Basimglurant

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'''Basimglurant''' ([[International Nonproprietary Name|INN]]) (developmental code names '''RG-7090''', '''RO-4917523''') is a [[negative allosteric modulator]] of the [[mGlu5 receptor|mGlu₅ receptor]] which is under development by [[Hoffmann-La Roche|Roche]] and [[Chugai_Pharmaceutical_Co.|Chugai Pharmaceutical]] for the treatment of [[treatment-resistant depression]] (as an [[adjunctive therapy|adjunct]]) and [[fragile X syndrome]].<ref name="Roche2014a">{{cite web|url=http://www.roche.com/research_and_development/who_we_are_how_we_work/pipeline.htm|title=Roche - Pipeline|year=2014|access-date=2014-08-01}}</ref><ref name="Roche2014b">{{cite web|url=http://www.roche.com/irp1q14e-annex.pdf|title=Roche Group Development Pipeline|year=2014|access-date=2014-08-01|url-status=dead|archive-url=https://web.archive.org/web/20140808043650/http://www.roche.com/irp1q14e-annex.pdf|archive-date=2014-08-08}}</ref> As of November 2016, it has undergone [[Phases of clinical research#Phase II|phase II]] [[clinical trial]]s for both of these indications.<ref name = "Adis_Insight_Basimglurant" />

'''Basimglurant''' ([[International Nonproprietary Name|INN]]; developmental code '''RG-7090''' and '''RO-4917523''') is a [[negative allosteric modulator]] of the [[mGlu5 receptor|mGlu₅ receptor]] which is under development by [[Hoffmann-La Roche|Roche]] and [[Chugai_Pharmaceutical_Co.|Chugai Pharmaceutical]] for the treatment of [[treatment-resistant depression]] (as an [[adjunctive therapy|adjunct]]) and [[fragile X syndrome]].<ref name="Roche2014a">{{cite web|url=http://www.roche.com/research_and_development/who_we_are_how_we_work/pipeline.htm|title=Roche - Pipeline|year=2014|access-date=2014-08-01}}</ref><ref name="Roche2014b">{{cite web|url=http://www.roche.com/irp1q14e-annex.pdf|title=Roche Group Development Pipeline|year=2014|access-date=2014-08-01|url-status=dead|archive-url=https://web.archive.org/web/20140808043650/http://www.roche.com/irp1q14e-annex.pdf|archive-date=2014-08-08}}</ref> As of November 2016, it has undergone [[Phases of clinical research#Phase II|phase II]] [[clinical trial]]s for both of these indications.<ref name = "Adis_Insight_Basimglurant" />

It was discovered in a medicinal chemistry effort conducted at Roche starting from the results of a small molecular weight compound library high-throughput screen based on a Ca21 mobilization assay with human mGlu5a (Jaeschke et al., 2015). The high-throughput screen identified several mGlu5 antagonists such as [[2-Methyl-6-(phenylethynyl)pyridine|MPEP]], [[MTEP]], and [[fenobam]].<ref name="Lindemann_2015">{{cite journal | vauthors = Lindemann L, Porter RH, Scharf SH, Kuennecke B, Bruns A, von Kienlin M, Harrison AC, Paehler A, Funk C, Gloge A, Schneider M, Parrott NJ, Polonchuk L, Niederhauser U, Morairty SR, Kilduff TS, Vieira E, Kolczewski S, Wichmann J, Hartung T, Honer M, Borroni E, Moreau JL, Prinssen E, Spooren W, Wettstein JG, Jaeschke G | display-authors = 6 | title = Pharmacology of basimglurant (RO4917523, RG7090), a unique metabotropic glutamate receptor 5 negative allosteric modulator in clinical development for depression | journal = The Journal of Pharmacology and Experimental Therapeutics | volume = 353 | issue = 1 | pages = 213–33 | date = April 2015 | pmid = 25665805 | doi = 10.1124/jpet.114.222463 | doi-access = free }}</ref> In partnership with Chugai Pharmaceutical, basimglurant is currently still undergoing revision from previous drug trials as of November 2016.<ref name = "Adis_Insight_Basimglurant">{{Cite web|url=http://adisinsight.springer.com/drugs/800024877|title=Basimglurant | work = Adis Insight | publisher = Springer Nature Switzerland AG |access-date=2016-11-20}}</ref>

It was discovered in a medicinal chemistry effort conducted at Roche starting from the results of a small molecular weight compound library high-throughput screen based on a Ca21 mobilization assay with human mGlu5a (Jaeschke et al., 2015). The high-throughput screen identified several mGlu5 antagonists such as [[2-Methyl-6-(phenylethynyl)pyridine|MPEP]], [[MTEP]], and [[fenobam]].<ref name="Lindemann_2015">{{cite journal | vauthors = Lindemann L, Porter RH, Scharf SH, Kuennecke B, Bruns A, von Kienlin M, Harrison AC, Paehler A, Funk C, Gloge A, Schneider M, Parrott NJ, Polonchuk L, Niederhauser U, Morairty SR, Kilduff TS, Vieira E, Kolczewski S, Wichmann J, Hartung T, Honer M, Borroni E, Moreau JL, Prinssen E, Spooren W, Wettstein JG, Jaeschke G | display-authors = 6 | title = Pharmacology of basimglurant (RO4917523, RG7090), a unique metabotropic glutamate receptor 5 negative allosteric modulator in clinical development for depression | journal = The Journal of Pharmacology and Experimental Therapeutics | volume = 353 | issue = 1 | pages = 213–33 | date = April 2015 | pmid = 25665805 | doi = 10.1124/jpet.114.222463 | doi-access = free }}</ref> In partnership with Chugai Pharmaceutical, basimglurant is currently still undergoing revision from previous drug trials as of November 2016.<ref name = "Adis_Insight_Basimglurant">{{Cite web|url=http://adisinsight.springer.com/drugs/800024877|title=Basimglurant | work = Adis Insight | publisher = Springer Nature Switzerland AG |access-date=2016-11-20}}</ref>