AZD2066 News - LARVOL Sigma

|||||||||| Review, Journal: Novel Glutamatergic Modulators for the Treatment of Mood Disorders: Current Status. (Pubmed Central) - Jan 7, 2022
Furthermore, to date, most have demonstrated relatively modest effects compared with (R,S)-ketamine and esketamine, though some have shown more favorable characteristics. Of these novel agents, the most promising, and the ones for which the most evidence exists, appear to be those targeting ionotropic glutamate receptors.

|||||||||| mavoglurant (AFQ056) / Novartis, AZD2066 / AstraZeneca, basimglurant (RG7090) / Roche
Journal: Location and cell-type specific bias of metabotropic glutamate receptor, mGlu5, negative allosteric modulators. (Pubmed Central) - Sep 27, 2020
Moreover, biotinylation studies reveal that more than 90% of the receptor is intracellular in these neurons. Taken together, these data indicate that the tested NAMs exhibit both location-dependent and cell type specific bias for mGlu5-mediated Ca2+ mobilization which may affect clinical outcomes.

|||||||||| Journal: Detailed in vitro pharmacological characterization of clinically tested negative allosteric modulators of the metabotropic glutamate receptor 5 (mGlu5). (Pubmed Central) - Aug 1, 2020
Negative allosteric modulators (NAMs) have shown promising results in preclinical models but have so far failed in human clinical trials. Here we provide the most comprehensive and comparative molecular pharmacological study to date of nine preclinical/clinical tested negative allosteric modulators (NAMs) at the mGlu5 receptor, which is also the first study to measure binding kinetics and negative allosteric modulation of mGlu5 receptor internalization.

|||||||||| Journal: Glutamatergic Modulators in Depression. (Pubmed Central) - Jun 7, 2019
These results have prompted the repurposing or development of other glutamatergic modulators, both as monotherapy or adjunctive to other therapies. Here, we highlight the evidence supporting the antidepressant effects of various glutamatergic modulators, including (1) broad glutamatergic modulators (ketamine, esketamine, dextromethorphan, dextromethorphan-quinidine [Nuedexta], AVP-786, nitrous oxide [N2O], AZD6765), (2) subunit (NR2B)-specific N-methyl-D-aspartate (NMDA) receptor antagonists (CP-101,606/traxoprodil, MK-0657 [CERC-301]), (3) glycine-site partial agonists (D-cycloserine, GLYX-13, sarcosine, AV-101), and (4) metabotropic glutamate receptor modulators (AZD2066, RO4917523/basimglurant, JNJ40411813/ADX71149, R04995819 [RG1578]).

||||||||||  AZD2066 / AstraZeneca
Enrollment change:  Study to Evaluate the Analgesic Efficacy of 28 Days' Oral Administration of AZD2066 Compared With Placebo in Patients With Painful Diabetic Neuropathy (clinicaltrials.gov) -  Sep 27, 2012
P2a, N=127, Completed,  Sponsor: AstraZeneca
Here, we highlight the evidence supporting the antidepressant effects of various glutamatergic modulators, including (1) broad glutamatergic modulators (ketamine, esketamine, dextromethorphan, dextromethorphan-quinidine [Nuedexta], AVP-786, nitrous oxide [N2O], AZD6765), (2) subunit (NR2B)-specific N-methyl-D-aspartate (NMDA) receptor antagonists (CP-101,606/traxoprodil, MK-0657 [CERC-301]), (3) glycine-site partial agonists (D-cycloserine, GLYX-13, sarcosine, AV-101), and (4) metabotropic glutamate receptor modulators (AZD2066, RO4917523/basimglurant, JNJ40411813/ADX71149, R04995819 [RG1578]). N=334 --> 127

||||||||||  AZD2066 / AstraZeneca
Enrollment change:  6-week Study Treatment to Evaluate the Safety and Effectiveness of AZD2066 in Patients With Major Depressive Disorder (clinicaltrials.gov) -  Aug 27, 2012
P2a, N=131, Terminated,  Sponsor: AstraZeneca
N=334 --> 127 N=210 --> 131

||||||||||  AZD2066 / AstraZeneca
Enrollment change:  AZD2066 Neuropathic Pain - Mechanical Hypersensitivity (clinicaltrials.gov) -  Aug 27, 2012
P2a, N=87, Terminated,  Sponsor: AstraZeneca
N=210 --> 131 N=385 --> 87



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