更新于：2024-11-15

Fluoxetine Hydrochloride

盐酸氟西汀

更新于：2024-11-15

概要

概要

基本信息

简介氟西汀盐酸盐，也称为PROZAC®，是一种选择性5-羟色胺再摄取抑制剂。它于1987年由Eli Lilly＆Co.在美国首次获批。PROZAC用于治疗重度抑郁障碍、强迫症、神经性厌食症和惊恐障碍。它还以Sarafem®的名字在市场上销售，用于治疗经前期失调症。PROZAC和奥氮平的联合用药适用于治疗双相情感障碍伴随的抑郁发作和治疗难治性抑郁症。然而，PROZAC单药疗法不适用于这些情况。当使用PROZAC和奥氮平联合用药时，临床医生应参考Symbyax®的包装说明书中的临床研究部分。

药物类型

小分子化药

别名

(+-)-N-Methyl-3-phenyl-3-((alpha,alpha,alpha-trifluoro-P-tolyl)oxy)propylamine、(+-)-N-Methyl-gamma-(4-(trifluoromethyl)phenoxy)benzenepropanamine、Fluoxetine hydrochloride (JAN/USP)

+ [16]

靶点

SERT

作用机制

SERT抑制剂(5-羟色胺转运体抑制剂)

治疗领域

其他疾病

在研适应症

躁郁症1型难治性抑郁症神经性贪食症+ [5]

非在研适应症

原研机构

在研机构

+ [2]

非在研机构

山德士有限公司

Sandoz Group AGAllergan Pharmaceuticals International Ltd.

+ [1]

最高研发阶段批准上市

首次获批日期

美国 (1987-12-29),

经前焦虑症

最高研发阶段(中国)批准上市

特殊审评孤儿药 (美国)

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结构

分子式C17H19ClF3NO

InChIKeyGIYXAJPCNFJEHY-UHFFFAOYSA-N

CAS号56296-78-7

关联

316

项与盐酸氟西汀相关的临床试验

NCT06225011 / Not yet recruiting临床1期IIT

Repurposing Drugs as Immunotherapeutic Agents: Changes in Colorectal Tumor Immune Cells After Targeting Serotonin

This phase I trial tests whether fluoxetine (prozac) works to modify the tumor immune cells before surgery in patients with colorectal cancer. Fluoxetine is a commonly used selective serotonin reuptake inhibitor (SSRI) prescribed for major depressive disorder and generalized anxiety. Giving fluoxetine may modify the immune cell composition in the tumor and its microenvironment and may induce changes in body's immune system and may interfere with the ability of tumor cells to grow and spread in patients with colorectal cancer.

开始日期2024-12-01

申办/合作机构

Jonsson Comprehensive Cancer Center

NCT05976347 / Not yet recruiting临床4期IIT

Identifying and Treating Depression in the Orthopaedic Trauma Population

The goal of this trial is to pilot a way for orthopaedic surgeons to safely screen for depression and provide treatment for depression with medication. The main questions it aims to answer are:
1. What are the outcomes of patients who screen positive for depressive symptoms and are prescribed either an Selective serotonin reuptake inhibitors (SSRI) or serotonin and norepinephrine reuptake inhibitors (SNRI).
2. What are the outcomes of patients who screen positive for depressive symptoms and choose not to pursue treatment with medication?

开始日期2024-11-01

申办/合作机构

Wake Forest School of Medicine

NCT06506136 / Not yet recruiting临床1/2期IIT

Evaluation of the Efficacy of Fluoxetine in the Treatment of Refractory Constipation: a Multicenter, Randomized, Double-blind, Placebo-controlled Trial

The goal of this clinical trial is to determine if fluoxetine is effective in treating refractory constipation in adults. It will also assess the safety profile of fluoxetine when used for this condition. The main questions it aims to answer are:
Does fluoxetine improve bowel movement frequency and Complete Spontaneous Bowel Movements (CSBM) in participants with refractory constipation? What adverse effects do participants experience while taking fluoxetine? Researchers will compare fluoxetine to a placebo (a look-alike substance that contains no active drug) to evaluate its efficacy and safety in treating chronic constipation.
Participants will:
Take fluoxetine or a placebo daily for 12 weeks Visit the clinic every 4 weeks for checkups and tests Maintain a diary of their CSBM, Spontaneous Bowel Movements (SBM), bowel movements, stool consistency, and any side effects experienced

开始日期2024-09-01

申办/合作机构

西京医院第四军医大学

100 项与盐酸氟西汀相关的临床结果

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100 项与盐酸氟西汀相关的转化医学

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100 项与盐酸氟西汀相关的专利（医药）

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13,832

项与盐酸氟西汀相关的文献（医药）

2025-02-01·BEHAVIOURAL BRAIN RESEARCH

Moringa oleifera Lam. seed lectin (WSMoL) reduces chronic stress-induced anxiety and depression in mice by lessening inflammation and balancing brain chemicals

Article

作者: Napoleão, Daniella Carla ; de Lima, Bárbara Raíssa Ferreira ; de Oliveira Marinho, Amanda ; de Siqueira Patriota, Leydianne Leite ; Paiva, Patrícia Maria Guedes ; da Costa, Jainaldo Alves ; Pereira, Michelly Cristiny ; Napoleão, Thiago Henrique ; Cavalcanti, Jorge Vinícius Fernandes Lima ; de Lucena, Alex Leandro Andrade ; da Rosa, Michelle Melgarejo

Phyto-based treatments for anxiety and depression are gaining attention. The efficacy of the water-soluble Moringa oleifera seed lectin (WSMoL) in reducing acute anxiolytic and depressive-like behaviors in mice has been previously demonstrated. In the present study, it was evaluated the effects of WSMoL on reducing anxiety and depressive-like symptoms in a mouse model of unpredictable chronic mild stress (UCMS). The animals were divided into groups and exposed to a four-week UCMS regimen. Following this, the mice received daily intraperitoneal injections of vehicle (non-stressed and UCMS control groups), WSMoL (2 or 4 mg/kg), or fluoxetine (10 mg/kg) for 21 days. Neurobehavioral tests included the open field test and elevated plus maze test to assess anxiety-like behavior, and the tail suspension test and sucrose preference test to evaluate depression-like behavior. Biochemical analyses measured serum corticosterone and cytokines as well brain levels of cytokines and monoamines. All tests indicated that WSMoL significantly (p < 0.05) reversed the anxiety and depression-like behaviors induced by UCMS. The stress protocol increased serum corticosterone levels and WSMoL treatment was not able to normalize corticosterone secretion. WSMoL treatment reduced serum and brain levels of IL-2, IL-6, and TNF-α, indicating reduced neuroinflammation, and increased brain levels of dopamine, serotonin, and noradrenaline. In summary, WSMoL mitigated UCMS-induced anxiety and depression-like behaviors by reducing neuroinflammation and modulating brain monoamine levels.

2025-02-01·BEHAVIOURAL BRAIN RESEARCH

Involvement of the serotonergic, GABAergic and glutamatergic systems of the rostral anterior cingulate cortex in the trait and state anxiety of adult male Wistar rats.

Article

作者: Santos, José Ronaldo Dos ; Franco, Heitor Santos ; Almeida-Souza, Thiago Henrique ; Santos, Leandra Martins ; Oliveira E Silva, Ana Mara de ; Melo, João Eduardo Conceição ; Oliveira e Silva, Ana Mara de ; Goes, Tiago Costa ; de Menezes, Edênia Cunha ; dos Santos, José Ronaldo ; Silva, Rodolfo Santos ; Teixeira-Silva, Flavia ; Marchioro, Murilo ; Menezes, Edênia Cunha de

Despite significant advancements to understand of the neural circuitry involved in anxiety, the neurobiology of trait anxiety remains unclear. The rostral anterior cingulate cortex (rACC) and various pathways have been implicated in its regulation, making it a key to trait anxiety. The present study aimed to investigate the role of these neurotransmitter systems in the rACC in trait anxiety. Since trait anxiety is known to modulate state anxiety, we further investigated this relationship. Specifically, in Experiment I, we used animals with high trait anxiety; in Experiment II, we used animals with low trait anxiety; and in Experiment III, we used animals with medium trait anxiety. Before each behavioral assessment, drugs that either increased or decreased serotonergic (Fluoxetine or WAY-100635), GABAergic (Muscimol or Bicuculline), and glutamatergic (NMDA or Ketamine) neurotransmission in the rACC were administered, along with their respective controls. Additionally, in Experiment IV, all animals from the previous experiments were subjected to the Elevated Plus Maze (EPM) and Hole board (HB) test and evaluated without taking into account their trait anxiety levels. The results of the present study showed that, in Exp I, the modulation of the serotonergic, GABAergic and glutamatergic systems in the rACC decreased trait anxiety in highly anxious rats, while by submitting the animals to HB, the administration of fluoxetine increased state anxiety. In Exp II, the modulation of all systems increased trait anxiety in rats with low trait anxiety, whereas, in HB, state anxiety levels were increased with the administration of NMDA. In Exp III, only the modulation of the glutamatergic system, with NMDA, increased both trait and state anxiety levels. However, none of the evaluated neurotransmitter systems altered the state anxiety modeled in the EPM. Overall, the results of the present study provide new insights into the role of the neurotransmitter systems in the rACC in the regulation of trait anxiety and state anxiety.

2025-01-01·COMPARATIVE BIOCHEMISTRY AND PHYSIOLOGY C-TOXICOLOGY & PHARMACOLOGY

Fluoxetine antagonizes the acute response of LPS: Blocks K2P channels

Article

作者: Elliott, Elizabeth R ; Cooper, Robin L. ; Elliott, Elizabeth R. ; Cooper, Robin L

The channels responsible for maintaining resting membrane potential are known as K2P (two-P-domain K⁺ subunit) channels, a subset of which are known to be blocked by Fluoxetine. In this experiment, the compound's effects on the membrane potential were examined on muscles in larval Drosophila overexpressing a subtype of K2P channel (known in Drosophila as dORKA1 or ORKA1) and compared to larvae without overexpression. The compound was also observed in sequence and/or combination with a form of lipopolysaccharide (LPS) that transiently activates K2P channels. Different concentrations of Fluoxetine were tested, and it was also examined in cocktail with the LPS. At 25 μM Fluoxetine exposure, muscle in control larvae underwent depolarization, while muscles overexpressing K2P channels hyperpolarized; at 50 μM, however, much more variable responses were observed. The LPS caused hyperpolarization in both larval strains, but the effect was more transient in the Canton-S line than in the K2P overexpressors. Finally, LPS continued to cause hyperpolarization even in the presence of Fluoxetine, while Fluoxetine quickly depolarized the muscle during exposure to LPS. The cocktail showed a smaller effect on muscles overexpressing ORKA1 as compared to the controls, indicating that Fluoxetine does not block the ORKA1 subtype. This study is significant because it demonstrates how overexpression of K2P channels alters membrane response to LPS and Fluoxetine exposure.

218

项与盐酸氟西汀相关的新闻（医药）

2024-10-31

·乐威医药

探索分子砌块：氧（氮）杂环丁烷磺酰氟

在药物研发的领域中，科学家们一直在探索新的分子结构和化学合成方法，以寻找更有效、更安全的药物。今天要给大家介绍的是一项来自伦敦帝国理工学院和辉瑞研发中心的研究，他们发现的「氧杂环丁烷和氮杂环丁烷磺酰氟」在药物发现中的巨大潜力。有感兴趣的朋友，点击“在看”与“转发”后，联系公众号助理索取原文！小分子杂环：药物设计的新宠 1.小分子杂环：药物设计的新宠在药物化学中，精确控制分子的性质和构象是至关重要的。小分子极性基团，如氧杂环丁烷和氮杂环丁烷，因其独特的空间电子性质，成为了备受瞩目的生物电子等排体。它们可以模拟更常见官能团的性质，通过调整极性和氢键特性来增强药物与靶点的结合能力，同时还能影响药物的代谢稳定性、溶解度、吸收、分布和 pKa 值。目前，已经有一些含有氧杂环丁烷的化合物进入了临床试验阶段，氮杂环丁烷在已批准的药物中也逐渐崭露头角。多样的反应路径，丰富的化学结构 Defluorosulfonylative（deFS）耦合反应 OSF 和 ASF 试剂通过 deFS 反应途径，生成的碳正离子中间体可与多种亲核试剂耦合，从而合成了一系列新颖的化学结构。研究人员利用这一反应，合成了 11 种药物类似物，包括一些具有重要生物活性的分子，如治疗糖尿病诱导的免疫功能障碍的 SERCA 激活剂类似物，以及 MAPK14 抑制剂类似物等。 Sulfur–Fluoride Exchange（SuFEx）反应在阴离子条件下，OSF 试剂还能通过 SuFEx 途径生成氧杂环丁烷 - 硫（VI）衍生物。通过调整溶剂和亲核试剂的强度，研究人员成功解锁了这一反应路径，为药物分子的设计提供了更多的选择。合并药效团，创造新的药物设计元素研究人员还探索了将氧杂环丁烷与其他极性官能团合并的可能性。例如，通过 deFS 反应将氧杂环丁烷与 NH - 唑、亚砜亚胺和含磷官能团等结合，形成了多种新颖的化学结构，这些结构可能作为有价值的新型生物电子等排体或替代基团，为药物化学家提供了新的设计思路。含磷官能团作为药物化学结构单元尚未得到充分研究。膦酸酯和磷酸酯基团已被用于前药中以促进细胞膜通透性，而氧化膦在布加替尼获批后才开始受到更广泛的研究。人们越来越关注将这些结构单元引入类药分子中以调节 LogD 和溶解度。我们假设可以利用亚磷酸烷基酯试剂来捕获氧杂环丁烷碳正离子并提供相应的磷酸化氧杂环丁烷产物。含有氧杂环丁烷的新型结构基元可进行进一步衍生化（方案 2d）。氧杂环丁烷叠氮化物59经铜催化的叠氮-炔烃环加成反应（CuAAC）生成三唑88，拓展了氧杂环丁烷 1,2,3 - 三唑的潜在应用范围。氮杂环丁烷磺酰氟的独特魅力首次报道的 ASF 试剂与 OSF 试剂具有相似的反应性。它可以通过 deFS 反应合成3-芳基-3-取代的氮杂环丁烷衍生物，并且与多种亲核试剂具有良好的兼容性，包括一些复杂的晚期示例，如氟西汀和氨氯地平的氮杂环丁烷功能化衍生物。此外，ASF 试剂还能通过 SuFEx 反应与醇盐反应，展示了其与复杂分子共轭的潜力。在药物发现中的实际应用 PROTAC 连接子和分子胶设计在靶向蛋白质降解这一新兴领域中，OSF 和 ASF试剂展现出了独特的应用价值。研究人员利用这些试剂引入了cereblon-结合基序，为PROTAC连接子和分子胶提供了新的设计思路。这些新的设计可能改善其物理化学性质或溶解度特性，从而提高药物的疗效。靶蛋白的降解通过与 pomalidomide等E3连接酶配体的耦合反应，OSF和ASF试剂生成了新的降解剂基序，展示了它们在靶向蛋白质降解领域的应用潜力。这为开发新的药物治疗方法提供了新的途径。结论与展望这项研究展示了OSF和ASF 试剂在药物发现中的强大潜力。它们不仅可以通过多种反应路径合成具有新颖结构的化合物，还能为药物分子的设计提供新的思路和方法。未来，我们期待这些试剂能够在药物研发中得到更广泛的应用，为人类健康带来更多的福祉。版权声明：本文内容及图片，如有侵权请联系删除。免责声明：本文内容仅作信息交流学习，并不反映任何意见及观点。往期推荐乐威医药（欧洲）分公司正式成立乐威医药沧州GMP生产基地高活生产线启用乐威医药亮相意大利CPHI Milan 2024

临床研究诊断试剂生物类似药上市批准

2024-10-15

·Healthcare Digital

Eli Lilly's US$364m UK Investment Targets Obesity Crisis

Obesity is on the rise, as are healthcare solutions Eli Lilly to make a US$364m investment in the UK, as the pharmaceutical leader strives to improve healthcare solutions for people living with obesity More than one billion people across the world are obese. Obesity is linked to a higher risk of cardiovascular disease, diabetes, stroke and even certain cancers. Yet despite the dangers, it’s on the rise. No matter personal feelings or preferences, obesity is a global public health issue that the healthcare industry is scrambling to solve. Now, Eli Lilly has shared that it wants to invest US$364m in the UK to tackle obesity, as well as other public health problems. Eli Lilly is one of the world’s oldest pharmaceutical companies, known for its clinical depression drug Prozac and its diabetes drugs, Humalog and Trulicity. Eli Lilly’s weight loss innovation supports those with obesity complications Eli Lilly’s proposal was revealed at the UK government's International Investment Summit, where the company also discussed the creation of a UK biotech hub, Lilly Gateway Labs (LGL). This facility will support early-stage life sciences businesses as they research new healthcare solutions. The LGL plan would receive £204m of funding over three years, offering start-ups with Lilly's expertise, access to laboratories and possible financial investments. This would establish the first LGL site in Europe, next to Lilly’s four other LGLs across the US. Lilly has announced plans to start a five-year study of real-world evidence looking at tirzepatide, the dual GIP/GLP-1 receptor agonist in the company's Mounjaro drug for type 2 diabetes and obesity. The SURMOUNT-REAL UK study will be led in partnership with Health Innovation Manchester, subject to relevant approvals and will explore the real-world effectiveness of tirzepatide in: Weight loss Diabetes prevention Prevention of obesity-related complications for adults with obesity. Mounjaro was authorised as a weight-loss treatment by the UK's Medicines and Healthcare products Regulatory Agency (MHRA) in 2023 and has been endorsed by the National Institute for Health and Care Excellence (NICE) for a phased rollout. This would make the drug available to obese people, with complications ranging from hypertension, dyslipidaemia, obstructive sleep apnoea, as well as cardiovascular disease. How the healthcare sector can partner with governments to tackle and prevent disease UK Health Secretary Wes Streeting has suggested that weight-loss jabs could be provided to people who are unemployed, to help them get back into work. "I think that some of these drugs can be game changing in terms of tackling obesity. For those people that are so obese, that diet, exercise doesn't feel like it's having much of an impact, it feels like you're on a losing battle. I think the drugs can make a really big impact in terms of getting weight under control,” he said. However, the Health Secretary was clear that the drugs were not to be used as an excuse to not do the right thing in terms of diet, nutrition and exercise. "Where I think we've just got to be careful, though, is that we don't see these drugs as cosmetic drugs for the Instagram perfect body. Drugs do come at a cost.” Prime Minister Sir Keir Starmer acknowledged that the government needed to ‘think differently’ to reduce pressure on the health system and Lilly's CEO, David Ricks, said he welcomed the opportunity to partner with the UK Government on tackling and preventing disease and accelerating innovation to advance care delivery models. "Today's announcement is an important milestone and we are pleased to reinforce Lilly's commitment to improving health for people living with obesity and its serious consequences," said David. ****** Make sure you check out the latest industry news and insights at Healthcare Digital and also sign up to our global conference series - Tech & AI LIVE 2024 ****** Healthcare Digital is a BizClik brand

上市批准

2024-10-09

·同写意

礼来，冲向万亿市值之巅？

本届大会以“共建创新生态共赢产业未来”为主题，聚焦生物医药出海与国际化创新、创新药投融资、医疗器械等产业发展风向标，打造“高端化、国际化、专业化、立体化”的年度盛会。时来天地皆同力——礼来正处于这样的上升期。华尔街投资者对减肥药股票的无限渴求，眼看将使该公司成为全球首家市值达1万亿美元的制药商。但是，当经营一家制药公司，关于更悲惨时期的战争故事就永远不会离你太远。2000年代末，礼来的Prozac、Zyprexa和Cymbalta等主要精神疾病药物专利到期，公司股价一度接近历史最低点。礼来首席执行官Dave Ricks回忆说，当时行业正掀起整合浪潮，礼来面临着被收购的风险。命运的齿轮从此开始转动。如今，该公司的主要问题是如何快速建设生产线，以满足人们对其降糖减肥药物Mounjaro、Zepbound的需求。过去四年来，礼来已投资200亿美元建设生产设施，并于10月初表示，将再投资45亿美元在其总部美国印第安纳州建设一个临床试验药物生产设施。该公司的潜在患者群体是历史上任何药物中最大的：美国有超过1亿肥胖成年人，全球有10亿肥胖患者。 “许多人从中获益，而且见效很快，因此形成了非常强大的消费者兴趣周期。”Ricks补充说，巨大的需求令GLP-1药物备受追捧。预计到2029年，减肥市场的年销售额将增长到1300亿美元峰值。凭借最强效的减肥针和11种在研实验性疗法，包括被广泛认为有望首个获批的小分子GLP-1药丸，礼来或许会成为的最大赢家。但Ricks并不满足。他花费大量时间致力于提高产能，以超越丹麦的竞争对手诺和诺德。与此同时，礼来正在与仿制药和其他新药开发商竞争，并面临着来自政界人士、患者对其产品价格越来越高的压力。投资者也对该公司泡沫估值产生了警惕。截至10月8日收盘，该公司市值超过8684亿美元，是未来12个月预计收益的54倍以上，达到了业内前所未有的高度。 “每个人都盲目地买入礼来等公司的股票，所以这些股票会继续上涨，但它们的定价非常合理，”礼来一位前十大股东表示，“如果投资者对其他10家生产减肥药的公司以及可能面临的定价压力感到害怕，他们可能就有麻烦了。” 礼来希望通过在竞争中保持领先局面，巩固其在美国MNC排名中的地位。对它来说，这意味着将巨额收入投进研发，为其产品在仿制药竞争到来时——大约是2030年代中期——面临所谓的“专利悬崖”做好准备。在礼来首席科学官Daniel Skovronsky看来，微软、苹果、英伟达和谷歌等这些科技巨头都具有“对客户的粘性……而这是过去制药行业所缺乏的”。所以，该公司的长期使命不仅是要更上一层楼，还要通过培养一些消费者忠诚度来避免重回黑暗时代。“我们的使命，是摆脱制药业的繁荣与萧条周期。”Skovronsky补充道。 1 成为霸主 2018年，瑞士制药商罗氏拒绝了由中外制药开发的一款GLP-1药物后，一场延续一个多世纪的竞争再度升温。据两位知情人士透露，经过短暂的竞价，礼来击败了诺和诺德，以5000万美元预付款获得了该候选药物的专利权。 Skovronsky不记得在签订许可协议时是否讨论过将之用于减肥的潜力，起初，它被设计成治疗2型糖尿病，但如今这种被称作orforglipron的药物倘若按计划于2026年上市，可能会成为首个小分子减肥药。减肥药市场，礼来似乎考虑从几个方面超越诺和诺德，夺取霸主地位。而这款减肥药，就是其中之一。 “一个世纪以来，我们一直与诺和诺德直接或间接地竞争，”Ricks说，“竞争对消费者有利：它加快了产品上市的速度，我们可以不断迭代，生产更好产品……因此，这是一种跳跃式的竞争。” 1923年，礼来首次推出用于治疗糖尿病的胰岛素产品，而在此之前，糖尿病一直被视为绝症。诺和（Novo）在与诺德（Nordisk）合并之前，开发了一款长效胰岛素产品和第一支胰岛素笔。 1982年，礼来推出首款合成、可量产的人类胰岛素。2005年，礼来又研制出首款GLP-1药物，每日注射两次，但2017年，诺和诺德公司在美国推出每周只需注射一次的Ozempic，彻底改变了市场格局。汇丰银行医疗保健股票研究主管Rajesh Kumar表示，尽管诺和诺德领先，礼来凭借其减肥药物的推出获得了“后发优势”。他认为，礼来“可以看到领先者陷入了什么陷阱”，这让其能更快提高生产速度，开发下一代产品。根据分析师的一致估算，今年，Mounjaro和Zepbound（均以活性成分替尔泊肽为基础）的销售额将达到188亿美元——尽管上市时间较短，但接近诺和诺德从Ozempic和Wegovy获得的270亿美元预计收入。预计到2027年，礼来GLP-1药物的销售额将超过诺和诺德。假设orforglipron如期于2026年上市，礼来将在竞争对手赶上前，拥有垄断减肥药市场两年的地位。该公司也在开发retatrutide，这是一种激活三种不同肠道肽的新药。中期试验显示，该药可减轻24%的体重，远比任何现有疗法的效果都显著。此外，礼来还想证明替尔泊肽对肥胖的连锁反应（如睡眠呼吸暂停、心血管风险和慢性肾病）具有额外益处，从而帮助简化获得更广泛保险覆盖的途径。在美国，Medicare主要针对65岁以上的人群，目前仅在患者患有其他合并症时才将报销范围覆盖减肥药物。 “我们要一步一步地解决这一问题……通过证明这些药物不仅能减轻体重，还能减轻体重带来的后果，”Ricks展望说，“我认为五年后，我们回过头来看会发现，大部分疾病都可以通过改变体重来缓解……而付款人会说，我们应该为替尔泊肽所有这些治疗费用买单。” 除了宿敌诺和诺德之外，礼来还面临来自其他领域的竞争。PitchBook称，到2029年，可能会有多达16种新型减肥药上市，其中包括制药商阿斯利康、辉瑞和安进的产品。但更紧迫的是，礼来正在打击一系列仿制减肥药。在专利药品短缺时，FDA允许配制药品的药房生产，而后者已充斥于市场。 Ricks认为，礼来正努力增加供应，替尔泊肽继续留在FDA的短缺名单上“毫无道理”，并补充说，配制会给患者带来风险。 “让我们携手解决生产问题，不要利用这个陷阱，让美国人接触到未经批准的（活性药物成分）掺假产品。”10月初，FDA表示，影响替尔泊肽的短缺问题已经“解决”，这意味着，该机构很可能要终止对该药物的配制授权。然而，竞争对手紧随礼来之后，让其关键优势逐渐减弱，投资者看到了该公司市值可能接近峰值的警告信号。一位前25大股东预测，礼来市值突破1万亿美元大关没有悬念，可这“已经接近顶峰”。这位投资者表示：“专利悬崖不可避免，竞争激烈，很快就会出现价格战。现在似乎是人们对礼来的追捧达到顶峰。” 2 未来之路如果礼来真的想摆脱制药业的兴衰周期，其研发团队就必须着手找到下一个划时代的药物。一位投资者说，礼来的任务是确定“你下一个巨大的、异想天开的目标是什么”。该公司希望，这样的机会可能隐藏在其推出的减肥药物的真实数据中。 Skovronsky表示，早期迹象表明，数十万接受替尔泊肽治疗的患者，开始看到治疗的其他惊人效果：焦虑和抑郁症状减轻，以及对吸烟和饮酒等行为得到更好的控制。礼来已将这些减肥疗法与其他药物联合用于治疗银屑病关节炎等自身免疫性疾病，但Skovronsky称，这些疗法对精神健康和成瘾的影响“足够有趣，因此我们正在考虑……如何解决这些药物是否有助于治疗这类疾病的问题”。该制药商还考虑，将那些体重尚未超标但有增加风险的人群，纳入其减肥药和其他疗法的未来试验中，这表明它已经在寻找扩大减肥药市场的方法。然而，礼来面临的最大问题是，该公司将如何处理减肥药带来的前所未有的意外之财。从现在到2030年，分析师预计，该业务将产生1870亿美元的自由现金流，礼来可以用这笔钱做任何想做的事情。正如一位风险投资者所说：虽然行业都在关注礼来的市值，但更关键的是“一旦钱到账”，礼来会做什么。 Ricks表示：“我们的支出能力正在上升，因此我们应该仔细考虑一切，但可能不会改变我们的原则。”他补充说，他更倾向于早期研发投资，而不是大规模的、固定的收购，因为这些收购虽然能增加收入，却会抑制成长。 “当这家公司的未来充满疑问时……我们把赌注押在了研发上，并且通过创新我们才得以生存。”Ricks指出，当其他制药巨头放弃时，礼来坚持进行糖尿病和肥胖症的研究。 “这或许就是我们通过创新保持发展势头的方式，”Ricks说道，“我们根据项目来部署资金，而不是通过某种自上而下的计算……因此，这要求我们深入研究每个项目，并决定是否为之投入。” 2014年，默沙东重磅癌症免疫疗法药物Keytruda上市，Skovronsky回忆，当时他们急于赶上并推出礼来自己的检查点抑制剂。事实证明，这个策略并不奏效。他预测，许多竞争对手也将错过下一波创新浪潮，因为他们正试图找到进入肥胖市场的途径。与此同时，礼来将有喘息的空间，来追求它的下一个重大创新：现在，其用于治疗早期阿尔茨海默病的药物Kisunla已在美国获得批准，礼来正在将该药物作为这种无法治愈的脑部疾病的预防性治疗。 Skovronsky补充道，礼来之前最成功的药物是治疗抑郁症的Prozac，该公司很可能会重新进军精神病学领域。随着美国继续寻找解决阿片类药物危机的方法，非阿片类止痛药也是一个潜在的增长领域。制药公司“在临近专利悬崖的几年里，之所以受到投资者的质疑，并不是因为其他业务没有突破悬崖，而是因为其他业务根本就没有吸引力”。按照礼来肿瘤部门负责人Jacob Van Naarden的这种看法，对于礼来，挑战在于向投资者证明，公司其他业务可以像其“重磅炸弹”GLP-1药物一样具有吸引力。 “如果去掉糖尿病和肥胖症业务，他们的表现就不那么好了，”一位投资者说，“进入新领域存在一定风险，因为就像诺和诺德一样，他们在这一领域确实很擅长……其他业务则好坏参半。” 还需要注意的是，这种探索的成功率很低。发现像他汀类药物Lipitor、自身免疫药物Humira、PD-1抑制剂Keytruda和现在的GLP-1这样的热门药物非常难得，而且通常不会连续两次由同一家公司做到。Van Naarden说：“如果我们能做到，那就太好了。” 参考资料： 1.Can Eli Lilly become the first $1tn drugmaker? 2.Roche Misses Out On Weight-Loss Blockbuster Drug, Now Playing Catch-Up In Booming Market 同写意媒体矩阵，欢迎关注↓↓↓

并购专利到期

100 项与盐酸氟西汀相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D00823	盐酸氟西汀	N06AB03	DB00472

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
躁郁症1型	美国	Eli Lilly & Co.	2009-03-19
难治性抑郁症	美国	Eli Lilly & Co.	2009-03-19
神经性贪食症	美国	Eli Lilly & Co.	2002-07-29
重度抑郁症	美国	Eli Lilly & Co.	2002-07-29
强迫症	美国	Eli Lilly & Co.	2002-07-29
惊恐障碍	美国	Eli Lilly & Co.	2002-07-29
抑郁症	中国	Lilly France SAS	1996-10-21
经前焦虑症	美国	Eli Lilly & Co.	1987-12-29

未上市

10 条进展最快的记录,

后查看更多信息

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3期	日本	Eli Lilly & Co.	2013-03-01
吸烟	临床3期	美国	Eli Lilly & Co.	1998-02-01

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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


NCT03390933 (CTgov)	临床4期	抑郁症 \| 肾病	16	Fluoxetine	窪廠繭鏇襯範鬱廠糧簾(鏇糧選築憲觸齋餘願觸) = 廠餘衊襯壓網積鹹構夢襯糧鑰夢鬱憲鑰餘製鬱 (製蓋窪襯繭簾齋遞築遞, 遞鏇鏇築夢積襯築齋製 ~ 廠積廠築構齋鹽鹽醖網) 更多	-	2024-10-17
NCT02357849 (FACT, CTgov)	临床4期	精神障碍	9	Aripiprazole (Aripiprazole)	遞蓋鹹夢簾獵艱遞醖鏇(衊網艱繭廠簾選願鬱鬱) = 廠鑰觸積鹽醖衊鏇繭構鹹憲蓋觸衊蓋壓獵醖選 (鑰艱窪簾夢觸醖選製遞, 獵蓋鹽繭齋壓襯醖獵窪 ~ 願糧鑰餘構築鏇襯襯夢) 更多	-	2023-11-15
				Fluoxetine (Fluoxetine)	遞蓋鹹夢簾獵艱遞醖鏇(衊網艱繭廠簾選願鬱鬱) = 選願鹽夢膚遞繭蓋醖鬱鹹憲蓋觸衊蓋壓獵醖選 (鑰艱窪簾夢觸醖選製遞, 艱願繭願廠壓糧選顧鑰 ~ 蓋築簾壓鬱憲淵糧齋齋) 更多
ESC2023	N/A	-	203	watchman FLX	醖網鬱糧淵憲築廠夢壓(獵願淵獵願蓋製鏇積製) = 夢膚繭簾選鹹簾遞淵遞淵願範積顧淵糧範鏇願 (艱範積醖鏇淵網窪醖衊 )	-	2023-08-28
				watchman FLX	醖網鬱糧淵憲築廠夢壓(獵願淵獵願蓋製鏇積製) = 築壓淵鬱簾壓糧襯選淵淵願範積顧淵糧範鏇願 (艱範積醖鏇淵網窪醖衊 )
NCT04377308 (CTgov)	临床4期	新型冠状病毒感染 \| 细胞因子释放综合征	16	fluoxetine (Treatment As Usual)	壓鏇築願製蓋觸遞觸遞(膚選獵窪積鑰顧鏇範網) = 衊願壓獵簾觸淵選簾鏇選獵範壓衊簾艱壓膚獵 (齋夢製廠網範齋餘獵選, 壓鏇鹽膚齋簾窪蓋簾醖 ~ 遞鏇遞構選艱積衊艱築) 更多	-	2022-09-30
				Fluoxetine (Fluoxetine)	壓鏇築願製蓋觸遞觸遞(膚選獵窪積鑰顧鏇範網) = 餘窪鏇顧憲鬱夢選夢繭選獵範壓衊簾艱壓膚獵 (齋夢製廠網範齋餘獵選, 廠艱顧選鑰鹽顧繭繭築 ~ 觸鏇願構夢糧醖齋壓蓋) 更多
NCT04676139 (Pubmed) 人工标引	临床3期	夜间遗尿症	110	Fluoxetine	遞餘窪壓鑰範選願淵廠(憲願築築襯襯繭簾夢襯) = 網遞憲衊鏇鏇鹽鑰艱鏇築觸醖遞蓋憲網窪遞網 (壓窪鑰築艱選憲糧鏇廠, 4.6) 更多	积极	2022-08-31
				Placebo	遞餘窪壓鑰範選願淵廠(憲願築築襯襯繭簾夢襯) = 積鏇壓選蓋襯獵觸遞齋築觸醖遞蓋憲網窪遞網 (壓窪鑰築艱選憲糧鏇廠, 3.4) 更多
NCT02737930 (FLUORESCE, Pubmed)	临床2期	急性缺血性卒中	17	Fluoxetine 20 mg	餘鹽積網築繭壓襯構鬱(鏇齋簾觸艱顧願範遞壓) = 齋簾構鑰膚築襯鹹艱淵鏇願繭築夢鏇艱膚壓糧 (鬱鏇夢簾鏇積觸鏇網壓 )	积极	2022-07-08
				Placebo	餘鹽積網築繭壓襯構鬱(鏇齋簾觸艱顧願範遞壓) = 艱築鑰餘夢窪糧憲壓積鏇願繭築夢鏇艱膚壓糧 (鬱鏇夢簾鏇積觸鏇網壓 )
NCT03728153 (MAMBO, CTgov)	临床2期	缺血性卒中	34	Fluoxetine 20 MG Oral Tablet	餘蓋鹹顧選淵鬱糧顧淵(鬱獵遞網遞醖觸製鑰餘) = 鑰鑰夢膚醖襯窪餘顧繭鹹艱憲膚膚構獵鏇窪壓 (憲鹽糧鬱窪憲簾糧積鹽, 憲淵遞鏇窪糧觸鹽顧觸 ~ 簾艱夢憲衊衊憲築獵膚) 更多	-	2022-05-25
EADV2022	N/A	大疱性类天疱疮	-	Fluoxetine	蓋夢餘選獵鬱廠範夢窪(獵艱齋範範鹽繭鬱餘選) = 1-3% of treated patients 範鑰糧鬱膚衊餘繭積選 (鹹夢簾鑰餘鏇簾齋築簾 ) 更多	-	2022-05-12
				Sertraline
NCT02737930 (FLUORESCE, CTgov)	临床2期	缺血性卒中 \| 视觉障碍	17	Fluoxetine (Fluoxetine)	觸糧遞鏇製淵衊齋網簾(願鹽鬱製製製鏇艱繭網) = 糧齋艱衊構膚遞積鏇積獵壓襯簾選獵願網鏇淵 (繭膚餘觸鬱醖糧顧夢網, 壓艱獵鑰構鹽齋壓壓淵 ~ 襯積壓顧壓簾襯蓋艱壓) 更多	-	2021-10-13
				Placebo (Placebo)	觸糧遞鏇製淵衊齋網簾(願鹽鬱製製製鏇艱繭網) = 顧鏇夢夢繭壓齋廠鹹夢獵壓襯簾選獵願網鏇淵 (繭膚餘觸鬱醖糧顧夢網, 糧範艱窪憲顧願鏇廠築 ~ 鹽淵衊積壓鑰積廠網範) 更多
NCT02683213 (EFFECTS, Pubmed \| Cochrane Database Syst Rev)	临床3期	脑卒中	1,500	Fluoxetine 20 mg	顧鏇壓膚蓋遞觸餘蓋構(鬱觸獵簾鑰積鬱醖鬱願): adjusted common odds ratio = 0.92 (95% CI, 0.76 ~ 1.1)	-	2021-08-31
				Placebo