Efinopegdutide(Efinopegdutide) - 药物靶点：GCGR x GLP-1R_在研适应症：肝硬化，非酒精性脂肪肝，非酒精性脂肪性肝炎_专利_临床

概要

基本信息

药物类型

融合蛋白

别名

Efinopegdutide (USAN/INN)、GLP-1/glucagon-agonist、Glucagon-like-peptides/glucagon

+ [13]

靶点

GCGR x GLP-1R

作用方式

激动剂

作用机制

GCGR激动剂(胰高血糖素受体激动剂)、GLP-1R激动剂(胰高血糖素样肽-1激动剂)

治疗领域

消化系统疾病内分泌与代谢疾病

在研适应症

肝硬化非酒精性脂肪肝非酒精性脂肪性肝炎+ [2]

非在研适应症

2型糖尿病终末期肾脏病2型糖尿病肥胖

原研机构

Hanmi Pharmaceutical Co., Ltd.

在研机构

Merck Sharp & Dohme LLC

Merck Sharp & Dohme Corp.

Hanmi Pharmaceutical Co., Ltd.

非在研机构

Janssen Research & Development LLC

Janssen Pharmaceuticals, Inc.

权益机构

Hanmi Pharmaceutical Co., Ltd.

Boehringer Ingelheim GmbH

Merck & Co., Inc.

+ [2]

最高研发阶段临床2期

首次获批日期-

最高研发阶段(中国)临床2期

特殊审评快速通道 (美国)

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结构/序列

Sequence Code 1191632819

来源: *****

Sequence Code 9133009

来源: *****

关联

17

项与 Efinopegdutide 相关的临床试验

NCT06482112

/ Active, not recruiting临床2期

A Phase 2a Randomized, Open-Label Study to Evaluate the Efficacy and Safety of Different Dosing Regimens of Efinopegdutide (MK-6024) in Adults With Metabolic Dysfunction-Associated Steatotic Liver Disease

This study will evaluate the effect of efinopegdutide administration once every 2 weeks (Q2W) versus once weekly (Q1W) on mean relative reduction from baseline in liver fat content (LFC) after 28 weeks, as well as the safety and tolerability of the different regimens of efinopegdutide.

开始日期2024-07-29

申办/合作机构

Merck Sharp & Dohme LLC

NCT06701305

/ Completed临床1期

A Single and Multiple-Ascending Dose Clinical Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of Efinopegdutide (MK-6024) in Otherwise Healthy Obese Participants and the Effect of Multiple Doses of Efinopegdutide on the Pharmacokinetics of Acetaminophen

The goal of this study is to learn about the safety of efinopegdutide (MK-6024) and how well overweight healthy people tolerate it. Researchers also want to know what happens to efinopegdutide in a person's body over time when taken as a single dose (Part 1) or as multiple doses (Part 2). In addition, the study will assess the amount of acetaminophen in the blood after receiving different strength doses of efinopegdutide (Part 2 only).

开始日期2024-06-13

申办/合作机构

Merck Sharp & Dohme LLC

NCT06052566

/ Completed临床1期

An Open-Label, Single-Dose Study to Evaluate the Pharmacokinetics of Efinopegdutide (MK-6024) in Participants With Moderate and Severe Hepatic Impairment

The purpose of this study is to evaluate the pharmacokinetics of efinopegdutide in participants with hepatic impairment compared to healthy participants, and to examine the safety and tolerability of efinopegdutide.

开始日期2023-11-21

申办/合作机构

Merck Sharp & Dohme LLC

100 项与 Efinopegdutide 相关的临床结果

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100 项与 Efinopegdutide 相关的转化医学

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100 项与 Efinopegdutide 相关的专利（医药）

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54

项与 Efinopegdutide 相关的文献（医药）

2025-05-01·Peptides

Multifunctional incretin peptides in therapies for type 2 diabetes, obesity and associated co-morbidities

Review

作者: Flatt, Peter R ; Conlon, J Michael ; Bailey, Clifford J

Recent studies with peptide-based incretin therapies have focussed mainly on the glucagon-like peptide-1 (GLP-1) receptor agonist semaglutide and the dual agonist tirzepatide that engages receptors for GLP-1 and glucose-dependent insulinotropic polypeptide (GIP). Randomised clinical trials and 'real-world' studies have confirmed the marked glucose-lowering and weight-lowering efficacy of these agents across diverse populations. These include different ethnic groups, young and elderly individuals with and without diabetes and/or overweight or obesity. Recent studies have also confirmed protections against the development and progression of cardiovascular and renal diseases that are additive to the benefits conferred by improved control of blood glucose and body weight. Emerging evidence suggests that incretin therapies could additionally ameliorate fatty liver disease, chronic inflammation, sleep apnea and possibly degenerative bone disorders and cognitive decline. New incretin-based peptide therapies in development include a long-acting glucagon receptor agonist (LY3324954), dual GLP-1/glucagon receptor agonists (survodutide, pemvidutide, mazdutide, G49), triple GLP-1/GIP/glucagon receptor agonists (retatrutide, efocipegtrutide), a combination of semaglutide with the amylin analogue cagrilintide (CagriSema), a unimolecular GLP-1/amylin receptor dual agonist (amycretin), and a GIP receptor antibody with GLP-1 receptor agonism (MariTide). The creation of multi-targeting incretin-based synthetic peptides provides opportunities for improved management of type 2 diabetes and obesity as well as new therapeutic approaches to an expanding list of associated co-morbidities. The aim of the review is to acquaint the reader with developments in the field from 2023 to the present (February 2025).

2025-03-04·Expert Opinion on Investigational Drugs

The pleiotropic effects of glucagon-like peptide-1 receptor agonists in patients with metabolic dysfunction-associated steatohepatitis: a review for gastroenterologists

Review

作者: Charlton, Michael ; Noureddin, Mazen ; Alkhouri, Naim ; Gray, Meagan

INTRODUCTIONGlucagon-like peptide-1 receptor agonists (GLP-1RAs), and dual GLP-1/glucose-dependent insulinotropic peptide (GIP) or glucagon receptor agonists have emerged as promising agents to treat metabolic dysfunction-associated steatotic liver disease (MASLD)/metabolic dysfunction-associated steatohepatitis (MASH). Although the beneficial effects of GLP-1RAs on glycemic control and weight are well-established, clinicians may be unfamiliar with other potential benefits of this class.AREAS COVEREDWe examined the pleiotropic effects of GLP-1RAs and how they relate to gastroenterologists for MASLD/MASH treatment. Our narrative review of English articles included four GLP-1RAs (subcutaneous semaglutide, liraglutide, dulaglutide, and efpeglenatide), a dual GLP-1/GIP agonist (tirzepatide), a dual GLP-1/glucagon receptor agonist (survodutide), MASLD/MASH, related disorders, clinical management, treatment outcomes and landscape.EXPERT OPINIONIn Phase I - III trials, GLP-1RAs are associated with clinically relevant hepatic improvements including MASH resolution, liver fat reduction, and preventing worsening fibrosis. Effects on cardiometabolic parameters align with type 2 diabetes/obesity Phase III data, comprising substantial improvements in glycemic, weight, and cardiovascular outcomes. Promising data also suggest benefits in common comorbidities, including obstructive sleep apnea, polycystic ovary syndrome, chronic kidney disease, and heart failure with preserved ejection fraction.GLP-1RAs represent a valuable pharmacotherapeutic option for gastroenterologists managing individuals with MASLD/MASH and cardiometabolic comorbid conditions.

2025-02-01·Journal of Hepatology

Beyond Metabolic Benefits: The Underexplored Immunomodulatory Effects of GLP-1/Glucagon Agonists

Letter

作者: Dallmeier, Kai ; Fevery, Johan ; van Niekerk, Gustav

71

项与 Efinopegdutide 相关的新闻（医药）

2025-04-15

·Endpoints

Merck explores potential of oral peptides in deal with Austrian biotech

Merck is looking for ways to make its drugs easier to administer. The large pharma is licensing a drug delivery platform from Austrian biotech Cyprumed in a pact worth $493 million in upfront and potential milestone payments. The technology is designed to develop oral formulations of peptide drugs, which could include Merck’s GLP-1 candidate. Merck will obtain non-exclusive rights to use Cyprumed’s oral peptide delivery platform for an undisclosed number of targets, according to a Tuesday release. The large pharma also has the option to exclusively license the same platform for individual targets, meaning the biotech may be eligible for further payments. Merck would be responsible for any additional development, manufacturing and commercialization work. The companies did not say which of Merck’s peptide programs will be investigated to become an oral formulation. But Cyprumed noted in Tuesday’s release that its technology can be applied to GLP-1 agonists, macrocycles and mini-proteins. Merck has at least two peptides in clinical development but one of these, enlicitide decanoate, is already administered orally. That PCSK9-targeting candidate is in Phase 3 development for high cholesterol. The other peptide program, efinopegdutide, is a subcutaneously administered dual GLP-1/glucagon receptor agonist in Phase 2 for MASH. The drugmaker has been making moves to boost its GLP-1 pipeline. In December, it licensed Hansoh Pharma’s oral candidate, called HS-10535, in a deal that featured $112 million upfront . Just weeks prior to that announcement, Merck CEO Rob Davis said of GLP-1s that the company is focused on opportunities for oral formulations that can be combined with other drugs to address obesity alongside a range of comorbidities. Cyprumed’s platform features “tablet formulations” based on already approved pharmaceutical vehicles, which should boost the “scalability, cost-efficiency and regulatory compliance” of any resulting candidates, the biotech said.

临床3期多肽偶联药物引进/卖出临床2期

2025-04-15

·BioSpace

Merck Eyes Oral Peptide Delivery With Cyprumed Deal Worth up to $493M

iStock, Sundry Photography Merck has not disclosed which of its peptide therapies it plans to develop oral formulations for. Merck on Tuesday entered into a nonexclusive licensing and option pact with Austrian biotech Cyprumed in a bid to make its peptide drugs orally available. Details of the deal were scant. Merck will pay up to $493 million, a sum inclusive of the upfront fee plus development, regulatory and commercialization milestones of any product that may arise from the partnership. In exchange for its investment, Merck will gain access to Cyprumed’s proprietary platform to develop novel oral formulations of the pharma’s peptide therapies, though Merck is tight-lipped about specifics. The company did not reveal how many and which of its assets it plans to make orally available. The pharma also did not disclose priority indications. According to Tuesday’s news release, Cyprumed’s platform can be used on several types of peptides, including GLP-1 analogs, mini-proteins and macrocycles. Under the terms of the agreement, Merck will also have the exclusive option to license Cyprumed’s technology for individual targets, in which case Cyprumed will be eligible for additional payments. Merck will be responsible for trialing these oral drug formulations and will take charge of their manufacturing and marketing. According to its pipeline page , Merck has two peptide therapies in development: the late-stage enlicitide decanoate, being studied for high cholesterol, and the Phase II efinopegdutide, a dual agonist of GLP-1 and GIP receptors, to treat metabolic dysfunction-associated steatohepatitis ( MASH ). Enlicitide decanoate, which blocks PCSK9, is already orally available. The pharma has five listed studies running for the asset under the CORALreef program. Merck is developing enlicitide decanoate in partnership with UCB Pharmaceuticals. Meanwhile, efinopegdutide is delivered via a subcutaneous injection. Currently, Merck has four listed studies for the asset, including one that directly compares it with Novo Nordisk’s semaglutide, looking at the drugs’ ability to lower liver fat levels in patients with MASH. Both the Cyprumed deal and the decision to study efinopegdutide in an obesity-adjacent indication fits with Merck’s strategy in the weight loss arena. At the 45th Goldman Sachs Healthcare Conference in June 2024, CEO Robert Davis said that the pharma will focus its R&D efforts on orals rather than injectables, and that it will prioritize drugs that deliver cardiometabolic benefits in addition to weight reduction. “I think everything is couched in terms of obesity first,” Davis said at the time, noting that pharma then considers other health outcomes for “supporting the reimbursement within the broader obesity space.”

引进/卖出临床2期

2025-03-24

·医药地理

【凤采鸾章·博文集】胰高血糖素样肽-1受体激动剂治疗代谢相关脂肪性肝炎的临床研究进展

胰高血糖素样肽-1受体激动剂治疗代谢相关脂肪性肝炎的临床研究进展 Clinical progress of glucagon-like peptide-1 receptor agonists in the treatment of metabolically associated steatohepatitis 曾艳艳1 ，兰志龙2 ，李英博2 ，姜山2 ，倪娜1*，王俊龙1* (1. 中国医药工业研究总院临床研究中心，上海 200437；2. 上海益临思医药开发有限公司，上海 200437) 引用曾艳艳, 兰志龙, 李英博, 等. 胰高血糖素样肽-1受体激动剂治疗代谢相关脂肪性肝炎的临床研究进展[J]. 世界临床药物, 2025, 46(2): 130-137. DOI:10.13683/j.wph.2025.02.003. 作者简介曾艳艳，硕士研究生，研究方向：临床药学及临床研究。通信作者：倪娜，副研究员，研究方向：创新药物的临床研究。王俊龙，副研究员，研究方向：创新药物的临床研究。 01 摘要代谢相关脂肪性肝炎(metabolic associated steatohepatitis，MASH)，原名为非酒精性脂肪性肝炎。若不加以控制，其可导致肝硬化及肝癌的发生。随着学科不断发展，MASH 的诊断和治疗均有很大进步，但由于其复杂的作用机制，不少临床试验即使进入Ⅲ期也以失败告终。该文从 MASH 的代谢障碍为考虑点，汇总其靶向代谢的胰高血糖素肽 -1 受体与其他肠促胰岛素信号通路的双重 / 三重受体激动剂，为更好地开发 MASH 治疗及设计相关临床试验提供一定参考。 02 关键词非胰高血糖素样肽 -1 ；胰高血糖素样肽 -1 受体激动剂；代谢相关脂肪性肝炎；非酒精性脂肪性肝炎；代谢相关脂肪性肝病；非酒精性脂肪性肝病 03 章节导览 1 疾病名称的变更及未满足的临床需求 2 MASH 的发病机制及相关靶点的治疗药物 3 GLP-1RA 代谢通路在 MASH 中的作用机制 4 GLP-1RA 代谢通路的临床研究进展 4.1 Efinopegdutide(HM12525A、INJ-6456511) 4.2 Pemvidutide(ALT-801) 4.3 Survodutide(BI456906) 4.4 Tirzepatide 4.5 GLP-1RA 代谢通路治疗 MASH 的疗效数据对比 5 结语 04 文章节选随着全球肥胖 (obesity) 和 2 型糖尿病 (type 2 diabetes mellitus，T2DM) 的发病率逐年上升，相关的肝病，尤其是代谢相关脂肪性肝炎 (metabolic associated steatohepatitis，MASH)，即非酒精性脂肪性肝炎 (non-alcoholic steatohepatitis，NASH) 的更新命名，正迅速成为全球健康领域的一个重大挑战。MASH 是由代谢相关脂肪性肝病 (metabolic associated fatty liver disease，MAFLD)，原名为非酒精性脂肪性肝病 (nonalcoholic fatty liver disease， NAFLD) 进展而来的严重慢性肝脏疾病，以 5% 以上的肝细胞脂肪变、小叶内炎症以及肝细胞气球样变和纤维化为特征。新更新的命名强调作为该病基础的代谢功能障碍的概念，尤其强调评估代谢综合征 (metabolic syndrome，MS) 个体特征的必要性。以司美格鲁肽 (semaglutide) 为代表的胰高血糖素肽 (glucagon-like peptide，GLP)-1 受体激动剂 (GLP-1 receptor agonists，GLP-1RA) 最初是为治疗 T2DM 而开发，其可显著改善 T2DM 的病理生理缺陷，并具有减少心血管死亡、改善动脉粥样硬化、减轻体质量、降低收缩压以及改善血脂谱等多重降糖外获益。更有研究显示，司美格鲁肽在改善患者肝纤维化方面具有潜力。基于其多效性的作用机制、显著的临床研究进展，GLP-1 与其他肠促胰岛素信号通路的双重 / 三重受体激动剂正成为治疗 MASH 的一个新兴且具有潜力的靶点。 ←长按二维码阅读原文 END 如需获取更多数据洞察信息或公众号内容合作，请联系医药地理小助手微信号：pharmadl001

临床2期临床结果临床3期

100 项与 Efinopegdutide 相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D11607	-	-	DB15077

研发状态

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
非酒精性脂肪性肝炎	临床2期	中国台湾	Merck Sharp & Dohme Corp.	2021-08-04
非酒精性脂肪性肝炎	临床2期	韩国	Merck Sharp & Dohme Corp.	2021-08-04
非酒精性脂肪性肝炎	临床2期	墨西哥	Merck Sharp & Dohme Corp.	2021-08-04
2型糖尿病肥胖	临床1期	美国	Janssen Research & Development LLC	2018-06-26
肥胖	临床1期	波兰	Janssen Research & Development LLC	2018-03-26
肥胖	临床1期	英国	Janssen Research & Development LLC	2018-03-26
肥胖	临床1期	美国	Janssen Research & Development LLC	2018-03-26
肥胖	临床1期	瑞典	Janssen Research & Development LLC	2018-03-26
肥胖	临床1期	比利时	Janssen Research & Development LLC	2018-03-26
肥胖	临床1期	加拿大	Janssen Research & Development LLC	2018-03-26

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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


NCT04944992 (EudraCT: 2020-005136-30 \| ###DELETE \| MK-6024-001 \| 6024-001, CTgov)	临床2期	非酒精性脂肪性肝炎	145	Efinopegdutide 20 mg/mL (Efinopegdutide)	夢壓鏇膚願壓鹹觸淵鹹(蓋繭積遞積積構鹹觸鏇) = 遞獵觸鬱衊繭繭膚醖範選積淵製夢壓構廠齋蓋 (顧願膚鏇鑰遞鹹網構襯, 壓簾廠鬱鬱鏇觸壓簾醖 ~ 醖鑰襯繭糧範鹹築醖觸) 更多	-	2023-11-15
				Semaglutide 1.34 mg/mL (Semaglutide)	夢壓鏇膚願壓鹹觸淵鹹(蓋繭積遞積積構鹹觸鏇) = 糧獵鏇獵簾淵網積衊遞選積淵製夢壓構廠齋蓋 (顧願膚鏇鑰遞鹹網構襯, 糧選鑰壓膚夢鬱齋繭憲 ~ 顧蓋艱鑰鹹艱網製觸夢) 更多
EUCTR2020-005136-30-ES \| NCT04944992 (EASD2023)	临床2期	2型糖尿病 \| 代谢功能障碍相关的脂肪肝病	145	Efinopegdutide 10 mg	(艱觸鹹窪鹹繭製醖遞鏇) = 繭願鹹鬱窪壓衊網簾獵醖鹽網膚鹹構製餘衊鹽 (壓糧築獵蓋製觸廠製醖, 57.2 ~ 76.3) 更多	积极	2023-10-04
				Semaglutide 1 mg	(艱觸鹹窪鹹繭製醖遞鏇) = 鏇醖鏇夢網觸艱憲鏇顧醖鹽網膚鹹構製餘衊鹽 (壓糧築獵蓋製觸廠製醖, 36.0 ~ 55.1) 更多
NCT03486392 (CTgov)	临床2期	肥胖	474	placebo+JNJ-64565111 (Double Blind: Placebo)	蓋積遞膚艱鬱製壓製蓋(構簾膚襯膚壓鏇顧觸憲) = 鹽鏇淵夢鹽獵壓廠鹽膚鹽壓製餘壓齋遞膚積鑰 (壓憲繭壓夢壓鬱憲艱餘, 鑰艱餘選鏇憲醖齋積鏇 ~ 壓襯鹽蓋憲觸壓製膚顧) 更多	-	2020-02-05
				JNJ-64565111 (Double Blind: JNJ-64565111 5.0 mg)	蓋積遞膚艱鬱製壓製蓋(構簾膚襯膚壓鏇顧觸憲) = 膚蓋選鬱遞淵衊醖鑰齋鹽壓製餘壓齋遞膚積鑰 (壓憲繭壓夢壓鬱憲艱餘, 遞鹹壓蓋鹹鏇鬱構簾鹽 ~ 醖醖淵廠顧鏇壓鏇齋鬱) 更多
NCT03586830 (CTgov)	临床2期	2型糖尿病肥胖	196	Placebo	遞鏇糧窪壓顧構鹹壓壓(積醖鹹鬱鏇鏇網窪遞顧) = 膚蓋艱襯鏇廠衊夢鏇鹽鑰製廠製憲艱鏇積鹽齋 (襯壓顧夢憲鑰遞鑰齋醖, 選齋鑰憲築憲觸衊範積 ~ 鹽鬱繭糧鹽鏇衊膚艱製) 更多	-	2020-01-07