- |||||||||| rislenemdaz (CERC-301) / Avalo Therap
Preclinical, Journal: Characterization of (R)- and (S)-[F]OF-NB1 in Rodents as Positron Emission Tomography Probes for Imaging GluN2B Subunit-Containing N-Methyl-d-Aspartate Receptors. (Pubmed Central) - Dec 7, 2023
A select panel of GluN1/2B antagonists (CP-101,606, CERC-301, and eliprodil) and the off-target sigma-1 receptor ligands (fluspidine and SA4503) were used to determine the specificity and selectivity of the tested enantiomers...Nonetheless, both enantiomers showed dose dependency when two different doses (1 and 5 mg/kg) of the GluN1/2B antagonist, CP-101,606, were used in the PET imaging study. Taken together, (R)-[F]OF-NB1 appears to exhibit the characteristics of a suitable PET probe for imaging of GluN2B-containing NMDARs in clinical studies.
- |||||||||| lithium carbonate ER / Generic mfg., ketamine / Generic mfg.
Review, Journal: Ketamine and Other Glutamate Receptor Modulating Agents for Treatment-Resistant Depression: A Systematic Review of Randomized Controlled Trials. (Pubmed Central) - Dec 8, 2022
Lithium, lanicemine, D-cycloserine, and decoglurant showed mixed results for efficacy, and, riluzole, and 7-chlorokynurenic acid were mostly comparable to placebo...Nevertheless, ketamine could be used as an efficacious drug in TRD; still, additional studies are needed to delineate the optimum dosage, duration of efficacy, and intervals. Further studies are also recommended on the effectiveness of glutamatergic system modulators other than ketamine on treatment-resistant depression.
- |||||||||| Review: Investigational Drugs for the Treatment of Depression (Part 2): Glutamatergic, Cholinergic, Sestrin Modulators, and Other Agents. (Pubmed Central) - Jul 20, 2022
Sestrin modulators, cholinergic receptor modulators, or onabotulinumtoxinA have also been investigated for potential antidepressant activity. In conclusion, there is hope for new treatments in uni- and bipolar depression, as it became clear, after almost 7 decades of monoamine-modulating antidepressants, that new pathogenetic pathways should be targeted to increase the response rate in this population.
- |||||||||| 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.
- |||||||||| ketamine / Generic mfg., atomoxetine / Generic mfg., memantine / Generic mfg.
Clinical, Review, Journal: Ketamine and other glutamate receptor modulators for depression in adults with unipolar major depressive disorder. (Pubmed Central) - Nov 29, 2021
The evidence for use of the remaining glutamate receptor modulators is limited as very few trials were included in the meta-analyses for each comparison and the majority of comparisons included only one study. Long term non-inferiority RCTs comparing repeated ketamine and esketamine, and rigorous real-world monitoring are needed to establish comprehensive data on safety and efficacy.
- |||||||||| rislenemdaz (CERC-301) / Cerecor
Preclinical, Journal: Rislenemdaz treatment in the lateral habenula improves despair-like behavior in mice. (Pubmed Central) - Jun 24, 2021
Specific knockdown of BDNF in the LHb prevented CRS-induced despair-like behavior, while preventing CRS-induced increases in BDNF and c-Fos expression in the LHb. Together these results suggest that Ris may exert its antidepressant effects through affecting the LHb such as downregulating BDNF expression in the LHb.
- |||||||||| ganaxolone oral (CCD-1042) / Marinus
Review, Journal: A new generation of antidepressants: an update on the pharmaceutical pipeline for novel and rapid-acting therapeutics in mood disorders based on glutamate/GABA neurotransmitter systems. (Pubmed Central) - Aug 3, 2019
Here, we review progress in the development of compounds that act on these systems as well as their purported mechanisms of action. We include glutamate-targeting drugs, such as racemic ketamine, esketamine, lanicemine (AZD6765), traxoprodil (CP-101,606), EVT-101, rislenemdaz (CERC-301/MK-0657), AVP-786, AXS-05, rapastinel (formerly GLYX-13), apimostinel (NRX-1074/AGN-241660), AV-101, NRX-101, basimglurant (RO4917523), decoglurant (RG-1578/RO4995819), tulrampator (CX-1632/S-47445), and riluzole; and GABA-targeting agents, such as brexanolone (SAGE-547), ganaxolone, and SAGE-217.
- |||||||||| memantine / generics
Journal: NMDA Antagonists for Treatment-Resistant Depression. (Pubmed Central) - Jul 24, 2019
...Of the other investigational agents, CERC-301 and rapastinel remain in clinical development...Research is still needed to determine the appropriate dose, schedule, and ways to mitigate against unwanted side effects of NMDA receptor blockade. These hurdles need to be overcome before ketamine and similar agents can be prescribed routinely to patients.
- |||||||||| 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]).
- |||||||||| rislenemdaz (CERC-301) / Avalo Therap
Trial completion: A Study of Intermittent Doses of CERC-301 in MDD (clinicaltrials.gov) - Jan 5, 2017
P2, N=115, Completed,
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]). Active, not recruiting --> Completed
- |||||||||| rislenemdaz (CERC-301) / Avalo Therap
Enrollment closed: A Study of Intermittent Doses of CERC-301 in MDD (clinicaltrials.gov) - Sep 29, 2016
P2, N=115, Active, not recruiting,
Active, not recruiting --> Completed Recruiting --> Active, not recruiting
- |||||||||| rislenemdaz (CERC-301) / Avalo Therap
Trial primary completion date: A Study of Intermittent Doses of CERC-301 in MDD (clinicaltrials.gov) - May 24, 2016
P2, N=104, Recruiting,
Recruiting --> Active, not recruiting Trial primary completion date: May 2016 --> Sep 2016
- |||||||||| rislenemdaz (CERC-301) / Avalo Therap
Enrollment open: A Study of Intermittent Doses of CERC-301 in MDD (clinicaltrials.gov) - Aug 26, 2015
P2, N=96, Recruiting,
Trial primary completion date: May 2016 --> Sep 2016 Not yet recruiting --> Recruiting
- |||||||||| rislenemdaz (CERC-301) / Avalo Therap
Enrollment closed: A Randomized, Double-Blind, Placebo-Controlled, Sequential Parallel Study of CERC-301 in the Adjunctive Treatment of Subjects With Severe Depression and Recent Active Suicidal Ideation Despite Antidepressant Treatment (clinicaltrials.gov) - Aug 1, 2014
P2, N=135, Active, not recruiting,
Active, not recruiting --> Completed | N=135 --> 1357 Recruiting --> Active, not recruiting
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