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更新于：2025-05-16
Enlicitide chloride
更新于：2025-05-16
概要
基本信息
非在研机构- |
权益机构- |
最高研发阶段临床3期 |
首次获批日期- |
最高研发阶段(中国)临床3期 |
特殊审评- |
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结构/序列
分子式C82H110ClFN14O15 |
InChIKeyCLOLWQCFULXMAR-DULRACIBSA-N |
CAS号2407527-16-4 |
Sequence Code 1142931824
来源: *****
关联
26
项与 Enlicitide chloride 相关的临床试验NCT06880874
A Clinical Study to Evaluate the Relative Bioavailability of Enlicitide Formulations in Healthy Adult Participants
The goal of the study is to learn what happens to different forms of enlicitide medications in a healthy person's body over time. Researchers will compare the amount of enlicitide in the healthy person's body over time when enlicitide is given in different formulations.
开始日期2025-04-02 |
申办/合作机构 |
NCT06719544
A Clinical Study to Evaluate the Effect of Enlicitide on the Pharmacokinetics of Lithium in Healthy Adult Participants
Researchers have designed a new study medicine called enlicitide decanoate (MK-0616) as a new way to lower the amount of low-density lipoprotein cholesterol (LDL-C) in a person's blood. Enlicitide decanoate will be called "enlicitide" from this point forward. Lithium (also called lithium carbonate) is a medicine used in bipolar disorder.
Researchers want to learn about lithium when taken at the same time with enlicitide.
They want to:
* Measure a person's blood to find out if the amount of lithium in the blood is the same when lithium is taken alone or with enlicitide
* Learn about the safety of lithium when taken alone or with enlicitide and if people tolerate it
Researchers want to learn about lithium when taken at the same time with enlicitide.
They want to:
* Measure a person's blood to find out if the amount of lithium in the blood is the same when lithium is taken alone or with enlicitide
* Learn about the safety of lithium when taken alone or with enlicitide and if people tolerate it
开始日期2025-01-02 |
申办/合作机构 |
NCT06643377
An Open-Label, Multiple-Dose Clinical Study to Evaluate the Pharmacokinetics of Enlicitide in Participants With Severe Renal Impairment
Researchers have designed a new study medicine called enlicitide decanoate as a new way to lower the amount of low-density lipoprotein cholesterol (LDL-C) in a person's blood. Enlicitide decanoate will be called "enlicitide" from this point forward, The purpose of this study is to learn what happens to enlicitide in a person's body over time (a pharmacokinetic (PK) study). Researchers will compare what happens to enlicitide in the body when it is given to people with severe renal impairment (meaning the kidneys do not work properly) and to people who are in good health. The researchers believe that the total amount of enlicitide in a person's body measured during the 24 hours after a dose will be similar in people with severe renal impairment and in healthy people.
开始日期2024-11-22 |
申办/合作机构 |
100 项与 Enlicitide chloride 相关的临床结果
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100 项与 Enlicitide chloride 相关的转化医学
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100 项与 Enlicitide chloride 相关的专利（医药）
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项与 Enlicitide chloride 相关的文献（医药）2025-12-01·Current Atherosclerosis Reports
Oral PCSK9 Inhibitors: Will They Work?
Review
作者: Catapano, Alberico L ; Pirillo, Angela ; Tokgözoğlu, Lale
PURPOSE OF REVIEW:
Lowering low-density lipoprotein cholesterol (LDL-C) is a crucial step in reducing the risk of atherosclerotic cardiovascular disease. Inhibitors of proprotein convertase subtilisin/kexin type 9 (PCSK9), an important regulator of circulating LDL-C levels, represent a modern approach for the treatment of hypercholesterolaemia. Approved approaches targeting PCSK9 to date include injectable biologics. Here, we provide an overview of the current state of research on the development of oral PCSK9 inhibitors.
RECENT FINDINGS:
Several small molecules have been developed in recent years. Enlicitide decanoate (formerly known as MK-0616) has been shown to significantly reduce LDL-C levels by a maximum of 66% from baseline with a good safety and tolerability profile. Its formulation with sodium caprate enabled a higher bioavailability. Several clinical trials are currently underway to evaluate the efficacy and safety of this drug, including an outcome trial. AZD0780 is another oral small molecule that lowers LDL-C levels by 52% and can be administered on top of a statin. Several other small molecules with the potential to inhibit PCSK9 have been identified, some of which have stopped the development. Oral PCSK9 inhibitors are showing promising results in early studies. If the results of the outcome studies will be positive, we will have a safe, effective and easy-to-use oral therapy. Oral PCSK9 inhibitors could provide a convenient alternative to injectable PCSK9 inhibitors and result in a greater number of patients receiving an effective LDL-C-lowering therapy.
2025-03-01·Atherosclerosis plus
Emerging oral therapeutic strategies for inhibiting PCSK9
Review
作者: Marodin, Giorgia ; Ferri, Nicola
Pharmacological inhibition of Proprotein Convertase Subtilisin/Kexin 9 (PCSK9) have been firmly established to be an effective approach to reduce low-density lipoprotein (LDL) cholesterol levels and cardiovascular events. Subcutaneous administration of monoclonal antibodies (evolocumab and alirocumab) every 2 or 4 weeks determined a 60 % reduction of LDL cholesterol levels, while the GalNac-siRNA anti PCSK9 (inclisiran) provided an effective lipid lowering activity (-50 %) after an initial subcutaneous dose, repeated after 3 months and followed by a maintenance dose every 6 months. Although these two approaches have the potentiality to bring the majority of patients at high and very-high cardiovascular risk to the appropriate LDL cholesterol targets, their cost and subcutaneous administration represent a strong limitation for their large-scale use. These problems could be overcome by the development of small chemical molecules anti PCSK9 as oral therapy for controlling hypercholesterolemia. In the present review, we summarized the pharmacological properties of oral anti PCSK9 molecules that are currently under clinical development (DC371739, CVI-LM001, and AZD0780), including the mimetic peptides enlicitide decanoate (MK-0616) and NNC0385-0434.
2025-02-01·TRENDS IN BIOCHEMICAL SCIENCES
From lead to market: chemical approaches to transform peptides into therapeutics
Review
作者: White, Andrew M ; Gare, Caitlin L ; Malins, Lara R
Peptides are a powerful drug modality with potential to access difficult targets. This recognition underlies their growth in the global pharmaceutical market, with peptides representing ~8% of drugs approved by the FDA over the past decade. Currently, the peptide therapeutic landscape is evolving, with high-throughput display technologies driving the identification of peptide leads with enhanced diversity. Yet, chemical modifications remain essential for improving the 'drug-like' properties of peptides and ultimately translating leads to market. In this review, we explore two recent therapeutic candidates (semaglutide, a peptide hormone analogue, and MK-0616, an mRNA display-derived candidate) as case studies that highlight general approaches to improving pharmacokinetics (PK) and potency. We also emphasize the critical link between advances in medicinal chemistry and the optimisation of highly efficacious peptide therapeutics.
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项与 Enlicitide chloride 相关的新闻（医药）2025-05-15
CVM（心血管及代谢），此词重量将堪比ADC、GLP-1。国内心血管疾病患者约3.3亿人、代谢性疾病患者约4.5亿人。据药融云，2018-2022年，中国心血管药物销售额市场规模保持在1450亿元左右。然而，这个超级市场一潭死水，长期被MNC和仿制药企盘踞。死水微澜，创新例外，国内创新药唯一接近百亿大单品，有望诞生于CVM，验证结构性增量逻辑成立。创新靶点成药，以及创新靶点进一步开发小分子药（口服优势）、小核酸药（超长效），让增量Buff拉满。Biotech在站稳肿瘤领域后，正挟创新靶点集体进军CVM。CVM市场将分层，保底层是集采仿制药，量大管饱，承担普惠的社会责任，中间层是口服创新药和次新靶点单抗药或多肽药，顶层是高价值的小核酸药、基因编辑疗法和全新靶点单抗药或多肽药。拿下中间层和顶层，Biotech将改变命运，享受慢病用药品牌依赖度高、生命周期长的红利。散发着腐烂气息的千亿江湖，因为鲶鱼涌入而重生。2023年主要降脂药品种价格梳理，初步呈现价格分层 资料来源：新康界，赛柏蓝，药智网，各药品说明书，华福证券研究所01 MNC凭老药霸屏依旧，仿制药拼老命只赚吆喝国内CVM慢病用药，曾经几乎被MNC垄断。据米内网，2021年中国城市实体药店终端降压药TOP10品牌市场份额、降糖药TOP10品牌市场份额、降脂药TOP10品牌市场份额，外企分别占9席、9席、6席。集采让原研药出局，打破药品阶层板结化？据米内网，2024年Q1-Q3重点省市公立医院终端高血压用药市场品牌TOP20中，外企占据15席；2024年中国零售药店终端糖尿病用药（化+生）品牌TOP20中，外企占据17席；2024年Q1-Q3中国零售药店终端内服血脂调节剂品牌TOP20中，外企占据7席。降压药、降糖药原研霸屏依旧，原研崇拜本质上是一种品牌依赖，客户粘度高，服用周期长，不会轻易中途换药。降脂药市场格局表面上受到国产集采品种的强劲冲击。据药智数据，阿托伐他汀钙片作为首批国家集采的血脂调节药大品种，在执行中标结果前的最后一个完整年度（2018年），在国内公立医疗机构的销售量为16.08亿片，辉瑞原研药为8.87亿片，占比55%，到2023年，阿托伐他汀钙片已增长至30.46亿片，辉瑞原研药为8.51亿片，占比降至28%。齐鲁制药勇夺阿托伐他汀钙片市场销量第一，销量占比47%，紧随其后的是乐普制药和东瑞制药（原兴安药业），销量占比分别为10%和9%。一看销售额，结局就反转。阿托伐他汀钙片2018年国内公立医疗机构销售额为105.01亿元，其中，辉瑞原研药占市场份额71%，集采之后，辉瑞市场份额不降反升，2023年达到83%。国产负责管饱，进口负责赚钱？然而，一旦涉及集采，终究没有赢家。CVM大品种被集采暴击，阿托伐他汀钙片销售额由2018年超100亿下滑至2020年不足55亿元；瑞舒伐他汀钙片由2018年超60亿元下滑至2021年不足25亿元；苯磺酸氨氯地平片由2018年近50亿元下滑至2020年不足23亿元。在CVM未被集采的领域，一个接近百亿元的大单品正冉冉升起。阿斯利康当家花旦达格列净（SGLT-2抑制剂），身披未被集采+原研战袍，据米内网，2024H1在国内三大终端六大市场的销售额接近35亿元，同比增长39.16%，按此趋势（据阿斯利康财报，达格列净全球销售额2024年同比增长31%，2025Q1同比增长16%），2025年或2026年将接近100亿元。达格列净被视为新型降糖药，其实不太新了，最早于2012年11月在欧洲批准上市，2017年3月在中国获批上市，到2022年，达格列净仍然占据国内SGLT-2药物82.6%的市场份额。整个CVM药物迭代缓慢。即使上市近30年，即使是被集采按在地上摩擦，他汀类药物仍是血脂异常治疗基石，据药智数据，2024年前三季度的样本医院血脂调节剂化药销售额中，阿托伐他汀钙片和瑞舒伐他汀钙片的占比超过50%。这一潭死水，体现为药物迭代缓慢，MNC凭借原研老药霸屏依旧，仿制药拼了老命只赚一个吆喝。是时候，来一群鲶鱼了。这群鲶鱼正是迅速崛起的创新药企。创新药大本营在港股，而港股跟踪创新药最权威的指数是HSHKBIO，恒生医药ETF（159892）是HSHKBIO指数下规模最大的ETF，最新规模达到约47亿元。今年以来（截至5月14日），HSHKBIO累计上涨26.35%，跑赢同期恒生科技指数。随着源头创新、差异化创新能力的增强，创新药是未来中国投资主线之一，不要错过这一历史机遇。由于对专业知识要求太高，港股医药投资，最稳妥的选择还是ETF基金（159892恒生医药ETF）。这只基金也有对应的场外基金(A类：016970；C类：016971)，费率在同类属于最低档水平，可供长期定投。02 国产创新靶点药物，冲击三大旧格局仿制药未竟的任务，将由国产创新药完成。如果非要给恒瑞医药的创新转型找一个拐点标志，当属2025年3月将Lp (a)口服小分子项目HRS-5346海外权益许可给默沙东，首付款2亿美元，交易总额19.7亿美元。这次BD令人全然耳目一新，不仅含新量远超恒瑞既往BD，而且在整个国产创新药出海事件中都属顶级水平，体现出恒瑞早研能力的巨大飞跃。这次BD不是发生于我们擅长的工程抗体领域，而是长期落后的CVM领域，更加意义非凡。对标海外大厂阿斯利康、罗氏的CVRM（心血管、肾脏及代谢疾病）业务线，信达生物搭建CVM领域全方位能力体系：降脂管线首个国产PCSK9单抗新进入国家医保目录生效；代谢管线玛仕度肽（GLP-1R/GCGR）——全球首个进入III期GLP-1R/GCGR双靶点减重药，预计2025年中获批；痛风管线替古索司他（XO抑制剂）美国II期数据疗效优异，海外II期和国内II期同时推进；降压管线小核酸药物AGT siRNA国内I期已启动。CVM三大旧格局将经受国产创新靶点药物冲击。代谢领域，以信达生物玛仕度肽为代表的GLP-1药物即将汹涌而至，围绕GLP-1升级，以来凯医药LAE102（ActRIIA单抗）为代表的早研药物，在增肌、增加能量消耗、停药不反弹的痛点上进行探索；降压领域，中国约有2.6亿高血压患者，且高血压控制率较低，仅为16%，AGT是RAAS通路的上游靶点，RNA疗法可沉默肝源性AGT基因表达，有望克服RAS逃逸，解决高血压治疗耐药和依从性差的问题，半年给药一次，国产8款靶向AGT小核酸药物已进入临床，包括舶望制药 BW-00163、圣因生物/信达生物SGB-3908、石药集团SYH2062、恒瑞医药HRS-9563、成都先衍生物LDR2402、昂拓生物ART101、施能康/华东医药SNK-2726、大睿生物RN1871；限于篇幅，今天分析重点为新型降脂药。降脂领域仍存较大未满足需求。任何一种他汀类药物剂量倍增时，LDL⁃C（低密度脂蛋白胆固醇）进一步降低幅度仅约6%，此所谓“他汀类药物疗效6%效应，即LDL-C疗效不足；部分患者存在他汀不耐受的情况，包括肝功能异常、他汀类药物相关肌肉并发症、新发糖尿病以及其他不良反应；脂蛋白(a)也称Lp(a)，Lp(a)水平的增加与心血管疾病风险的增加直接相关，其浓度几乎完全由遗传决定，传统降脂药物（如他汀类）作用有限。全球靶向PCSK9药物在研情况梳理 截至2025年2月PCSK9PCSK9蛋白与LDL-R直接结合，相较他汀类药物的间接作用，PCSK9抑制剂可以更精准地降低LDL-C水平，对他汀不耐受的血脂异常患者，或难治性高胆固醇血症患者，均有较好疗效，肝肾副作用也相对较小。PCSK9单抗可使LDL-C水平降低达50%~70%，每2周1次皮下注射，但“一辈子打针”的心理负担沉重，长期依从性不佳。安进依洛尤单抗（2015年上市）、赛诺菲/再生元阿利西尤单抗（2015年上市）2024年全球销售额分别为22.2亿美元、12.5亿美元，分别同比增长35.4%、14.7%，并没有成为超级爆款。PCSK9三个潜力方向或可期待。一是开发小核酸药物，诺华Leqvio是全球首款上市的siRNA降血脂药物，2024年全球销售额7.5亿美元，同比增长108.3%，能够强效持久降低LDL-C，长期达标率达80%，亚洲人群降幅高于PCSK9单抗，关键是一年仅需两针（第三个月加强针后）。阿斯利康反义寡核苷酸（ASO）AZD8233可显著降低PCSK9及LDL-C水平73%~79%，这是迄今为止报道的所有PCSK9靶向药物中可使LDL-C水平降低最高的药物。国内石药集团、悦康药业、瑞博生物、圣因生物均在开发PCSK9 siRNA。二是开发口服药物。默沙东MK-0616是全球首个口服PCSK9抑制剂，属于大环肽类药物，可阻断PCSK9蛋白和LDLR的结合，IIb期临床研究中30mg组降低LDL-C水平达60.9%，已推至临床III期。阿斯利康AZD0780是一种PCSK9小分子抑制剂，基于瑞舒伐他汀再用药，LDL-C水平下降52%（联用下降78%）。三是开发PCSK9基因编辑技术。通过CRISPR–Cas基因编辑技术可实现PCSK9的永久抑制，有望实现一次注射，终生降血脂。今年4月，信立泰从尧唐生物引进的靶向PCSK9碱基编辑药物YOLT-101临床试验申请获得受理。YOLT-101 IIT研究数据显示，4周时，高剂量组受试者LDL-C最高降幅近80%。Lp（a）Lp(a)作为降脂治疗的新靶点，全球暂无药物获批上市。在中国，约有20%人群的Lp(a)水平异常。目前全球约有13款用于降低Lp(a)水平的药物处于研发阶段，其中进展最快的3个项目均已进入III期临床试验，分别为ASO疗法诺华Pelacarsen，以及siRNA疗法安进Olpasiran、礼来Lepodisiran。今年3月，礼来长效siRNA疗法II期研究结果出炉，lepodisiran在最高剂量（400mg）下，使Lp(a)水平在治疗后60至180天期间平均降低93.9%，达到主要终点，其中一些患者的降低时间持续近1.5年。国内进展最快的为舶望制药siRNA药物BW-01，已进入II期临床。恒瑞医药、石药集团、信立泰、京新药业、靖因药业均在布局靶向Lp(a)药物。APOC3siRNA热门靶点之一，改善脂质紊乱的新途径，主要针对高甘油三酯血症及罕见疾病。瑞博生物RBD5044是全球第二个进入临床开发的APOC3 siRNA。Arrowhead Pharmaceuticals/维亚臻研发的APOC3 siRNA 药物Plozasiran（VSA001），2025年 3 月针对中国家族性乳糜微粒血症综合征（FCS）患者的 III 期临床试验获得积极顶线数据，成功达到主要疗效终点和所有关键次要终点。ANGPTL3主要针对他汀类药物无效的高甘油三酯血症和家族性混合型高脂血症，有望成为罕见遗传病患者的曙光，目前全球仅有一款药物获FDA批准上市。恒瑞医药SHR-1918是ANGPTL3靶向单抗药物，进入Ⅲ期临床。润佳医药/君实生物、Arrowhead Pharmaceuticals/维亚臻、诺华/舶望制药均在开发ANGPTL3 siRNA。CETP一度被视为心血管重要靶点，却成为MNC的坟场，辉瑞、罗氏、礼来和默沙东均受阻。现存在研药物仅4款，均为口服小分子，NewAmsterdam制药公司于2024年12月公布了ObicetrapibⅢ期BROADWAY试验的积极结果，或成为该靶点的破局者。在CVM创新靶点上，国内创新药与MNC不存在技术代差，部分甚至站在同一起跑线上。恒瑞医药、信达生物、信立泰已成为CVM领军企业，大量Biotech更是风起云涌，不仅分享国内千亿市场的增量机会，还将出现更多大型BD。
核酸药物抗体药物偶联物带量采购基因疗法
2025-05-08
·空之客
1整体表现AZN在去年底中国区高管被查导致的股价急跌后，随着业绩极其刚健的成长，又迅速回稳到$220b左右，从大趋势上仍延续着“戴维斯双击”的范式。一季度收入同比增长10%、EPS同比增长21%，与去年的超高增速相比，二阶导虽然有所回落，但在MNC中依然是靠前的水平；而且公司在肿瘤/心血管/呼吸/罕见病等板块、美/欧/中等市场的增长都较为均衡（即使是粗了大事的中国市场也保持着5%正增长），属于一眼看去没毛病的健康水平。全年指引基本维持不变，收入同比增长预计5-10%、EPS同比增长预计10-15%。2已上市产品分产品的增量来源将AZN的均衡性展露无遗，有5-10个产品都能贡献可观的增量，且都还没临近LOE，这就能够对未来相当长时间的增长提供支撑。AZN可以说这几年是扛起了肿瘤一哥的大旗，肿瘤板块坐拥五个以上的重磅品种，而且几乎都还有持续爬坡的潜力：Osimertinib在上市多年的情况下，在基于LAURA三期临床获批的针对III期不可切除NSCLC获批后，销售额仍在持续爬升，LTM累计已接近$6.7b，在这个卷疯了的适应症里展现出惊人的统治力；Durvalumab看似在PD-(L)1队伍中排不上号，但通过BTC/HCC/SCLC等差异化适应症，也不声不响爬到LTM累计$4.9b、增速保持在15%以上；Acalabrutinib与泽布替尼共同侵蚀着Ibrutinib的份额，特别是在1L CLL，LTM累计$3.2b，不过近一年与泽布替尼的差距在不断拉近，直至本季度正式被后者反超（$762m vs $792m）；Olaparib仍旧是PARP抑制剂中的带头大哥，加上MRK的部分LTM累计达到$4.4b；备受关注的Enhertu，主要其实是靠DS带飞，特别是在HER2 Low乳腺癌和泛肿瘤等适应症在美国市场获批和中国市场纳入医保目录后，近几个季度持续爬坡，单季度站上$1b大关，总算有点对得起ADC一哥的咖位。心血管板块就靠大腿Dapagliflozin的炸裂表现带飞，在心衰和CKD两大适应症获批后，销售额爬升姿态完全不似已经上市超过10年的老药，单季冲破$2b大关、LTM累计已接近$7.9b，在降糖领域已经有GLP-1这种毁天灭地大杀器存在的情况下依然十分耀眼。吸入制剂板块的Symbicort和Pulmicort等传统强势品种依然保持平稳，Breztri单季站上$300m、LTM累计突破$1b。自免板块虽然没有那么闪耀的超重磅品种，但也都还算有看点，特别是TSLP单抗Tezepelumab上市两年来爬坡势头不错，单季度$371m（加上Amgen部分）。在后新冠时代，传染病板块主要靠RSV，不过Nirsevimab上市后的体量还远不及预期，LTM累计$621m。收购Alexion得到的C5 franchise近期愈发不景气，gMG和PNH等重要适应症的竞争日趋激烈、再加上Part D的重拳，Ravulizumab增长明显遇到天花板，而Eculizumab在生物类似药上市后持续下滑，导致LTM累计销售额下滑到$6.4b，看起来跟当初$39b的收购对价渐行渐远；至于刚获批的TTR ASO产品Eplontersen，在ATTR-CM适应症之前估计销售额都还上不得台面。3在研管线Enhertu这个季度又取得了向一线迈进的关键进展，在三期临床DESTINY-Breast09试验的中期分析中，Enhertu联用Perjeta对照当前1L HER2+ BC的标准治疗方案“妥妥组合”（Taxane+Herceptin+Perjeta，THP），在PFS终点达到统计学显著性，OS虽未成熟但早期趋势也有利于Enhertu；此外，在针对高风险早期患者的新辅助治疗三期临床DESTINY-Breast11试验中，Enhertu联用THP对照标准新辅助治疗方案（剂量密集多柔比星+环磷酰胺联用THP，ddAC-THP），显著提升了病理完全缓解率（pCR），EFS虽未成熟但早期趋势也有利于Enhertu。口服SERD药物Camizestrant公布三期临床SERENA-6试验的中期分析，联用CDK4/6抑制剂治疗一线ESR1m HR+/HER2-乳腺癌患者，在PFS终点达到统计学显著性，这使得Camizestrant成为首个成功挤入一线的新一代口服SERD。心血管代谢板块也终于迎来了好消息，小分子PCSK9抑制剂AZD-0780公布了2b期临床PURSUIT试验结果，共入组428例患者，给药12周后，30/10/3/1mg剂量组与安慰剂组的LDL-c变化分别为-46.6%/-41.1%/-33.8%/-31.2%/+4.1%，，此外总胆固醇、non-HDL-c、ApoB等次要终点也均呈现剂量依赖性；安全性整体不错，SAE和停药比例都较低且与安慰剂组相当。这个结果其实是大超预期，毕竟之前一期只是在他汀基础上能额外带来50%获益而已；然而对比此前的口服多肽PCSK9结果，例如MK-0616（30mg组-60.9%）和已终止开发的NN-6435（100mg组-61.8%），又显得略逊一筹。这大概就能解释为何要急吼吼地引入石药的小分子Lp(a)，把联用作为与MRK拼一拼的退路了。去年$1.05b从Amolyt买来的PTH1激动剂Eneboparatide终于公布了三期临床结果，针对成人慢性甲状旁腺功能减退患者，在24周达到首个主要临床终点，包括调节血钙水平、降低对维生素D和口服钙的依赖。TSLP单抗Tezepelumab在NEJM发表了三期临床WAYPOINT试验的完整结果，针对408例CRSwNP患者，Tezepelumab与安慰剂相比，52周鼻息肉总评分NPS和周平均鼻塞评分NCS都有显著改善，患者的嗅觉、鼻窦病变、生活质量得到显著改善，NP手术或SCS需求得到显著降低。该适应症的上市申请已提交。有趣的是，AZN果断割掉了一批神经领域的临床管线，包括偏头痛、骨关节痛、阿尔茨海默症等，并关闭神经部门，明确要把临床资源让位于减重、血脂调控、呼吸、免疫等更有价值的领域。针对减重市场以及中国从业者普遍关注的诚益ECC-5004，被问及怎么看近期竞争对手的数据，AZN的态度却略有些微妙：明确了“小分子GLP-1需要与SGLT-2联用”的定位，而且主要聚焦“BMI>35”的市场，再结合这张CVRM领域的R&D highlights图从去年三季报之后再没出现过，多多少少有点向Orforglipron认怂的意思。除此以外，还值得关注的进展包括：Durvalumab获批MIBC适应症、公布早期胃癌围手术期三期临床结果，AKT抑制剂Capivasertib联用多西他赛+去势治疗的三期临床CAPItello-280试验失败等。回顾AZN整个管线的布局，减重、ADC、核药、TCE、CAR-T等一众热门方向都有覆盖，以至于对于去年公司发下的2030年$80b收入宏愿，有分析师认为可能过于保守，把Pascal都给整不会了……虽然这个季度增速有所放缓，但AZN仍然是产品梯队和管线布局最硬核的大药企，特别是在近十年的重大战略决策上几乎可谓算无遗策，打造出布局极其均衡全面的格局，包括各个适应症领域、各新兴技术方向、各主要地区市场，都把握住了历史级的机遇。如果将公司的战略拟人化，AZN这种气度颇有武侯之风，与贾诩这等以奇谋毒计立身之辈不同，诸葛平生不弄险，堂堂之阵依法进兵，又何忧不胜呢？阿斯利康AZN往期季报分析：【医苑观畴】主流技术方向谁说了算：2022年上半年全球大药企核心产品管线进展总览【医苑观畴】主流技术方向谁说了算：2022年下半年全球大药企核心产品管线进展总览【医苑观畴】2023年上半年全球大药企核心进展总览【医苑观畴】2024年一季度海外药企进展更新：阿斯利康AZN【医苑观畴】2024年二季度海外药企进展更新：阿斯利康AZN
临床3期抗体药物偶联物引进/卖出临床结果
2025-05-08
LEQVIO marks a significant advancement in hypercholesterolemia management, particularly for patients not achieving target LDL-C levels despite maximally tolerated statin therapy. As the first FDA-approved siRNA therapy for LDL-C reduction, it introduces a novel mechanism of action with sustained efficacy and biannual dosing, enhancing patient adherence.
LAS VEGAS, May 8, 2025 /PRNewswire/ -- DelveInsight's "
LEQVIO Market Size, Forecast, and Market Insight Report" highlights the details around LEQVIO, which is a PCSK9 Inhibitor. The report provides product descriptions, patent details, and competitor products (marketed and emerging therapies) of LEQVIO. The report also highlights the historical and forecasted sales from 2020 to 2034 segmented into 7MM [the United States, the EU4 (Germany, France, Italy, and Spain), the United Kingdom, and Japan].
Novartis/Alnylam Pharmaceuticals' LEQVIO (inclisiran) Overview
LEQVIO (inclisiran) is a first-of-its-kind therapy developed by Novartis based on small interfering RNA (siRNA) technology. It targets the mRNA of PCSK9 (proprotein convertase subtilisin/kexin type 9), reducing the production of this protein in the liver. Unlike traditional treatments, LEQVIO lowers LDL-C levels by enhancing the liver's ability to absorb and eliminate it from the bloodstream.
In the US, LEQVIO is approved for use alongside diet and statin therapy in adults with primary hyperlipidemia, including those with heterozygous familial hypercholesterolemia (HeFH), to help reduce low-density lipoprotein cholesterol (LDL-C).
The recommended LEQVIO dosage is 284 mg, given via subcutaneous injection initially, followed by a dose at 3 months, and then every 6 months thereafter, in combination with statins. In 2034, the market size of inclisiran is expected to be
USD 2.2 billion in the US.
Learn more about LEQVIO projected market size for PCSK9 inhibitors @
LEQVIO Market Potential
Proprotein convertase subtilisin/kexin type 9 (PCSK9) is a serine protease essential to cholesterol metabolism, primarily by controlling the breakdown of low-density lipoprotein (LDL) receptors. This mechanism decreases the removal of LDL particles from the blood, thereby influencing LDL cholesterol (LDL-C) levels. There is an inverse relationship between PCSK9 activity and LDL-C levels: gain-of-function mutations in the PCSK9 gene lead to increased LDL-C and a higher cardiovascular risk, as seen in familial hypercholesterolemia, while loss-of-function mutations are associated with lower LDL-C levels and reduced atherosclerotic cardiovascular disease (ASCVD) risk. In 2023, approximately
640,000 cases of familial hypercholesterolemia were diagnosed across the 7MM, with homozygous forms being extremely rare.
PCSK9 inhibitors have emerged as a vital therapeutic option for hypercholesterolemia management, especially for patients at elevated cardiovascular risk or those unresponsive to standard treatments like statins. These drugs inhibit PCSK9, a protein that promotes LDL receptor degradation. By blocking PCSK9, these therapies enhance the presence of LDL receptors on liver cells, improving LDL-C clearance from the bloodstream. According to DelveInsight, the PCSK9 inhibitor market in the 7MM was valued at
USD 2 billion in 2023.
In summary, the PCSK9 inhibitor market is projected to witness substantial growth, driven by their use in statin-intolerant patients, expanding applications of PCSK9 inhibition, potential in broader therapeutic areas, and their role in preventive strategies to help reduce the overall cardiovascular disease burden.
Discover more about the PCSK9 inhibitors market in detail @
PCSK9 Inhibitors Market Report
Emerging Competitors of LEQVIO
Several drugs are currently under development in the PCSK9 inhibitor pipeline, including
Lerodalcibep (LIB Therapeutics),
MK-0616 (Merck),
VERVE-101 and VERVE-102 (Verve Therapeutics), and
CiVi 008 (CiVi Biopharma), among others.
Lerodalcibep is a third-generation PCSK9 inhibitor designed to overcome the limitations of traditional LDL-C-lowering therapies like statins and ezetimibe. It aims to help patients reach the more aggressive LDL-C targets recommended by recent cardiovascular guidelines. The drug is being developed as a once-monthly, low-volume injection with long shelf stability at room temperature. Currently in Phase III clinical trials, LIB Therapeutics intends to file a Biologics License Application (BLA) by year-end, with a potential PDUFA decision expected in the latter half of 2025.
MK-0616, an oral PCSK9 inhibitor from Merck, is a novel macrocyclic peptide that blocks the interaction between PCSK9 and LDL receptors, thus reducing LDL cholesterol. It is currently in Phase III trials and could become the first oral treatment in its class.
Verve Therapeutics is advancing two gene-editing candidates—
VERVE-101 and VERVE-102—targeting PCSK9. These one-time treatments are designed to permanently switch off the PCSK9 gene in the liver, thereby lowering LDL-C levels. VERVE-102 is being evaluated in the Heart-2 Phase Ib trial for patients with heterozygous familial hypercholesterolemia (HeFH) or early-onset coronary artery disease. Meanwhile, enrollment in the Heart-1 trial for VERVE-101 has been paused due to lab abnormalities, and an investigation is ongoing. Based on the results, Verve will work with regulators to decide the next steps for VERVE-101. The company plans to initiate a randomized, placebo-controlled Phase II trial based on data from both the Heart-1 and Heart-2 studies.
As these next-generation therapies move closer to approval, they have the potential to significantly disrupt and redefine the PCSK9 inhibitor market, ultimately giving fierce competition to LEQVIO.
To know more about the number of competing drugs in development, visit @
LEQVIO Market Positioning Compared to Other Drugs
Key Milestones of LEQVIO
In
July 2023, the US FDA approved an expanded indication for Novartis LEQVIO to include treatment of adults with high LDL-C and who are at increased risk of heart disease. The updated indication for primary hyperlipidemia allows for the expanded use of LEQVIO as an adjunct to diet and statin therapy beyond the previously approved ASCVD and HeFH patient populations.
In
2023, LEQVIO (inclisiran) was approved by MHLW for familial and non-familial hypercholesterolemia and for patients who are at a high risk of developing cardiovascular events.
In
August 2022, Novartis selected Soleo Health as a Limited Drug Distribution Partner for the Administration of LEQVIO. Under this partnership, Soleo Health will administer the drug to patients in their homes or at one of the Company's Ambulatory Infusion Centers (AICs) in the US.
In
2021, Novartis reached an agreement with the National Health Service (NHS) in England to implement a first-of-its-kind population health management approach designed to provide faster and broader access to LEQVIO for certain high-risk patients with ASCVD.
In
December 2020, Novartis announced that the European Commission (EC) approved LEQVIO to treat adults with hypercholesterolemia or mixed dyslipidemia, two common forms of elevated cholesterol.
Discover how LEQVIO is shaping the PCSK9 inhibitors treatment landscape @
LEQVIO Injection
LEQVIO Market Dynamics
LEQVIO, as a first-in-class
small interfering RNA (siRNA) that helps maintain bad cholesterol levels and improve mortality rates, strengthens its market position with a
value-based price per dose and promising market access and reimbursement. Ongoing trials for
CVRR and Pediatric Hyperlipidemia expansion pave the way for label expansion, addressing diverse medical needs. The
escalating patient population presents a favorable trend for expanding LEQVIO's market reach and driving growth.
However, its market is currently
constrained by its specific indication for HeFH in adults, potentially limiting its reach compared to competitors like
REPATHA and PRALUENT, which are approved for both HoHF and HeHF in adults and pediatrics. The market is expected to face
heightened competition post-2027, which may impact LEQVIO's market share, and similar
annual treatment costs across PCSK9 inhibitors may pose a challenge, affecting LEQVIO's competitive edge despite better reimbursement policies.
Dive deeper to get more insight into LEQVIO's strengths & weaknesses relative to competitors @
LEQVIO Market Drug Report
Table of Contents
Related Reports
PCSK9 Inhibitor Market
PCSK9 Inhibitor Market Size, Target Population, Competitive Landscape & Market Forecast – 2034 report deliver an in-depth understanding of the disease, historical and forecasted epidemiology, as well as the market trends, market drivers, market barriers, and key PCSK9 inhibitor companies, including
LIB Therapeutics, Merck, Verve Therapeutics, CiVi Biopharma, among others.
PCSK9 Inhibitors Pipeline
PCSK9 Inhibitors Pipeline Insight – 2025 report provides comprehensive insights about the pipeline landscape, pipeline drug profiles, including clinical and non-clinical stage products, and the key PCSK9 inhibitors companies, including
Ionis Pharmaceuticals, Akeso Biopharma, Amgen, Novo Nordisk, Civi BioPharma, among others.
Hypercholesterolemia Market
Hypercholesterolemia Market Insights, Epidemiology, and Market Forecast – 2034 report delivers an in-depth understanding of the disease, historical and forecasted epidemiology, as well as the market trends, market drivers, market barriers, and key hypercholesterolemia companies, including
Novartis Pharmaceuticals, Merck Sharp & Dohme LLC, Esperion Therapeutics, Inc., Arrowhead Pharmaceuticals, LIB Therapeutics LLC, Medpace, Inc., AstraZeneca, NewAmsterdam Pharma, among others.
Homozygous Familial Hypercholesterolemia Market
Homozygous Familial Hypercholesterolemia Market Insights, Epidemiology, and Market Forecast – 2034 report delivers an in-depth understanding of the disease, historical and forecasted epidemiology, as well as the market trends, market drivers, market barriers, and key homozygous familial hypercholesterolemia companies, including
Arrowhead Pharmaceuticals, Novartis, Alnylam Pharmaceuticals, LIB Therapeutics, among others.
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100 项与 Enlicitide chloride 相关的药物交易
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 动脉粥样硬化 | 临床3期 | 美国 | 2023-10-09 | |
| 动脉粥样硬化 | 临床3期 | 美国 | 2023-10-09 | |
| 动脉粥样硬化 | 临床3期 | 中国 | 2023-10-09 | |
| 动脉粥样硬化 | 临床3期 | 日本 | 2023-10-09 | |
| 动脉粥样硬化 | 临床3期 | 日本 | 2023-10-09 | |
| 动脉粥样硬化 | 临床3期 | 阿根廷 | 2023-10-09 | |
| 动脉粥样硬化 | 临床3期 | 阿根廷 | 2023-10-09 | |
| 动脉粥样硬化 | 临床3期 | 澳大利亚 | 2023-10-09 | |
| 动脉粥样硬化 | 临床3期 | 澳大利亚 | 2023-10-09 | |
| 动脉粥样硬化 | 临床3期 | 巴西 | 2023-10-09 |
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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 |
|---|
临床1期 | 18 | (Panel A - Moderate Renal Impairment (RI)) | 遞網膚繭淵積鬱鹽簾觸(鹹願膚夢鏇憲構夢衊襯) = 夢願範繭鏇齋繭構鏇鑰 餘鹽網簾餘鹽積艱範蓋 (選積顧廠廠構鬱遞艱願, 醖鹹鹽襯糧蓋選範膚鑰 ~ 鏇鏇夢淵夢願遞蓋網觸) 更多 | - | 2024-09-26 | ||
(Panel B - Healthy Controls) | 遞網膚繭淵積鬱鹽簾觸(鹹願膚夢鏇憲構夢衊襯) = 築糧醖醖糧選窪壓蓋糧 餘鹽網簾餘鹽積艱範蓋 (選積顧廠廠構鬱遞艱願, 願鹽艱淵選選顧鹹顧鑰 ~ 網鏇獵範憲遞積選構獵) 更多 |
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