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Bitopertin

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Bitopertin (GLYT-1; RO-4917838; RG1678) is a drug under development intended to be used in combination with antipsychotics for the treatment of persistent negative symptoms or sub-optimally controlled positive symptoms associated with schizophrenia. If licensed, bitopertin would represent the first in a new class of treatments for this patient group.[1]

Bitopertin
Bitopertin structure.svg
Clinical data
ATC code
  • none
Identifiers
CAS Number
ChemSpider
UNII
ChEMBL
E number{{#property:P628}}
CompTox Dashboard (EPA)
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Chemical and physical data
FormulaC21H20F7N3O4S
Molar mass543.455022 g/mol g·mol−1
3D model (JSmol)

Bitopertin is a glycine transporter type 1 (GlyT1) inhibitor that increases levels of the neurotransmitter glycine by inhibiting its reuptake from the synaptic cleft. Glycine acts as a required co-agonist along with glutamate at N-methyl-D-aspartate receptors. Dysfunction of NMDA receptors may play a key role in the pathogenesis of schizophrenia and modulation of glutamatergic signalling via increased concentrations of glycine in the synaptic cleft may help potentiate NMDA receptor function and improve the symptoms of schizophrenia. Bitopertin is administered orally at 10 mg or 20 mg once daily for 56 weeks.[2]

Roche is co-developing RG1678 globally with Chugai.[2]

In a Phase II proof-of-concept study patients on RG1678 experienced a significant improvement in the change of the Negative Symptom Factor Score from baseline within 8 weeks (from −4.86 in the placebo group to −6.65 in the treatment group, p<0.05, per-protocol population). In addition, 83% of patients on RG1678 described an improvement of negative symptoms on the CGI-I1 vs 66% on placebo (p<0.05, per-protocol population).[3]

Phase III trials are currently underway and expected to be completed by 2015.[4]

References

  1. "Bitopertin for schizophrenia: primary, persistent negative symptoms; sub-optimally controlled positive symptoms – in combination with antipsychotics", "NIHR Horizon Scanning Centre, School of Health & Population Sciences, University of Birmingham", 1 June 2012
  2. 2.0 2.1 "Bitopertin for schizophrenia", "EuroScan", 14 August 2012
  3. Glycine Transporter Type 1 (GLYT1) Inhibitor RG1678: Positive Results of the Proof-of-Concept Study for the Treatment of Negative Symptoms in Schizophrenia, Umbricht D. et al., ACNP 2010
  4. "Bitopertin for schizophrenia: primary, persistent negative symptoms; sub-optimally controlled positive symptoms – in combination with antipsychotics", "NIHR Horizon Scanning Centre, School of Health & Population Sciences, University of Birmingham", 1 June 2012

External links

"Bitopertin for schizophrenia", "NIHR Horizon Scanning Centre", June 2012

 

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