• N&PD Moderators: Skorpio | someguyontheinternet

Tesofensine

Ham-milton

Bluelighter
Joined
Jul 20, 2007
Messages
5,746
structure
Tesofensine.png


An obvious cocaine analogue, but probably distant enough to be entirely legal, at least Wikipedia says it's legal. Not that anyone should make a decision that might end them up in court based on what a Wikipedia entry says.

Does anyone know if any abusability studies have been conducted on this one? It seems that these things are done as late as possible in a drugs's life, but it's being looked at as an anorectant, so I suppose the DEA will require these studies.

Too bad these sorts of things aren't commercially available like diphenyl prolinol.
 
i think it's a triple reuptake inhibitor. definitely recreational though
 
Tesofensine is owned by Neurosearch and is in late stage trials for obesity and diabetes and possibly ADHD, I think it has moved recently from phase II to phase III trials. So it will be commercially available fairly soon, but the rights will be owned by neurosearch or their commercial partner so don't expect a generic for a while. Though I doubt their patents would hold if challenged, because the compound has been described in the literature long before neurosearch and there seems to be a distinct lack of a novel step in the neurosearch patents.

It isn't really a cocaine analog more a distant cousin, it has the wrong stereochemistry, the phenyl is attached directly to the ring and the methoxycarbonyl has been replaced with an ether.

Neurosearch have a family of these phenyltropanes, brasofensine being another.

I do not expect any serious abuse potential if it has got to this stage it will have next to none.

V
 
It's fairly clear that Neurosearch are the exclusive holders of this compound, although obvious Boehringer Ingelheim did front some money in the stage 2 trials but then withdrew support since they were only interested in Parkinson's and wernt convinced with the serendiptious discovery that the compound was/is anorectic. I would hazard to guess this might be to do with 5-HT2C agonist activity but this is purely speculative.

In reality I know very little about this but I am eager to try some though i'll probably never have the opportunity to do so. I mean if cocaine is for rich people, tesofensine must be for the super super super elite. I'm pretty sure brasofensine has been abandoned but thats also speculative.

More recent patents have described the X-ray crystallography spectra of methoxymethyl (c.f. ethoxyethyl) salts. If I was a journalist I would say this is indicative that they might be more interested in the MOM compound even though it was not the subject of clinical trials, yet.
 
many anorectics are disqualified for their abuse potential (RE: recreational capacity) so either this company is a bunch of morons not to look at that carefully or this has minimal rec potential

same reason nomifensine was eventually disallowed as a viable pharma

why was brasofensine not pursued even though Phase II were shoing no adverse effects?
 
Making it non-recreational seems to be part of the design. I mean, didn't desoxypipradrol stem from people looking at the pipradrol patents...
 
I would have to think it though similar in effect to Nomifensine and thus would be similar abuse potential which was not overwhelming high perhaps, but perhaps enough to thwart an anorectic as i think FDA will be very inclined to be stricter for that criteria for that class of pharma

the only thing this offers greater than Sibutramine is greater abuse potential having the DA and higher NA capacity and hence i gotta think it will NOT be approved
 
Last edited:
Nomifensine actually got the axe because it causes hemolytic anemia, it was amineptine that got judged to have ''recreational capacity.'' We just have to change peoples brain chemistry so that they see this as a good thing. Amineptine did have some negative side-effects though, so it wasnt all bad news that these dopaminergic agents fell by the wayside.
 
I think there's a bit of exageration about amineptines abuse liability. If you like to take a pill for three days and get high on the fourth, I suppose there's something to it, but not enough for me.
 
Amineptine was being abused. Initially the PDR (or French equivalent) noted that it should not be prescribed to people with a history of drug abuse. I think that a peek at the patents would be in order. Nomifensine has an aromatic amine group which very generally speaking is not a good thing...
 
But it wasn't abused in any way similar to other stimulants. I've tasted it quite a bit in the past few months, but there's no similarity to dose wait 60 minutes enjoy.

Definitely toward the end of a week I was euphoric as hell, but there's so much seperation between action and consequence that I don't think it can be compared to other drugs in it's league. If it's in that league.

Anyway, I would think that tesofensine has more abuse potential than Nomifensine, but I've been mistaken before.

I don't think that it'll necessarily *not* get approved if it's got a high abuse potential. There are quite a few commonly prescribed CII meds.
 
Wow, someone who has actually come across the stuff. My reference say that it's not been produced since 2005 and that it's an 'orphen drug'.
 
I got it from Thailand. The description fit with what I'd found (though it was really difficult finding that) so I'm pretty sure it's real. Could be a few years old, certainly.

They had Mianserin as well, which wasn't nearly as good, imho.
 
The official dose range is 100-200mg per day. I saw someone in the US selling it at about $200 for a months supply...
 
I took 100mg twice a day. Few side effects when starting, a litte nausea that went away after about 3 days, as I remember.
 
At that dose, I had enough for 20 days of dosing. Took about 3 or 4 days before any euphoria was noticed, and it seemed to persist until I stopped dosing, though it was a little touch and go. Some days it was pretty strong, others less so, with no apparent change in what I did.

Possibly due to old pills or just amineptine itself. There are a lot more enjoyable drugs out there, but for someone who's seriously, chronically depressed, I don't think you can do much better.
 
I have the opportunity to participate in a trial for this. Any advice on whether this is a good/bad/dangerous/fatal idea?

My experience with stimulants is mixed. Cocaine is practically non-reactive with me, only making me tired and anesthetized. Same with meth. Dextro/levo-amphetamine works fine.

I am also terribly wary of SSRI anti-depressants, so the serotonin reuptake properties of tesofensine has me wondering (that is, wondering if it is at all similar since I don't have a clue :) ).

Any advice would be apprecieated.

P.S. Hopefully this doesn't violate the board rules too much....
 
Top