About: Bitopertin

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Bitopertin (developmental code names RG1678; RO-4917838) is a glycine reuptake inhibitor which was under development by Roche as an adjunct to antipsychotics for the treatment of persistent negative symptoms or suboptimally controlled positive symptoms associated with schizophrenia. Research into this indication has been largely halted as a result of disappointing trial results.

Attributes	Values
rdf:type	Thing dul:ChemicalObject chemical substance Drug yago:Agent114778436 yago:CausalAgent100007347 yago:Drug103247620 yago:Matter100020827 yago:PhysicalEntity100001930 drug yago:Substance100020090 yago:WikicatDrugs
rdfs:label	Bitopertin (en)
rdfs:comment	Bitopertin (developmental code names RG1678; RO-4917838) is a glycine reuptake inhibitor which was under development by Roche as an adjunct to antipsychotics for the treatment of persistent negative symptoms or suboptimally controlled positive symptoms associated with schizophrenia. Research into this indication has been largely halted as a result of disappointing trial results. (en)
foaf:depiction
dcterms:subject	Experimental drugs Organofluorides Trifluoromethyl compounds Benzosulfones Glycine reuptake inhibitors N-benzoylpiperazines
Wikipage page ID	36716273 (xsd:integer)
Wikipage revision ID	1084694348 (xsd:integer)
Link from a Wikipage to another Wikipage	Schizophrenia Hoffmann-La Roche Neurotransmitter Experimental drugs Organofluorides Trifluoromethyl compounds Co-agonist Glycine Synaptic cleft Antipsychotic Benzosulfones Glutamatergic Glycine reuptake inhibitor Glycine reuptake inhibitors N-benzoylpiperazines Positive symptoms Glycine transporter 1 Negative symptoms ORG-25935 Phases of clinical research Reuptake NMDA receptor Glutamate Adjunctive therapy
sameAs	Bitopertin Bitopertin Bitopertin Bitopertin Bitopertin Bitopertin
dbp:wikiPageUsesTemplate	dbt:Drugbox dbt:Glycine_receptor_modulators dbt:Reflist dbt:Short_description dbt:Use_dmy_dates
thumbnail	wiki-commons:Special:FilePath/Bitopertin.svg?width=300
ATC prefix	none (en)
c	21 (xsd:integer)
CAS number	845614 (xsd:integer)
ChEMBL	1169880 (xsd:integer)
ChemSpiderID	25034798 (xsd:integer)
F	7 (xsd:integer)
H	20 (xsd:integer)
IUPAC name	{4-[3-Fluoro-5-pyridin-2-yl]piperazin-1-yl}{5--2-[-2,2,2-trifluoro-1-methylethoxy]phenyl}methanone (en)
KEGG	D10186 (en)
n	3 (xsd:integer)
O	4 (xsd:integer)
s	1 (xsd:integer)
SMILES	CCOc1cccSC (en)
StdInChI	1 (xsd:integer)
StdInChIKey	YUUGYIUSCYNSQR-LBPRGKRZSA-N (en)
UNII	Q8L6AN59YY (en)
width	270 (xsd:integer)
has abstract	Bitopertin (developmental code names RG1678; RO-4917838) is a glycine reuptake inhibitor which was under development by Roche as an adjunct to antipsychotics for the treatment of persistent negative symptoms or suboptimally controlled positive symptoms associated with schizophrenia. Research into this indication has been largely halted as a result of disappointing trial results. Bitopertin is a glycine transporter 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 (NMDA) 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. In a phase II proof-of-concept study, patients on bitopertin 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 bitopertin described an improvement of negative symptoms on the CGI-I1 versus 66% on placebo (p<0.05, per-protocol population). In January 2014, Roche reported that bitopertin failed to meet its endpoints in two phase III trials assessing its efficacy in reducing negative symptoms of schizophrenia. Subsequently, in April 2014, Roche announced that it was discontinuing all except one of its phase III trials of bitopertin for schizophrenia. (en)
IUPHAR ligand	7546 (xsd:integer)
gold:hypernym	Inhibitor
prov:wasDerivedFrom	wikipedia-en:Bitopertin?oldid=1084694348&ns=0
page length (characters) of wiki page	4255 (xsd:nonNegativeInteger)
CAS number	845614-11-1
ChEMBL	1169880
FDA UNII code	Q8L6AN59YY
KEGG	D10186
foaf:isPrimaryTopicOf	wikipedia-en:Bitopertin
is Link from a Wikipage to another Wikipage of	List of investigational obsessive–compulsive disorder drugs C21H20F7N3O4S Tilapertin Glycine reuptake inhibitor Sodium- and chloride-dependent glycine transporter 1 Mesylate
is Wikipage redirect of	C21H20F7N3O4S
is foaf:primaryTopic of	wikipedia-en:Bitopertin

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