预约演示

更新于：2025-01-23

GluN2B

更新于：2025-01-23

基本信息

别名

GluN2B、Glutamate [NMDA] receptor subunit epsilon-2、glutamate ionotropic receptor NMDA type subunit 2B

+ [9]

简介

Component of NMDA receptor complexes that function as heterotetrameric, ligand-gated ion channels with high calcium permeability and voltage-dependent sensitivity to magnesium. Channel activation requires binding of the neurotransmitter glutamate to the epsilon subunit, glycine binding to the zeta subunit, plus membrane depolarization to eliminate channel inhibition by Mg(2+) (PubMed:8768735, PubMed:26919761, PubMed:26875626, PubMed:28126851). Sensitivity to glutamate and channel kinetics depend on the subunit composition (PubMed:8768735, PubMed:26875626). In concert with DAPK1 at extrasynaptic sites, acts as a central mediator for stroke damage. Its phosphorylation at Ser-1303 by DAPK1 enhances synaptic NMDA receptor channel activity inducing injurious Ca2+ influx through them, resulting in an irreversible neuronal death. Contributes to neural pattern formation in the developing brain. Plays a role in long-term depression (LTD) of hippocampus membrane currents and in synaptic plasticity (By similarity).

关联

磺胺甲噁唑/甘草酸二钾/氨基己酸/牛磺酸

靶点

11β-HSD1 x GluN2B x Plasminogen activators x bacterial DHPS

作用机制

11β-HSD1抑制剂 [+4]

在研机构

OPTUS Pharmaceutical Co., Ltd.

原研机构

OPTUS Pharmaceutical Co., Ltd.

在研适应症

睑缘炎 [+2]

非在研适应症-

最高研发阶段批准上市

首次获批国家/地区

韩国

首次获批日期2024-10-17

Taurine

牛磺酸

靶点

GluN2B

作用机制

GluN2B拮抗剂 [+1]

在研机构-

原研机构-

在研适应症

膳食补充剂

非在研适应症-

最高研发阶段批准上市

首次获批国家/地区-

首次获批日期1800-01-20

Salfaprodil

索法地尔

靶点

GluN2B

作用机制

GluN2B拮抗剂

在研机构

原研机构

在研适应症

非在研适应症

最高研发阶段临床3期

首次获批国家/地区-

首次获批日期1800-01-20

项与 GluN2B 相关的临床试验

NCT06721949

/ Not yet recruiting临床2/3期IIT

Taurine Supplementation as a Novel Therapeutic Approach for Neurocognitive Symptoms in Long COVID

The COVID-19 pandemic has swept across the globe, affecting millions of individuals with varying degrees of severity. While many individuals recover from the acute phase of the infection, a significant proportion continue to experience persistent and debilitating symptoms long after the initial SARS-CoV-2 infection. This condition, known as Long COVID (LC) or sometimes referred to as Post-COVID Condition (PCC) or post-acute sequelae of COVID-19, has emerged as a complex multisystemic condition and challenging health issue, affecting approximately 10% of COVID-19 patients. Various symptoms characterize LC, including fatigue, sleep disturbances, cognitive impairment, and mood disturbances. Some of the symptoms are shared with Myalgic Encephalomyelitis/Chronic Fatigue Syndrome (ME/CFS) - a condition marked by debilitating fatigue and a host of other symptoms without precise biomarkers or objective tests for diagnosis. Effective LC treatments remain elusive and LC patients continue to grapple with persistent symptoms that significantly impact their quality of life. Given the lack of effective treatments, it is imperative to explore novel therapeutic approaches that may alleviate the suffering of this patient population.

开始日期2025-02-01

申办/合作机构

University of Alberta

[+2]

ACTRN12624001440516

/ Not yet recruiting临床1期

An Open-label, 2 Part, Study to Assess the Pharmacokinetics of a Spray Dried Dispersion Formulation of Radiprodil Under Fasted and Fed Conditions in Healthy Adult Subjects: Part B

开始日期2025-01-16

申办/合作机构

GRIN Therapeutics, Inc.

[+1]

ACTRN12624001366549

/ Not yet recruiting临床1期

An Open-label, 2 Part, Study to Assess the Pharmacokinetics of a Spray Dried Dispersion Formulation of Radiprodil Under Fasted and Fed Conditions in Healthy Adult Subjects: Part A

开始日期2024-11-18

申办/合作机构

GRIN Therapeutics, Inc.

[+1]

100 项与 GluN2B 相关的临床结果

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100 项与 GluN2B 相关的转化医学

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0 项与 GluN2B 相关的专利（医药）

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5,557

项与 GluN2B 相关的文献（医药）

2025-12-31·Animal Cells and Systems

Loss of neuronal βPix isoforms impairs neuronal morphology in the hippocampus and causes behavioral defects

Article

作者: Park, Dongeun ; Choi, June-Seek ; Lee, Seung Joon ; Shin, Yoon Kyung ; Kwon, Younghee ; Shin, Jung Eun

βPix is a guanine nucleotide exchange factor for the Rac1 and Cdc42 small GTPases, which play important roles in dendritic spine morphogenesis by modulating actin cytoskeleton organization. The formation and plasticity of the dendritic spines are essential for normal brain function. Among the alternatively spliced βPix isoforms, βPix-b and βPix-d are expressed specifically in neurons. Our previous studies using cultured hippocampal neurons identified the roles of βPix-b and βPix-d in spine formation and neurite development, respectively. Here, we analyzed the in vivo role of the neuronal βPix isoforms in brain development and function by using βPix neuronal isoform knockout (βPix-NIKO) mice, in which the expression of the βPix-b and βPix-d isoforms is blocked, while the expression of the ubiquitous βPix-a isoform is maintained. Loss of the neuronal βPix isoforms leads to reduced activity of Rac1 and Cdc42, decreased dendritic complexity and spine density, and increased GluN2B and Ca²⁺/calmodulin-dependent protein kinase IIα expression in the hippocampus. The defects in neurite development, dendritic spine maturation, and synaptic density in cultured βPix-NIKO hippocampal neurons were rescued by the expression of βPix-b or βPix-d. In behavioral studies, βPix-NIKO mice exhibited robust deficits in novel object recognition and decreased anxiety levels. Our findings suggest that neuronal morphogenetic signaling by the neuronal βPix isoforms contributes to normal behaviors.

2025-12-01·Cognitive Neurodynamics

Alterations of synaptic plasticity and brain oscillation are associated with autophagy induced synaptic pruning during adolescence

Article

作者: Wang, Hui ; Yang, Zhuo ; Xu, Xiaxia ; Zhang, Tao

Adolescent brain development is characterized by significant anatomical and physiological alterations, but little is known whether and how these alterations impact the neural network. Here we investigated the development of functional networks by measuring synaptic plasticity and neural synchrony of local filed potentials (LFPs), and further explored the underlying mechanisms. LFPs in the hippocampus were recorded in young (21 ~ 25 days), adolescent (1.5 months) and adult (3 months) rats. Long term potentiation (LTP) and neural synchrony were analyzed. The results showed that the LTP was the lowest in adolescent rats. During development, the theta coupling strength was increased progressively but there was no significant change of gamma coupling between young rats and adolescent rats. The density of dendrite spines was decreased progressively during development. The lowest levels of NR2A, NR2B and PSD95 were detected in adolescent rats. Importantly, it was found that the expression levels of autophagy markers were the highest during adolescent compared to that in other developmental stages. Moreover, there were more co-localization of autophagosome and PSD95 in adolescent rats. It suggests that autophagy is possibly involved in synaptic elimination during adolescence, and further impacts synaptic plasticity and neural synchrony.

2025-03-01·Behavioural Brain Research

Molecular and behavioral effects of Acamprosate in male rats with sodium salicylate-induced tinnitus

Article

作者: Shahbazi, Ali ; Mahmoudian, Saeid ; Akbarnejad, Zeinab ; Farhadi, Mohammad ; Farrahizadeh, Maryam ; Joghataei, Mohammad Taghi

BACKGROUNDImbalance in inhibitory and excitatory neurotransmitters have been reported in tinnitus. Acamprosate modulates the excitatory and inhibitory neurotransmission in the nucleus accumbens (NAc). This study aims to assess the effect of Acamprosate on tinnitus, anxiety, depression, and molecular changes in nucleus accumbens (NAc), in Sodium-Salisylate (S-salicylate) model of tinnitus.METHODSForty-four adult male wistar rats were used in this study. The study included Control, Saline, and S-salicylate groups during the first week, which then subdivided into five groups as Control, Saline, S-salicylate, Acamprosate, and S-salicylate+Acamprosate. Gap-in Noise (GIN) and pre-pulse inhibition (PPI) were used to assessment of tinnitus at baseline, day7 and day14. Anxiety and depression were evaluated on day 14, by elevated plus maze (EPM), open field (OF), and tail suspension (TST) tests. The protein expression of GABAAR-δ, NR1 and NR2B in NAc were also measured using western blot technique.RESULTSAfter seven days GIN reduced in S-salicylate compare to Control and Saline groups (P < 0.5), while PPI unchanged. After 14 days, GIN reduced in S-salicylate and S-salicylate+Acamprosate groups compare to Control; Saline; and Acamprosate groups (P < 0.5). Additionally, GIN was higher in S-salicylate+Acamprosate compare to S-salicylate group (P < 0.5). PPI was not changed after 14 days. Open arm time in EPM test was decreased in S-salicylate and S-salicylate+Acamprosate groups compare to Control; Saline; and Acamprosate groups (P < 0.5). Central Zone time in OF test was reduced in S-salicylate group compare to Control, Saline, Acamprosate, and S-salicylate+Acamprosate groups (P < 0.5). Immobility Time in TST was increased in S-salicylate group compare to Control, Saline, Acamprosate, and S-salicylate+Acamprosate groups (P < 0.5). GABAAR-δ was decreased in S-salicylate groups compare to Control, Saline, Acamprosate; and S-salicylate+Acamprosate groups (P < 0.5). NR1 and NR2B in NAc were increased in S-salicylate group compare to Control, Saline, Acamprosate, and S-salicylate+Acamprosate groups (P < 0.5).CONCLUSIONS-salicylate can induce tinnitus-like behaviors in rat. Furthermore, S-salicylate induced depression/anxiety like behaviors, and changed the expression of GABAR and NMDAR subunits in NAc. Acamprosate partially reversed these changes. In conclusion, NAc may be involved in the pathophysiologic mechanisms of tinnitus.

项与 GluN2B 相关的新闻（医药）

2025-01-18

·氨基观察

强生艾伯维的CNS分歧

氨基观察-创新药组原创出品作者 | 蔡九又一家药企在精神分裂症治疗领域栽了跟头。 1月16日，勃林格殷格翰公布了iclepertin治疗成人精神分裂症认知障碍的3期临床项目CONNEX的主要结果，该项目的主要终点和关键次要终点均未达到预期。基于此，勃林格殷格翰决定立即终止长期拓展试验CONNEX-X。这是近期在精神分裂症领域折戟的第二家巨头药企。此前不久，艾伯维收购Cerevel所得的“王牌项目”emraclidine，在两项针对精神分裂症的II期研究中未能达到预期终点。这一教训迫使艾伯维重新审视其在中枢神经系统疾病领域的投资策略。在2025年的JPM大会上，艾伯维对外透露：“未来在早期数据研究上投入大量资金时，我们肯定会重新权衡考量。” 不过，在CNS领域，药企们的态度呈现两极分化。有的更为谨慎，有的却仍在大举进攻。 2025年JPM会议首日，强生成为焦点，其宣布以146亿美元收购专注于CNS领域的Intra-Cellular，旨在获取其重磅抗精神病药物Caplyta。一旦收购成功，这将超越对Karuna、Cerevel的收购案，成为2023年以来CNS领域最具规模的一笔并购交易。态度的巨大差异也反映出，在CNS领域，跨国大药企们已产生明显分歧。 / 01 / 更谨慎的艾伯维艾伯维变得更谨慎在情理之中，Cerevel的收购让其损失惨重。 2023年年底，艾伯维宣布以87亿美元收购Cerevel，后者的核心管线是毒蕈碱受体M4的选择性正变构调节剂emraclidine，这是精神分裂症领域的潜在突破选手。庞大的患者群体和对新疗法的迫切需求，使精神分裂症成为大药企的掘金之地，艾伯维也希望有所建树。Emraclidine或许能让艾伯维实现这一愿望。根据1b期试验B部分的结果，52名精神分裂症患者总体耐受性良好，没有与治疗相关的严重不良事件或因治疗导致的受试者停药。也正因此，Cerevel赢得了艾伯维的青睐，最终以高溢价出售。然而，结果并不如人意。正如上文所述，两项针对精神分裂症的II期研究未能达到预期终点。Emraclidine的表现远不如Cerevel公布的1b期试验结果，这也让艾伯维吃了哑巴亏。上周，艾伯维计提了大约35亿美元的减值费用，以反映emraclidine临床挫折对其账面的影响。不过，这场赌局的失利，既有天灾，也有人祸因素。从第一次提出收购邀约，到最终拿下Cerevel，艾伯维只用了不到两个月的时间，难以判断是果断还是武断。冲动的决策付出了代价。艾伯维必然需要重新反思其对神经精神病学的投资。因此，在2025年JPM大会上，尽管艾伯维高管表示，公司仍然愿意承担“经过计算的风险”，但同时也明确表示，对于早期CNS资产的重大投资，会更加谨慎。 / 02 / 大举进攻的强生而强生的乐观也不让人感到意外。作为一家专注CNS药物研发的创新药企，Intra-Cellular目前的核心资产是一款每日1次口服抗精神病药物Caplyta。这是一款5-羟色胺2A（5-HT2A）受体拮抗剂和多巴胺受体D2调节剂，最早由百时美施贵宝研发，2015年Intra-Cellular获得许可，进行全球开发。从机制上看，lumateperone可部分激动多巴胺D1和D2受体，拮抗5-HT2A受体，抑制DA和5-HT转运体，以及促进NMDA受体的NR2B亚基活化，因此Caplyta在多种CNS疾病中展现出了治疗潜力。 2019年12月，Caplyta被FDA批准用于治疗精神分裂症成人患者，2021年12月又获批用于辅助治疗与I型或Ⅱ型双相情感障碍（双相抑郁症）相关的抑郁发作。在这两大适应症的支撑下，Caplyta已经展现出了不菲的商业化潜力。2023年，其销售额已经达到4.62亿美元，同比增长86%；2024年继续增长，前三季度销售额达到4.82亿美元，预计全年最高可达6.85亿美元。不出意外，Caplyta还将继续快速增长。就在去年底，Intra-Cellular向FDA提交了Caplyta的第3项新适应症上市申请，用于重度抑郁症（MDD）的辅助治疗，这是更大的适应症。在美国，大约240万成年人患有精神分裂症，610万成年人患有双相情感障碍，2100万成年人患有MDD。按照强生的说法，如果获批，Caplyta有望成为过去15年中首个获批治疗MDD及双相I型和II型抑郁症状的药物。正因此，在强生眼中，Caplyta的销售峰值将达到50亿美元。对于强生来说，拿下一款峰值50亿美元的重磅炸弹，既能补强CNS布局，更能在应对即将到来的专利悬崖面前，多几分从容。 / 03 / 持续存在的分歧艾伯维、强生的一左一右，反映了CNS领域可能会持续存在的“分歧”：谨慎的人存在，乐观的人也不会消失。乐观在于，CNS领域巨大的机遇。CNS疾病是公认的药物治疗贡献度最低和临床未满足需求最高的疾病领域之一。据WHO预测，20年内，CNS疾病将成为第二大致死源。大多数中枢神经系统疾病患病人数不亚于肿瘤及心血管疾病患者，药物市场空间足够大；多数中枢神经系统疾病的临床有效性不足，存在大量未满足的临床需求。所以，CNS领域注定会吸引诸多药企的入局。但谨慎也不会消失。虽然CNS领域前景诱人，但成功的难度堪称地狱模式：有数据显示，中枢神经系统药物研发成功率仅为6%，不足其他药物研发成功率的一半。核心原因在于，从机制不明，到动物模型难验证、临床开发难度大，每一项都是CNS药物开发的拦路虎。以精神分裂症阴性症状药物为例，当前全球尚未有治疗精神分裂症阴性症状的药物获得批准上市，原因在于两点：第一，机制并不明确。精神分裂症是一类极为复杂的疾病，目前来看，阳性和阴性症状患者的发病机制并不相同。例如，认可度最高的多巴胺假说显示，阳性症状是边缘通路中多巴胺能神经传递过度活跃的结果，而阴性症状、动力丧失和认知障碍则被认为是由额叶和其他中脑边缘结构的低多巴胺能功能引起的。患病机制尚不明确，这使得对症药物研发面临着极大的挑战。第二，临床开发难度极大。由于精神分裂症阴性症状的不明显，以及症状的多样性等诸多因素，导致针对该疾病的临床开发难度极大。例如，由于患者的异质性很大，最终效果无法有效评估；再比如，患者的发病时间可能不是持续的，只是在特定节点发作，这也导致很难评估药物的长期效果。种种因素导致，精神分裂症阴性症状的药物研发，埋葬了太多充满理想的淘金者。而这，也恰恰是CNS领域研发的一个缩影。所以，是在稳健前行中守护既有成果，还是在大胆突破中开辟全新版图，在CNS领域的抉择，承载着企业对医药创新价值的深刻理解，更关乎当下的风险权衡。客观存在的现实，注定了“分歧”注定不会消失。 PS：欢迎扫描下方二维码，添加氨基君微信号交流。

并购临床2期临床3期临床结果临床成功

2025-01-14

·氨基观察

揭秘2025百亿美元并购第一枪

氨基观察-创新药组原创出品作者 | 武月 JPM会议第一天，强生抢了聚光灯。强生宣布以146亿美元收购专注CNS领域的Intra-Cellular，以获得其重磅抗精神病药物Caplyta。一旦成行，这将超越Karuna、Cerevel，成为2023以来，CNS领域最重磅的一笔并购交易，也能够为历经挫折的CNS领域，重新添上一把火。对于强生来说，拿下一款峰值50亿美元的重磅炸弹，既能补强CNS布局，更能在应对即将到来的专利悬崖面前，多几分从容。对于Intra-Cellular来说，也将彻底上岸。 2024年至今，整个行业仅一笔超过百亿美元的并购，来自诺和诺德收购CDMO企业Catalent，若聚焦到生物制药领域，强生收购Intra-Cellular则是唯一一起超百亿美元的收购案。当然，强生CEO Joaquin Duato表示：“大额交易更像是例外，我们创造的大部分价值来自于小型交易和合作，在这些交易中我们可以利用自身规模的优势。” 无论JPM大会期间是否还会有其他重磅并购交易浮出水面，2025年才刚刚开始，手握重金的大药企，不会也不能放过寻求增长的机会。这也将酝酿新的一轮洗牌。 / 01 / 50亿美金重磅炸弹让强生斥资146亿美元收购的Intra-Cellular，到底什么来头？作为一家专注CNS药物研发的创新药企，Intra-Cellular目前的核心资产是一款每日1次口服抗精神病药物Caplyta。这是一款5-羟色胺2A（5-HT2A）受体拮抗剂和多巴胺受体D2调节剂，最早由百时美施贵宝研发，2015年Intra-Cellular获得许可，进行全球开发。从机制上看，lumateperone可部分激动多巴胺D1和D2受体，拮抗5-HT2A受体，抑制DA和5-HT转运体，以及促进NMDA受体的NR2B亚基活化，因此Caplyta在多种CNS疾病中展现出了治疗潜力。 2019年12月，Caplyta被FDA批准用于治疗精神分裂症成人患者，2021年12月又获批用于辅助治疗与I型或Ⅱ型双相情感障碍（双相抑郁症）相关的抑郁发作。在这两大适应症的支撑下，Caplyta已经展现出了不菲的商业化潜力。2023年，其销售额已经达到4.62亿美元，同比增长86%；2024年继续增长，前三季度销售额达到4.82亿美元，预计全年最高可达6.85亿美元。不出意外，Caplyta还将继续快速增长。就在去年底，Intra-Cellular向FDA提交了Caplyta的第3项新适应症上市申请，用于重度抑郁症（MDD）的辅助治疗。在两项全球范围内开展的双盲、安慰剂对照的3期研究中，Caplyta作为抗抑郁药的辅助治疗，在减轻抑郁症状方面显示出统计学显著和具有临床意义的改善。除此之外，Intra-Cellular还在探索其儿童适应症和长效方案。要知道，MDD的潜在患者人数要远多于精分和双相。根据强生披露的数据，全球超过10亿人——即每8人中就有1人患有神经精神或神经退行性疾病。而在美国，大约240万成年人患有精神分裂症，610万成年人患有双相情感障碍，2100万成年人患有MDD。按照强生的说法，如果获批，Caplyta有望成为过去15年中首个获批治疗MDD及双相I型和II型抑郁症状的药物。正因此，在强生眼中，Caplyta的销售峰值将达到50亿美元。 / 02 / 一场双赢自2019年Caplyta获批以来，Intra-Cellular股价不断上涨，近一年涨幅超30%，市值已经接近百亿美元。强生溢价收购消息传出后，其股价大涨34%，市值来到134亿美元。在部分市场人士眼中，Caplyta不断进击，还有其他在研管线正在加速推进，Intra-Cellular没必要卖身。现实是，根据氨基君此前对海外顶级biotech的复盘，起码要5年、10亿美元才能迈过营收平衡点。如何在保持研发竞争实力的同时，提高销售额、摊薄费用率，始终拷问着所有步入商业化阶段的biotech。对于Intra-Cellular来说，Caplyta已经上市5年，销售额也超过5亿美元，但仍处于爬坡阶段。销售费用居高不下，研发投入也不能停，同时还有仿制药虎视眈眈。Caplyta的新化学实体独占权于去年12月到期，尽管根据橙皮书列出的专利可以将其针对仿制药的保护延长至2040年，但目前已经有多家仿制药企提交了简化新药申请。就在上周，Intra-Cellular刚刚解决了与山德士的专利纠纷，后者同意在2040年之前不会推出Caplyta的仿制药版本。这一消息公布后，其股价上涨超14%。而根据外媒报道，Intra-Cellular此前共起诉了7家仿制药申请者，山德士之外，还有多起诉讼正在等待着判决。这种情况下，投入强生怀抱也是一个不错的选择。正如Intra-Cellular CEO在内部信中所说，这是一个难得的机会，公司也将达到另一个里程碑。在他眼中，强生将提高Caplyta的销售预期。支持公司寻求MDD获批，扩大销售团队；同时，借助强生在神经科学领域全球推出疗法的经验，会加速Caplyta放量，以及推进其他管线的研发。对于强生来说，重金收购Intra-Cellular，最直接的好处就是囊括一款50亿美元的重磅炸弹。除了这款药，强生还将获得ITI-1284、lenrispodun、ITI-1020、ITI-333、ITI-1549等多个在研管线，这会进一步加强其神经领域的管线布局。目前，强生的神经科学业务的支柱是抗精神病药物Invega和抗抑郁鼻腔喷雾剂Spravato。2024年5月，强生表示其在研的MDD新药seltorexant在III期MDD3001研究成功，患者抑郁症状和睡眠有了显著和有意义的改善。强生的神经科学业务也并非一切都好。10月份，强生终止了3个神经科学领域的临床研究项目：seltorexant治疗阿尔兹海默病的II期临床研究、JNJ-0376治疗帕金森病的I期临床研究以及P2X7拮抗剂治疗双相障碍的II期临床研究。显然，尽管强生已经在该领域布局多年，但依然无法改变CNS的研发困境。而随着几款重磅炸弹的专利即将到期，STELARA（2023年专利到期）、SIMPONI（2024年专利到期）以及DARZALEX（2029年专利到期），都是强生单品销售额前十的药物，其不得不加速战略调整。过去一年，彻底剥离消费者业务后，强生进行了一系列动作，包括集团品牌焕新、重大收购等，一个“新的强生”开始完全专注于创新制药和医疗科技两大领域。具体到创新药领域，强生全面聚焦肿瘤、免疫、神经三大领域。此前，其向外披露了新的五年计划，预计到2030年推出20多种新药和50多种产品。其中，10种或更多药物的峰值销售潜力至少为50亿美元，包括特立妥单抗注射液和JNJ-2113；15种销售潜力为10亿-50亿美元的产品，包括Spravato、seltorexant、aticaprant和 JNJ-4804等。而随着收购Intra-Cellular，强生也将再度收获一款50亿美元大单品，为其应对专利悬崖危机，增添新的助力。 / 03 / 并购与洗牌 CNS市场规模巨大，吸引着越来越多大药企加码。强生之前，渤健选择抄底CNS开拓者Sage。由于临床试验接连失败，2024年Sage股价暴跌近75%。截至2024年1月10日收盘，Sage股价报5.5美元/股，市值只有3.4亿美元。渤健则以7.22美元的非约束性报价，收购Sage，总估值为4.42亿美元。此前双方就达成合作，共同开发和商业化两款CNS产品：用于治疗PPD/MDD的Zurzuvae，以及治疗原发性震颤的SAGE-324。根据协议，渤健需要支付首付款8.75亿美元，后续最高16亿美元的里程碑付款，以及溢价40%（104.14美元/股）的股权投资。可以说，仅上述这笔交易的首付款就是此次收购的两倍。去年10月，灵北制药以26亿美元的价格，收购Longboard Pharmaceuticals，获得一款高选择性的5-HT2C超级激动剂，用于治疗难治性癫痫DEE。艾伯维则再次押注阿尔兹海默症，以14亿美元收购Aliada，后者的核心资产是ALIA-1758，目前处于临床I期试验开发阶段的抗淀粉样蛋白抗体。当然，不只是CNS领域，整个生物制药领域的并购，都将升温。尽管2024年大型交易数量大幅减少，并购金额相较2023年有所下滑，但是，从大药企在这次JPM大会就能看出，大药企依旧对小型并购有着极高的兴趣，也十分渴望那些专注于早期或中期资产。抄底Sage后，渤健明确表示将在2025年继续通过并购方式扩充自身实力。罗氏则在大会上展示了其强大的“并购火力”，每年可以调动约100亿美元的资金。同时，其CEO强调，公司并不打算盲目花钱，而是更青睐那些能与现有产品组合形成良好互补，或能在关键疾病领域带来颠覆性突破的目标资产。吉利德CEO表示，现有产品能够每年稳定产生数十亿美元的收入，因而可以进行“适当的并购及构建合作伙伴关系”来补充管线。在JPM2025大会开展期间，吉利德也达成了一笔交易，以17亿美元的总交易额引进Leo Pharma的STAT6抑制剂。礼来则在大会首日，宣布以10亿美元预付款“抢下”Scorpion Therapeutics的PI3Kα抑制剂项目，并承诺在后续的监管与销售里程碑达成后追加15亿美元；GSK则宣布以11.5亿美元收购IDRx，囊获一款罕见病药物。 JPM大会期间的这些交易，为2025年生物医药并购带来了更多希望。事实上，无论是高盛还是美国医药VC机构Atlas，均认为并购市场未来值得期待，因为这些大药企弹药充足。根据高盛测算，在债务杠杆为2.5倍EBITDA的情况下，这些公司潜在的融资能力约为5000亿美元。若杠杆水平提升至4倍EBITDA，其融资空间更可接近9000亿美元。而目前，XBI的总市值约4000亿美元。也就是说，即使不加大杠杆，大药企也有实力买下所有的biotech。在专利悬崖与新技术兴起的双重压力下，通过收购企业或引进资产，早已成为巨头们保持长期增长与竞争力的主要路径。从JPM大会首日传递的信息来看，生物医药领域出现更多超10亿美元甚至更大规模的并购交易，也许只是时间问题。而这，也将引领新一轮行业洗牌。 PS：欢迎扫描下方二维码，添加氨基君微信号交流。

并购临床3期

2024-12-11

·PRNewswire

GNT Pharma Reports Significant Improvements in Stroke Patients Treated with its pioneering Phase 3 Drug Nelonemdaz™

** IND submitted to the FDA showing significantly improved patient condition when administered within 70 minutes of arrival at the Emergency Room ** *Multinational Phase 3 Clinical Trial protocols confirmed and initiated with leading global stroke research centers * SEOUL, South Korea, Dec. 11, 2024 /PRNewswire/ -- GNT Pharma Co. Ltd, a late-stage pharmaceutical company founded in 1998 with offices in Seoul Korea, Italy and USA, announced today the results of its latest Phase II ('SONIC') and Phase III ('Rodin') clinical trials study showing that stroke patients who received early administration of Nelonemdaz in combination with endovascular thrombectomy, demonstrated significant improvements in outcomes. These results were presented by Professor Jin Soo Lee, Chair of the Department of Neurology at Ajou University Medical Center at the recent International Conference Stroke Update 2024 (ICSU 2024). Dr BJ Gwag, Chairman and CEO of GNT Pharma commented "we are extremely encouraged with the SONIC and RODIN clinical trials results and excited to announce we have initiated multinational Phase 3 Clinical Trials (RENEW) with world class partners, including more than 20 top university hospitals in Korea as well as UCLA and UPMC Stroke Centers in the USA." Nelonemdaz is the world's first "multi-target" neuroprotection drug designed to reduce brain damage after a stroke or cardiac arrest. It offers superior efficacy compared to single-target neuroprotectants offering dual target action: (1) Inhibition of NMDA receptor subtype NR2B to safely reduce excitotoxicity; and (2) Removal of free radicals to reduce oxidative stress – two major causes of brain cell death following a stroke. Unlike non-selective NMDA receptor inhibitors, Nelonemdaz does not cause adverse effects and its safety has been verified in two Phase 1 trials, three Phase 2 trials, and two Phase 3 trials. There are over 5 million stroke-related deaths globally each year, with a further 5 million survivors annually left with permanent disabilities. This puts a huge strain on healthcare systems worldwide - the World Stoke Organization estimates total stroke-related costs to tip US$1 trillion by 2030. Moreover, stroke frequency is not abating, with the USA seeing an increase of 60% over the past 30 years. Almost 80% of all strokes are Ischemic Strokes and require emergency medical treatment, typically thrombolysis or endovascular thrombectomy. Given these alarming statistics, there is a global imperative to further improve the efficacy of current stroke treatments. Dr Gwag adds: "In 2015, fast endovascular thrombectomy was proven to improve functional outcome in acute ischemic stroke patients and is the de facto standard for stroke care across the world. It is therefore encouraging that the outcome of stroke patients is further improved by the fast administration of Nelonemdaz along with rapid thrombectomy," The prior Phase 2 SONIC trial results, published in Stroke Journal in 2022, showed the promising efficacy and safety of Nelonemdaz administered to stroke patients receiving thrombectomy. In the latest 498 patient Phase 3 RODIN Trial, administration of Nelonemdaz within 12 hours of ischemic stroke onset did not show significant efficacy in patients treated with thrombectomy. However, post-hoc analyses revealed potential interactions between treatment effects and time-related metrics. The RODIN results are to be published in the 'JAMA' (Journal of the American Medical Association) Network Open. The interactions were shown in the pooled analysis of stroke patients participating in the SONIC and RODIN trials, and in the subsequent subgroup analysis, the first infusion time of Nelonemdaz for improved functional outcome was established to be within 70 minutes from ER arrival. The efficacy of Nelonemdaz was assessed using the modified Rankin Scale (mRS), an ordinal scale ranging from 0 (normal) to 6 (death), at 12 weeks post-treatment. Compared to the placebo, the nelonemdaz caused a significantly beneficial shift in the mRS distribution (common odds ratio 2.2, p<0.05). The proportion of patients in mRS 0-2 corresponding to functional independence was 50.0% in the placebo group and improved to 68.6% in the Nelonemdaz group (p=0.059). Dr Lee adds " "Our post-hoc analyses unveiled a best clinical trial condition that showed a significant benefit of Nelonemdaz, and a protocol for the global phase 3 RENEW trial was established to confirm beneficial effects of Nelonemdaz in ischemic stroke patients in combination with endovascular thrombectomy." Dr. Lee will lead the RENEW trial alongside principal USA investigators Dr. Raul Nogueira, director of the UPMC Stroke Institute and Professor of Neurology and Dr. David S. Liebeskind, Director of the UCLA Stroke Center and Professor of Neurology. About GNT Pharma: GNT Pharma Co., Ltd ('GNTP') was founded in April 1998 by eight highly accomplished professors in subjects ranging from neuroscience and pharmacology to cell biology researching neuronal cell death. Since then, GNTP has discovered and developed an enviable pipeline of late stage drug candidates from nervous system disorders to chronic inflammatory diseases. As well as Nelonemdaz, GNTP's other flagship drug candidates include: Crisdesalazine for the treatment of Alzheimer's and neurodegenerative diseases and depression; and Flusalazine for inflammatory and respiratory diseases including COPD and Asthma. GNTP also has two commercial products in market, including Gedacure (Crisdesalazine) for the treatment of CDS or 'doggy dementia' that shares similar pathology to Alzheimers; and (2) Radipair, skin care products. Forward-Looking Statements Notice: This news release contains statements about expectations, plans, projections, and strategies of GNTP that constitute forward-looking statements to shareholders, investors, and partners. Statements included in this document that are not historical data and fact constitute forward-looking statements about future clinical and financial results. FURTHER INFORMATION: Media Inquiries: Byung Chul Kim, (M) +82-318005-9910; (E) [email protected] Investors/ Korea: Daeyong Kim, (M) +82-704261-0788; (E) [email protected] Investors /International: Sam Cho, (M) + 82-108948-7142; (E) [email protected] SOURCE GNT Pharma WANT YOUR COMPANY'S NEWS FEATURED ON PRNEWSWIRE.COM? 440k+ Newsrooms & Influencers 9k+ Digital Media Outlets 270k+ Journalists Opted In GET STARTED

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