https://wikimd.com/index.php?action=history&feed=atom&title=BitopertinBitopertin - Revision history2026-04-20T16:36:25ZRevision history for this page on the wikiMediaWiki 1.44.2https://wikimd.com/index.php?title=Bitopertin&diff=4968065&oldid=prevPrab at 17:10, 13 September 20232023-09-13T17:10:05Z<p></p>
<p><b>New page</b></p><div>[[File:Bitopertin structure.svg|Bitopertin structure|thumb]]<br />
<br />
[[Bitopertin]] (also known as GLYT-1, RO-4917838, or RG1678) is an investigational drug that is currently being explored for its potential to enhance the efficacy of [[antipsychotics]] in treating specific symptoms of [[schizophrenia]]. If approved for use, bitopertin would stand out as a pioneering member of a novel class of treatments for patients with schizophrenia.<br />
<br />
== Mechanism of Action ==<br />
Bitopertin functions as a glycine transporter type 1 ([[GlyT1]]) inhibitor. This mechanism works to increase concentrations of the [[neurotransmitter]] glycine, by inhibiting its reuptake from the [[synaptic cleft]]. Glycine operates as a co-agonist, together with [[glutamate]], at [[N-methyl-D-aspartate]] (NMDA) receptors. There is evidence to suggest that malfunctions of NMDA receptors could be intricately tied to the onset of schizophrenia. By modulating glutamatergic signalling and raising glycine levels in the synaptic cleft, NMDA receptor function may be potentiated, potentially alleviating symptoms of schizophrenia.<br />
<br />
== Dosage ==<br />
Bitopertin is intended to be taken orally. The recommended doses under investigation are 10 mg or 20 mg, to be taken once daily, with a treatment duration of 56 weeks.<br />
<br />
== Development and Collaboration ==<br />
[[Roche]], a global healthcare company, is currently working in collaboration with [[Chugai]] to co-develop RG1678 on an international scale.<br />
<br />
== Clinical Studies ==<br />
In a notable Phase II proof-of-concept study, patients who were administered RG1678 witnessed a marked improvement in their Negative Symptom Factor Score within a span of 8 weeks. More specifically, scores shifted from −4.86 in the placebo group to −6.65 in the treatment group (with a significance of p<0.05, based on the per-protocol population). Moreover, a significant 83% of RG1678-treated patients reported an enhancement of negative symptoms on the CGI-I1, as opposed to the 66% observed in the placebo group (with a significance of p<0.05, according to the per-protocol population).<br />
<br />
== Potential Impact ==<br />
Should bitopertin gain licensing approval, it would pave the way for a novel treatment approach that could significantly benefit patients experiencing persistent negative symptoms or sub-optimally managed positive symptoms associated with schizophrenia.<br />
{{stub}}<br />
{{Glycine receptor modulators}}<br />
[[Category:Experimental drugs]]<br />
[[Category:Glycine reuptake inhibitors]]<br />
[[Category:N-benzoylpiperazines]]<br />
[[Category:Trifluoromethyl compounds]]<br />
[[Category:Benzosulfones]]<br />
[[Category:Organofluorides]]<br />
[[Category:Schizophrenia]]<br />
[[Category:Drugs]]</div>Prab