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Re: Ruoxinlin (Ansofaxine) SNDRI in 2023 - thoughts?

Posted by SLS on January 22, 2023, at 19:06:31

In reply to Ruoxinlin (Ansofaxine) SNDRI in 2023 - thoughts?, posted by PeterMartin on January 22, 2023, at 12:53:50

> Looks as thought Ansofaxine (tradename will be Ruoxinlin) might get approval in 2023. Seems to be a prodrug of Effexor but aparently it has different effects and no sexual/weight side effects. I only learned about this medication being close to approval this morning. Has anyone been following its progress? Is there any reason to be excited about it as an alternative to say the MAOis?
>
> https://en.wikipedia.org/wiki/Ansofaxine
>
> https://www.biospace.com/article/luye-pharma-releases-top-line-results-from-a-phase-ii-clinical-trial-of-its-new-antidepressant-ansofaxine-hydrochloride-extended-release-tablets/
>
> Wiki:
> ---
> Toludesvenlafaxine (former developmental code names LY03005, LPM570065), also known as ansofaxine or as 4-methylbenzoate desvenlafaxine, is a serotoninnorepinephrinedopamine reuptake inhibitor (SNDRI) which is under development by Luye Pharma Group for the treatment of major depressive disorder (MDD).[1][2][3][4] It is described as an SNDRI and prodrug to desvenlafaxine.[2] However, unlike desvenlafaxine, which has in vitro IC50 values of 53 nM and 538 nM for inhibition of serotonin and norepinephrine reuptake, respectively, toludesvenlafaxine has respective in vitro IC50 values of 723 nM, 763 nM, and 491 nM for serotonin, norepinephrine, and dopamine reuptake inhibition.[2] As of July 2018, the drug is in preregistration for MDD in the United States, the European Union, Japan, and China.[1] In December 2018 the drug is in phase III trial in the United States and China.[5] In March of 2020 the FDA accepted Luye Pharma's new drug application for ansofaxine.[6] In December 2021 Luye Pharma released results from phase II clinical trials on ansofaxine. [7] Luye Pharma Group has issued the brand name Ruoxinlin for the upcoming medication Ansofaxine.[8] In November of 2022 Ruoxinlin was approved for MDD in China.[9]


As I read this, ansofaxine is a more potent reuptake inhibitor of dopamine than it is of norepinephrine and serotonin.


Interestingly, combining Wellbutrin with Effexor boosts the levels of extracellular dopamine dramatically compared to Wellbutrin or Effexor alone.

https://cdnsciencepub.com/doi/abs/10.1139/y2012-045

I have seen a combination of Effexor + Wellbutrin or Pristiq + Wellbutrin bring previously treatment-refractory people into remission. Wellbutrin + Zoloft works for quite a few people, too. "Welloft". Wellbutrin monotherapy makes me feel worse, so I never combined it with a SRI. I even experienced a worsening of depression when Wellbutrin was added to Parnate. A friend of mine who had been taking Parnate for years with minimal improvement switched to Pristiq 100 mg/day + Wellbutrin 300 mg/day. This regime has kept her in remission for 15 years. As best as I can tell, she had some medication breakthrough during a time of severe stress.


- Scott


Some see things as they are and ask why.
I dream of things that never were and ask why not.

The only thing necessary for the triumph of evil is that good men do nothing.

 

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URL: http://www.dr-bob.org/babble/20230117/msgs/1121617.html