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更新于：2026-02-28
ENX-102
更新于：2026-02-28
概要
基本信息
药物类型 小分子化药 |
别名 ENX 102、ENX-102 |
作用方式 调节剂 |
作用机制 GABAA receptor调节剂(γ-氨基丁酸 A 受体调节剂) |
治疗领域 |
在研适应症 |
非在研适应症- |
非在研机构- |
权益机构- |
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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关联
6
项与 ENX-102 相关的临床试验NCT07193563
The ENCalmSocial Trial: A Randomized, Double-Blind, Placebo-Controlled Monotherapy Trial to Evaluate the Efficacy and Safety of ENX-102 in Participants With Social Anxiety Disorder
NCT06653296
A Randomized, Double-blind, Placebo-controlled Study to Evaluate the Safety and Tolerability of ENX-102 and Determine a Dose-response for ENX-102 in Patients With Generalized Anxiety Disorder (GAD)
NCT05749055
The ENCALM Trial: A Randomized, Double-blind, Placebo-controlled Monotherapy Trial to Evaluate the Efficacy and Safety of ENX-102 in Patients With Generalized Anxiety Disorder
100 项与 ENX-102 相关的临床结果
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100 项与 ENX-102 相关的转化医学
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100 项与 ENX-102 相关的专利（医药）
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1
项与 ENX-102 相关的文献（医药）Cells
Biomarker-Based Pharmacological Characterization of ENX-102, a Novel α2/3/5 Subtype-Selective GABAA Receptor Positive Allo-Steric Modulator: Translational Insights from Rodent and Human Studies
Article
作者: Nettesheim, Pauline ; Vanover, Kimberly E. ; Sudarsan, Vikram ; Brubaker, William ; Serrats, Jordi ; Parks, Stephanie ; Cunningham, Stephen ; Borghans, Laura G. J. M. ; Arce, Estibaliz ; Taylor, Eve ; Jacobs, Gabriel E. ; Klaassen, Erica ; Vadodaria, Krishna C. ; Stuurman, Frederik E.
Gamma-aminobutyric acid type A receptors (GABAARs) are pentameric ligand-gated ion channels essential for inhibitory neurotransmission in the central nervous system. Subtype-specific expression patterns of GABAAR subunits underlie their diverse roles in regulating anxiety, motor function, and sedation. While non-selective GABAAR positive allosteric modulators (PAMs), such as benzodiazepines, are clinically effective anxiolytic drugs, their non-selective activity across α1/2/3/5 subunit-containing GABAARs leads to sedation, cognitive impairment, and risk of dependence. To address this, we evaluated ENX-102, a novel GABAAR PAM, which exhibits selectivity for α2/3/5 subunits. In rodents, ENX-102 demonstrated dose-dependent anxiolytic-like activity following acute and sub-chronic administration, without sedation. ENX-102 exhibited a dose-dependent quantitative electroencephalography (qEEG) spectral signature in rodents that was distinct from that of benzodiazepines. In a double-blind, placebo-controlled, multiple-ascending dose study in healthy human volunteers, ENX-102 was evaluated using the NeuroCart, a CNS test battery including saccadic peak velocity (SPV), adaptive tracking, pupillometry, body sway, the Bond and Lader Visual Analog Scale (VAS), the Visual Verbal Learning Task (VVLT), and qEEG. ENX-102 produced reductions in SPV that were indicative of central target engagement, with minimal effects on alertness and motor coordination, which is consistent with subtype-selective GABAAR targeting. Notably, qEEG revealed increased β-band power and decreased δ- and θ-band activity, which were distinct from the spectral profile of non-selective PAMs, supporting translational alignment with preclinical findings. Across dose levels, ENX-102 was well tolerated and exhibited favorable pharmacokinetics. These results support further clinical development of ENX-102 as a next-generation GABAAR subtype-selective anxiolytic drug.
100 项与 ENX-102 相关的药物交易
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研发状态
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 广泛性焦虑障碍 | 临床2期 | 美国 | 2023-07-03 | |
| 焦虑症 | 临床1期 | 荷兰 | 2021-11-03 |
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临床结果
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