A safer form of Clozapine?

[whopper]

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OK people, I really need your help on this one.

As we know, clozapine, despite being the most effective atypical antipsychotic, is rarely prescribed because of its dangerous side effects.

Acadia Pharmaceuticals is an up & coming company that is producing a new medication they are hoping to market within the next few years.

http://www.acadia-pharm.com/programs/schizophrenia.htm

Its called ACP-104

In more recognizable terms its N-desmethylclozapine, the active metabolite of clozapine.

Supposedly N-desmethylclozapine is efficacious in treating schizophrenia, and perhaps may be safer. To what degree (if any) I do not know.

I have done several pubmed searches but I'm not getting too much info on N-desmethylclozapine that is clinically relevant.

Anyone know anything about desmethylclozapine and any superior effects it may have to Clozapine? This may be a potential wonder drug, or perhaps something not better or only slightly better.

 

[OldPsychDoc]

Safer clozapine is the Holy Grail of pharmaceutical research. The key phrase in your post is "potential wonder drug". Expectations have been raised and dashed before. Wait and see what actually pans out of controlled clinical research before getting too excited.

 

[Anasazi23]

There are some who postulate that clozapine isn't working properly unless you have the associated weight gain.

What OPD says is true...the same thing was touted for aripiprazole.

As an aside, I don't think Clozaril is that rarely prescribed. Of course, the blood draws are a major drawback to a population that is already notoriously non-compliant.

Grand rounds this week was on pharmacotherapy of the violent patient.
A famous speaker gave a talk on his research, which boiled down to:
Clozaril>Zyprexa>haldol

The entire time I kept thinking...and who's doing the bloods on these supposed violent and uncontrollable patients? I don't miss those days.
😳

 

[Anasazi23]

From what I'm reading, it's not so much the 'safety' of the metabolite, but the cognitive-enhancing properties of the drug, which is a potent agonist of m1 receptors. Clozaril is a blocker of muscarinic receptors...so they feel and state that the newer form will result in similar efficacy, possibly better safety profile, and improved cognition.

We'll see a lot of these newer cognitive enhancers in the near future. We'll have to wait and see.

 

[whopper]

I'm getting the same.

But I did read that clozapine has the same benefit. Maybe I'm remembering this wrong?

I'll double check. However if I am remembering it correctly than I don't really see much better reason to take this med over clozaril. If it causes just as much weight gain and agranulocytosis--well then heck why take it if its not really better?

The company IMHO is limiting the data being released perhaps to protect their investment, and even if they did release their own data-well that too is a problem because its not 3rd party data.

The same company has another med called ACP-103 that is designed to enhnance treatment of schizophrenia as an adjunct treatment. It works on the serotonin receptors and it not designed to be a treatment alone.

Both have me interested because of the novel schizophrenic treatments, both seem to be the only new pharmacodynamic approaches I've read about. All the other ones I've read seem to simply be dopamine modulators like Aripiprazole.