Effectiveness and Safety of Bempedoic Acid in Combination With Ezetimibe and Either Rosuvastatin or Atorvastatin in Patients With Primary Hypercholesterolemia or Mixed Dyslipidemia: an Observational Study

Data on the real-world use and effectiveness and safety of bempedoic acid combined with both a statin and ezetimibe in clinical practice is limited. There is an increased focus on using combination therapy to lower LDL-C.

开始日期2025-03-03

申办/合作机构

Daiichi Sankyo Europe GmbH

DRKS00034752 / RecruitingN/AIIT

Combination therapy with Oral Bempedoic Acid to reach LDL-CholesterolTargets (COBALT) - a real-world secondary prevention setting study - COBALT

开始日期2024-10-23

申办/合作机构-

CTRI/2024/07/070838 / Not yet recruiting临床4期IIT

A Comparative study to evaluate the efficacy and safety of Bempedoic acid versus Ezetimibe in patients with Dyslipidemia - NIL

开始日期2024-08-01

申办/合作机构-

100 项与贝派地酸相关的临床结果

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100 项与贝派地酸相关的转化医学

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100 项与贝派地酸相关的专利（医药）

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299

项与贝派地酸相关的文献（医药）

2024-12-01·Atherosclerosis plus

Efficacy and safety of lipid-lowering therapies in combination with or without statin to reduce the cardiovascular risk: A systematic review of randomised controlled trials

Review

作者: Dongare, Shirish ; Jawla, Shantanu ; Kamboj, Geetank ; Barman, Parinita ; Iannuzzo, Gabriella

Background and aims:

Cardiovascular diseases (CVD) pose a significant global health burden. Lowering low-density lipoprotein-cholesterol is the primary therapeutic aim for preventing primary and secondary CVD events. While statins are the standard treatments, their limitations, such as side effects and intolerance in certain patient groups, necessitate exploration of alternative lipid-lowering therapies (LLTs). We systematically reviewed randomised controlled trials (RCTs) evaluating cardiovascular outcomes associated with non-statin LLTs (bempedoic acid, alirocumab, evolocumab, ezetimibe, and inclisiran) in adults with CVD or high cardiovascular risk.

Methods:

EMBASE, Medline, Cochrane Library, and clinical trial registries were systematically searched for eligible studies, from inception until February 08, 2023. Two reviewers independently screened the studies, with discrepancies resolved by a third reviewer. Data extraction and validation were conducted, and the risk of bias was assessed using the Cochrane Risk-of-Bias tool-2 for RCTs.

Results:

The search strategy yielded 2104 citations. Post screening for eligibility, nine unique trials/studies (84 publications) were identified. Among these, one trial each was identified for bempedoic acid and alirocumab, three for evolocumab, and four for ezetimibe. No published literature documenting the cardiovascular outcomes of inclisiran was identified. Only one trial (CLEAR Outcomes) included statin-intolerant patients at baseline. Most studies evaluated a 3-component, 4-component, or 5-component major adverse cardiovascular events composite as an outcome along with individual components. The quality of the included trials was found to be fair-to-good.

Conclusions:

The systematic review findings emphasise the significance of considering non-statin LLTs as viable treatment options for individuals with CVD or high cardiovascular risk who cannot tolerate or achieve optimal lipid control with statin therapy alone.

2024-12-01·Expert Opinion on Drug Metabolism & Toxicology

Drug interactions in cardiology: focus on statins and their combination with other lipid-lowering drugs

Review

作者: Bellosta, Stefano ; Corsini, Alberto

INTRODUCTION:

Statins are the primary therapeutic approach for treating hypercholesterolemia in hyperlipidemic high cardiovascular-risk patients, as stated by the recent European and American guidelines. However, in some patients, statin treatment is not sufficient to achieve the recommended plasma LDL-C levels, and the addition of a second hypolipidemic drug becomes mandatory. Concomitant administration of multiple medications may increase the risk of adverse events, potentially leading to statin-associated muscle or liver symptoms and non-adherence or discontinuation of statin therapy, such as in women. The addition of a second hypolipidemic drug (such as ezetimibe, anti-PCSK9 monoclonal antibodies, bempedoic acid, and inclisiran) may lead to drug-drug interactions (DDIs). The evaluation of the different pharmacokinetic profiles may improve and personalize the treatment.

AREAS COVERED:

We aimed to give an update on the potential DDIs between statins and other hypolipidemic drugs currently used to treat high-risk hyperlipidemic patients.

EXPERT OPINION:

It is fundamental to understand the risk associated with DDIs to manage better the addition of a concomitant hyperlipidemic drug to a statin-treated patient. Many health agencies have published specific guidelines for assessing DDIs, but these mainly apply to in vitro studies. New predictive approaches are being proposed and may help evaluate and manage DDIs.

2024-12-01·Current Atherosclerosis Reports

Ezetimibe: Integrating Established Use with New Evidence - A Comprehensive Review

Review

作者: Xie, Sining ; Scotti, Stefano ; Olmastroni, Elena ; Galimberti, Federica ; Casula, Manuela

PURPOSE OF REVIEW:

To consolidate key information on the efficacy and safety of ezetimibe, with a focus on the latest evidence.

RECENT FINDINGS:

While ezetimibe has long been used alongside statins to help achieve lipid goals when statins are insufficient or in statin-intolerant patients, recent studies confirm and extend its benefits. Ezetimibe, when added to statins, is now recognized as an effective option for high-risk cardiovascular patients. Additionally, for those intolerant to statins, it can be combined with bempedoic acid, offering significant LDL cholesterol reduction. Ezetimibe's favourable tolerability, with fewer side effects than statins, along with the availability of fixed-dose combinations, enhances both treatment efficacy and patient adherence. Overall, this review underscores ezetimibe's evolving role in lipid management, providing valuable guidance for optimizing cardiovascular risk reduction strategies.

项与贝派地酸相关的新闻（医药）

2024-11-26

·医药观澜

大冢制药6000万美元首付款引进！降脂新药在日本申报上市

▎药明康德内容团队报道今日（11月26日），大冢制药（Otsuka）宣布向日本厚生劳动省提交bempedoic acid的新药申请（NDA），拟用于治疗高胆固醇血症和家族性高胆固醇血症。Bempedoic acid是一种“first-in-class”三磷酸腺苷（ATP）柠檬酸裂解酶抑制剂，可在不耐受他汀类药物治疗的患者中降低胆固醇。此前该产品曾入选美国克利夫兰诊所（Cleveland Clinic）评选出的《2020年度十大医疗创新》榜单。 Bempedoic acid由Esperion Therapeutics开发，具有一种新的作用机制。2020年4月，大冢制药从Esperion获得了该产品在日本的独家开发和商业化权利。大冢制药将一次性向Esperion公司支付6000万美元，并根据开发和销售目标的实现支付里程碑付款。 ATP柠檬酸裂解酶是肝脏胆固醇合成过程中的的关键蛋白酶。通过抑制ATP柠檬酸裂解酶，bempedoic acid能够降低肝脏中LDL-C的合成，引发LDL受体（LDL-R）的表达水平上升。LDL受体水平的升高导致血液中更多的LDL-C能够被清除，降低血液中的LDL-C水平。 2020年2月，美国FDA批准bempeoic acid上市，作为饮食和最大耐受剂量他汀疗法的辅助疗法，治疗杂合体家族性高胆固醇血症成人患者，或者需要进一步降低LDL-C的动脉粥样硬化性心血管疾病患者。彼时新闻稿指出，该产品为高胆固醇患者提供了一种非他汀类的口服降胆固醇疗法。今年3月，FDA还批准该产品扩展适应症，用于在一级预防和二级预防群体中降低心血管疾病风险和进一步降低LDL-C。根据大冢制药新闻稿介绍，一项在日本开展的3期试验纳入96例他汀类药物疗效不足或不能耐受的高LDL胆固醇患者，试验参与者被给予180mg bempedoic acid或安慰剂，每天一次，持续12周，以评估bempedoic acid的疗效和安全性。在第12周，主要终点LDL-C从基线变化的百分比于bempedoic acid治疗组为-25.25%，在安慰剂组为- 3.46%，试验组与安慰剂相比显示出积极的结果，具有统计学意义。此外，bempedoic acid的安全性和耐受性与先前的试验结果一致，没有观察到严重的不良事件。高胆固醇患者通常会使用他汀类药物进行治疗。然而，并非所有人对这一类疗法都能耐受，部分患者接受他汀类药物会导致严重的肌肉疼痛，还有一些高胆固醇血症患者即使服用他汀类药物也无法达到目标值（对他汀类药物反应不足）。Bempedoic acid为这类病人提供了可选择的替代疗法，这类药物在降低患者胆固醇的同时，还能避免他汀类药物肌肉疼痛的副作用。参考资料： [1] Otsuka Submits New Drug Application in Japan for Bempedoic Acid in the Treatment of Hypercholesterolemia. Retrieved Nov 26，2024, From https://www.otsuka.co.jp/en/company/newsreleases/2024/20241126_1.html [2]Otsuka Enters into Licensing Agreement in Japan for Bempedoic Acid, a Treatment for Hypercholesterolemia. Retrieved Apr 20，2020, from https://www.otsuka.co.jp/en/company/newsreleases/2020/20200420_1.html 本文来由药明康德内容团队根据公开资料整理编辑，欢迎个人转发至朋友圈。转发授权及其他合作需求，请联系wuxi_media@wuxiapptec.com。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。

上市批准临床3期

2024-11-16

·动脉网

超50亿里程碑到账，中国创新药正在告别“一次性”BD

虽然市场当前仍处于寒冬，但总有人在悄悄变富。 10月31日，和黄医药发布公告，因呋喹替尼用于治疗转移性结直肠癌的销售额超过2亿美元，按照协议，和黄医药将收到武田2千万美元里程碑付款。事实上，这并不是和黄医药第一笔里程碑到账，2023年11月，因呋喹替尼在美正式获批上市，和黄医药还收到武田3500万美元里程碑付款。图1.中国创新药企业2024年部分里程碑事件（数据来源：公开资料）接连达成两笔里程碑，这并不容易，但和黄医药并非个例。10月23日，诚益生物宣布收到阿斯利康6000万美元里程碑付款，此次里程碑由小分子GLP-1受体激动剂ECC5004/AZD5004完成2b期临床首例患者给药触发。如果将时间再往前推，包括科伦药业、百奥泰、百奥赛图、金斯瑞生物、亿帆医药、和铂医药、亚盛医药等也在今年相继收到了里程碑付款，总到款金额现已超过7亿美元。这绝对是难以见到的一幕，虽然在近一两年，天价BD及超高额首付款频出，但作为后续款项，里程碑付款披露相对较少。而随着当前一笔又一笔里程碑到账，这是否意味着，中国医药行业“只见首付款，不见里程碑”的时代已经成为过去式？ 01 半年大卖10亿，和黄医药如何躺赢？在BD浪潮的推动下，不少创新药企业都借此实现了扭亏为盈，这其中的典型代表就有和黄医药。根据年报显示，2023年和黄医药收入和净利润分别为8.38亿美元和1.01亿美元，收入同比增长97%，利润较2022年则是扭亏为盈。值得一提的是，这是和黄医药2021年登陆港交所后首次实现盈利，同时也是其五年来首度扭亏。这当然离不开旗下首款创新药品呋喹替尼的成功“出海”。2023年1月，和黄医药正式将呋喹替尼中国之外的全球权益授予武田，交易总额最高可达11.3亿美元，这一度刷新了中国小分子新药出海授权的交易纪录。不过，和黄医药最初能拿到的只有首付款4亿美元，但即便如此，这也占据了和黄医药整个2023年营收的一半，是其实现盈利的关键所在。到这里，其实与当前大多数创新药企业扭亏为盈的逻辑相似，主要依靠“天价BD+超高额首付款”，但和黄医药不同的是，它并没有将其作为一次性收入，而是在持续挖掘这笔交易的变现潜力，在不到一年的时间里，已先后获得两笔里程碑付款。并且这可能还只是开始，根据呋喹替尼的市场预期，其海外销售峰值将有望超过15亿美元，这意味着，和黄医药的好日子还在后头，未来还将继续躺赢。那么，原因是为何呢？首先一点当然是在于呋喹替尼的产品力。事实上，呋喹替尼是由和黄医药与礼来共同研发，2013年，双方签订合作协议，礼来获得呋喹替尼的国内权益，并负责产品的大部分开发成本。而借力礼来，呋喹替尼最终在2018年9月获批国内结直肠癌三线治疗，并成为首个获批用于治疗转移性结直肠癌的创新靶向疗法。在这之后，呋喹替尼开始崭露头角，到2023年，其在国内市场销售额就已超过1亿美元，并且市场份额极高，在三线经治患者中的占有率达47%。不过受医保降价等因素影响，呋喹替尼近一两年虽然营收不断增加，但增速放缓明显，而与武田的合作，又为其打开了新的增长阀门。一方面是在获批进度上，2023年11月呋喹替尼正式登录美国市场，今年6月和9月，呋喹替尼又先后在欧盟和日本获批，现已成为上海首个且目前唯一一个成功出海美、欧、日三大标杆市场的中国原创新药。图2.呋喹替尼销售情况另一方面是在变现速度上。呋喹替尼在美正式登陆以后，市场定价为每盒25200美元，这是中国定价的20倍以上。即便如此，呋喹替尼的销量并未受任何影响，反倒呈爆发式增长，在美上市48小时内就开出首张处方，不到2个月后，呋喹替尼在美销售额就已达到0.15亿美元。今年上半年，呋喹替尼又收入1.51亿美元，这与呋喹替尼2023年在中国市场的全年销售额相当。而在这个快速推进的过程中，武田当然功不可没，事实上，受制于多款重磅药品专利到期影响，武田正需要新鲜血液来补充，所以对于呋喹替尼的推动格外卖力，包括助力海外审批，以及加速市场渠道拓展等等。而借力武田，呋喹替尼市场份额正不断扩大，这意味着后续里程碑将逐步解锁，和黄医药未来还会有更多款项到账。 01 22%兑现率，容易生变的里程碑付款和黄医药只是一个缩影，它代表的是一种“销售阶段的里程碑付款”，而这也正在成为中国创新药出海的一种典型模式，即“借船出海”。不过，里程碑并非只有市场指标，研发进度以及产品获批等重要节点同样包含在内。以科伦药业为例，今年2月，因正式启动Trop2 ADC新药SKB264（MK-2870）三项全球关键三期临床，其收到默沙东支付的7500万美元里程碑付款。另外还有金斯瑞生物，今年6月，其全资子公司传奇获得总计4.1亿美元里程碑付款，触发节点来源于授权产品西达基奥仑赛开发进展显著。图3.2024年1-11月中国创新药TOP10 BD交易情况事实上，诸如此类的“研发进展式里程碑”还有很多，并且都有望在未来批量兑现。据动脉网不完全统计，在中国药企今年已完成的近50笔BD交易中，Ⅰ期临床及之前占比超过80%。在这其中不乏大额合作，比如刚刚敲定的一笔总价32.88亿美元的BD合作，默沙东引进礼新医药的PD-1/VEGF双抗LM-299就正处于Ⅰ期临床；另外还有今年年初诺华与舶望签订的41亿美元的重磅BD，同样是基于一款Ⅰ期临床项目。而根据里程碑付款计划来看，其都有很大可能在未来1-2年内到手多笔里程碑款项。图4.生物制药领域2023年年中到期的各研发阶段里程碑事件达成情况（图源：研发客）当然，这只是理性化估计，虽然当前里程碑到账愈发增多，但不可忽略的事实是，里程碑的不确定性仍然较大，尤其是随着交易项目不断往后推进，涉及到的争议或潜在争议也会逐渐凸显，而这都会对里程碑的兑现产生直接影响。根据2023年的数据显示，生物制药并购交易中里程碑的实现率仅为22%，至于实现里程碑所触发的金额则更少，能够拿到的里程碑金额仅为总金额的3%。那么，里程碑到底卡在哪了呢？首先第一点当然是未触发里程碑，包括临床研究失败、产品迟迟未获批以及市场销售不达预期等。事实上，在生物医药领域的BD交易中，里程碑的设置本身就是为了对冲最终产品研发或上市失败的风险，而从过往众多退货案例来看，这一种情形的发生较为普遍，核心原因主要是交易产品本身并不过硬。图5.GSK与万泰生物约定的里程碑付款计划其次是里程碑界定不明，这在后续的履约环节中同样容易产生纠纷。以Esperion与第一三共的解约为例，2019年，第一三共以1.5亿美元和最高9亿美元里程碑付款，获得Esperion两款复方制剂在欧洲等地区的独家商业化权益。2022年12月，Nexletol扩展适应症的Ⅲ期临床CLEAR Outcomes达到主要终点MACE-4（注：MACE-4包含心脏病发作在内的脑中风、心血管死亡以及冠状动脉血运重建四种心血管发作风险。）目标，Esperion认为按照合作协议，其将收到3亿美元里程碑付款。但第一三共表示拒绝，认为如果触发里程碑付款，MACE-4风险应至少降低15%，目前这一数据为12.98%，差了2％。当然，Esperion也有说辞，认为其达到了协议中的终点目标，即Nexletol将心脏病发作风险率降低了27%。所以，双方分歧的焦点实际上是在于两家公司在协议条款中对试验终点的界定不清晰，到底是概指所有心血管事件风险，还是特指心脏病发作风险，这在早期协议中显然没有明确说明。最后一点是战略调整，即买方根据市场情况变化而选择主动终止合作。以诺华“退货”百济PD-1为例，虽然在退货之前，PD-1刚在欧洲获批，同时在美国FDA的上市申请也获得受理，但诺华仍然选择忍痛割爱，核心原因就是市场竞争格局已经发生突变，2023年“K药”适应症已经超过45个，成为新的全球药物。而作为竞争对手，诺华暂避锋芒、及时止损无疑不是一个好的选择。另外还有默沙东近期接连终止与科伦博泰的两项临床前ADC合作，关键原因同样是因为市场格局变化，目前正在开发的Claudin18.2 ADC药物已接近10款，并且三家公司已经启动三期临床试验，默沙东的SKB315显然不占临床进度优势，未来也很难弯道超车。对此，某资深BD负责人谈道，“相比于实实在在能拿到的首付款，里程碑在BD交易中的获取难度的确很大，这是因为其中掺杂的因素众多，除产品因素外，市场环境以及产业变化都会对其造成直接影响。因此，越是面对那些看起来数字大的天价交易，越应该保持清醒的头脑，不仅要关注交易总额，更要关注交易中能够真正落袋为安的数额是多少，这才是BD交易的关键。” 03 断崖式下滑，BD不能只停留于解“燃眉之急” 首付款也好，里程碑也好，近年来都已经成为推动一些创新药企业业绩增长的重要引擎，并且靠其翻身、扭亏为盈的也不在少数，包括恒瑞医药、亚盛医药、百利天恒、科伦博泰、康方生物等均在内。尤其以康方生物为例，2023年，其营收创下历史新高，达到45.26亿元，同比增长440.35%，在此推动下，其归母净利润达20.28亿元，上市后首次实现年度盈利。这主要归因于一笔重磅交易，2023年一季度，康方生物收到依沃西许可授权的5亿首付款，这占年度营收的比例高达80%，是其扭亏为盈的关键。图6.康方生物业绩表现（数据来源：企业年报）不过好景不长，从最新的2024年半年报来看，康方生物业绩下滑明显，同比降幅比例达到72.13%，并且再度陷入亏损怪圈，净利润为-2.39亿元。而之所以会如此，就是因为少了大额许可收入，所以从某种意义上来说，康方生物的业绩变动都直接与BD相关，可谓成也BD，败也BD。事实上这并非个例，随着当前天价BD愈发增多，类似的案例未来还将大量涌现。因此，一个行业疑问已经愈发凸显，即如何延续BD的价值，将钱再生为更多的钱？通过对典型案例进行分析，并结合专业人士观点，动脉网认为解决办法主要有两个方面，第一个方面就是尽可能地兑现更多的里程碑付款，具体而言就是与买方深度绑定，并借助其优势，加速授权产品在研发、获批以及市场等关键方面的进程，以此换取更为丰厚的里程碑入账。第二个方面就是将获得的现金流投入到新的研发之中，或者补充现有管线，以此搭建产品组合，逐步向Biopharma迈进。这实际上与投资机构的变现逻辑相似，即将源源不断的收入投向新的价值标的，并以此换取更大的回报。当然，在这个过程之中，鉴别被投项目的能力至关重要，是投资机构脱颖而出的关键。而将其放在研发环节，“鉴别项目的能力”就等同于创新药企业找到并开放出有价值的管线及产品的能力。对此，某药企创始人谈道，“BD收入就相当于一笔投资，金额一般较大，一定程度上也能缓解企业资金困境。但从长远来看，这并不能支撑业绩持续增长，药企真正的成长力还是在产品上。因此，对于药企来说，在BD交易兑现的同时，创新成果也要持续兑现，而只有这样，才能真正推动药企走出亏损泥沼，BD的价值也将不断放大。” 这无疑为当前正处于增长瓶颈的创新药企业提供了一种思路。 * 参考资料： 1.《里程碑付款，我们能拿到多少？》——研发客； 2.《中国创新药，在美国半年就卖了10个亿》——健识局； 3.《和黄医药：老钱漂流记》——深蓝观。 *封面图片来源：123rf 如果您认同文章中的观点、信息，或想进一步讨论，请与我们联系；也可加入动脉网行业社群，结交更多志同道合的好友。近期推荐声明：动脉网所刊载内容之知识产权为动脉网及相关权利人专属所有或持有。未经许可，禁止进行转载、摘编、复制及建立镜像等任何使用。动脉网，未来医疗服务平台

引进/卖出财报上市批准

2024-09-27

·Business Wire

Final Real-World Results from MILOS German Cohort Demonstrate Strong Increase in LDL-C Goal Achievement With Addition of Bempedoic Acid

MUNICH--( BUSINESS WIRE )--For EU media only Daiichi Sankyo Europe, (hereafter, Daiichi Sankyo) today announced final 2-year follow-up data from the German cohort of the multinational, European observational MILOS study. 1 The study evaluated the real-world use of bempedoic acid, marketed as NILEMDO ® ▼ and its FDC with ezetimibe, NUSTENDI ® ▼, in patients with primary hypercholesterolaemia or mixed dyslipidaemia. The results, presented in Hamburg, Germany at DGK Hertztage 2024, demonstrated the effectiveness and safety profile of bempedoic acid, both alone and in combination with other lipid-lowering therapies (LLTs) in clinical practice. 1 Raised LDL-C is a key modifiable contributor to risk of major cardiovascular events, with studies showing that every 1 mmol/L reduction in LDL-C is associated with a 22% reduction in major cardiovascular events after one year. 5,6 The German cohort of MILOS study comprising 973 patients from 125 sites in Germany, is one of the most comprehensive assessments of bempedoic acid in a real-world clinical setting to-date in Germany. 1 Patients were followed-up for two years, with LDL-C levels assessed at pre-treatment, one year (1Y) and two years (2Y). Overall, 638 of 973 patients (65.6%) completed 2Y follow up, with LDL-C values at pre-treatment, 1Y and 2Y available for 451 patients. In these 451 patients, a mean reduction of LDL-C levels from 3.1 mmol/L (121.4 mg/dL) at pre-treatment, to 2.0 mmol/L (77.2 mg/dL) was observed, representing an average relative reduction of 30.3% in the overall population. 1 Additionally, the percentage of patients reaching their LDL-C goals increased from 4.9% at pre-treatment to 35.3% at the 2Y follow-up – an approximately 7-fold increase. 1 The proportions of high-risk and very high-risk patients reaching LDL-C goals increased from 5.6% to 32.5%, and 3.6% to 35.2%, respectively. 1 Overall, more than 80% of patients received bempedoic acid in combination with other LLTs at pre-treatment and 2Y, including statins and ezetimibe. The safety profile of bempedoic acid in this real-world population was assessed at 1Y and 2Y and was consistent with that observed in the CLEAR clinical trial programme. 2,3,4 “By significantly lowering LDL-C levels toward guideline goals, we are taking a vital step in reducing the risk of cardiovascular events, which can have a profound impact on a person’s long-term health and quality of life,” said Professor Ioanna Gouni-Berthold, University of Cologne, Center for Endocrinology, Diabetes, and Preventive Medicine and Executive Board Member of the International Atherosclerosis Society . “Cardiovascular disease remains Europe’s leading cause of death, yet the majority of premature CV events are preventable,” 7,8 said Dr. Stefan Seyfried, Vice President Medical Affairs, Specialty Medicines, at Daiichi Sankyo Europe GmbH . “ The findings from this cohort reinforce the benefit provided by bempedoic acid for reducing LDL-C levels. Our long-term goal is to empower the medical community with real-world insights to improve CVD prevention and, ultimately, improve patient care.” -ENDS- About MILOS MILOS (NCT04579367) is an ongoing, multinational, European observational study in adult patients diagnosed with primary hypercholesterolaemia or mixed dyslipidaemia. The aim is to evaluate the real-world use of bempedoic acid and bempedoic plus ezetimibe FDC. Patients in the German cohort were recruited from 125 sites between January 2021 and January 2022 and were followed up for 2 years after baseline measurements. 1 Change in LDL-C levels and the proportion of patients achieving LDL-C goal were assessed in patients at pre-treatment, 1Y and 2Y visits. Analyses were stratified by investigator-assessed CV risk, based on the ESC/EAS dyslipidaemia guidelines. 1 Beyond Germany, MILOS has sites in Austria, Belgium, Italy, the Netherlands, Spain, Switzerland and the UK. 9 About Bempedoic Acid and its Fixed-Dose Combination with Ezetimibe Bempedoic acid (NILEMDO ® ) is a first-in-class, oral, once-daily treatment to lower cholesterol, and can be combined with other oral treatments to help lower cholesterol even further. 10 Bempedoic acid inhibits ATP citrate lyase (ACL), an enzyme which is involved in the production of cholesterol in the liver. 10 Bempedoic acid acts on the well-known cholesterol synthesis pathway, upstream of the statin target in the liver, which allows additional LDL-C lowering when added to statin or other LDL-C-lowering therapies. 11 Bempedoic acid is not activated in skeletal muscle. 10 Bempedoic acid is indicated in adults with primary hypercholesterolaemia (heterozygous familial and nonfamilial) or mixed dyslipidaemia, as an adjunct to diet: 10 in combination with a statin or statin with other lipid-lowering therapies in patients unable to reach LDL-C goals with the maximum tolerated dose of a statin or, 10 alone or in combination with other lipid-lowering therapies in patients who are statin-intolerant, or for whom a statin is contraindicated. 10 Bempedoic acid is indicated in adults with established or at high risk for atherosclerotic CV disease to reduce CV risk by lowering LDL-C levels, as an adjunct to correction of other risk factors: 10 in patients on a maximum tolerated dose of statin with or without ezetimibe or, 10 alone or in combination with ezetimibe in patients who are statin-intolerant, or for whom a statin in contraindicated. 10 The bempedoic acid / ezetimibe FDC (NUSTENDI ® ) combines two complementary ways of reducing cholesterol in a once-daily tablet. Bempedoic acid / ezetimibe FDC is indicated in adults with primary hypercholesterolaemia (heterozygous familial and nonfamilial) or mixed dyslipidaemia, as an adjunct to diet: 12 in combination with a statin in patients unable to reach LDL-C goals with the maximum tolerated dose of a statin in addition to ezetimibe, 12 alone in patients who are either statin-intolerant or for whom a statin is contraindicated, and are unable to reach LDL-C goals with ezetimibe alone, 12 in patients already being treated with the combination of bempedoic acid and ezetimibe as separate tablets with or without statin. 12 Bempedoic acid / ezetimibe FDC is indicated in adults with established or at high risk for atherosclerotic CV disease to reduce CV risk by lowering LDL-C levels, as an adjunct to correction of other risk factors: 12 in patients on a maximum tolerated dose of statin and not adequately controlled with additional ezetimibe treatment or, 12 in patients who are either statin-intolerant, or for whom a statin in contraindicated, and not adequately controlled with ezetimibe treatment or, 12 in patients already being treated with the combination of bempedoic acid and ezetimibe as separate tablets. 12 Daiichi Sankyo Europe has licensed exclusive commercialisation rights to bempedoic acid and its FDC with ezetimibe (marketed as NILEMDO ® and NUSTENDI ® ) in the European Economic Area, UK, Turkey and Switzerland from Esperion and is the full Marketing Authorisation Holder in these territories. About Daiichi Sankyo Daiichi Sankyo is an innovative global healthcare company contributing to the sustainable development of society that discovers, develops, and delivers new standards of care to enrich the quality of life around the world. With more than 120 years of experience, Daiichi Sankyo leverages its world-class science and technology to create new modalities and innovative medicines for people with cancer, cardiovascular, and other diseases with high unmet medical need. For more information, please visit https://www.daiichi-sankyo.eu/ ▼ This medicinal product is subject to additional monitoring. References 1 DGK Hertztage 2024 Abstract. Real-world effectiveness and safety of bempedoic acid in Europe: final 2-year results from the MILOS German cohort. Gouni-Berthold, I et al. 2 Nissen SE, et al. Bempedoic Acid and Cardiovascular Outcomes in Statin-Intolerant Patients. N Engl J Med . 2023;388:1353–64 3 Ray KK, et al. Safety and Efficacy of Bempedoic Acid to Reduce LDL Cholesterol. N Engl J Med . 2019; 380:1022–32 4 Ballantyne CM, et al . Bempedoic acid plus ezetimibe fixed-dose combination in patients with hypercholesterolemia and high CVD risk treated with maximally tolerated statin therapy. Eur J Prev Cardiol . 2020; 27(6): 593–603 5 Cholesterol Treatment Trialists’ (CTT) Collaboration. Efficacy and safety of more intensive lowering of LDL cholesterol: a meta-analysis of data from 170 000 participants in 26 randomised trials. Lancet. 2010. 376(9753): 1670–1681 6 NHS England. Improving lipid management to reduce cardiovascular disease and save lives. Available at: https://www.england.nhs.uk/long-read/improving-lipid-management-to-reduce-cardiovascular-disease-and-save-lives/#:~:text=Raised%20LDL%20cholesterol%20is%20one,vascular%20events%20after%201%20year . Last accessed September 2024. 7 Eurostat. (2023) Causes of death statistics. Available at: https://ec.europa.eu/eurostat/statistics-explained/index.php?title=Causes_of_death_statistics#Major_causes_of_death_in_the_EU_in_2020 . Last accessed September 2024. 8 World Heart Federation. Prevention. Available at: https://world-heart-federation.org/what-we-do/prevention/#:~:text=An%20estimated%2080%25%20of%20cardiovascular,and%20“knowing%20your%20numbers ”. Last accessed September 2024 9 ClinicalTrials.gov. Treatment With Bempedoic Acid and/or Its Fixed-dose Combination With Ezetimibe in Primary Hypercholesterolemia or Mixed Dyslipidemia (MILOS). Available at: https://clinicaltrials.gov/study/NCT04579367#contacts-and-locations . Last accessed September 2024. 10 European Medicines Agency. Nilemdo – Summary of Product Characteristics. Available at: https://www.ema.europa.eu/en/documents/product-information/nilemdo-epar-product-information_en.pdf . Last accessed September 2024. 11 Pinkosky, S.L., et al . Liver-specific ATP-citrate lyase inhibition by bempedoic acid decreases LDL-C and attenuates atherosclerosis. Nat Commun . 2016. 7: 13457. 12 European Medicines Agency. Nustendi –Summary of Product Characteristics. Available at: https://www.ema.europa.eu/en/documents/product-information/nustendi-epar-product-information_en.pdf . Last accessed September 2024 HQ/BIL/09/24/0001

上市批准临床结果AHA会议临床研究引进/卖出

100 项与贝派地酸相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D10691	贝派地酸	C10AX15	DB11936

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
心血管疾病	美国	Esperion Therapeutics, Inc.	2024-03-22
心肌梗塞	美国	Esperion Therapeutics, Inc.	2024-03-22
原发性高脂血症	美国	Esperion Therapeutics, Inc.	2024-03-22
血脂障碍	欧盟	Daiichi Sankyo Europe GmbH	2020-04-01
血脂障碍	冰岛	Daiichi Sankyo Europe GmbH	2020-04-01
血脂障碍	列支敦士登	Daiichi Sankyo Europe GmbH	2020-04-01
血脂障碍	挪威	Daiichi Sankyo Europe GmbH	2020-04-01
原发性高胆固醇血症	欧盟	Daiichi Sankyo Europe GmbH	2020-04-01
原发性高胆固醇血症	冰岛	Daiichi Sankyo Europe GmbH	2020-04-01
原发性高胆固醇血症	列支敦士登	Daiichi Sankyo Europe GmbH	2020-04-01
原发性高胆固醇血症	挪威	Daiichi Sankyo Europe GmbH	2020-04-01
动脉粥样硬化	美国	Esperion Therapeutics, Inc.	2020-02-21
杂合子家族性高胆固醇血症	美国	Esperion Therapeutics, Inc.	2020-02-21

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
高胆固醇血症	申请上市	日本	Otsuka Pharmaceutical Co., Ltd.	2024-11-26
高低密度脂蛋白胆固醇血症	临床3期	日本	Otsuka Pharmaceutical Co., Ltd.	2023-02-13
高脂血症	临床3期	美国	Esperion Therapeutics, Inc.	2017-10-23
高血压	临床2期	美国	Esperion Therapeutics, Inc.	2014-06-16
2型糖尿病	临床2期	美国	Esperion Therapeutics, Inc.	2012-04-01

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临床结果

适应症

分期

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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


ESC2024	N/A	心血管疾病	-	Bempedoic acid 180 mg daily	廠餘廠繭鹹繭積膚範衊(遞夢鹹築糧鏇鹹築廠遞): OR = 0.84 (95% CI, 0.76 ~ 0.96)	积极	2024-08-30
				Placebo
NCT05683340 (Company_Website) 人工标引	临床3期	高胆固醇血症	96	Bempedoic acid 180 mg	艱廠鏇獵餘獵鑰艱鹹鹽(願淵願淵膚顧醖艱範夢) = 選積繭餘獵餘積艱醖網鑰繭夢廠廠積觸鏇鑰餘 (獵鹽餘顧艱夢壓餘蓋遞 ) 达到	积极	2024-05-20
				Placebo	艱廠鏇獵餘獵鑰艱鹹鹽(願淵願淵膚顧醖艱範夢) = 繭鹽齋範範蓋積鏇願獵鑰繭夢廠廠積觸鏇鑰餘 (獵鹽餘顧艱夢壓餘蓋遞 ) 达到
NCT04784442 (CTgov)	临床2期	高胆固醇血症	188	Placebo	淵鹽鑰糧壓齋淵網網鬱(鏇網膚醖遞觸製鏇顧鏇) = 醖鏇簾衊壓齋積繭齋襯範築夢餘憲觸鹹夢繭襯 (鹹繭蓋顧構餘鑰齋繭築, 網艱築鏇構簾蓋鹹獵獵 ~ 壓觸艱築構衊窪獵鹹觸) 更多	-	2024-03-04
NCT02993406 (CLEAR Outcomes, CTgov)	临床3期	心血管疾病	13,970	Bempedoic acid 180 mg tablet (Bempedoic Acid 180 mg)	網製製艱觸鏇鏇襯窪齋(網鑰觸鬱齋蓋壓繭觸鏇) = 範蓋構膚壓鬱網獵簾網襯憲鹽鑰窪觸製齋窪鏇 (鑰夢選網衊獵構網觸觸, 鑰鏇簾膚網願廠鏇齋蓋 ~ 網觸鏇獵製製願鑰築獵) 更多	-	2024-01-03
				Matching placebo tablet (Placebo Comparator)	網製製艱觸鏇鏇襯窪齋(網鑰觸鬱齋蓋壓繭觸鏇) = 觸衊觸廠選觸選鏇鹽淵襯憲鹽鑰窪觸製齋窪鏇 (鑰夢選網衊獵構網觸觸, 積選製餘簾蓋構壓壓夢 ~ 鏇餘廠衊窪鑰淵壓襯鑰) 更多
MILOS (ESC2023)	N/A	-	992	Bempedoic acid	製顧艱膚遞餘廠襯獵襯(廠艱鏇艱廠獵鏇憲範壓) = 齋淵遞獵淵遞積淵蓋鏇廠壓衊構襯選窪構獵獵 (膚願鬱窪襯窪衊築選鏇, (84.1)) 更多	-	2023-08-26
				Bempedoic acid + ezetimibe	製顧艱膚遞餘廠襯獵襯(廠艱鏇艱廠獵鏇憲範壓) = 願襯醖蓋鬱繭範襯醖簾廠壓衊構襯選窪構獵獵 (膚願鬱窪襯窪衊築選鏇, (123.6)) 更多
NCT02993406 (Pubmed \| JAMA)	临床3期	-	4,206	Bempedoic Acid	(衊選選鏇鏇範遞遞簾鑰): HR = 0.61 (95% CI, 0.39 ~ 0.98) 更多	积极	2023-06-24
				Placebo
NCT02178098 (CTgov)	临床2期	高血压 \| 高胆固醇血症	143	Placebo	蓋繭憲鏇選廠繭襯夢積(構壓鑰製淵顧壓製顧觸) = 餘網窪鹹觸觸遞網繭願顧鹽範鬱遞鹽廠糧遞鏇 (壓選鏇糧構築積衊衊憲, 鹹築蓋製襯獵願網願選 ~ 網窪繭衊艱築鏇衊壓淵) 更多	-	2023-04-04
NCT02993406 (CLEAR Outcomes, Pubmed \| N Engl J Med)	临床3期	-	14,014	Bempedoic acid	糧觸鏇積壓艱製製淵鏇(鏇築鑰襯鹽範夢製顧襯) = 2.2% vs. 1.2% 齋鹹顧選夢鏇構壓齋鬱 (鑰網鏇顧顧願製壓獵艱 ) 更多	积极	2023-03-04
				Placebo
NCT02666664 (CLEAR Harmony, Pubmed \| J Clin Lipidol)	临床3期	炎症	817	Bempedoic acid 180 mg	(鏇鏇製壓襯鹽願夢觸鹽) = 憲壓窪夢襯齋醖醖觸襯糧蓋壓築繭構齋築鑰鹹 (壓獵壓遞鹹壓製鏇觸齋, -10.1 ~ -6.6) 更多	-	2023-02-14
NCT02993406 (CLEAR Outcomes, BusinessWire) 人工标引	临床3期	-	14,014	Bempedoic acid	選積遞繭憲觸淵窪廠淵(鬱襯窪積鹹夢衊築製夢) = significant relative risk reduction in major adverse CV events (MACE-4) in patients treated with 180 mg/day bempedoic acid compared to placebo (with no or very low statin background 製淵醖醖鬱遞齋餘壓簾 (簾鬱壓獵膚繭膚憲網鏇 )	积极	2022-12-08
				Placebo