Tesofensine

[LuxEtVeritas]

Uh, lucky you...

seriously i would see no real qualms with this compound

what dosing(s) are they testing?...for weight loss i assume and i believe may be thus entering Phase III

 

[Kudos]

I believe she said Phase II testing. It is in trial for obesity at the moment but I didn't get specific dosing details. The call is for recreational drug users who have experience with stimulants, so perhaps its to test for abuse potential, too?

 

[LuxEtVeritas]

yes perhaps

much higher dosings than what is instructed will be needed to even court abuse, but it indeed has abuse potential i am sure, though not as bad as many other anti-obesity agents that are neuromodulators


prior PhaseIIb dose testing i think was done on 0.25,0.50, and 1.0mg dosings

 

[GES]

Hi Kudos

Can you tell more about the trial? Where is it and how many are they going to enroll? Any news about the dose?

It is a bit interesting because the drug have actually been tested in an abuse set up once before.
If you take a look on page 34 then you can see the trial I am mention. Those days the drug was known by NS2330. So it has already been tested up to 6mg. What more do they want to test for this time?

http://www.uclaisap.org/documents/2004 Biennial Report.pdf

 

[Riemann Zeta]

I don't think that Nomifensine had rediculous addictive liability. At least, that is not why the drug was abandoned. Alas, nomifensine seems to be quite toxic to the kidneys and hard on the liver. Too many cases of hepatotoxicity spells instant market removal for a compound (and with good cause, as it's not called a liver for nothing).


I think it would be really interesting to formally alpha/beta test drugs in the Phase II/III (or even I, if you want to be balls-to-the-wall) development stage, but I am disqualified from nearly all drug trials a priori because I am (obviously) already on drugs .

 

[Smyth]

That link above is interesting. 6mg is obviously because the test subjects are stimulant abusers and therefore already have a significant tolerance.

What it basically shows us is that trials with this and other stuff obviously does go-on, rather because it is happening behind closed-doors, the information is not immediately available in the public domain.

I'd also like to know about those epibatidine analogs tested and developed by Abbott laboratories, who are the same company that has licenses to make methamphetamine pills.

ABT-594, most likely is not abandoned, just that progress in the area can be slow sometimes. On the other hand, I think brasofensine may have been abandoned in favor of tesofensine, and the methoxymethyl side-chain analog.

 

[Ham-milton]

nicotinic drugs? ew! I'm kinda thinking that nothing worthwhile will come out of that area. It's all so toxic.

 

[Adrenochrome]

I take dexamph drugs for adhd, I'll ask my nurse 2 prescribe this if it gets the adhd indication

 

[Smyth]

^What drug are u referring to Adrenochrome (tesofensine or ABT-594)?

There was a thread not long ago that wrongly identified one of Abbott laboratories trials for atomoxetine as a nicotinic agonist, but I didn't bother to clarify it since I was using somebody elses computer at the time.

See, the thread quoted shows clinical trials data for atomoxetine (a.k.a. ABT-894).

 

[Ham-milton]

I was talking about the epibatidine analogues you mentioned above.

 

[fastandbulbous]

same reason nomifensine was eventually disallowed as a viable pharma

Nomifensine actually got the axe because it causes hemolytic anemia, it was amineptine that got judged to have ''recreational capacity.''

Was going to say that nomifensine was dropped because of side effects, not abuse potential, but see I was beaten to it. Just one more bit of evidence IMO of why drugs should not contain an amino group attached top an an aromatic ring - there are exceptions w.r.t. safety, but they are very few & far between as fasar as I'm concerned

 

[Smyth]

Just one more bit of evidence IMO of why drugs should not contain an amino group attached top an an aromatic ring

That makes sense. I'd say such a rule could be formed concerning the 4-aryl piperidines containing 4-hydroxy groups or unsaturation across this position.

http://dx.doi.org/10.1016/S0960-894X(01)00132-9
http://dx.doi.org/10.1016/S0968-0896(01)00090-6
http://dx.doi.org/10.1016/S0960-894X(00)00703-4

The second article in the above interesting list is an example of such a compound.

Neurosearch (Tesofensine) also recently got a patent where they added 3,4-dichlorobenzene to tropinone and then dehydrated the alcohol. Such a compound skirts the above generalization since it is tropane and not piperidine based. Nevertheless, I was not impressed with this attempt at a novel SRI other than to knock out some Ki data.

 

[vecktor]

^What drug are u referring to Adrenochrome (tesofensine or ABT-594)?

There was a thread not long ago that wrongly identified one of Abbott laboratories trials for atomoxetine as a nicotinic agonist, but I didn't bother to clarify it since I was using somebody elses computer at the time.

See, the thread quoted shows clinical trials data for atomoxetine (a.k.a. ABT-894).

^ most confusing....

ABT 894 is mentioned repeatedly in the literature as a nicotinic agonist.
In the above mentioned trial it is used in combination with atomoxetine which is a different drug entirely a fairly selective NRI also called Stattera and not the NAChR agonist ABT 894. from what I can determine it may be atomoxetine is a positive control???
ABT 894 is not Atomoxetine

I still haven't found anything which discloses the structure of ABT 894, if anyone can help.....

 

[GES]

Smyth

ABt594 was closed down by Abbott for several years ago due to adverse events. Abbott did make that public. In the process of making a safer drug ABT894 emerged.

Vector

Yes you’re right. Strattera is just a plain and simple positive control to ABT894. Results from that trial will come within very few days.

 

[bupropion]

How much do you get paid to take part in clinical trials?

I doubt I'd qualify but I'm definitely interested in tesofensine since I find Wellbutrin to be an OK "intermediate" stimulant (but with too many side effects).

 

[fastandbulbous]

Neurosearch (Tesofensine) also recently got a patent where they added 3,4-dichlorobenzene to tropinone and then dehydrated the alcohol. Such a compound skirts the above generalization since it is tropane and not piperidine based. Nevertheless, I was not impressed with this attempt at a novel SRI other than to knock out some Ki data.

I think the ethylene bridge between the (effective)2 & 6 position of the piperidine structure must serically inhibit ir's metabolism to an MPP+ specied of neurotoxin as I can't believe they'd be so stupid as to try anything with a compound that showed even slight MPTP like properties.

Actually, the 3,4-dichlorophenyl group attached to the 4 position gives a natural crossover intermediate between DAT inhibitors and prodine-like mu agonist opiates. If the dehydration product isn't neurotoxic like MPTP then I'd have thought some clandestine chappies would have investigated it by now - an opiate with central stimulant properties is basically a speedball in one compound (although probably horribly addictive)

 

[newbie1]

Information please

I would like information on how to get involved in the clinical trials for this - could you give me the info please???? Not a bluelighter yet, so you can send the info to [email protected]


Thanks so much!

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....