you know what I mean?

Also Trobalt is a kind of a dirty drug so to speak. It's not as specific as the ones that are tested. It's like going to the butcher for a surgery. But as we don't have any surgeons yet it's the best we can do for now.

 

In America yes, the rest of the world? No.

 

Since Autifony is British we can only hope they act like it.

By the way. Dr. Large....dat name

 

Well, Doctor Large surely won't be happy hahahahha. Anyway, that KV2 channels is notorious for fluid retention and can cause kidney failure.

 

Maybe it can be used with other medications. Drinking Alcohol causes excessive production of urine so maybe a cheeky little mix?

 

I'll just stick with Autifony and the KV3 channels. Nice to have other drugs though.

 

Yeah, drugs are nice.

 

Trobalt isn't though lol

 

@Christian78 what was the cause of your T?

 

You investigative brillant people all of you in this tread. Love you all!!

 

damaged hearing on high freq left ear, and on 6khz, i got it when i got one medicine

Medicine is developed for all for very rich people...