Just a brief "mini-update" adding a bit more information and also addressing a few of the comments further up (re: efficacy). The following post from the ATA-petition thread has a pdf-document included as an attachment file:
www.tinnitustalk.com/threads/retigabine-trobalt-potiga-%E2%80%94-petition-to-the-ata.6896/page-8#post-103579
Not many people opened it (just 28 in a period of a month or so) despite alerts being sent internally on TinnitusTalk. However, those who did open it may have noticed that the introduction reads as follows:
In the above excerpt, I have specifically underlined a couple of sentences. The attentive reader will know why. There are a number of professors who reviewed the thesis, and while Team Trobalt does not disclose sources, I can at least say that none of the professors mentioned are behind the quote in this post of mine that I referred to yesterday:
www.tinnitustalk.com/threads/retigabine-trobalt-potiga-%E2%80%94-petition-to-the-ata.6896/page-4#post-80103
However, the paper is still very relevant due to affiliations and the last line "
In vivo and
in vitro testing is underway to determine efficacy" provides a clue as to why that is.
I should also mention that the summary of what tinnitus is (see pages 17-19) is first rate. You will not find many family-, ENT-, or neurologist- physicians in the world who can account for the description of tinnitus as provided in this document.
Those who are interested in chemistry (and tinnitus) will appreciate the document very much, I am sure. As pertains to efficacy, I should mention that Trobalt is a so-called dirty-drug (= wide spectrum MoA). I have tracked down a few testimonials in relation to this, and there seems to be differences of opinion (at the professor-level) as to whether a high selectivity compound is better than a dirty drug for the treatment of tinnitus. I can, however, say that one professor mentioned that he/she considered Kv7.x-channels to be more important than Kv3.x-channels in relation to the treatment of symptoms of tinnitus.
In relation to SF0034, I can specifically mention the following:
SciFluor Life Sciences, LLC presented new preclinical data for SF0034, a novel potassium channel opener for the treatment of partial-onset seizure. Results show that SF0034 demonstrated a five-fold increase in potency, improved selectivity and a favorable pharmacological profile in a series of in vitro and in vivo preclinical models compared to ezogabine, a therapy currently approved in the U.S. and other global markets for the treatment of partial-onset seizure. SF0034 is one of the lead compounds in the expanding SciFluor portfolio of Fluoropeutics(TM). SciFluor scientists have discovered small-molecule new chemical entities (NCEs) by strategically introducing fluorine or fluorine groups into the molecular structure of known compounds directed toward precedented biological targets. SciFluor utilizes the incorporation of fluorine to create drugs with improved pharmacological profiles that provide important benefits over existing therapies. SF0034 was discovered by incorporating fluorine into ezogabine, an approved treatment for partial-onset seizure that must be administered three times a day. Data show that SF0034 is five times more potent with decreased QTc liabilities and a more balanced excretion pro le. In addition, SF0034 is less active at the potassium channel that causes urinary retention, potentially alleviating a key side effect of ezogabine.
Anyway, I have now shared what I know. I will update the forum if I learn more from SciFluor Life Sciences LLC.
attheedgeofscience
06/MAY/2015.