预约演示
更新于：2026-09-07
Osavampator
更新于：2026-09-07
概要
基本信息
药物类型 小分子化药 |
别名 NBI 1065845、NBI-'845、TAK 653 + [1] |
作用方式 激动剂 |
作用机制 AMPA receptor激动剂(离子型谷氨酸受体AMPA激动剂) |
治疗领域 |
在研适应症 |
非在研适应症 |
最高研发阶段临床3期 |
首次获批日期- |
最高研发阶段(中国)- |
特殊审评- |
登录后查看时间轴
结构/序列
分子式C19H23N3O3S |
InChIKeyPXJBHEHFVQVDDS-UHFFFAOYSA-N |
CAS号1358751-06-0 |
关联
9
项与 Osavampator 相关的临床试验NCT07196501
A Randomized, Double-Blind, Placebo-Controlled Study to Evaluate the Maintenance of Effect of NBI-1065845 as an Adjunctive Treatment in Subjects With Major Depressive Disorder (MDD)
NCT06963021
A Randomized, Double-Blind, Placebo-Controlled Study to Assess the Efficacy and Safety of NBI-1065845 as Adjunctive Treatment in Subjects With Major Depressive Disorder (MDD)
NCT06966401
A Long-Term, Open-Label Study to Assess the Safety and Tolerability of NBI-1065845 as Adjunctive Treatment in Subjects With Major Depressive Disorder (MDD)
100 项与 Osavampator 相关的临床结果
登录后查看更多信息
100 项与 Osavampator 相关的转化医学
登录后查看更多信息
100 项与 Osavampator 相关的专利（医药）
登录后查看更多信息
10
项与 Osavampator 相关的文献（医药）2025-10-01PHARMACOLOGICAL RESEARCH
All roads lead to glutamate: NMDA and AMPA receptors as targets for rapid-acting antidepressants
Review
作者: Freudenberg, Florian ; Reif, Andreas ; McKernan, Ruth M ; Dawson, Gerard R ; Reif-Leonhard, Christine
Treatment-resistant depression (TRD) represents a major clinical challenge. Affecting about 30 % of major depressive disorder (MDD) patients, effective treatments for TRD are urgently needed. While depression research and antidepressant (AD) development have long centred on monoaminergic targets, research over the past 35 years has increasingly explored glutamatergic mechanisms. Here we present an extended discussion on developments in glutamatergic drug discovery, focusing on mechanistic convergence between NMDA and AMPA receptor signalling. Beyond established rapid-acting antidepressants (RAADs), such as (es)ketamine and dextromethorphan/bupropion (AXS-05), we highlight novel therapeutic directions involving esmethadone (REL-1017), nitrous oxide, and positive allosteric modulators (PAMs) of NMDA receptors (e.g. rapastinel, zelquistinel, and apimostinel). Moreover, we discuss forward-looking strategies using AMPA receptor PAMs (e.g. osavampator and tulrampator) and targeting of AMPA receptor-interacting proteins. By integrating recent clinical evidence with molecular and physiological findings, we highlight a convergent mechanism across these compounds. This involves increased AMPA receptor activation, triggering BDNF release and mTOR signalling, promoting synaptic strengthening through enhanced AMPA receptor trafficking and dendritic spine formation. Together, targeting glutamatergic signalling represents a transformative path for TRD treatment with high efficacy by more directly modulating pathologically affected signalling modules. These developments place glutamatergic agents at the forefront of next-generation AD strategies.
2024-05-01CTS-Clinical and Translational Science
Effects of the selective AMPA modulator NBI ‐1065845 on the pharmacokinetics of midazolam or ethinyl estradiol–levonorgestrel in healthy adults
Article
作者: Adrian Ionescu ; Jaskaran B. Singh ; David P. Walling ; Jessica Maynard‐Scott ; Mike Kennedy ; Swan Lin ; Maura Furey
Abstract:
This parallel‐arm, phase I study investigated the potential cytochrome P450 (CYP)3A induction effect of NBI‐1065845 (TAK‐653), an investigational α‐amino‐3‐hydroxy‐5‐methyl‐4‐isoxazolepropionic acid receptor potentiator in phase II development for major depressive disorder. The midazolam treatment arm received the sensitive CYP3A substrate midazolam on Day 1, followed by NBI‐1065845 alone on Days 5–13; on Day 14, NBI‐1065845 was administered with midazolam, then NBI‐1065845 alone on Day 15. The oral contraceptive treatment arm received ethinyl estradiol–levonorgestrel on Day 1, then NBI‐1065845 alone on Days 5–13; on Day 14, NBI‐1065845 was administered with ethinyl estradiol–levonorgestrel, then NBI‐1065845 alone on Days 15–17. Blood samples were collected for pharmacokinetic analyses. The midazolam treatment arm comprised 14 men and 4 women, of whom 16 completed the study. Sixteen of the 17 healthy women completed the oral contraceptive treatment arm. After multiple daily doses of NBI‐1065845, the geometric mean ratios (GMRs) (90% confidence interval) for maximum observed concentration were: midazolam, 0.94 (0.79–1.13); ethinyl estradiol, 1.00 (0.87–1.15); and levonorgestrel, 0.99 (0.87–1.13). For area under the plasma concentration–time curve (AUC) from time 0 to infinity, the GMRs were as follows: midazolam, 0.88 (0.78–0.98); and ethinyl estradiol, 1.01 (0.88–1.15). For levonorgestrel, the GMR for AUC from time 0 to the last quantifiable concentration was 0.87 (0.78–0.96). These findings indicate that NBI‐1065845 is not a CYP3A inducer and support its administration with CYP3A substrates. NBI‐1065845 was generally well tolerated, with no new safety signals observed after coadministration of midazolam, ethinyl estradiol, or levonorgestrel.
2023-01-01Neuropharmacology
Role of the AMPA receptor in antidepressant effects of ketamine and potential of AMPA receptor potentiators as a novel antidepressant
Review
作者: Atsushi Suzuki ; Hiroe Hara ; Haruhide Kimura
Ketamine exerts rapid and long-lasting antidepressant effects in patients with treatment-resistant depression. However, its clinical use is limited by its undesirable psychotomimetic side effects. Accumulating evidence from preclinical studies has shown that the antidepressant effects of ketamine are dependent on α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor (AMPA-R) activation, which triggers activation of the mechanistic target of rapamycin pathway and brain-derived neurotrophic factor release. Thus, AMPA-R has emerged as a promising new target for novel antidepressants with a rapid onset of action. However, almost all known AMPA-R potentiators carry the risk of a narrow bell-shaped dose-response curve and a poor safety margin against seizures. Our data suggest that agonistic activity is not only related to the risks of bell-shaped dose-response curves and seizures but also to the reduced synaptic transmission and procognitive effects of AMPA-R potentiators. In this review, we describe our original screening approach that led to the discovery of an investigational AMPA-R potentiator with low agonistic activity, TAK-653. We further review the in vitro and in vivo profiles of TAK-653, including its procognitive and antidepressant-like effects, as well as its safety profile, in comparison with known AMPA-R potentiators with agonistic activity and AMPA, an AMPA-R agonist. The low agnostic activity of TAK-653 may overcome limitations of known AMPA-R potentiators. This article is part of the Special Issue on 'Ketamine and its Metabolites'.
100 项与 Osavampator 相关的药物交易
登录后查看更多信息
研发状态
10 条进展最快的记录, 后查看更多信息
登录
| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 重度抑郁症 | 临床3期 | 美国 | 2025-01-22 | |
| 难治性抑郁症 | 临床2期 | - | 2018-02-15 | |
| 抑郁症 | 临床1期 | 英国 | 2015-08-26 |
登录后查看更多信息
临床结果
临床结果
适应症
分期
评价
查看全部结果
临床2期 | 183 | (High Dose) | 鑰範簾鑰築膚繭網鏇醖(鹹獵積蓋繭願簾艱繭鏇) = 範範壓遞鬱壓憲糧艱構 襯醖網簾鏇鬱夢願壓鏇 (鹹鹹艱襯餘築鏇觸鹹餘 ) 达到 更多 | 积极 | 2024-04-23 | ||
(Low Dose) | 鑰範簾鑰築膚繭網鏇醖(鹹獵積蓋繭願簾艱繭鏇) = 遞顧願衊餘範觸壓鏇鹹 襯醖網簾鏇鬱夢願壓鏇 (鹹鹹艱襯餘築鏇觸鹹餘 ) 达到 更多 | ||||||
临床1期 | - | 24 | 淵淵衊醖鑰廠繭廠鏇衊(獵鏇糧繭壓齋餘鹽膚鹹) = 鬱遞鑰遞鹽襯製壓顧鬱 鏇壓齋夢膚願淵廠衊積 (製願獵廠鹽窪鏇餘選鑰, 5.98 ~ 32.99) | - | 2022-09-24 | ||
TAK-653 6 mg | 衊鹹選築齋廠蓋遞鹹襯(鹽願遞遞鑰觸觸齋範蓋) = 蓋製獵蓋繭獵築糧製網 獵網糧繭餘繭廠襯願範 (壓夢築淵構鬱繭壓糧襯, 0.51 ~ 2.84) 更多 | ||||||
临床1期 | - | 24 | placebo+TAK-653 (Placebo) | 願鏇顧壓衊選鹹壓鏇鑰(憲製範構壓糧襯齋艱衊) = 壓簾憲製鑰齋網蓋遞夢 築鹹鹹鬱襯鬱製鏇遞鹽 (獵鹹選淵築窪顧餘夢鑰, 693.1535) 更多 | - | 2020-07-02 | |
(TAK-653 0.5 mg) | 願鏇顧壓衊選鹹壓鏇鑰(憲製範構壓糧襯齋艱衊) = 顧簾繭鹹廠餘遞窪衊衊 築鹹鹹鬱襯鬱製鏇遞鹽 (獵鹹選淵築窪顧餘夢鑰, 591.1367) 更多 |
登录后查看更多信息
转化医学
使用我们的转化医学数据加速您的研究。
登录
或
药物交易
使用我们的药物交易数据加速您的研究。
登录
或
核心专利
使用我们的核心专利数据促进您的研究。
登录
或
临床分析
紧跟全球注册中心的最新临床试验。
登录
或
批准
利用最新的监管批准信息加速您的研究。
登录
或
特殊审评
只需点击几下即可了解关键药物信息。
登录
或
提出任何生物医药研究问题
让每一步生物医药决策都精准制胜
基于十亿级生物数据与全球情报的精准 AI，赋能早期药物发现
立即开始免费试用!
智慧芽新药情报库是智慧芽专为生命科学人士构建的基于AI的创新药情报平台，助您全方位提升您的研发与决策效率。
立即接入生物医药数据包
智慧芽新药库数据也通过智慧芽开放平台，以MCP或API服务形式对外开放。立即使用我们的MCP服务定制您的LLM智能体。
生物序列数据库
生物药研发创新
免费使用
化学结构数据库
小分子化药研发创新
免费使用