Literature DB >> 22722029

Clinical development of pomaglumetad methionil: a non-dopaminergic treatment for schizophrenia.

Bruce J Kinon1, Juan-Carlos Gómez.   

Abstract

Pomaglumetad methionil (LY2140023 monohydrate, hereafter referred to as LY2140023) is currently in clinical development as a potential new treatment for schizophrenia. If found to be effective, LY2140023 would represent a novel non-dopaminergic based therapy for this disorder that may restore balance to the glutamate dysregulation hypothesized to underlie schizophrenia. This article presents available clinical trial data that describe the safety, tolerability, and efficacy of LY2140023 in patients with schizophrenia. Data indicate that this compound appears to have an efficacy profile consistent with currently available antipsychotic drugs, although confirmation of its efficacy awaits further clinical testing. LY2140023 is generally well tolerated and appears to have a low association with adverse events related to dopamine D2 receptor antagonism and with weight gain, which are commonly seen with current antipsychotics. A potential association of LY2140023 treatment and seizure events has been identified, although an accurate and reliable understanding of the incidence of these events requires further clinical testing, which is underway. Evaluation of the safety, tolerability, and efficacy of LY2140023 is continuing. This article is part of a Special Issue entitled 'Metabotropic Glutamate Receptors'.
Copyright © 2012 Elsevier Ltd. All rights reserved.

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Year:  2012        PMID: 22722029     DOI: 10.1016/j.neuropharm.2012.06.002

Source DB:  PubMed          Journal:  Neuropharmacology        ISSN: 0028-3908            Impact factor:   5.250


  11 in total

1.  Allosteric signaling through an mGlu2 and 5-HT2A heteromeric receptor complex and its potential contribution to schizophrenia.

Authors:  José L Moreno; Patricia Miranda-Azpiazu; Aintzane García-Bea; Jason Younkin; Meng Cui; Alexey Kozlenkov; Ariel Ben-Ezra; Georgios Voloudakis; Amanda K Fakira; Lia Baki; Yongchao Ge; Anastasios Georgakopoulos; José A Morón; Graeme Milligan; Juan F López-Giménez; Nikolaos K Robakis; Diomedes E Logothetis; J Javier Meana; Javier González-Maeso
Journal:  Sci Signal       Date:  2016-01-12       Impact factor: 8.192

Review 2.  Practical Strategies and Concepts in GPCR Allosteric Modulator Discovery: Recent Advances with Metabotropic Glutamate Receptors.

Authors:  Craig W Lindsley; Kyle A Emmitte; Corey R Hopkins; Thomas M Bridges; Karen J Gregory; Colleen M Niswender; P Jeffrey Conn
Journal:  Chem Rev       Date:  2016-02-16       Impact factor: 60.622

Review 3.  Perspectives on the mGluR2/3 agonists as a therapeutic target for schizophrenia: Still promising or a dead end?

Authors:  Meng-Lin Li; Xi-Quan Hu; Feng Li; Wen-Jun Gao
Journal:  Prog Neuropsychopharmacol Biol Psychiatry       Date:  2015-02-24       Impact factor: 5.067

4.  Group II metabotropic glutamate receptor agonist prodrugs LY2979165 and LY2140023 attenuate the functional imaging response to ketamine in healthy subjects.

Authors:  Mitul A Mehta; Anne Schmechtig; Vasileia Kotoula; Juliet McColm; Kimberley Jackson; Claire Brittain; Sitra Tauscher-Wisniewski; Bruce J Kinon; Paul D Morrison; Thomas Pollak; Timothy Mant; Steven C R Williams; Adam J Schwarz
Journal:  Psychopharmacology (Berl)       Date:  2018-03-21       Impact factor: 4.530

Review 5.  Group I and group II metabotropic glutamate receptor allosteric modulators as novel potential antipsychotics.

Authors:  Adam G Walker; P Jeffrey Conn
Journal:  Curr Opin Pharmacol       Date:  2014-11-27       Impact factor: 5.547

Review 6.  Managing Negative Symptoms of Schizophrenia: How Far Have We Come?

Authors:  Joshua T Kantrowitz
Journal:  CNS Drugs       Date:  2017-05       Impact factor: 5.749

Review 7.  Metabotropic Glutamate Receptors As Emerging Targets for the Treatment of Schizophrenia.

Authors:  Shalini Dogra; P Jeffrey Conn
Journal:  Mol Pharmacol       Date:  2022-03-03       Impact factor: 4.054

Review 8.  Targeting metabotropic glutamate receptors for novel treatments of schizophrenia.

Authors:  James Maksymetz; Sean P Moran; P Jeffrey Conn
Journal:  Mol Brain       Date:  2017-04-26       Impact factor: 4.041

Review 9.  The Role of G Protein-Coupled Receptors (GPCRs) and Calcium Signaling in Schizophrenia. Focus on GPCRs Activated by Neurotransmitters and Chemokines.

Authors:  Tomasz Boczek; Joanna Mackiewicz; Marta Sobolczyk; Julia Wawrzyniak; Malwina Lisek; Bozena Ferenc; Feng Guo; Ludmila Zylinska
Journal:  Cells       Date:  2021-05-17       Impact factor: 6.600

10.  Effects of N-acetylcysteine on brain glutamate levels and resting perfusion in schizophrenia.

Authors:  Grant McQueen; John Lally; Tracy Collier; Fernando Zelaya; David J Lythgoe; Gareth J Barker; James M Stone; Philip McGuire; James H MacCabe; Alice Egerton
Journal:  Psychopharmacology (Berl)       Date:  2018-08-23       Impact factor: 4.530

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