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Dr. Bob is Robert Hsiung, MD,
bob@dr-bob.orgShown: posts 1 to 14 of 14. This is the beginning of the thread.
Posted by SLS on October 21, 2013, at 13:31:14
Cariprazine is an investigational antipsychotic with antidepressant properties. It is a DA receptor partial agonist, as is Abilify, but is preferential for D3 receptors. It is D2 antagonism that is most responsible for prolactin release and weight gain. Therefore, cariprazine should be weight-neutral compared to Abilify, and perhaps less apt to produce diabetes.
I'll be first in line to try this drug.
- Scott----------------------------------------------------
"Forest has filed New Drug Applications (NDAs) with the U.S. Food and Drug Administration (FDA) for cariprazine for the treatment of schizophrenia and manic or mixed episodes associated with bipolar I disorder. Cariprazine is an orally active and potent dopamine D3-preferring D3 /D2 receptor partial agonist. Cariprazine has a low affinity at other receptor sites such as 5-HT2C, muscarinic, and adrenergic which have been associated with adverse events. Cariprazine is also under development as an adjunctive treatment for MDD and for the treatment of bipolar depression. Cariprazine was discovered by Gedeon Richter Plc and is licensed to Forest Laboratories Inc., in the U.S. and Canada." - Business Wire
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Posted by linkadge on October 21, 2013, at 17:23:02
In reply to Cariprazine - A better Abilify?, posted by SLS on October 21, 2013, at 13:31:14
I have read conflicting research on which dopamine receptors are most responsible for antipsychotic effect. I wonder if selective d3 antagonists have antipsychotic efficacy?
Linkadge
Posted by Phillipa on October 21, 2013, at 18:51:40
In reply to Re: Cariprazine - A better Abilify?, posted by linkadge on October 21, 2013, at 17:23:02
Posted by SLS on October 21, 2013, at 19:04:23
In reply to Re: Cariprazine - A better Abilify?, posted by linkadge on October 21, 2013, at 17:23:02
> I have read conflicting research on which dopamine receptors are most responsible for antipsychotic effect. I wonder if selective d3 antagonists have antipsychotic efficacy?
I had thought the same thing.
Cariprazine might make for a better antidepressant augmenter than Abilify.
http://clinicaltrials.gov/show/NCT01715805
- Scott
Posted by SLS on October 21, 2013, at 19:05:41
In reply to Re: Cariprazine - A better Abilify?, posted by Phillipa on October 21, 2013, at 18:51:40
Thanks, Phillipa.
- Scott
Posted by Phillipa on October 21, 2013, at 21:20:46
In reply to Re: Cariprazine - A better Abilify? » Phillipa, posted by SLS on October 21, 2013, at 19:05:41
Scott no idea if it's a good site or not but did a google search as had no idea what it was. Phillipa
Posted by SLS on October 22, 2013, at 5:39:56
In reply to Re: Cariprazine - A better Abilify?, posted by linkadge on October 21, 2013, at 17:23:02
Do you think that the D3 receptor in the nucleus accumbens makes a good target in treating schizophrenia? Negative symptoms only? It is important to recognize that D2 receptors in the striatum will still be antagonized. I don't know what the D3/D2 ratio in binding affinity is for cariprazine.
http://www.ncbi.nlm.nih.gov/pubmed/9473144
http://en.wikipedia.org/wiki/Cariprazine
http://www.ncbi.nlm.nih.gov/pubmed/?term=cariprazine+striatum
- Scott
Posted by SLS on October 22, 2013, at 5:41:18
In reply to Re: Cariprazine - A better Abilify?, posted by SLS on October 22, 2013, at 5:39:56
Posted by Jeroen on October 22, 2013, at 15:34:47
In reply to Re: Cariprazine - A better Abilify?, posted by SLS on October 22, 2013, at 5:39:56
does anyone knows if ordering minocycline online is safe?
the site is [xxx]
since no doc wants to help me get rid of negative symptoms
they claim they send in few days and have lot of pos feedback
its coming from the ukplease advice
Posted by Bob on October 22, 2013, at 21:21:31
In reply to Re: Cariprazine - A better Abilify?, posted by SLS on October 22, 2013, at 5:39:56
> Do you think that the D3 receptor in the nucleus accumbens makes a good target in treating schizophrenia? Negative symptoms only? It is important to recognize that D2 receptors in the striatum will still be antagonized. I don't know what the D3/D2 ratio in binding affinity is for cariprazine.
>
> http://www.ncbi.nlm.nih.gov/pubmed/9473144
>
> http://en.wikipedia.org/wiki/Cariprazine
>
> http://www.ncbi.nlm.nih.gov/pubmed/?term=cariprazine+striatum
>
>
> - ScottScott,
Did you notice that the Wiki entry you gave the link for said that one of the most common side effects was weight gain?
Bob
Posted by SLS on October 23, 2013, at 5:59:23
In reply to Re: Cariprazine - A better Abilify? » SLS, posted by Bob on October 22, 2013, at 21:21:31
> Did you notice that the Wiki entry you gave the link for said that one of the most common side effects was weight gain?
I did not. I was relying on the other sources I found.
For example:
http://www.ncbi.nlm.nih.gov/pubmed/24048386
http://www.ncbi.nlm.nih.gov/pubmed/23966785
Right now, Lurasidone is the antipsychotic considered least likely to produce weight gain.
I guess it is important to note that Abilify was touted as being weight-neutral when it was first approved.
- Scott
Posted by SLS on December 17, 2013, at 9:06:09
In reply to Cariprazine - A better Abilify?, posted by SLS on October 21, 2013, at 13:31:14
> Cariprazine is an investigational antipsychotic with antidepressant properties. It is a DA receptor partial agonist, as is Abilify, but is preferential for D3 receptors. It is D2 antagonism that is most responsible for prolactin release and weight gain. Therefore, cariprazine should be weight-neutral compared to Abilify, and perhaps less apt to produce diabetes.
>
> I'll be first in line to try this drug.
>
>
> - Scott
>
> ----------------------------------------------------
>
> "Forest has filed New Drug Applications (NDAs) with the U.S. Food and Drug Administration (FDA) for cariprazine for the treatment of schizophrenia and manic or mixed episodes associated with bipolar I disorder. Cariprazine is an orally active and potent dopamine D3-preferring D3 /D2 receptor partial agonist. Cariprazine has a low affinity at other receptor sites such as 5-HT2C, muscarinic, and adrenergic which have been associated with adverse events. Cariprazine is also under development as an adjunctive treatment for MDD and for the treatment of bipolar depression. Cariprazine was discovered by Gedeon Richter Plc and is licensed to Forest Laboratories Inc., in the U.S. and Canada." - Business Wire
>
> --------------------------------------------------
Cariprazine update:
----------------------------------------------http://www.reuters.com/article/2013/11/21/forest-richter-idUSL5N0J625E20131121
"UPDATE 1-FDA declines to approve new Forest, Richter psychosis drug
Thu Nov 21, 2013 5:49am EST
0 Comments* FDA issues complete response letter for cariprazine
* Move set to delay launch of antipsychotic drug in U.S.
* Richter shares fall 2.8 percent
BUDAPEST, Nov 21 (Reuters) - U.S. health regulators have declined to approve a new antipsychotic drug from Forest Laboratories and Richter, citing the need for more information, including likely additional clinical trial data.
The Food and Drug Administration (FDA) delivered its verdict on cariprazine for schizophrenia and bipolar disorder in a so-called "complete response letter," the type of letter issued by the agency to convey that it cannot approve a drug application in its current form.
Cariprazine was discovered by Hungarian drugmaker Richter and licensed to Forest in the United States and Canada.
Industry analysts have forecast North American sales of the drug of $250 million in 2017, according to consensus forecasts compiled by Thomson Reuters Pharma.
In its letter the FDA acknowledged that cariprazine demonstrated effectiveness but the two companies said on Thursday it appeared regulators wanted more tests on the optimal dose of the treatment to avoid potential side effects.
"This is likely to cause a delay ... (but) we cannot tell how much; we will be able to tell after consultations with the FDA," said Richter spokeswoman Zsuzsa Beke.
The companies said that the FDA had indicated that its request for more information included the need for additional clinical trial data. But Beke said it was possible this might not turn out to be necessary.
"Whether we need more clinical tests, we can also tell that after the consultations - it is possible that the existing data will be sufficient," she said.
Richter's shares were down 2.8 percent by 1040 GMT."
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- Scott
Posted by phidippus on December 30, 2013, at 14:02:40
In reply to Re: Cariprazine - A better Abilify?, posted by SLS on December 17, 2013, at 9:06:09
What impliccations does the D3 action have?
Eric
Posted by SLS on December 30, 2013, at 16:53:03
In reply to Re: Cariprazine - A better Abilify?, posted by phidippus on December 30, 2013, at 14:02:40
> What impliccations does the D3 action have?
>
> EricThe actions of cariprazine comprise more limibic (D3) and less striatal (D2) involvement than Abilify as a DA receptor partial agonist. My unprofessional conclusion is that this would produce less risk of motoric EPS (akathisia might remain problematic) and greater therapeutic effects on depressive mood and negative shizoid symptomatology (deficit syndrome). Even if my thinking is flawed, in the absence of safety issues, I would want to try cariprazine anyway, as it might work better for depression and produce less weight gain than Abilify.
The FDA is not impressed with cariprazine because they do not find any advantage to this drug over those currently available (Efficacy and side effects). This is dangerous thinking, in my estimation. It will prevent a subset of people from having access to a drug that might save their lives or enhance their quality. The FDA can't yet conclude using the available science that cariprazine won't help people who were not helped by currently available drugs. Why have more than one SSRI? Hopefully, the FDA is asking only for evidence that will better define the dosage range for cariprazine. I don't think they have any problems with the data demonstrating efficacy.
- Scott
This is the end of the thread.
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