草酸艾司西酞普兰(Escitalopram Oxalate) - 药物靶点：5-HT receptor x SERT_在研适应症：社交恐怖症，抑郁症，惊恐障碍_专利_临床

概要

基本信息

简介Escitalopram 以商品名 Esertia 销售，是一种小分子药物，可作为选择性 5-羟色胺再摄取抑制剂 (SSRI)。它以 SERT-5 转运蛋白为靶点，该靶点负责突触间隙中血清素的再摄取。通过抑制 SERT-5 转运蛋白，Escitalopram增加了大脑中血清素的细胞外浓度，这被认为是其治疗效果的潜在机制。Escitalopram还被批准用于治疗抑郁症，并已被证明可有效减少焦虑症和恐慌症的症状。它也被用于其他疾病，如强迫症和创伤后应激障碍。该药由 H. Lundbeck 开发，于 2002 年 8 月 14 日在美国首次获得批准，随后陆续在中国和日本获批上市。

药物类型

小分子化药

别名

Cipralex、Entact、Escitalopram

+ [17]

靶点

5-HT receptor x SERT

作用方式

拮抗剂、抑制剂

作用机制

5-HT receptor拮抗剂(5-羟色胺受体拮抗剂)、SERT抑制剂(5-羟色胺转运体抑制剂)

治疗领域

神经系统疾病其他疾病

在研适应症

社交恐怖症抑郁症惊恐障碍+ [4]

非在研适应症

获得性免疫缺陷综合征行为障碍创伤性脑损伤+ [3]

原研机构

H. Lundbeck A/S

在研机构

H. Lundbeck A/S

Generic Health Pty Ltd.Forest Laboratories, Inc.

+ [5]

非在研机构

Forest Laboratories LLC

Lundbeck LLC

最高研发阶段批准上市

首次获批日期

瑞典 (2002-05-07),

焦虑症重度抑郁症强迫症

最高研发阶段(中国)批准上市

特殊审评-

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结构/序列

分子式C22H23FN2O5

InChIKeyKTGRHKOEFSJQNS-BDQAORGHSA-N

CAS号219861-08-2

关联

388

项与草酸艾司西酞普兰相关的临床试验

NCT05603104

/ Recruiting临床3期IIT

A Randomised, Controlled Trial to Investigate the Effect of an Intensified Pharmacological Treatment for Schizophrenia, Major Depressive Disorder and Bipolar Depression in Subjects Who Had a First-time Treatment Failure on Their First-line Treatment.

Schizophrenia, bipolar and major depressive disorders collectively affect over 10 million people across the EU and are associated with annual healthcare and societal costs in excess of 100 billion Euros. When diagnosed with one of these disorders, patients are prescribed psychotropic medication such as antidepressants, mood stabilisers or antipsychotics. It is unknown whether this first-line treatment will be successful. After this first-line treatment fails, usually a second-line treatment is initiated, and when this is not successful either a third-line treatment is initiated. Third-line treatments are quite successful, especially when compared to second-line treatments. The research question is whether the third-line treatments (early-intensified treatments) would be more efficacious than the current second-line treatments (treatment as usual) for schizophrenia, bipolar and major depressive disorders. If this is indeed the case, this could lead to the prevention of unnecessary trials of ineffective treatments and adaptations of worldwide guidelines as well as a reduction of healthcare and societal costs.

开始日期2025-04-30

申办/合作机构

University Medical Center of Utrecht

[+1]

NCT06705478

/ Not yet recruiting临床2期IIT

An Open-Label, Randomized Controlled Trial of Pramipexole Versus Escitalopram to Treat Major Depressive Disorder (MDD) and Comorbid MDD With Mild Neurocognitive Disorder (MND) in Persons With HIV

A phase II, randomized, open-label, two-arm clinical trial evaluating the safety and efficacy of pramipexole extended release (ER) versus escitalopram for the treatment of major depressive disorder (MDD) and comorbid MDD with mild neurocognitive disorder (MND) in persons with HIV (PWH). Participants will be assessed comprehensively and briefly at intercurrent visits to monitor for toxicity, response to therapy, and to assess for dose changes.
An optional sub-study to evaluate treatment impact on the cerebrospinal fluid (CSF) profile will be conducted in a subset of 36 participants.

开始日期2025-04-24

申办/合作机构

National Institute of Allergy & Infectious Diseases

[+1]

NCT06796946

/ Not yet recruiting早期临床1期

Intervention for Antidepressant Deprescription in Primary Care: a Randomized Community Clinical Trial

Introduction The consumption of antidepressants has increased considerably worldwide, including in Spain. Despite their effectiveness in cases of moderate to severe depression, their long-term use in mild cases is questioned. This study aims to evaluate the effectiveness of a deprescribing intervention in primary care, to reduce the unnecessary consumption of these drugs and improve patients' quality of life.
Material and Methods A community-based clinical trial will be carried out before and after in an adult population of residents of an urban area of Cadiz (Spain) who have been prescribed antidepressants in the last year. Participants will be randomly selected and followed up for a predetermined period after consensus.
The intervention will consist of a comprehensive evaluation of antidepressant treatment by a team of health professionals. Factors such as indication, dose, and response to treatment will be evaluated, and the Hamilton scale for anxiety and the Beck Inventory for depression will be used. In those cases where it is considered appropriate, a gradual reduction or suspension of the drug will be proposed, always under medical supervision.
Conclusions This research will contribute to generating scientific evidence on the safety and efficacy of deprescribing in primary care, promoting a more rational use of antidepressants, and improving the quality of life of patients. The results obtained could have important implications for clinical practice and for the development of clinical practice guidelines.

开始日期2025-04-01

申办/合作机构

Universidad De Huelva

100 项与草酸艾司西酞普兰相关的临床结果

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100 项与草酸艾司西酞普兰相关的转化医学

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100 项与草酸艾司西酞普兰相关的专利（医药）

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3,090

项与草酸艾司西酞普兰相关的文献（医药）

2025-03-11·PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Logic-based machine learning predicts how escitalopram attenuates cardiomyocyte hypertrophy

Article

作者: Travers, Joshua G. ; Saucerman, Jeffrey J. ; Wolf, Matthew J. ; Eggertsen, Taylor G. ; Hardy, Elizabeth J. ; McKinsey, Timothy A.

Cardiomyocyte hypertrophy is a key clinical predictor of heart failure. High-throughput and AI-driven screens have the potential to identify drugs and downstream pathways that modulate cardiomyocyte hypertrophy. Here, we developed LogiRx, a logic-based mechanistic machine learning method that predicts drug-induced pathways. We applied LogiRx to discover how drugs discovered in a previous compound screen attenuate cardiomyocyte hypertrophy. We experimentally validated LogiRx predictions in neonatal cardiomyocytes, adult mice, and two patient databases. Using LogiRx, we predicted antihypertrophic pathways for seven drugs currently used to treat noncardiac disease. We experimentally validated that escitalopram (Lexapro) and mifepristone inhibit hypertrophy of cultured cardiomyocytes in two contexts. The LogiRx model predicted that escitalopram prevents hypertrophy through an “off-target” serotonin receptor/PI3Kγ pathway, mechanistically validated using additional investigational drugs. Further, escitalopram reduced cardiomyocyte hypertrophy in a mouse model of hypertrophy and fibrosis. Finally, mining of both FDA and University of Virginia databases showed that patients with depression on escitalopram have a lower incidence of cardiac hypertrophy than those prescribed other serotonin reuptake inhibitors that do not target the serotonin receptor. Mechanistic machine learning by LogiRx discovers drug pathways that perturb cell states, which may enable repurposing of escitalopram and other drugs to limit cardiac remodeling through off-target pathways.

2025-02-01·JOURNAL OF ETHNOPHARMACOLOGY

Inhibitory effects of Valeriana fauriei root extract on serotonin uptake in vitro caused by the interaction among its active ingredients including a new compound

Article

作者: Xu, Ling-Yu ; Ota, Misato ; Makino, Toshiaki ; Sekiguchi, Mitsuhiro ; Maki, Yasuhito ; Oiwa, Yuki

ETHNOPHARMACOLOGICAL RELEVANCE:

The root of Valeriana fauriei Briq. (VF) is a folk medicine registered in the Japanese Pharmacopeia 18th Edition. Valeriana plants have been utilized as sedatives and antidepressants in Europe, but only a few pharmacological reports have focused on VF.

AIM OF THE STUDY:

This study aimed to determine the active ingredients of VF and the mechanisms underlying its antidepressant effects.

MATERIALS AND METHODS:

We investigated the binding activity of VF ethanol extract on rat serotonin transporter (SERT) by competing against (S)-citalopram with a 96-well plate assay system and high-performance liquid chromatography coupled with tandem mass spectrometry (HPLC-MS/MS). Additionally, we evaluated the inhibitory effect of the VF extract and its constituents on [³H]serotonin uptake into human embryonic kidney 293 (HEK293) cells that transiently express the recombinant human serotonin transporter (hSERT). We then examined the active ingredients of VF. The interaction between the compounds in VF was assessed by regression analysis with the definitive screening design.

RESULTS:

VF ethanol extract significantly inhibited both (S)-citalopram binding to SERT and serotonin uptake into HEK293 cells in concentration-dependent manners. Several fractions of the VF extract demonstrated synergistic action for serotonin uptake inhibition. Kanokonyl acetate (KNA) inhibited serotonin uptake in a concentration-dependent manner, and this activity was significantly enhanced by adding kessyl glycol diacetate (KGD), the major component of VF, which is not as active on its own. In addition, we found a new compound, kanokol, which significantly enhanced the interaction of KNA and KGD. The activity due to the interaction accounted for approximately 40% of the total VF activity. We obtained the regression equations that predicted VF extract activity by KNA and KGD contents in the presence of kanokol.

CONCLUSIONS:

The antidepressant effects of VF via serotonin uptake inhibition are derived from the interactions among its constituents, KNA and KGD, which play crucial roles exhibiting the interaction. Additionally, a key compound that improves the interaction is the new compound kanokol.

2025-02-01·ENVIRONMENTAL POLLUTION

Population size, income and poor sanitation interact to explain widespread streamwater contamination by antidepressants in the Metropolitan Region of São Paulo

Article

作者: Martins, Aline Franco ; Costa, José Luiz ; Brejão, Gabriel Lourenço ; Barsoumian, Hagop Armenio ; Taniwaki, Ricardo ; Pelinson, Rodolfo Mei ; Bispo, Giulia Baldaconi ; Schiesari, Luis ; Cursino de Moura Hirye, Mayumi

The expansion of urban settlements over native environments may expose biodiversity to a host of emerging contaminants, with unintended ecological effects. This study evaluated patterns of contamination of streamwater by antidepressants in the Upper Tietê River Basin, a watershed of high social, economic and environmental relevance for comprising both the largest urban settlement in South America (the Metropolitan Region of São Paulo) and remnants of a globally important biodiversity hotspot (the Atlantic Rainforest). We sampled 53 third-order streams draining catchments regularly distributed across a gradient in urban cover. Antidepressant contamination was found to be widespread. Whereas no antidepressants were detected in any of the 11 streams draining entirely forested catchments, 39 of 42 remaining streams were contaminated with one to eight antidepressant molecules. Concentrations increased monotonically with urban cover and bracketed the entire range found in global freshwaters. Concentrations increased with the number of inhabitants in the catchment and with number of households with no sanitation, but only in catchments with higher mean per capita income. Although concentrations in the range of tens to hundreds of nanograms-per-liter as found may appear to be low, literature data demonstrate effects on individual performance, population growth rates, and even transgenerational effects in which short-term exposure at the embryonic stage may affect life history traits over three generations of descendants. These findings highlight the need to expand sanitation infrastructure and to adopt policies of urban planning that reconcile human settlement with biodiversity conservation in Latin America.

142

项与草酸艾司西酞普兰相关的新闻（医药）

2025-03-31

·药融圈

净利逆增61%！全球VD3霸主靠‘全产业链+合成生物’逆袭集采寒冬

注：本文不构成任何投资意见和建议，以官方/公司公告为准；本文仅作医疗健康相关药物介绍，非治疗方案推荐（若涉及），不代表平台立场。任何文章转载需得到授权。2024年，花园生物交出了一份“逆周期增长”的答卷：营业收入12.43亿元（+13.58%），归母净利润3.09亿元（+60.76%）。在维生素行业底部震荡与医药集采常态化的双重压力下，公司通过全产业链成本优势与高端仿制药差异化布局，实现了利润增速远超营收增长的质变。业绩逆势增长：成本管控与结构优化双轮驱动维生素板块：毛利率提升至60.52%，核心产品维生素D3全球市占率超40%，自产胆固醇使成本低于同行30%以上。医药板块：6个产品中选国家/地方集采，新增3个仿制药批件，带动毛利率稳定在73%高位，展现强抗压能力。核心业务解析：纵向深耕与横向突破1.维生素全产业链：构筑护城河的三重壁垒作为全球唯一实现维生素D3全产业链布局的企业，花园生物已形成三大竞争壁垒：技术壁垒：拥有维生素D3、NF级胆固醇、25-羟基维生素D3三大国际领先工艺，获国家科技进步奖等30余项技术认证。成本壁垒：东阳+金华双基地协同，胆固醇自给率100%，饲料级D3粉生产成本较行业平均低25%。规模壁垒：四大核心产品（胆固醇、VD3、25-OH-D3、精制羊毛脂）产能全球第一，2024年出口占比44.4%。产品矩阵升级：25-羟基维生素D3（活性代谢物）收入占比提升至16.9%，替代普通D3趋势显著；维生素A粉新产能2025年投产，剑指千亿VA/VE市场。2.医药制造：集采时代的“破局者逻辑”面对集采降价压力，花园药业通过“抢首仿+控成本+拓渠道”构建增长韧性：产品梯队：10个主力品种覆盖高血压、呼吸系统、抗感染等赛道，2024年新增阿仑膦酸钠片（骨质疏松一线用药）等3个批件，在审评品种6个。集采策略：缬沙坦氨氯地平片（26省续标）、多索茶碱注射液（23省续标）等核心品种通过“以价换量”维持市场份额，草酸艾司西酞普兰片（抑郁症用药）借广东联盟集采打开华南市场。成本优化：原料集采+工艺改进使单位生产成本下降12%，抵消部分价格下行影响。募投项目变更：战略调整背后的产业逻辑公司12亿元可转债募投项目经历重大调整，折射出对市场的前瞻判断：1.项目进展与产能释放2.募投变更的深层动因聚焦核心赛道：终止部分仿制药研发，转向更具技术壁垒的JAK抑制剂（自身免疫疾病）、酰胺类局麻药等高附加值领域。产业链延伸：新增L-丙氨酸项目向上游发酵原料布局，预计使VB6生产成本再降15%，强化全球竞争力。风险规避：原计划高端仿制药项目因集采不确定性调整，资金向确定性更高的维生素衍生品倾斜。未来增长与风险透视：技术+需求双轮驱动增长引擎：①技术降本：合成生物学突破（如7-去氢胆固醇工艺）提升胆固醇提取效率20%，夯实全球成本优势；②银发经济：阿仑膦酸钠片（骨质疏松）、氨氯地平阿托伐他汀钙片（高血压+高血脂）精准卡位400亿老年慢病市场；③出海加速：维生素D3获欧盟认证，25-羟基产品打入北美宠物市场，海外收入占比剑指50%。风险博弈：①产能释放：2025年维生素A/E新产能或冲击价格；②集采压力：仿制药续标价格竞争加剧。长期价值：维生素领域：全球50%饲料添加需求刚性，公司D3系列成本优势构筑“压舱石”；医药板块：“首仿+难仿”产品梯队2025年迎来密集上市期，预计贡献30%利润增量；合成生物学：生物制造中试基地孵化5个在研项目，远期或再造一个“技术型花园”。版权声明：本文转自原料药情报局，如不希望被转载的媒体或个人可与我们联系，我们将立即删除植根上海、辐射全球,药融圈作为生物医药产业级战略平台,以"让智慧与人脉无界流动"为使命,构建覆盖药物研发、生产、流通、商业化的全产业链赋能体系。通过智能化云服务、精准资源链接、产业智库与生态社群四大核心引擎,打造中国医药价值流动的基础设施。在全球化与数字化双重浪潮下,药融圈正重新定义医药资源的流通范式--这里不仅是信息与人脉的枢纽站,更是催生产业变革的化学反应器。我们以中国为原点,编织全球医药智慧网络,让每一次精准链接都成为企业跨越式增长的催化剂。点点赞点分享点推荐

带量采购财报核酸药物医药出海

2025-03-01

·药明康德

超越蛋白降解！全新双特异性抗癌小分子进入临床

▎药明康德内容团队编辑日前，Halda Therapeutics公司宣布，在研调节诱导接近靶向嵌合体（RIPTAC）药物HLD-0915，已经完成首个人体临床试验的第一位患者给药，用于治疗转移性去势抵抗性前列腺癌（mCRPC）。RIPTAC是一种双功能性分子，通过将两种不同蛋白拉近并构成复合体，达到在肿瘤细胞中特异性抑制蛋白功能的作用。Nature Reviews Drug Discovery今日发表的评论文章表示，HLD-0915是首个进入临床开发阶段的RIPTAC分子，也代表着诱导接近（induced proximity）作用机制在靶向蛋白降解之外的研究方向。从PROTAC到RIPTAC Halda Therapeutics公司由耶鲁大学蛋白降解先驱Craig M. Crews教授联合创建。在创建Halda之前，Crews教授联合创建的Arvinas公司旨在利用诱导接近原理促进靶点蛋白的降解。在2008年，Crews教授和合作伙伴发表的论文描述了一种双功能性分子，它的一端可以与靶点蛋白结合，另一端则可以和E3泛素连接酶结合，这样就能让泛素连接酶与靶点蛋白拉近，给靶点蛋白打上泛素标签，然后被细胞的蛋白酶体系统降解。研究人员称这种分子为蛋白降解靶向嵌合体（PROTAC）。与常见的小分子抑制剂不同，PROTAC分子不需要抑制靶点蛋白的活性，就可以通过选择性降解有害蛋白来消除各种疾病的病因。基于PROTAC技术开发的蛋白降解疗法已经成为新药开发的热点领域。Arvinas公司已有多款靶向蛋白降解疗法进入临床开发阶段。该公司与辉瑞（Pfizer）联合开发的雌激素受体靶向降解剂vepdegestrant目前正在多个3期临床试验中接受评估，它被业内知名机构科睿唯安（Clarivate）列为未来5年可能成为重磅的新药之一。诺华（Novartis）公司也已经与Arvinas公司达成超10亿美元合作，开发新一代雄激素受体（AR）靶向降解剂ARV-766。 Halda公司的潜在“first-in-class”在研疗法HLD-0915与PROTAC分子有些类似。这种异双功能分子的一端与富集于癌细胞中的靶点蛋白结合，另一端结合对细胞生存必不可少的关键蛋白。当细胞同时表达这两种蛋白时，RIPTAC分子会将它们牢固地结合成一个复合体，从而使关键蛋白失活，导致癌细胞死亡。 ▲RIPTAC分子的作用机制（图片来源：参考资料[3]）在一项概念验证研究中，科学家在细胞系中人工高度表达了名为HaloTag-FKBP的重组蛋白，然后科学家们设计了一系列双功能分子，它们的一端可以和HaloTag-FKBP结合，另一端可以与不同维持细胞生存的细胞内蛋白结合，包括BET，PLK1，CDK等等。 ▲不同类型的RIPTAC分子的分子结构（图片来源：参考资料[3]）实验结果显示，这些分子在高度表达HaloTag-FKBP蛋白的细胞系中表现出抑制细胞增殖的作用，而且这一抑制细胞增殖的作用与HaloTag-FKBP蛋白/RIPTAC分子/维持细胞生存的蛋白构成的三元复合体在细胞内的积累相关。研究结果为RIPTAC分子选择性杀伤肿瘤细胞的作用机制提供了概念验证。研究人员指出，RIPTAC分子与传统靶向疗法的区别在于它不需要抑制靶点蛋白的活性，只需要肿瘤细胞表达的蛋白水平显著高于健康细胞，就可能发现有效的治疗窗口。这一作用机制与抗体偶联药物（ADC）非常相似，而RIPTAC分子的优势在于可以靶向细胞内蛋白，从而大幅度扩展了可以靶向的靶点范围。为了将科学突破转化为新药，Halda首先选择将雄激素受体作为肿瘤组织中富集的靶点蛋白。癌细胞经常通过提高AR的表达水平来对抗AR拮抗剂并产生耐药性。药物研发人员正在致力于开发下一代AR拮抗剂和针对AR的PROTAC药物，但这些候选药物仍需克服AR表达水平增加以及转移性疾病中可能出现的各种AR突变的挑战。然而采用RIPTAC技术，AR表达水平的增加反而成为优势而非障碍。HLD-0915通过将AR与一个与转录调控相关的关键蛋白“绑”在一起，让细胞启动凋亡程序并死亡。在前列腺癌小鼠模型中，RIPTAC的表现已经优于多款获批的AR拮抗剂和雄激素合成抑制剂，以及Arvinas开发的第一代AR降解剂bavdegalutamide。值得一提的是，作为全球支持蛋白降解疗法研发的重要赋能平台之一，药明康德也一路见证了Arvinas和Halda这两家“明星”公司从萌芽、成长，到如今的快速发展。在2024年药明康德举办的投资者日期间，药明康德联席首席执行官杨青博士提到了这些成就背后的创业和合作故事。公开信息显示，早在2016年，药明康德在蛋白降解疗法开发尚在起步阶段时就建设了相应能力，是全球最早赋能PROTAC和RIPTAC类药物研发的公司之一。作为Arvinas和Halda的合作伙伴，药明康德在多个环节深度赋能两家公司的新药研发，助力一流基础科学发现转化为创新疗法。诱导接近机制在蛋白降解之外的新天地 Halda公司以外，其它新锐公司也在探索诱导接近机制在蛋白降解之外的应用。比如，Magnet Biomedicine公司致力于开发名为TrueGlues的创新分子胶药物，将靶点蛋白与被称为呈现蛋白（presenter protein）的内源性蛋白拉在一起形成复合物。这一作用机制可以让TrueGlues分子只在呈现蛋白表达的细胞中与靶点蛋白结合，达到组织特异性靶点抑制的效果。 Magnet公司首席执行官Brian Safina博士在接受Nature Reviews Drug Discovery采访时表示，该公司的一款在研疗法可以同时与布鲁顿氏酪氨酸激酶（BTK）和磷脂酰肌醇3激酶δ（PI3Kδ）结合。它们是两种在癌症、炎症和免疫疾病中具有重要作用的激酶。然而，PI3Kδ抑制剂在这些环境中尚未充分发挥其潜力，因为它们在T细胞中会产生毒性。而BTK在T细胞中的表达极少或根本不表达。因此，一种能够将PI3Kδ与BTK“粘合”在一起的药物，预期不会在T细胞中产生副作用，从而提高PI3Kδ抑制剂的安全性，扩展治疗窗口。Magnet公司今日宣布与礼来（Eli Lilly and Company）公司达成超过12亿美元的研发合作，共同开发创新分子胶疗法。此外Vicinitas、Stablix、Entact Bio和Photys等公司的研发人员正在探索利用诱导接近机制改变目标蛋白的翻译后修饰。通过引入参与目标蛋白去泛素化或磷酸化的分子机制，他们希望能够驱动显著的生物效应。Revolution Medicines公司的分子胶疗法通过将难以靶向的KRAS蛋白与附近的蛋白“粘合”在一起，达到抑制KRAS活性的目的。该公司多款基于这一机制的KRAS抑制剂已经在临床试验中显示出可喜的活性。相关阅读：“癌症之王”患者生存率近100%！靶向多种KRAS突变小分子临床试验结果亮眼基于诱导接近机制的双功能性分子已经激发了靶向蛋白降解药物的研发浪潮并且在临床试验中显示了可喜的治疗效果。期待利用诱导接近机制调节其它生物过程的药物在临床开发过程中进展顺利，早日成为造福患者的新药好药。 ▲欲了解更多前沿技术在生物医药产业中的应用，请长按扫描上方二维码，即可访问“药明直播间”，观看相关话题的直播讨论与精彩回放参考资料： [1] Induced proximity pushes beyond protein degraders, as first RIPTAC moves into the clinic. Retrieved February 28, 2025, from https://www-nature-com.libproxy1.nus.edu.sg/articles/d41573-025-00037-7 [2] Halda Therapeutics Announces First Patient Dosed in Phase 1/2 Clinical Trial Evaluating HLD-0915 in Metastatic Castration-Resistant Prostate Cancer. Retrieved February 28, 2025, from https://haldatx.com/halda-therapeutics-announces-first-patient-dosed-in-phase-1-2-clinical-trial-evaluating-hld-0915-in-metastatic-castration-resistant-prostate-cancer/ [3] Raina et al., (2023). Regulated Induced Proximity Targeting Chimeras (RIPTACs): a Novel Heterobifunctional Small Molecule Therapeutic Strategy for Killing Cancer Cells Selectively. bioRxiv, doi: https://doi-org.libproxy1.nus.edu.sg/10.1101/2023.01.01.522436 免责声明：药明康德内容团队专注介绍全球生物医药健康研究进展。本文仅作信息交流之目的，文中观点不代表药明康德立场，亦不代表药明康德支持或反对文中观点。本文也不是治疗方案推荐。如需获得治疗方案指导，请前往正规医院就诊。版权说明：本文来自药明康德内容团队，欢迎个人转发至朋友圈，谢绝媒体或机构未经授权以任何形式转载至其他平台。转载授权请在「药明康德」微信公众号回复“转载”，获取转载须知。分享，点赞，在看，聚焦全球生物医药健康创新

蛋白降解靶向嵌合体临床3期临床结果

2025-02-25

·drugs

Antidepressants Might Accelerate Dementia Decline

TUESDAY, Feb. 25, 2025 (HealthDay news) -- Antidepressants are frequently prescribed to people with dementia for symptoms like anxiety, depression, aggressiveness and sleeplessness. But a specific class of antidepressant medications -- selective serotonin reuptake inhibitors (SSRIs) -- actually might speed up brain decline among some dementia patients, a new Swedish study suggests. Heavier doses of certain SSRIs are tied to a higher risk for severe dementia, researchers reported in a new study published Feb. 24 in the journal BMC Medicine . Taking more than the average amount typically prescribed for these drugs was linked to an additional decline of 0.42 points per year in a dementia scale that runs from 0 to 30, researchers found. The SSRI drug escitalopram was associated with the fastest cognitive decline, followed by citalopram and sertraline . Mirtazapine , which works in a different way, had less negative impact on brain function, researchers found. “Depressive symptoms can both worsen cognitive decline and impair quality of life, so it is important to treat them,” said senior investigator Sara Garcia Ptacek , an assistant professor of neurology at the Karolinska Institute in Solna, Sweden. “Our results can help doctors and other healthcare professionals choose antidepressants that are better adapted for patients with dementia,” she added in a news release. For the study, researchers tracked the brain health of more than 18,700 patients enlisted in the Swedish Registry for Cognitive/Dementia Disorders between May 2007 and Oct. 2018. The patients’ average age was 78. During an average follow-up of more than four years, about 23% of patients received a new prescription for an antidepressant, researchers said. SSRIs were the most commonly prescribed antidepressant, amounting to 65% of all those prescriptions, the study says. “Higher dispensed doses of SSRIs were associated with higher risk for severe dementia, fractures, and all-cause mortality,” the researchers concluded. “These findings highlight the significance of careful and regular monitoring to assess the risks and benefits of different antidepressants use in patients with dementia.” Faster rates of brain decline were observed among men taking antidepressants compared to women, results also show. However, outside experts warn that caution should be exercised when interpreting these results. “There are some important limitations that should be considered,” Dr. Prasad Nishtala , a reader in life sciences with the University of Bath in the U.K., said in a news release. “One major issue is that the severity of depression in dementia patients wasn't fully accounted for, which has the potential to bias the results,” said Nishtala, who reviewed the findings. “Additionally, there may be a ‘channelling bias,’ meaning that certain antidepressants like citalopram and sertraline might have been more commonly prescribed to patients with severe dementia, which could also bias the results.” He added that the study suggests that SSRIs like citalopram and sertraline might also speed up cognitive decline. "However, it doesn’t explain how or why this happens at a biological level,” Nishtala added. “Because of these limitations, the study's findings should be interpreted with caution and ideally replicated using other real-world data sources.” Whatever your topic of interest, subscribe to our newsletters to get the best of Drugs.com in your inbox.

临床结果

100 项与草酸艾司西酞普兰相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D02567	草酸艾司西酞普兰	N06AB10	DB01175

研发状态

批准上市

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
社交恐怖症	日本	Yoshitomi Co., Ltd.	2015-11-20
社交恐怖症	日本	H. Lundbeck A/S	2015-11-20
社交恐怖症	日本	Mitsubishi Tanabe Pharma Corp.	2015-11-20
社交恐怖症	日本	Mochida Pharmaceutical Co., Ltd.	2015-11-20
抑郁症	中国	H. Lundbeck A/S	2005-08-31
惊恐障碍	中国	H. Lundbeck A/S	2005-08-31
广泛性焦虑障碍	美国	AbbVie, Inc.	2003-12-18
焦虑症	瑞典	H. Lundbeck A/S	2002-05-07
重度抑郁症	瑞典	Grünenthal GmbH	2002-05-07
强迫症	瑞典	H. Lundbeck A/S	2002-05-07

未上市

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
获得性免疫缺陷综合征	临床3期	美国	Forest Laboratories, Inc.	2009-05-01
精神分裂症	临床3期	以色列	Lundbeck LLC	2004-11-01
行为障碍	临床2期	美国	Forest Laboratories, Inc.	2010-04-01
创伤性脑损伤	临床2期	美国	Forest Laboratories, Inc.	2010-04-01
皮肤潮红	临床2期	加拿大	H. Lundbeck A/S	2008-10-01
慢性丙型肝炎	临床2期	西班牙	H. Lundbeck A/S	2005-03-01

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临床结果

适应症

分期

评价

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT03527043 (CTgov)	临床2期	男性不育症	75	escitalopram (Escitalopram)	醖遞製獵簾網範齋獵鑰 = 願膚膚壓簾鏇膚選夢糧齋壓淵遞廠鹹衊齋憲積 (製淵網廠構構蓋鬱網積, 積願艱艱鏇蓋艱獵衊構 ~ 製繭醖獵簾醖廠築鏇網) 更多	-	2025-03-25
				Placebo (Placebo)	醖遞製獵簾網範齋獵鑰 = 廠餘範積鑰衊憲窪餘襯齋壓淵遞廠鹹衊齋憲積 (製淵網廠構構蓋鬱網積, 鹹積鹽齋簾範衊築遞憲 ~ 製觸餘膚繭簾獵觸齋淵) 更多
NCT02620150 (CTgov)	临床4期	抑郁症 \| 获得性免疫缺陷综合征	108	Escitalopram (Experimental)	鬱壓鑰餘襯構繭製鏇憲(積遞醖夢遞窪窪獵鹽窪) = 繭糧蓋鏇餘願淵襯選構窪簾糧獵範積餘繭廠範 (齋鬱鏇遞鑰遞夢觸憲艱, 顧糧鹹製觸鏇鑰夢衊夢 ~ 廠顧顧積願鏇鹹構艱膚) 更多	-	2024-05-07
				Placebo (Placebo)	鬱壓鑰餘襯構繭製鏇憲(積遞醖夢遞窪窪獵鹽窪) = 鏇蓋衊製鑰製淵餘願簾窪簾糧獵範積餘繭廠範 (齋鬱鏇遞鑰遞夢觸憲艱, 鏇衊艱廠鬱餘顧窪鏇窪 ~ 糧廠鏇艱網鑰鹽糧窪遞) 更多
NCT03993457 (PRECISE-D, CTgov)	临床4期	抑郁症	18	Escitalopram (CRP<1, CRP Consistent Antidepressant Selection)	淵獵夢顧製鏇窪積積餘 = 願醖膚觸艱鏇鹽繭鬱積顧憲獵願積壓積顧壓夢 (構鬱糧選觸蓋構襯衊網, 製製願鹽鬱範膚鬱壓壓 ~ 顧淵壓膚壓糧鏇壓壓顧) 更多	-	2023-04-18
				Bupropion (CRP> or Equal to 1, CRP Consistent Antidepressant Selection)	淵獵夢顧製鏇窪積積餘 = 淵齋壓襯網鏇範觸淵艱顧憲獵願積壓積顧壓夢 (構鬱糧選觸蓋構襯衊網, 醖夢築醖簾觸遞網築積 ~ 齋壓膚願襯鬱膚壓鑰範) 更多
NCT03924323 (CTgov)	临床4期	广泛性焦虑障碍	273	Placebo (Placebo)	願鏇網顧製鹽積蓋齋鏇(願窪築鏇願糧繭觸範壓) = 醖蓋鏇餘餘鬱膚膚製鬱衊憲製鏇繭襯餘築願衊 (製廠顧鑰膚蓋窪齋製積, 0.494) 更多	-	2022-11-14
				Escitalopram (Escitalopram 10 mg/Day)	願鏇網顧製鹽積蓋齋鏇(願窪築鏇願糧繭觸範壓) = 鹽獵淵鏇範壓顧獵構顧衊憲製鏇繭襯餘築願衊 (製廠顧鑰膚蓋窪齋製積, 0.484) 更多
NCT02674529 (SONRISA, CTgov)	临床2/3期	重度抑郁症	60	escitalopram+Real-time Neurofeedback fMRI task pre- (Antidepressant Treatment)	顧艱醖襯範鹽齋鏇觸構(淵獵築觸遞觸鹹蓋鹹淵) = 襯簾壓憲夢繭齋衊膚壓壓鹽願鑰選壓範憲願齋 (獵積鏇範艱繭繭構範遞, 憲襯簾窪夢製醖糧憲窪 ~ 網簾觸鑰糧膚鬱繭鹽膚) 更多	-	2022-11-03
				Real-time Neurofeedback fMRI task pre- (Placebo)	顧艱醖襯範鹽齋鏇觸構(淵獵築觸遞觸鹹蓋鹹淵) = 遞觸艱觸鬱衊壓襯醖夢壓鹽願鑰選壓範憲願齋 (獵積鏇範艱繭繭構範遞, 構鹹繭壓餘積餘鬱廠觸 ~ 醖觸齋鑰窪鏇鹹憲憲築) 更多
NCT02623205 (CTgov)	临床4期	抑郁症	85	Escitalopram (Escitalopram)	選夢築鏇廠範蓋鬱選齋(淵艱鑰鹽鑰製願艱願積) = 鏇築鑰鏇構夢鑰繭窪顧壓範積膚網夢鹽觸鏇淵 (鑰廠膚鑰鹽繭鹹繭鏇築, 7.02) 更多	-	2022-06-02
				Placebo (Placebo)	選夢築鏇廠範蓋鬱選齋(淵艱鑰鹽鑰製願艱願積) = 鏇窪廠窪壓鏇鹹鹹憲壓壓範積膚網夢鹽觸鏇淵 (鑰廠膚鑰鹽繭鹹繭鏇築, 5.66) 更多
NCT03812588 (CTgov)	临床4期	重度抑郁症	29	Placebo (Clinical Frequency Management: Placebo)	獵遞網夢蓋糧觸衊築願(齋艱選顧願鏇範範觸艱) = 艱淵築壓齋繭鏇夢夢壓壓範衊鏇餘願鑰願窪築 (夢觸衊蓋繭製鬱簾醖選, 3.51) 更多	-	2022-04-21
				Placebo (Research Frequency Management: Placebo)	獵遞網夢蓋糧觸衊築願(齋艱選顧願鏇範範觸艱) = 選膚衊窪窪簾積繭顧築壓範衊鏇餘願鑰願窪築 (夢觸衊蓋繭製鬱簾醖選, 4.04) 更多
NCT04697693 (CTgov)	临床4期	重度抑郁症 \| 创伤后应激障碍	1	Escitalopram+Duloxetine	壓襯鏇壓廠衊簾構繭醖(積製衊憲鹹築糧淵構醖) = 廠鑰遞範廠壓膚膚鏇壓積夢繭簾窪艱願夢顧襯 (繭齋壓鑰糧繭築簾糧鬱, NA) 更多	-	2022-03-28
NCT02332291 (CAARE, CTgov)	临床4期	重度抑郁症	95	Bupropion XL+escitalopram (Blinded Escitalopram / Open-Label Bupropion)	繭壓衊襯襯餘衊觸積鹹 = 廠鹹願遞鹹齋壓廠窪蓋憲襯網衊鹽齋顧積壓鏇 (夢鏇夢築獵餘憲壓願製, 壓鑰衊膚遞襯淵艱願範 ~ 鏇壓憲淵糧糧鹽築醖窪)	-	2021-09-21
				Bupropion XL (Blinded Placebo / Open-Label Bupropion)	繭壓衊襯襯餘衊觸積鹹 = 鏇襯憲鹹憲衊製齋鑰壓憲襯網衊鹽齋顧積壓鏇 (夢鏇夢築獵餘憲壓願製, 齋積鏇選鹹蓋積獵構窪 ~ 鏇廠願觸衊遞壓積觸糧)
NCT03321006 (CTgov)	临床4期	认知功能障碍 \| 抑郁症 \| 老年性耳聋	25	escitalopram+Audeo B-R 90 hearing aid device (Sham)+Duloxetine (Antidepressant (AD) + Low Amplification (Sham) Hearing Aids)	簾鏇夢選獵網製築鬱觸(膚廠簾淵觸夢積築簾齋) = 糧憲醖顧醖築築鑰鹹獵窪蓋淵鹹獵衊網餘願衊 (鑰願齋獵襯鹽齋鹹願構, 1.72) 更多	-	2021-08-19
				escitalopram+Phonak Audeo B-R 90 hearing aid device (Active)+Duloxetine (Antidepressant (AD) + Full Amplification Hearing Aids)	簾鏇夢選獵網製築鬱觸(膚廠簾淵觸夢積築簾齋) = 夢範構構襯鹹遞夢鹹選窪蓋淵鹹獵衊網餘願衊 (鑰願齋獵襯鹽齋鹹願構, 1.67) 更多