排名前五的靶点	数量

HIV-1 RT(人类免疫缺陷病毒1型逆转录酶)	7
TGF-β(转化生长因子β)	6
PD-1(细胞程序性死亡-1)	5
STING(干扰素基因刺激蛋白)	5
GR(糖皮质激素受体)	4

关联

1,552

项与 Merck & Co., Inc. 相关的药物

Gefapixant

靶点

P2X3 receptor

作用机制

P2X3 receptor拮抗剂

在研机构

Merck Gesellschaft mbH [+4]

原研机构

F. Hoffmann-La Roche Ltd.

在研适应症

难治性慢性咳嗽 [+9]

非在研适应症

特发性肺纤维化 [+3]

药物最高研发状态批准上市

首次获批国家/地区

日本

首次获批日期2022-01

Molnupiravir

莫诺拉韦

靶点

RdRp

作用机制

RdRp抑制剂 [+1]

在研机构

Emory University [+7]

原研机构

Emory University

在研适应症

新型冠状病毒感染 [+8]

非在研适应症-

药物最高研发状态批准上市

首次获批国家/地区

英国

首次获批日期2021-11

Belzutifan

贝组替凡

靶点

HIF-2α

作用机制

HIF-2α抑制剂

在研机构

Peloton Therapeutics, Inc. [+5]

原研机构

Merck Sharp & Dohme Corp.

在研适应症

血管母细胞瘤 [+19]

非在研适应症

铁过剩

药物最高研发状态批准上市

首次获批国家/地区

美国

首次获批日期2021-08

5,489

项与 Merck & Co., Inc. 相关的临床试验

NCT05093972 / Not yet recruiting临床1期

An Open-Label, Single-Dose Clinical Study to Evaluate Pharmacokinetics of MK-8507 in Participants With Mild or Moderate Hepatic Impairment.

The purpose of this study is to evaluate pharmacokinetics (PK) and safety of a single oral dose of ulonivirine in participants with mild or moderate hepatic impairment (HI). It is hypothesized that the area under the plasma concentration-time curve from dosing to (extrapolated) infinity (AUC0-∞) in participants with mild or moderate HI is similar to that of healthy control participants.

开始日期2024-10-29

申办/合作机构

Merck Sharp & Dohme Corp.

NCT04901741 / Not yet recruiting临床2期

An Open-label Phase 2 Study of Olaptesed Pegol (NOX-A12) Combined With Pembrolizumab and Nanoliposomal Irinotecan/5-FU/Leucovorin or Gemcitabine/Nab-paclitaxel in Microsatellite-stable Metastatic Pancreatic Cancer Patients

The purpose of this study is to provide a go/no-go decision for a randomized expansion study by assessing the disease control rate (DCR) at 6 weeks for the combination of olaptesed pegol on top of pembrolizumab and (Arm 1) nanoliposomal irinotecan, 5-FU and leucovorin or (Arm 2) gemcitabine and nab-paclitaxel, to assess safety and tolerability and time-to-event endpoints.

开始日期2024-06-01

申办/合作机构

TME Pharma NV

[+1]

NCT05986071 / Not yet recruiting临床1/2期IIT

A Phase I/II Study Evaluating M1774, an ATR Inhibitor, in Combination With Fulvestrant in Hormone Receptor-positive and HER2-negative, Advanced Breast Cancers, Resistant to CDK4/6 Inhibitor Plus Aromatase Inhibitor-based Endocrine Treatment

CDK4/6 inhibitor in combination with endocrine treatment is the standard of care in advanced breast cancer (ABC) with expression of hormone receptors and without HER2 overexpression (ER+/HER2-). When patients experience disease progression under this strategy, options of second-line endocrine treatment in combination with other targeted therapies are limited and have failed to improve overall survival to date over endocrine treatment alone. A significant fraction of ER+/HER2- ABC display genetic alterations associated with homologous recombination deficiency (HRD) which may be associated with efficacy of therapeutic targeting DNA damage response (DDR) pathways. Moreover, other molecular alterations associated with replicative stress may be found in ER+/HER2- ABC patients which may also favor antitumor activity of DDR targeting therapeutics. M1774 is a novel orally administered inhibitor of ataxia telangiectasia and rad3-related (ATR), a protein kinase with key activity in DDR pathway. MATRIx is a phase I/II study aiming to determine the recommended phase II dose (RP2D, phase I) as well as efficacy and safety (phase II) of M1774 in combination with fulvestrant in ER+/HER2-ABC patients whose disease has become resistant to aromatase inhibitor plus CDK4/6 inhibitor, and whose tumor displays molecular alterations associated with HRD, oncogenic driver activation and/or replicative stress. Primary endpoints will include: maximum tolerated dose (MTD) of M1774 in combination with fulvestrant (phase I), the clinical benefit rate and toxicity of the combination at RP2D of M1774 in the molecularly selected population (phase II). Baseline, on-treatment and post-treatment blood and tumor tissue samples will be collected for pharmacokinetics and translational analyses including genomic characterization of tumor tissue and ctDNA as well as functional studies focusing on DDR pathways.

开始日期2024-04-01

申办/合作机构

Institut Jean Paoli & Irene Calmettes

[+1]

0 项与 Merck & Co., Inc. 相关的专利（医药）

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23,268

项与 Merck & Co., Inc. 相关的文献（医药）

2023-09-01·Bioengineering & translational medicine

A high-throughput microfluidic mechanoporation platform to enable intracellular delivery of cyclic peptides in cell-based assays

Article

作者: Kasper, Stephen H. ; Otten, Stephanie ; Squadroni, Brian ; Orr-Terry, Cionna ; Kuang, Yi ; Mussallem, Lily ; Ge, Lan ; Yan, Lin ; Kannan, Srinivasaraghavan ; Verma, Chandra S. ; Brown, Christopher J. ; Johannes, Charles W. ; Lane, David P. ; Chandramohan, Arun ; Partridge, Anthony W. ; Roberts, Lee R. ; Josien, Hubert ; Therien, Alex G. ; Hett, Erik C. ; Howell, Bonnie J. ; Peier, Andrea ; Ai, Xi ; Cassaday, Jason

Cyclic peptides are poised to target historically difficult to drug intracellular protein-protein interactions, however, their general cell impermeability poses a challenge for characterizing function. Recent advances in microfluidics have enabled permeabilization of the cytoplasmic membrane by physical cell deformation (i.e., mechanoporation), resulting in intracellular delivery of impermeable macromolecules in vector- and electrophoretic-free approaches. However, the number of payloads (e.g., peptides) and/or concentrations delivered via microfluidic mechanoporation is limited by having to pre-mix cells and payloads, a manually intensive process. In this work, we show that cells are momentarily permeable (t _1/2 = 1.1-2.8 min) after microfluidic vortex shedding (μVS) and that lower molecular weight macromolecules can be cytosolically delivered upon immediate exposure after cells are processed/permeabilized. To increase the ability to screen peptides, we built a system, dispensing-microfluidic vortex shedding (DμVS), that integrates a μVS chip with inline microplate-based dispensing. To do so, we synced an electronic pressure regulator, flow sensor, on/off dispense valve, and an x-y motion platform in a software-driven feedback loop. Using this system, we were able to deliver low microliter-scale volumes of transiently mechanoporated cells to hundreds of wells on microtiter plates in just several minutes (e.g., 96-well plate filled in <2.5 min). We validated the delivery of an impermeable peptide directed at MDM2, a negative regulator of the tumor suppressor p53, using a click chemistry- and NanoBRET-based cell permeability assay in 96-well format, with robust delivery across the full plate. Furthermore, we demonstrated that DμVS could be used to identify functional, low micromolar, cellular activity of otherwise cell-inactive MDM2-binding peptides using a p53 reporter cell assay in 96- and 384-well format. Overall, DμVS can be combined with downstream cell assays to investigate intracellular target engagement in a high-throughput manner, both for improving structure-activity relationship efforts and for early proof-of-biology of non-optimized peptide (or potentially other macromolecular) tools.

2023-05-11·ACS medicinal chemistry letters

High-Throughput Photo- and Electrochemical sp-sp Cross-Electrophile Coupling to Access Novel Tedizolid Analogs

Article

作者: Montero Bastidas, Jose Raul ; LHeureux, Scott ; Liu, Wenbin ; Lee, Ken ; El Marrouni, Abdellatif

The development of practical synthetic protocols integrating novel technologies may enable rapid and broad exploration of chemical space in medicinal chemistry campaigns. Cross-electrophile coupling (XEC) allows the diversification of an aromatic core with alkyl halides to increase the sp³ character. Herein, we apply two alternative approaches via either photo- or electro-catalyzed XEC and showcase their complementarity to access novel tedizolid analogs. The parallel photochemical and electrochemical reactors with high light intensity and constant voltage respectively were chosen to yield good conversions, which allowed access to a wide range of derivatives in a much shorter time frame.

2023-05-11·ACS medicinal chemistry letters

Beyond 20 in the 21st Century: Prospects and Challenges of Non-canonical Amino Acids in Peptide Drug Discovery

Review

作者: Hickey, Jennifer L. ; Sindhikara, Dan ; Zultanski, Susan L. ; Schultz, Danielle M.

Life is constructed primarily using a toolbox of 20 canonical amino acids-relying upon these building blocks for the assembly of proteins and peptides that regulate nearly every cellular task, including cell structure, function, and maintenance. While Nature continues to be a source of inspiration for drug discovery, medicinal chemists are not beholden to only 20 canonical amino acids and have begun to explore non-canonical amino acids (ncAAs) for the construction of designer peptides with improved drug-like properties. However, as our toolbox of ncAAs expands, drug hunters are encountering new challenges in approaching the iterative peptide design-make-test-analyze cycle with a seemingly boundless set of building blocks. This Microperspective focuses on new technologies that are accelerating ncAA interrogation in peptide drug discovery (including HELM notation, late-stage functionalization, and biocatalysis) while shedding light on areas where further investment could not only accelerate the discovery of new medicines but also improve downstream development.

7,721

项与 Merck & Co., Inc. 相关的新闻（医药）

2023-09-29

·PRNewswire

From Managing Chronic Diseases to Monitoring Nutrition: Patient-Centric Apps are the Next Big Thing in Healthcare

DUBLIN, Sept. 29, 2023 /PRNewswire/ -- The "Patient Centric Healthcare App Market: Global Industry Trends, Share, Size, Growth, Opportunity and Forecast 2023-2028" report has been added to ResearchAndMarkets.com's offering. The report offers in-depth insights into the fast-evolving landscape of the global patient-centric healthcare app market, emphasizing its growth trajectory, key market trends, and potential opportunities. The global patient-centric healthcare app market reached a monumental US$ 10.4 Billion in 2022. As per the analysis, the market is projected to soar to an impressive US$ 32.4 Billion by 2028, marking a CAGR of 20.85% during the 2022-2028 period. This substantial growth can be attributed to the increased collaboration between mobile app developers and healthcare experts, which has resulted in applications that offer uninterrupted access to vital health services even without an internet connection. These transformative apps serve to amplify patient-healthcare professional interactions and cater to individual health needs. Users can monitor vital health aspects, manage chronic diseases, and interact seamlessly with healthcare professionals. Furthermore, with a significant uptick in telehealth utilization due to the COVID-19 outbreak, the demand for patient-centric healthcare apps has surged globally. Key market trends highlighted in the report include: Uninterrupted Access: Mobile app developers, in collaboration with healthcare experts, are designing apps that can function without internet connectivity, ensuring continued access to vital health data and services. Health Monitoring & Management: These apps aid in chronic disease management, tracking nutritional intake, smoking cessation, vaccinations, and even enable the personalization of treatments based on individual patient needs. The rise in wearable devices further bolsters the market as they can monitor diverse health metrics, including heart rate and sleep patterns. Enhanced Patient Involvement: Patient-centric apps are increasingly being adopted by cancer patients to log medications, monitor treatment progress, note side effects, and set follow-up appointments, underscoring the depth of their utility. The report also provides a detailed market segmentation: By Technology: Phone-Based Apps, Web-Based Apps, Wearable Patient Centric Apps By Operating System: iOS, Android, Windows, and Others By Application: Wellness Management and Disease and Treatment Management By End User: Hospitals, Clinics, and Home Use By Region: North America, Asia-Pacific, Europe, Latin America, and the Middle East and Africa. Furthermore, the competitive landscape reveals key industry players, including Allscripts Healthcare Solutions Inc., Athenahealth Inc., Bayer Aktiengesellschaft, Boston Scientific Corporation, Hill-Rom Services Inc. (Baxter International Inc.), iPatientCare LLC, Koninklijke Philips N.V., Merck & Co. Inc., Mobilesmith Inc., Pfizer Inc., and Siemens Healthineers AG (Siemens AG). For a detailed breakdown, analysis, and to tap into the lucrative growth opportunities the patient-centric healthcare app market offers, visit About ResearchAndMarkets.com ResearchAndMarkets.com is the world's leading source for international market research reports and market data. We provide you with the latest data on international and regional markets, key industries, the top companies, new products and the latest trends. Media Contact: Research and Markets Laura Wood, Senior Manager [email protected] For E.S.T Office Hours Call +1-917-300-0470 For U.S./CAN Toll Free Call +1-800-526-8630 For GMT Office Hours Call +353-1-416-8900 U.S. Fax: 646-607-1907 Fax (outside U.S.): +353-1-481-1716 Logo: SOURCE Research and Markets

2023-09-29

·PRNewswire

Real-World Evidence and Data Analytics Conference (Frankfurt, Germany - October 5-6, 2023): Paving the Path for Next-Gen Medicinal Research

DUBLIN, Sept. 29, 2023 /PRNewswire/ -- The "Real-World Evidence and Data Analytics Conference" set to take place on October 5th and 6th, 2023, in Frankfurt, Germany has been added to ResearchAndMarkets.com's offering. Building on five triumphant installments held in Boston, USA, this year's European chapter promises an invigorating assembly of experts, leaders, and stakeholders. The confluence aims to shed light on the accelerating evolution of real-world evidence (RWE) and its vital impact on drug benefit elucidation. RWE, hinging on real-world data analysis, is transforming healthcare by expediting regulatory decision-making processes. Its pivotal role in patient monitoring through digital platforms, coupled with aiding clinical data organization for regulatory inclusions, is noteworthy. However, to fully harness its potential, industry leaders emphasize the importance of comprehensive guidelines and shared annotations. Conference Highlights: Delving into regulatory parameters concerning data quality & standards Exploiting RWE for superior market accessibility Embracing the nexus between AI, ML, and clinical trials Broadening RWE's role in the digital health domain Advanced analytical approaches to real-world data Employing RWE to inform decisions in rare diseases Who Should Participate?: Professionals from pharmaceutical and biopharmaceutical sectors, specifically those vested in RWE, data analytics, HEOR, market access, clinical development, epidemiology, oncology-RWE, pharmacovigilance, life science analytics, big data, data science, and more. Speakers Spotlight: Helene Vioix, Director Global Evidence & Value Development Oncology, Merck KGaA Antje Hottgenroth, Associate Director, Real World Data Europe/International Value, Evidence, and Outcomes (VEO) - Center of Innovation, Lilly Deutschland GmbH Ahmed H. Seddik, Senior Manager, Global HEOR & RWE, Oncology, Daiichi Sankyo Europe GmbH Beyond keynotes and panel discussions, attendees will benefit from extensive networking opportunities and direct interactions with esteemed speakers from leading pharmaceutical firms, global regulatory bodies, and innovative solution providers. Agenda: Day 1 Thu, 05-Oct-2023 Keynote- Real World Data - To Drive Integrated Evidence Generation Maximizing the influence of RWD in cases of Rare Diseases Role of Data Quality in advancing the use of RWE for Regulatory Decision Making Application of RWD/RWE in Strategy Framework and Regulatory Considerations Solution Providers Presentation Panel Discussion - Creating Value from Next Generation RWE Research and Related Initiatives to Evaluate and Improve RWD for Evidence Generation RWD in Drug Development Program Evening Refreshments and Poster Presentation - One-to-One Networking Current Trends in Patient-Centric Clinical Research amid the Rapidly evolving Landscape Patient Engagement Strategy and Execution Achieving Patient Diversity using RWE in Clinical Trials Day 2 Fri, 06-Oct-2023 RWE- Trends in Global Market and Network Access Patient Access to Precision Medicine Oncology Obtain Insight into HEOR Complexities, Parameters and Opportunities Global Landscape around Real- World Evidence Panel Discussion - Patient Engagement Strategy and Execution Pricing Market Access Strategies Case Studies Assessing Patient centered approach to value-based approach Secure Your Seat: To further explore the conference details, please visit About ResearchAndMarkets.com ResearchAndMarkets.com is the world's leading source for international market research reports and market data. We provide you with the latest data on international and regional markets, key industries, the top companies, new products and the latest trends. Media Contact: Research and Markets Laura Wood, Senior Manager [email protected] For E.S.T Office Hours Call +1-917-300-0470 For U.S./CAN Toll Free Call +1-800-526-8630 For GMT Office Hours Call +353-1-416-8900 U.S. Fax: 646-607-1907 Fax (outside U.S.): +353-1-481-1716 Logo: SOURCE Research and Markets

2023-09-29

·PMLiVE

Austrian State Secretary to speak at FlyPharma Europe 2023

FlyPharma Europe will welcome Mr Florian Tursky, the Austrian State Secretary, to the conference on 10 October, where he will deliver an opening speech. He will join a host of expert industry speakers from both pharma and cargo sectors With just over a week to go until the conference doors open, there is still time to register for your place at FlyPharma Europe and hear this important address from the State Secretary. With your ticket, as well as access to a series of networking events and a Vienna Airport site tour, you will get industry insights from pharma speakers such as: You will also hear from experienced logistics and cargo companies, including: About FlyPharma Conference Europe 2023 FlyPharma Europe is an event for the pharma logistics industry, connecting professionals from across the globe to advance the sector and set new industry standards. With a focus on addressing key shared challenges, highlighting best practices and fostering collaboration, FlyPharma Europe provides a unique platform to learn, network and drive innovation. Vienna AirportCity are Host Sponsors of FlyPharma Europe 2023 and will offer delegates a site tour of the airport’s state-of-the-art pharmaceutical handling facilities. Join us for this year's event, taking place on 10-11 October in Vienna, Austria, to stay ahead of industry developments and connect with thought leaders. Register now to secure your place at https://flypharmaeurope.com/tickets .

管线布局

2023年10月04日管线快照

管线布局中药物为当前组织机构及其子机构作为药物机构进行统计，早期临床1期并入临床1期，临床1/2期并入临床2期，临床2/3期并入临床3期

药物发现

临床前

临床申请

临床1期

临床2期

临床3期

申请上市

117

批准上市

其他

1186

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当前项目

药物(靶点)	适应症	全球最高研发状态

苄星青霉素 ( PBPs )	细菌感染更多	批准上市
麻疹/腮腺炎/风疹/水痘减毒活疫苗(Merck & Co., Inc.)	风疹更多	批准上市
西司他丁钠/亚胺培南 ( Enzymes + PBPs )	简单的皮肤和皮肤结构感染(uSSSI) 更多	批准上市
依折麦布 ( NPC1L1 )	家族性混合型高脂血症更多	批准上市
盐酸多佐胺 ( CAs )	高眼压症更多	批准上市