4 ms·
Esketamine is just an enantiomer. Both enantiomers are similarly active, and to me it's not 100% clear to me why Esketamine was the enantiomer chosen.
by bentona 8y ago
Esketamine is just an enantiomer. Both enantiomers are similarly active, and to me it's not 100% clear to me why Esketamine was the enantiomer chosen.
- dawhizkid 8y agoThere is no rhyme or reason other than the fact that one or the other could be patented by a private co unlike Ketamine. I assume trying to patent both would've doubled their costs, so why bother, especially if it's highly probable both do the same thing.
- mveety 8y agoEsketamine doesn’t have the same activity as racemic or Arketamine (S- hits some of the dopamine receptors harder and doesn’t bind with the sigma ones iirc). Patients seem to find esketamine more pleasant because of this and it’s eliminated faster than R- so patients can (probably) get back to normal faster. (Edit: had my right from left mixed up. It’s been a while)
- dawhizkid 8y agoSo maybe it makes you a little less groggy but at 300x the price? Don't think anyone can say that justifies the price multiple.
- xkcd-sucks 8y agoNow r-ket can be developed as a patentable improvement over the state of the art :)
- Lazare 8y agoSome studies suggested that the enantiomer they chose was slightly better at driving the effect people thought was causing the anti-depressive effect. Unfortunately, newer studies suggest that 1) that effect isn't responsible for the anti-depressive effect and 2) the enantiomer they chose doesn't seem to be as good as normal ketamine. Too soon to say, but early signs suggest this may have all been a fantastically expensive mistake. :(
- jokowueu 8y agoThey started the trials before the NIH study that proved that nmda receptor only played a small role it it's effects and that R-ket and it's metabolite was more important . They were already too deep it