German Research Points Way To Better Anxiety Drug

Tchort

Tchort

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By Ben Hirschler

LONDON (Reuters) - German scientists believe they may have found a better anxiety drug that can counteract panic attacks without the side effects caused by existing treatments like Valium.

Anxiety drugs such as Valium work well but produce side-effects that include drowsiness, forgetfulness and clumsiness and, when taken over time, can induce dependency.

The new compound, XBD173, appears to avoid these problems by targeting a different biological "don't panic" button, making it a good potential candidate for use as a safe and fast-acting anxiety pill.

Researchers published details of their experimental drug in the journal Science on Thursday, including encouraging results from an initial Phase I clinical study, which was sponsored by Swiss drugmaker Novartis.

A company spokesman said XBD173 was no longer in clinical development at Novartis but had been given to co-development partner Dainippon Sumitomo Pharma.

"What is needed right now is a rapid-acting anxiolytic (anxiety drug) that is effective but lacks the side effects of benzodiazepines," lead researcher Rainer Rupprecht of Munich's Ludwig Maximilian University said in a telephone interview.

"This shows that there is a possibility."

Roche's drug Valium, known generically as diazepam, is the best known of the benzodiazepine class of drugs, which have dominated the anxiety treatment market since the 1960s.

Antidepressants called selective serotonin reuptake inhibitors (SSRIs), such as Eli Lilly's Prozac, which is sold generically as fluoxetine, are also given for anxiety disorders but are of no use in acute episodes since they take several weeks to have an effect.

By contrast XBD173 worked within one hour of being given to rats in laboratory tests and also reduced panic in a week-long clinical study involving 70 healthy male volunteers given the new drug, an older benzodiazepine or a placebo.

The German team tested effectiveness by injecting subjects with a chemical called CCK-4 that is known to trigger a short-lived anxiety attack, which raises both heart rate and blood pressure.

They found that XBD173 produced a fast anti-anxiety response without any withdrawal symptoms after use.

The new compound works by promoting the synthesis of neurosteroids that modulate the effects of a brain chemical called GABA. Benzodiazepines also affect GABA, but in a different way.

Drug companies have been trying for some time to develop next-generation benzodiazepines by tweaking their chemical make-up to deliver a more selective effect that avoids unwanted side effects -- but it has proved an uphill struggle.

In 2003 Merck & Co abandoned one such drug, known as GABA Alpha 2/Alpha 3, after disappointing mid-stage clinical trials.

(Editing by Greg Mahlich)
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http://www.reuters.com/article/healthNews/idUSTRE55H57N20090618
 
is this as revolutionary as it sounds like it might be? dependency-less alcohol/benzo/get faded? i suppose euphoria is hard to test for
 
This sounds promising. Very promising. I'm quite aware of how limited the options are in anxiety treatment.
 
qwe said:
is this as revolutionary as it sounds like it might be? dependency-less alcohol/benzo/get faded? i suppose euphoria is hard to test for
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Not really. We can test for self administration, which gives a good idea of reinforcing properties, and with human subjects, self reporting euphoria isn't really a problem. If people like it, they'll make it known.
 
I'd be intrigued to read more about it when there's more information about it :)
Could be a step forward.. But how many times have they announced a "new chemical with X side effects and no potential for addiction" ?
We shall see I guess.
 
^^yeah maybe this will be to benzos what heroin was to morphine. That sounds fanfuckingtastic to me
 
XBD-173 is a zolpidem or zopiclone derivative (it has features unique to each, so you can't really say it's more of a derivative of one or the other).

I've posted the structure here with zolpidem and zopiclone next to it. The funny thing is that I can't find info about affinity for CCK-A receptors (this is what CCK-4 binds to), but I can find info about peripheral benzodiazepine receptors. Until I started looking into this, I didn't know that we had PBRs in our brain, actually.

xbd173.gif
 
Right, I don't think this has the same subtype affinity as the others - or maybe it is indeed a CCK-A antagonist. I just cant find the data and the structure seems to suggest not.
 
remember when ambien was claimed as not addictive for a while before everyone started having retrograde amnesia, docs give it out like candy so whatev....
 
retrograde amnesia was a well known side effect before it even made it to market, don't get the point. And it was never claimed to not be addicted- it was scheduled from the very beginning. It was claimed to produce less physical dependence than benzodiazepines which still seems to be true.
 
Wiki claims that there have been no withdrawal symptoms with cessation or even sedation. To what extent is this true?
 
JoeM said:
Is there a way to find out why GABA Alpha 2/Alpha 3 were abandoned?
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I don't even understand this question. Are you asking why people aren't targetting GABA-A alpha2 and alpha3 subunit selective drugs? They are, they just haven't made it to market yet. They might not make it to market, who knows. There are plenty of drugs that target these subunits with varying degrees of affinity at other receptor containing subunits.
 
Hammilton said:
I don't even understand this question. Are you asking why people aren't targetting GABA-A alpha2 and alpha3 subunit selective drugs? They are, they just haven't made it to market yet. They might not make it to market, who knows. There are plenty of drugs that target these subunits with varying degrees of affinity at other receptor containing subunits.
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In the original article it says

In 2003 Merck & Co abandoned one such drug, known as GABA Alpha 2/Alpha 3, after disappointing mid-stage clinical trials.
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I think he is curious what happened in the trials
 
I anxiously wait to hear more! ;) I could care less if it produces any euphoria at all. What I care about is that it effectively combats anxiety without blunting ones mental faculties.
 
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