更新于：2024-11-13
CERC-301
更新于：2024-11-13
概要
基本信息
非在研机构 |
最高研发阶段临床2期 |
首次获批日期- |
最高研发阶段(中国)- |
特殊审评- |
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结构
分子式C19H23FN4O2 |
InChIKeyRECBFDWSXWAXHY-IAGOWNOFSA-N |
CAS号808732-98-1 |
关联
4
项与 CERC-301 相关的临床试验A Randomized, Double-Blind, Placebo-Controlled Study of Intermittent Doses of CERC-301 in the Treatment of Subjects With Severe Depression Despite Antidepressant Treatment
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
A Randomized, Double-Blind, Placebo-Controlled, 2-Period Crossover Study to Evaluate Effectiveness of Single-Dose MK0657 in Combination With Levodopa on Motor Symptoms and Dyskinesias in Patients With Parkinson's Disease
100 项与 CERC-301 相关的临床结果
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100 项与 CERC-301 相关的转化医学
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100 项与 CERC-301 相关的专利（医药）
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24
项与 CERC-301 相关的文献（医药）2023-12-20ACS chemical neuroscience
Characterization of (R)- and (S)-[18F]OF-NB1 in Rodents as Positron Emission Tomography Probes for Imaging GluN2B Subunit-Containing N-Methyl-d -Aspartate Receptors
Article
作者: Gruber, Stefan ; Gisler, Livio ; Sippl, Wolfgang ; Liang, Steven H ; Haider, Ahmed ; Keller, Claudia ; Wallimann, Rahel ; Ametamey, Simon M ; Ahmed, Hazem ; Elghazawy, Nehal H
The N-methyl-d-aspartate receptor (NMDAR) subtype 2B (GluN1/2B) is implicated in various neuropathologies. Given the lack of a validated radiofluorinated positron emission tomography (PET) probe for the imaging of GluN1/2B receptors, we comprehensively investigated the enantiomers of [18F]OF-NB1 in rodents. Particularly, the (R)- and (S)- enantiomers were evaluated using in silico docking, in vitro autoradiography, in vivo PET imaging, and ex vivo biodistribution studies. 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. Additionally, a nonmetal-mediated radiofluorination strategy was devised that harnesses the potential of diaryliodoniums in the nucleophilic radiofluorination of nonactivated aromatic compounds. Both enantiomers exhibited known GluN1/2B binding patterns; however, the R-enantiomer showed higher GluN1/2B-specific accumulation in rodent autoradiography and higher brain uptake in PET imaging experiments compared to the S-enantiomer. Molecular simulation studies provided further insights with respect to the difference in binding, whereby a reduced ligand-receptor interaction was observed for the S-enantiomer. 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)-[18F]OF-NB1 appears to exhibit the characteristics of a suitable PET probe for imaging of GluN2B-containing NMDARs in clinical studies.
2022-10-01European neuropsychopharmacology : the journal of the European College of Neuropsychopharmacology
New antidepressants: New day or false dawn?
Article
作者: Young, Allan H ; Jelen, Luke A
A review.This review is on the new antidepressants.Building on evidence for the rapid antidepressant effects of ketamine, investigators have explored whether alternative NMDA receptor antagonists may share ketamine′s antidepressant properties, however clin. studies of several other NMDA receptor antagonists and NMDA receptor site modulators (e.g., memantine, GLYX-13, CERC-301) have failed to produce convincing results.However, despite intranasal esketamine and brexanolone receiving licenses for the treatment of TRD and post-partum depression resp., there are ongoing debates with regards to cost-effectiveness, deliverability, and in ketamine′s case, particular concerns regarding longer-term efficacy, safety, and abuse liability.
2021-09-12Cochrane Database of Systematic Reviews
Ketamine and other glutamate receptor modulators for depression in adults with unipolar major depressive disorder.
Review
作者: Hollingsworth, Sarah ; Turner, Erick H ; Marquardt, Tahnee ; Smith, Rebecca ; Cipriani, Andrea ; McShane, Rupert ; Barnes, Annabelle ; Hawton, Keith ; Hurducas, Claudia ; Spyridi, Styliani ; Dean, Rebecca L ; Cowen, Philip J
BACKGROUND:
Many studies have recently been conducted to assess the antidepressant efficacy of glutamate modification in mood disorders. This is an update of a review first published in 2015 focusing on the use of glutamate receptor modulators in unipolar depression.
OBJECTIVES:
To assess the effects - and review the acceptability and tolerability - of ketamine and other glutamate receptor modulators in alleviating the acute symptoms of depression in people with unipolar major depressive disorder.
SEARCH METHODS:
We searched the Cochrane Central Register of Controlled Trials (CENTRAL), Ovid MEDLINE, Embase and PsycINFO all years to July 2020. We did not apply any restrictions to date, language or publication status.
SELECTION CRITERIA:
Double- or single-blinded randomised controlled trials (RCTs) comparing ketamine, memantine, esketamine or other glutamate receptor modulators with placebo (pill or saline infusion), other active psychotropic drugs, or electroconvulsive therapy (ECT) in adults with unipolar major depression.
DATA COLLECTION AND ANALYSIS:
Three review authors independently identified studies, assessed trial quality and extracted data. The primary outcomes were response rate (50% reduction on a standardised rating scale) and adverse events. We decided a priori to measure the efficacy outcomes at different time points and run sensitivity/subgroup analyses. Risk of bias was assessed using the Cochrane tool, and certainty of the evidence was assessed using GRADE.
MAIN RESULTS:
Thirty-one new studies were identified for inclusion in this updated review. Overall, we included 64 studies (5299 participants) on ketamine (31 trials), esketamine (9), memantine (5), lanicemine (4), D-cycloserine (2), Org26576 (2), riluzole (2), atomoxetine (1), basimglurant (1), citicoline (1), CP-101,606 (1), decoglurant (1), MK-0657 (1), N-acetylcysteine (1), rapastinel (1), and sarcosine (1). Forty-eight studies were placebo-controlled, and 48 were two-arm studies. The majority of trials defined an inclusion criterion for the severity of depressive symptoms at baseline: 29 at least moderate depression; 17 severe depression; and five mild-to-moderate depression. Nineteen studies recruited only patients with treatment-resistant depression, defined as inadequate response to at least two antidepressants. The majority of studies investigating ketamine administered as a single dose, whilst all of the included esketamine studies used a multiple dose regimen (most frequently twice a week for four weeks). Most studies looking at ketamine used intravenous administration, whilst the majority of esketamine trials used intranasal routes. The evidence suggests that ketamine may result in an increase in response and remission compared with placebo at 24 hours odds ratio (OR) 3.94, 95% confidence interval (CI) 1.54 to 10.10; n = 185, studies = 7, very low-certainty evidence). Ketamine may reduce depression rating scale scores over placebo at 24 hours, but the evidence is very uncertain (standardised mean difference (SMD) -0.87, 95% CI -1.26 to -0.48; n = 231, studies = 8, very low-certainty evidence). There was no difference in the number of participants assigned to ketamine or placebo who dropped out for any reason (OR 1.25, 95% CI 0.19 to 8.28; n = 201, studies = 6, very low-certainty evidence). When compared with midazolam, the evidence showed that ketamine increases remission rates at 24 hours (OR 2.21, 95% CI 0.67 to 7.32; n = 122,studies = 2, low-certainty evidence). The evidence is very uncertain about the response efficacy of ketamine at 24 hours in comparison with midazolam, and its ability to reduce depression rating scale scores at the same time point (OR 2.48, 95% CI 1.00 to 6.18; n = 296, studies = 4,very low-certainty evidence). There was no difference in the number of participants who dropped out of studies for any reason between ketamine and placebo (OR 0.33, 95% CI 0.05 to 2.09; n = 72, studies = 1, low-certainty evidence). Esketamine treatment likely results in a large increase in participants achieving remission at 24 hours compared with placebo (OR 2.74, 95% CI 1.71 to 4.40; n = 894, studies = 5, moderate-certainty evidence). Esketamine probably results in decreases in depression rating scale scores at 24 hours compared with placebo (SMD -0.31, 95% CI -0.45 to -0.17; n = 824, studies = 4, moderate-certainty evidence). Our findings show that esketamine increased response rates, although this evidence is uncertain (OR 2.11, 95% CI 1.20 to 3.68; n = 1071, studies = 5, low-certainty evidence). There was no evidence that participants assigned to esketamine treatment dropped out of trials more frequently than those assigned to placebo for any reason (OR 1.58, 95% CI 0.92 to 2.73; n = 773, studies = 4,moderate-certainty evidence). We found very little evidence for the remaining glutamate receptor modulators. We rated the risk of bias as low or unclear for most domains, though lack of detail regarding masking of treatment in the studies reduced our certainty in the effect for all outcomes.
AUTHORS' CONCLUSIONS:
Our findings show that ketamine and esketamine may be more efficacious than placebo at 24 hours. How these findings translate into clinical practice, however, is not entirely clear. 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.
1
项与 CERC-301 相关的新闻（医药）2024-09-12
临床2期快速通道临床1期并购
100 项与 CERC-301 相关的药物交易
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研发状态
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 中度重度抑郁症 | 临床2期 | 美国 | 2015-06-01 | |
| 自杀意念 | 临床2期 | 美国 | 2013-11-01 | |
| 重度抑郁症 | 临床2期 | 美国 | 2013-11-01 | |
| 运动失调 | 临床1期 | - | 2007-05-01 | |
| 帕金森病 | 临床1期 | - | 2007-05-01 | |
| 直立性低血压 | 临床1期 | 美国 | - | |
| 痛觉过敏 | 临床前 | 美国 | 2007-01-24 | |
| 伤害性疼痛 | 临床前 | 美国 | 2007-01-24 |
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临床结果
临床结果
适应症
分期
评价
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临床1期 | 22 | 蓋鑰窪鏇襯夢繭夢襯膚(鏇壓窪觸選壓範繭顧壓) = 廠願壓壓膚築餘糧鏇範 衊鏇構壓醖構壓鏇遞齋 (襯餘廠夢鹽艱構簾壓選, -5.1 ~ 0.4) 更多 | 不佳 | 2017-01-01 |
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