Phase 1, Open Label, Single Dose Study to Investigate the Effect of Renal Impairment on the Pharmacokinetics of Enpatoran in Male and Female Participants

The purpose of this study is to assess the effect of renal impairment on the pharmacokinetics of enpatoran.

开始日期2024-09-24

申办/合作机构

Merck Healthcare KGaA

[+1]

NCT06589726

/ Completed临床1期

A Single-Dose, Randomized, Double-Blind, Placebo- and Positive-Controlled, 4-Way Crossover Study to Evaluate the Effect of Enpatoran on the QTc (Corrected QT) Interval in Healthy Adult Participants

The purpose of this study is to assess potential effects of enpatoran on cardiac repolarization (i.e. prolongation of QT interval).

开始日期2024-09-10

申办/合作机构

Merck Healthcare KGaA

[+1]

CTR20222533

/ Recruiting临床2期

一项II 期、双盲、剂量范围探索、平行分组、长期扩展研究，在已完成WILLOW（MS200569_0003）研究治疗的亚急性皮肤红斑狼疮、盘状红斑狼疮和/或系统性红斑狼疮受试者中，评价Enpatoran 的安全性和有效性

主要目的：评价enpatoran在SCLE、DLE和/或SLE受试者中的长期安全性和耐受性。次要目的：评价enpatoran在SCLE、DLE和/或SLE受试者中的长期安全性和耐受性及疾病控制方面的长期有效性；第三/探索性目的：评价enpatoran在SCLE、DLE和/或SLE受试者中的疾病控制方面的长期有效性；评价enpatoran在SLE受试者中的疾病控制方面的长期有效性；评价enpatoran在SCLE、DLE和/或SLE受试者中对患者报告的症状和功能状态方面的长期有效性；评价enpatoran在活动性SLE受试者中对患者报告的症状和功能状态方面的长期有效性；研究活动性SLE受试者中，Enpatoran对生物标志物的影响；研究Enpatoran对免疫细胞亚群和免疫球蛋白的影响；研究Enpatoran对PD生物标志物的影响；通过稀疏PK采样采集enpatoran血浆浓度数据；评价enpatoran对疫苗免疫状态的长期影响。评价Enpatoran对比安慰剂对活动性狼疮皮疹受试者红斑的影响。

开始日期2023-03-16

申办/合作机构

R-Pharm Germany GmbH初创企业

[+3]

100 项与 Enpatoran 相关的临床结果

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100 项与 Enpatoran 相关的转化医学

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100 项与 Enpatoran 相关的专利（医药）

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项与 Enpatoran 相关的文献（医药）

2024-10-01·British Journal of Pharmacology

Factor XII and prekallikrein promote microvascular inflammation and psoriasis in mice

Article

作者: Wang, Miao ; Wan, Qing ; Zhang, Yurong ; Rao, Haojie ; Li, Huihui ; Xu, Pengfei ; Yang, Jianfeng ; Zhang, Yingjie ; Guo, Junyan ; Chen, Zengrong ; Chen, Hong

Background and Purpose:

Psoriasis is an autoimmune inflammatory skin disease, featuring microvascular abnormalities and elevated levels of bradykinin. Contact activation of Factor XII can initiate the plasma kallikrein‐kinin cascade, producing inflammation and angioedema. The role of Factor XII in psoriasis is unknown.

Experimental Approach:

The effects of deficiency of Factor XII or its enzymatic substrate, prekallikrein, were examined in the imiquimod‐induced mouse model of psoriasis. Skin microcirculation was assessed using intravital confocal microscopy and laser Doppler flowmeter. A novel antibody blocking Factor XII activation was evaluated for psoriasis prevention.

Key Results:

Expression of Factor XII was markedly up‐regulated in human and mouse psoriatic skin. Genetic deletion of Factor XII or prekallikrein, attenuated imiquimod‐induced psoriatic lesions in mice. Psoriatic induction increased skin microvascular blood perfusion, causing vasodilation, hyperpermeability and angiogenesis. It also promoted neutrophil‐vascular interaction, inflammatory cytokine release and enhanced Factor XII / prekallikrein enzymatic activity with elevated bradykinin. Factor XII or prekallikrein deficiency ameliorated these microvascular abnormalities and abolished bradykinin increase. Antagonism of bradykinin B2 receptors reproduced the microvascular protection of Factor XII / prekallikrein deficiency, attenuated psoriatic lesions, and prevented protection by Factor XII / prekallikrein deficiency against psoriasis. Furthermore, treatment of mice with Factor XII antibody alleviated experimentally induced psoriasis and suppressed microvascular inflammation.

Conclusion and Implications:

Activation of Factor XII promoted psoriasis via prekallikrein‐dependent formation of bradykinin, which critically mediated psoriatic microvascular inflammation. Inhibition of contact activation represents a novel therapeutic strategy for psoriasis.

2024-10-01·CTS-Clinical and Translational Science

Asia‐inclusive drug development leveraging principles of ICH E5 and E17 guidelines: Case studies illustrating quantitative clinical pharmacology as a foundational enabler

Review

作者: Kuroki, Yoshihiro ; Venkatakrishnan, Karthik ; Bolleddula, Jayaprakasam ; Dong, Jennifer ; Strotmann, Rainer ; Lu, Hong ; Klopp‐Schulze, Lena ; Mukker, Jatinder Kaur ; Gao, Wei ; Terranova, Nadia ; Li, Dandan ; Goteti, Kosalaram

Abstract:

With the International Conference on Harmonization of Technical Requirements for Pharmaceuticals for Human Use (ICH) E17 guidelines in effect from 2018, the design of Asia‐inclusive multiregional clinical trials (MRCTs) has been streamlined, thereby enabling efficient simultaneous global development. Furthermore, with the recent regulatory reforms in China and its drug administration joining the ICH as a full regulatory member, early participation of China in the global clinical development of novel investigational drugs is now feasible. This would also allow for inclusion of the region in the geographic footprint of pivotal MRCTs leveraging principles of the ICH E5 and E17. Herein, we describe recent case examples of model‐informed Asia‐inclusive global clinical development in the EMD Serono portfolio, as applied to the ataxia telangiectasia and Rad3‐related inhibitors, tuvusertib and berzosertib (oncology), the toll‐like receptor 7/8 antagonist, enpatoran (autoimmune diseases), the mesenchymal–epithelial transition factor inhibitor tepotinib (oncology), and the antimetabolite cladribine (neuroimmunological disease). Through these case studies, we illustrate pragmatic approaches to ethnic sensitivity assessments and the application of a model‐informed drug development toolkit including population pharmacokinetic/pharmacodynamic modeling and pharmacometric disease progression modeling and simulation to enable early conduct of Asia‐inclusive MRCTs. These examples demonstrate the value of a Totality of Evidence approach where every patient's data matter for de‐risking ethnic sensitivity to inter‐population variations in drug‐ and disease‐related intrinsic and extrinsic factors, enabling inclusive global development strategies and timely evidence generation for characterizing benefit/risk of the proposed dosage in Asian populations.

2024-06-01·Clinical pharmacology and therapeutics

Asia‐Inclusive Global Development of Enpatoran: Results of an Ethno‐Bridging Study, Intrinsic/Extrinsic Factor Assessments and Disease Trajectory Modeling to Inform Design of a Phase II Multiregional Clinical Trial

Article

作者: Gopalakrishnan, Sathej ; Krebs‐Brown, Axel ; Nogueira Filho, Marco ; Lu, Hong ; Goteti, Kosalaram ; Shaw, Jamie ; Kuroki, Yoshihiro ; Gradhand, Ulrike ; Klopp‐Schulze, Lena ; Dong, Jennifer ; Fluck, Markus ; Yalkinoglu, Özkan ; Venkatakrishnan, Karthik

Enpatoran is a novel, highly selective, and potent dual toll‐like receptor (TLR)7 and TLR8 inhibitor currently under development for the treatment of autoimmune disorders including systemic lupus erythematosus (SLE), cutaneous lupus erythematosus (CLE), and myositis. The ongoing phase II study (WILLOW; NCT05162586) is evaluating enpatoran for 24 weeks in patients with active SLE or CLE and is currently recruiting. To support development of WILLOW as an Asia‐inclusive multiregional clinical trial (MRCT) according to International Conference on Harmonisation E5 and E17 principles, we have evaluated ethnic sensitivity to enpatoran based on clinical pharmacokinetic (PK), pharmacodynamic (PD), and safety data from an ethno‐bridging study (NCT04880213), supplemented by relevant quantitative PK, PD, and disease trajectory modeling (DTM) results, and drug metabolism/disease knowledge. A single‐center, open‐label, sequential dose group study in White and Japanese subjects matched by body weight, height, and sex demonstrated comparable PK and PD properties for enpatoran in Asian vs. non‐Asian (White and other) subjects across single 100, 200, and 300 mg orally administered doses. DTM suggested no significant differences in SLE disease trajectory for Asian vs. non‐Asian individuals. Aldehyde oxidase (AOX) is considered to be a key contributor to enpatoran metabolism, and a literature review indicated no relevant ethnic differences in AOX function based on in vitro and clinical PK data from marketed drugs metabolized by AOX, supporting the conclusion of low ethnic sensitivity for enpatoran. Taken together, the inclusion of Asian patients in MRCTs including WILLOW was informed based on a Totality of Evidence approach.

项与 Enpatoran 相关的新闻（医药）

2024-11-04

·PRNewswire

Lupus Research Alliance Announces Lupus Research Highlights at ACR Convergence 2024

Sixteen presentations of preclinical studies funded by the Lupus Research Alliance (LRA) to advance understanding of lupus and potential treatment pathways, including four oral presentations Two reports by Lupus Therapeutics, the clinical affiliate of the LRA, and the Lupus Clinical Investigators Network (LuCIN) on promoting equity in lupus clinical trials, and identifying trial barriers and solutions Fifteen industry-sponsored clinical research studies supported by Lupus Therapeutics and LuCIN, including positive results from the late-breaking Phase 3 dapirolizumab pegol trial NEW YORK, Nov. 4, 2024 /PRNewswire/ -- The Lupus Research Alliance (LRA), the largest private funder of lupus research worldwide, today announced that a total of 33 studies, funded by the organization or supported by its clinical research affiliate Lupus Therapeutics, will be presented at ACR Convergence 2024. The annual meeting of the American College of Rheumatology takes place November 14-19, at the Walter E. Washington Convention Center in Washington, D.C. The LRA, which seeks to accelerate the discovery and development of patient-centered treatments and diagnostics, pursues strategies to spur advancements from "bench to bedside." LRA-supported studies presented at ACR Convergence 2024 represent the full continuum of lupus research, from foundational research exploring new avenues of knowledge, to clinical trials evaluating potential new treatments. "ACR Convergence 2024 is met with pride and excitement by the Lupus Research Alliance and Lupus Therapeutics – pride in seeing the fruits of our funding and other initiatives to accelerate drug discovery and development, and excitement as we stand on the precipice of some important advancements," said LRA President and CEO Albert T. Roy. "There are more trials in mid-to-late-stage development than ever before, including dapirolizumab pegol in Phase 3 from UCB/Biogen, a Lupus Therapeutics partner. And we are gratified to witness the volume of CAR T cell therapy approaches in clinical development, having invested in 2014 in early research suggesting this approach as a promising intervention to explore for treating lupus," Roy added. Foundational Research Funded by the LRA Sixteen studies of LRA-funded research (four oral presentations and 12 posters) will be presented. Several focus on Childhood-Onset Systemic Lupus Erythematosus (cSLE), including: a detailed characterization of the disease; the effects of fatigue on pediatric patients' mental and physical health; and the discovery of Anti-Mitochondrial Antibodies (AMA), which are linked to higher disease activity. Other studies include: the development of a precision immunotherapy to target harmful B cells in Antiphospholipid Syndrome (APS) patients; the discovery of innate signaling pathways crucial in causing inflammation in lupus patients; and the epidemiology of strokes in children and adults with lupus. ORAL PRESENTATIONS Saturday, Nov. 16 Abstract #0837: Bispecific Autoantigen-T Cell Engagers (BaiTE) to Selectively Target Autoreactive B Cells in Antiphospholipid Syndrome 3:00-3:15 PM, Room 103AB Sunday, Nov. 17 Abstract #1702: Placental Developmental Defects in a Humanized-TLR8 Mouse Model of Spontaneous Anti-Phospholipid Antibody Induced Pregnancy Loss 3:15-3:30 PM , Room 103AB Monday, Nov. 18 Xist and XChromosome Inactivation in Female Biased Autoimmunity 9:00-9:30 AM, Room 145AB Abstract #2625: Brain Injury Markers Correlate with Impaired Executive Function and Disease Activity in Children with Systemic Lupus Erythematosus 3:30-3:45 PM, Room 202AB POSTERS Saturday, Nov. 16 Poster Session A, 10:30 AM-12:30 PM, Poster Hall: Abstract #0091: Targeting Endothelial Dysfunction in Lupus Nephritis: Effect of Sepiapterin, a Drug That Restores Endothelial Nitric Oxide Synthase Function, in a Murine Model of Lupus Nephritis Abstract #0098: Anti-HSP90α as a Protective Natural Antibody Against Secondary Antiphospholipid Syndrome in Systemic Lupus Erythematosus Sunday, Nov. 17 Poster Session B, 10:30 AM-12:30 PM , Poster Hall: Abstract #1266: Anti-Mitochondrial Antibodies Associate with Disease Activity and IFNα Expression in Childhood-onset Systemic Lupus Erythematosus Abstract #1273: An Investigation of Traumatic Events and Mental Health in cSLE Abstract #1274: Comparing Performance-Based Measures and Self-Reported Questionnaires for Assessment of Executive Function for Youth with Childhood-Onset Systemic Lupus Erythematosus Abstract #1278: The Effects of Fatigue on Self-Reported Mental and Physical Health in Childhood-Onset Systemic Lupus Erythematosus: A Cross-Sectional Study Abstract #1279: Cerebrovascular Accidents in Pediatric and Adult Systemic Lupus Erythematosus: A Comparison of Epidemiology and Outcomes Abstract #1280: Abnormal Cortical Gyrification Patterns in Adolescents with Childhood-onset SLE: Early Associations with Perceived Fatigue Abstract #1504: Novel Analytes Associated with Cognitive Impairment in Patients with Systemic Lupus Erythematosus: Serum S100A8/A9, MMP-9 and IL-6 Abstract #1506: Cognitive Impairment Prevalence and Most Affected Domains in Patients with SLE by the ACR Comprehensive Neuropsychological Battery Monday, Nov. 18 Poster Session C, 10:30 AM-12:30 PM, Poster Hall: Abstract #1788: Memory B Cell Activation and Dysregulation in Systemic Lupus Erythematosus Abstract #2380: Characterizing SLE Patients into Type 1 and Type 2 Disease States: Insights from a Single Lupus Cohort Research Conducted by Lupus Therapeutics and the Lupus Clinical Investigators Network (LuCIN) Lupus Therapeutics, the clinical affiliate of the Lupus Research Alliance, oversees the Lupus Clinical Investigators Network (LuCIN), consisting of 50+ premier, leading medical research institutions in North America, comprised of 200+ providers with expertise in lupus care and clinical trials. The following studies are based on annual surveys of LuCIN investigators and research teams on promoting equity in lupus clinical trials and identifying trial barriers and solutions. POSTERS Saturday, Nov. 16 Abstract 0180: Collaborative Solutions to Lupus Trial Challenges for Underrepresented Participant Recruitment & Engagement: Perspectives from the Lupus Clinical Investigators Network (LuCIN) Poster Session A, 10:30 AM-12:30 PM, Poster Hall Sunday, Nov. 17 Abstract #1039: Through the LuCIN Lens: Defining Barriers and Forging Solutions for Lupus Clinical Trials in North America Poster Session B, 10:30 AM-12:30 PM, Poster Hall Clinical Research Supported by Lupus Therapeutics and LuCIN The primary goal of Lupus Therapeutics and LuCIN is to accelerate and enhance the quality of lupus clinical trials through clinical expertise, advisory services, patient engagement and partnership/collaboration with biopharmaceutical companies and research partners. Lupus Therapeutics and LuCIN are involved in nearly 25% of active lupus clinical trials. Fifteen Lupus Therapeutics/LuCIN-supported programs and collaborations are being presented at ACR Convergence 2024: ORAL PRESENTATIONS Sunday, Nov. 17 Abstract #1773: Safety and Efficacy of CABA-201, a Fully Human, Autologous 4-1BB Anti-CD19 CAR T Cell Therapy in Patients with Immune-Mediated Necrotizing Myopathy and Systemic Lupus Erythematosus from the RESET-MyositisTM and RESET-SLETM Clinical Trials 3:30-3:45 PM, Room 145AB Monday, Nov. 18 Abstract #2577: Efficacy and Safety of ABBV-599 (Elsubrutinib and Upadacitinib Combination) and Upadacitinib Monotherapy for the Treatment of Systemic Lupus Erythematosus: Results Through 104 Weeks in a Long-Term Extension Study 1:30-1:45 PM, Room 146AB Abstract #2580: Safety and Efficacy of Subcutaneous Ianalumab (VAY736) for up to 68 Weeks in Patients with Systemic Lupus Erythematosus: Results from Phase 2 Study 2:15-2:30 PM Room 146AB Tuesday, Nov. 19 ***LATE-BREAKING ABSTRACT*** Abstract #L16: Dapirolizumab Pegol Demonstrated Significant Improvement in Systemic Lupus Erythematosus Disease Activity: Efficacy and Safety Results of a Phase 3 Trial 8:00-9:30 AM, 146AB POSTERS Saturday, Nov. 16 Poster Session A, 10:30 AM-12:30 PM, Poster Hall: Abstract #0087: SYNCAR: An Engineered IL-2/IL-2R-system That Selectively Enhances CD19 CAR T Cells to Deplete B Cells and Provide Therapeutic Benefit in SLE and RA Mouse Models Without Lymphodepletion Abstract #0324: Correlative Studies of CABA-201, a Fully Human, Autologous 4-1BB Anti-CD19 CAR T Cell Therapy in Patients with Immune-Mediated Necrotizing Myopathy and Systemic Lupus Erythematosus from the RESET-MyositisTM and RESET-SLETM Clinical Trials Abstract #0620: Clinical Efficacy and Patient-Reported Outcomes in Anti-Ro/Sjögren's Syndrome–Related Antigen a Antibody–Positive Patients with Active SLE Treated With Deucravacitinib in the Phase 2 PAISLEY Trial Abstract #0659: Obinutuzumab Benefits Patients with Active Lupus Nephritis Irrespective of Baseline Proteinuria Severity: A Post Hoc Analysis of a Phase II Trial Abstract #0662: Deucravacitinib, a First-in-Class, Oral, Selective, Allosteric Tyrosine Kinase 2 Inhibitor, in SLE: Efficacy by Baseline Demographics and Disease Characteristics in the Phase 2 PAISLEY Trial Abstract #0671: Effect of Litifilimab on Cutaneous Lupus Disease Area and Severity Index–Activity (CLASI-A) Subcomponents and Physician Global Assessment–Skin (PGA–Skin) in Patients with Cutaneous Lupus Erythematosus (CLE) in a Phase 2 Study Sunday, Nov. 17 Poster Session B, 10:30 AM-12:30 PM, Poster Hall: Abstract #1496: Dysregulated Serum Cytokines in Association with Clinical Manifestations in Patients with Systemic Lupus Erythematosus Abstract #1552: Kinetics of Mucocutaneous and Musculoskeletal Responses to Deucravacitinib in Patients with Active SLE in the Phase 2 PAISLEY Trial Abstract #1553: Safety, Pharmacokinetics, Clinical Efficacy and Exploratory Biomarker Results from a Randomized, Double-Blind, Placebo-Controlled Phase 1b Study of Enpatoran in Active Systemic and Cutaneous Lupus Erythematosus (SLE/CLE) Monday, Nov. 18 Poster Session C, 10:30 AM-12:30 PM, Poster Hall: Abstract #2425: Ianalumab Induced Durable Depletion of Circulating B Cell Subsets and Associated Changes in B Cell and Neutrophil Transcriptomic and Proteomic Profiles in Patients with Systemic Lupus Erythematosus: 52-Week Treatment Results from a Phase 2 Trial Abstract #2430: Dapirolizumab Pegol Impacts Important Immunologic Pathways in Systemic Lupus Erythematosus: Pharmacodynamic Analysis of T Cell and Antigen Presenting Cell Pathways from a Phase 2b Trial About Lupus Lupus is a chronic, complex autoimmune disease that affects millions of people worldwide. In lupus, the immune system, meant to defend against infections, produces autoantibodies that mistake the body's own cells as foreign, causing other immune cells to attack organs such as the kidneys, brain, heart, lungs and skin, as well as blood and joints. Ninety percent of people with lupus are women, most often diagnosed between the ages of 15-45. Black, Latinx, Indigenous, Asian and Pacific Islander people are disproportionately affected by lupus and more likely to experience severe lupus symptoms. About the Lupus Research Alliance The Lupus Research Alliance is the largest non-governmental, non-profit funder of lupus research worldwide. The organization aims to transform treatment by funding the most innovative lupus research, fostering diverse scientific talent, and driving discovery toward better diagnostics, improved treatments and ultimately a cure for lupus. Because the Lupus Research Alliance's Board of Directors funds all administrative and fundraising costs, 100% of all donations goes to support lupus research programs. For more information, please visit the LRA at LupusResearch.org and on social media at: X, Facebook, LinkedIn, and Instagram. About Lupus Therapeutics Lupus Therapeutics, the clinical research affiliate of the Lupus Research Alliance, aims to accelerate the development of curative treatments for all patients living with lupus. Lupus Therapeutics collaborates with premier research institutions, biopharmaceutical partners, and those living with lupus through the unprecedented Lupus Clinical Investigators Network (LuCIN) to drive rapid and meaningful progress in treatment development. The organization elevates the patient voice, engages community stakeholders, and strives for representation of the diverse lupus community in the clinical research process with the most innovative and renowned experts throughout North America. Visit LupusTherapeutics.org for more information. This information is brought to you by the Lupus Research Alliance and is not sponsored by, nor a part of, the American College of Rheumatology. SOURCE Lupus Research Alliance WANT YOUR COMPANY'S NEWS FEATURED ON PRNEWSWIRE.COM? 440k+ Newsrooms & Influencers 9k+ Digital Media Outlets 270k+ Journalists Opted In GET STARTED

临床2期临床结果临床3期免疫疗法

2024-10-16

·Merck Group

Capital Markets Day 2024: Merck KGaA, Darmstadt, Germany, Reiterates Confidence in Returning to Sustainable Growth

Tailwind thanks to robust global growth trends in all three business sectors Life Science to be back on course as company’s growth engine Healthcare with ambition for mid-single-digit long-term growth Age of artificial intelligence (AI) drives medium-term growth upgrade for Electronics Acquisitions remain an integral component of company strategy Merck KGaA, Darmstadt, Germany, a leading science and technology company, is looking confidently toward the future. At today’s Capital Markets Day, the company shared its expectation of profitable and financially strong growth in the coming years. After the transitional year of 2023, Merck KGaA, Darmstadt, Germany, considers the medium-term growth opportunities in its markets to be intact. With its three business sectors, the company is in a strong strategic position to partake in these opportunities. In Electronics, which develops solutions for the semiconductor and display industries, the Group even expects business performance to accelerate in the next few years. This is thanks in particular to the trend toward artificial intelligence. “We committed to return to growth in 2024 and this is materializing already,” said Belén Garijo, Chair of the Executive Board and CEO of Merck KGaA, Darmstadt, Germany. “Furthermore, we are well positioned to deliver sustainable growth through innovation and our high-performing global talent.” Innovations as growth drivers Merck KGaA, Darmstadt, Germany, relies on its diversified business model to spark discovery and elevate humanity in accordance with its new company vision. In its Life Science business sector, the company sees the globally growing later-stage pipeline of complex molecules and novel modalities, among other things, as key growth drivers. Novel modalities include new therapies such as viral vector-based cell and gene therapies, antibody-drug conjugates (ADCs), and mRNA applications. The company has in-depth knowledge and offers a broad portfolio of products and services in these areas. ADCs are experiencing remarkable growth, for example. The Group has significantly increased its ADC and highly potent active pharmaceutical ingredient (HPAPI) capacities in recent years. In Healthcare, Merck KGaA, Darmstadt, Germany, takes up leading positions in therapeutic areas within its Fertility and Cardiovascular, Metabolic & Endocrinology franchises, leveraging the company’s broad geographical footprint. Innovations in Oncology and Neurology & Immunology will continue to drive long-term growth. In June 2024, the company started a Phase III trial with cladribine capsules to treat the neurological disease myasthenia gravis. With enpatoran, developed for lupus erythematosus, it expects the full Phase II readout in early 2025. For pimicotinib [1] for the treatment of benign tumors of the joints, the Phase III readout is expected later this year. In addition, the company is executing its early-stage oncology development strategy, which it outlined in its R&D update call earlier this year . In the Electronics business sector, Merck KGaA, Darmstadt, Germany, has deliberately focused on solutions for the semiconductor and display industries. The company supports its customers in developing ever smaller, more powerful, and more efficient chips, among other things. In doing so, it helps to meet global demand for AI applications and modern semiconductors. For example, with the intended acquisition of Unity-SC , the Group will expand its portfolio with high-precision metrology instruments to optimize the quality and production yield and thus also the manufacturing costs of chips for its customers. Merck KGaA, Darmstadt, Germany, is also recording growing sales from sustainable solutions. For example, the company has increased its portfolio of more sustainable products in Life Science by an average of 30% annually since 2020. For example, Milli-Q ® systems for the purification of lab water that contain the ERA ™ technology can save up to 50% in water usage compared with other systems. The company’s innovative power drives organic growth. At the same time, the strong market position and stringent cost management of Merck KGaA, Darmstadt, Germany, ensure good profitability. It intends to normalize its current capital expenditure (capex) of approximately € 1.6 billion to € 1.8 billion per year at a slightly lower level once again from 2026 onwards. In previous years, the company had significantly increased its capex to prepare for medium- and long-term growth trends by expanding capacities in research and development as well as production, for example. Having reached these goals, Merck KGaA, Darmstadt, Germany, now expects less capital-intensive growth, which will facilitate stronger cash flow development. Strategic acquisitions Acquisitions also remain an integral component of the strategy of Merck KGaA, Darmstadt, Germany. On July 31, 2024, it acquired Mirus Bio . The U.S. life science company specializes in transfection reagents, which help introduce genetic material into cells and play a key role in the production of viral vectors for cell and gene therapies. Also in July 2024, Merck KGaA, Darmstadt, Germany, announced the acquisition of Unity-SC . For larger future transactions, the company is focusing on the Life Science business sector. The company will additionally intensify the in-licensing of drug candidates in Healthcare. Belén Garijo said: “M&A remains a key priority for us. And we remain disciplined and patient in our approach in order to maximize the strategic impact of any acquisitions. Our guiding principle is and always has been: The right target, at the right time, for the right price.” Medium-term ambitions: Growth trends in the markets remain intact At Capital Markets Day 2024, Merck KGaA, Darmstadt, Germany, slightly adjusted the mid-term growth ambitions for its three business sectors. The company is confident that the growth opportunities in its markets remain intact after the transitional year of 2023. It expects the following average annual organic sales growth rates: Life Science: 7% to 9% (previously: 7% to 10%) and therefore still above the market average. The main reason for the refined ambition is the updated view on China’s mid-term growth prospects. Healthcare: slight growth (previously: growth in the mid-single-digit percentage range). This is due to the recently announced pipeline setbacks. In the long term, the company intends to return to growth in the mid-single-digit percentage range, also supported by external innovation. Electronics: 5% to 9%, a significant uplift from the previous 3% to 6%. This is largely driven by Electronics becoming a pure play in the areas of Semiconductor and Display Solutions and enabling the trend toward artificial intelligence. The company benefits here from its unique position as a supplier of semiconductor solutions that meet the high demands of chips for AI applications. Company confirms guidance for fiscal 2024 For fiscal 2024, Merck KGaA, Darmstadt, Germany, confirms its guidance and the return to profitable growth : Sales: between € 20.7 billion and € 22.1 billion (organic growth: +2% to +5%). EBITDA pre: between € 5.8 billion and € 6.4 billion (organic growth: +4% to +10%). EPS pre: € 8.20 to € 9.30. [1] Sponsor: Abbisko Therapeutics Co. Ltd.; Merck KGaA, Darmstadt, Germany, holds an exclusive license to commercialize pimicotinib in China, Hong Kong, Macau, and Taiwan, with an option for the rest of the world. About Merck KGaA, Darmstadt, Germany Merck KGaA, Darmstadt, Germany, a leading science and technology company, operates across life science, healthcare and electronics. Around 63,000 employees work to make a positive difference to millions of people’s lives every day by creating more joyful and sustainable ways to live. From providing products and services that accelerate drug development and manufacturing as well as discovering unique ways to treat the most challenging diseases to enabling the intelligence of devices – the company is everywhere. In 2023, Merck KGaA, Darmstadt, Germany, generated sales of € 21 billion in 65 countries. The company holds the global rights to the name and trademark “Merck” internationally. The only exceptions are the United States and Canada, where the business sectors of Merck KGaA, Darmstadt, Germany, operate as MilliporeSigma in life science, EMD Serono in healthcare and EMD Electronics in electronics. Since its founding in 1668, scientific exploration and responsible entrepreneurship have been key to the company’s technological and scientific advances. To this day, the founding family remains the majority owner of the publicly listed company. All Merck KGaA, Darmstadt, Germany, press releases are distributed by e-mail at the same time they become available on the EMD Group website. In case you are a resident of the USA or Canada, please go to www.emdgroup.com/subscribe to register for your online, change your selection or discontinue this service.

并购临床3期引进/卖出

2024-08-01

·Insight数据库

默克上半年财报：制药业务收入超 41 亿欧元；肿瘤产品收入增长超 14%

8 月 1 日，德国默克（Merck KGaA）发布了 2024 年第二季度和上半年财报。该集团所有业务净销售额增长 1.7% 至 54 亿欧元。其中，该公司的制药业务（Healthcare）第二季度销售额为 21.37 亿欧元，增长 5.3%；上半年销售额为 41.84 亿欧元，增长 7.6%。报告指出，这一增长主要得益于肿瘤、心血管、代谢和内分泌学领域的收入增长。肿瘤领域肿瘤业务第二季度收入为 4.9 亿欧元，增长 9.2%；上半年收入为 9.9 亿欧元，增长 14.1%。截图来自：默克财报 Erbitux（西妥昔单抗）在肿瘤领域，EGFR 单抗 Erbitux 仍然是默克最畅销的抗癌药物，该药第二季度销售额为 2.76 亿欧元，增长 8.2%；上半年销售额为 5.63 亿欧元，增长13.6%。根据报告，Erbitux 二季度销售额的强劲增长主要得益于欧洲、拉丁美洲和亚太地区的增长。西妥昔单抗是 EGFR 表达、RAS 野生型转移性结直肠癌以及复发性和/或转移性和局部晚期头颈部鳞状细胞癌患者的标准治疗。目前，默克开展了近 200 项涉及西妥昔单抗的活跃临床试验，包括超 15 项 III 期研究。 Bavencio (Avelumab) 抗 PD-L1 抗体 Bavencio 第二季度销售额为 1.86 亿欧元，增长 6.4% ；上半年销售额为 3.72 亿欧元，增长 10.2%。Bavencio 在第二季度的稳健增长主要得益于除北美以外的所有其它地区的收入贡献。 Bavencio 已获准在 70 多个国家/地区作为晚期尿路上皮癌的一线维持治疗。根据 JAVELIN Bladder 100 试验的结果，它已成为治疗这种疾病的标准治疗。Bavencio 还获准与阿昔替尼联合用于晚期肾细胞癌的一线治疗，并且是转移性默克尔细胞癌（一种罕见皮肤癌）的单药疗法的标准治疗。其它肿瘤管线进展默克也披露了该公司肿瘤领域其它产品管线的进展。其中，口服 MET 抑制剂 Tepmetko(Tepotinib) 已在全球约 40 个市场上市，其它市场的监管申请正在审评查中。今年 2 月份，FDA 正式批准了 Tepmetko（此前该药物已获 FDA 加速批准）。今年 6 月，默克宣布停止了 IAP 抑制剂 Xevinapant 的随机 III 期 TrilynX 研究，该研究旨在评估 xevinapant 联合放化疗对未切除局部晚期头颈部鳞状细胞癌 (LA SCCHN) 患者的疗效。xevinapant 的另一项 III 期临床试验 XRay Vision 也已停止，该研究旨在评估 xevinapant 联合放疗对已切除 LA SCCHN 患者的疗效。 2024 年上半年，默克还在 ASCO 年会上以口头报告的形式介绍了抗 CEACAM5 抗体-药物偶联物 (ADC) M9140 在晚期结直肠癌中的 Ia 期研究结果。这是默克开发的第一个进入临床开发的 ADC，目前已进入到结直肠癌的 Ib 期阶段。此外，在 DNA 损伤反应 (DDR) 产品组合中，默克表示将继续推进 ATR 抑制剂 Tuvusertib (M1774) 的开发。该公司正在三项 II 期临床研究中探索 Tuvusertib 的四种组合，涉及适应症包括非鳞状非小细胞肺癌、PARP 抑制剂抗药性卵巢癌、晚期尿路上皮癌。神经病学和免疫学领域神经病学和免疫学产品第二季度销售额为 4.34 亿欧元，下降-7.4%；上半年销售额为 8.53 亿欧元，与去年同期基本持平。截图来自：默克财报在神经病学和免疫学领域，默克目前的产品组合包括两种用于治疗复发性 MS (RMS) 的获批产品 ---- Rebif（干扰素 β-1a）和 Mavenclad（克拉屈滨片）。 Rebif 是一种改善病情的药物，20 多年来一直是 RMS 的标准治疗方法。该药 Q2 销售额为 1.68 亿欧元，下降-18.5% ；上半年销售额为 3.26 亿欧元，下降 -9.0% 。报告指出，Rebif 二季度销售额的下降是由于干扰素市场持续激烈的竞争所致，以及口服剂型和高效 MS 疗法的竞争，预计未来这些因素将会导致该药的销售额进一步下降。 Mavenclad 是一种用于治疗各种形式的高活性 RMS 成人患者的短期口服疗法，已在全球 95 个国家/地区获得批准，包括欧盟、瑞士、澳大利亚、加拿大和美国。该药第二季度销售额为 2.66 亿欧元，增长 1.3% ；上半年销售额为 5.27 亿欧元，增长 6.5% 。除了 MS，默克表示还将继续扩大神经病学和免疫学领域的产品，为医疗需求尚未得到满足的患者开发潜在 first-in-class 疗法。2023 年 6 月，FDA 授予一种用于治疗重症肌无力的口服克拉屈滨（Cladribine）新配方孤儿药资格。默克已于 2024 年 6 月启动了一项全球 III 期临床试验。此外，默克开发的 Enpatoran 是一种 Toll 样受体 7 和 8 (TLR7/8) 抑制剂，处于 II 期临床开发阶段。默克预计 Enpatoran 在皮肤型红斑狼疮和系统性狼疮中的 II 期结果将于 2025 年初公布。心血管、代谢和内分泌学心血管、代谢和内分泌领域产品组合包括 Glucophage、Euthyrox、Concor 和 Saizen 等药物，是默克制药业务部门销售额最大的版块。该领域业务第二季度销售额为 7.46 亿欧元，增长 13.7%；上半年销售额为 14.35 亿欧元，增长 8.9%。截图来自：默克财报 Glucophage 含有活性成分二甲双胍，是治疗 2 型糖尿病的一线药物，在 100 多个国家有售。该药二季度销售额为 2.38 亿欧元，增长 23.5% ；上半年销售额为 4.59 亿欧元，增长 13.8% 。 Concor 含有比索洛尔，它是一种 β 受体阻滞剂，用于治疗高血压和心血管疾病。除了 Concor/Concor Cor，Concor 系列还包括固定剂量组合，例如 Concor Plus/Lodoz（比索洛尔与氢氯噻嗪）。Concor 第二季度销售额为 1.58 亿欧元，增长 13.2% ；上半年销售额为 2.97 亿欧元，增长 7.4%。 Euthyrox 含有活性成分左旋甲状腺素，是治疗甲状腺功能减退症的药物。该药二季度销售额为 1.55 亿欧元，增长 19.2% ；上半年销售额为 2.94 亿欧元，增长 14.1%。 Saizen 含有活性成分生长激素，是默克的主要内分泌产品，用于治疗儿童和成人的多种生长激素紊乱。该药二季度销售额为 9700 万欧元，增长 23.0% ；上半年销售额为 1.86 亿欧元，增长 20%。参考资料：Merck Returns to Organic Sales Growth. https://www.merckgroup.com/en/news/q2-2024-01-08-2024.html 封面来源：企业 Logo 免责声明：本文仅作信息分享，不代表 Insight 立场和观点，也不作治疗方案推荐和介绍。如有需求，请咨询和联系正规医疗机构。编辑：馨药 PR 稿对接：微信 insightxb 投稿：微信 insightxb；邮箱 insight@dxy.cn 多样化功能、可溯源数据…… Insight 数据库网页版等你体验点击阅读原文，立刻解锁！

临床3期财报ASCO会议抗体药物偶联物加速审批

100 项与 Enpatoran 相关的药物交易

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研发状态

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适应症	最高研发状态	国家/地区	公司	日期
皮肌炎	临床2期	美国	Merck KGaA	2023-01-19
皮肌炎	临床2期	捷克	Merck KGaA	2023-01-19
皮肌炎	临床2期	希腊	Merck KGaA	2023-01-19
皮肌炎	临床2期	意大利	Merck KGaA	2023-01-19
皮肌炎	临床2期	波兰	Merck KGaA	2023-01-19
皮肌炎	临床2期	西班牙	Merck KGaA	2023-01-19
皮肌炎	临床2期	英国	Merck KGaA	2023-01-19
盘状红斑狼疮	临床2期	美国	R-Pharm Germany GmbH初创企业	2022-02-14
盘状红斑狼疮	临床2期	日本	R-Pharm Germany GmbH初创企业	2022-02-14
盘状红斑狼疮	临床2期	阿根廷	R-Pharm Germany GmbH初创企业	2022-02-14

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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


NCT05162586 (ACR2022) 人工标引	临床1期	-	36	Enpatoran	夢醖廠積範醖製憲積觸(願網糧選積糧願艱鹹鏇) = Cmax: 0.9409 [0.7855–1.1270]; AUC0-inf: 0.8959 [0.7497–1.0704] and AUC0-tlast: 0.8963 [0.7511–1.0695]). 鬱壓窪構廠壓網蓋構鑰 (襯鹹願積襯選鹹遞顧網 ) 更多	积极	2022-09-12
NCT04448756 (ANEMONE, CTgov)	临床2期	新型冠状病毒感染	149	Placebo (Placebo)	淵窪網願顧鑰鑰窪夢蓋(窪蓋簾鹹積積衊窪願膚) = 製憲簾夢選鑰繭壓選淵廠願壓餘齋顧鹹網簾積 (鏇遞鑰壓餘夢餘網築衊, 齋製鏇膚壓壓觸構鬱糧 ~ 窪製壓鑰鑰憲衊衊夢獵) 更多	-	2022-06-06
				M5049 (M5049 100 mg)	淵窪網願顧鑰鑰窪夢蓋(窪蓋簾鹹積積衊窪願膚) = 鹹淵齋選鏇遞獵鏇蓋築廠願壓餘齋顧鹹網簾積 (鏇遞鑰壓餘夢餘網築衊, 夢窪餘遞壓齋鹹顧顧簾 ~ 鏇蓋遞範築鏇夢構繭憲) 更多
NCT04448756 (ANEMONE, EULAR2022)	临床2期	新型冠状病毒感染 cytokines \| C-reactive protein \| D-dimer ... 更多	149	Enpatoran 50 mg BID	齋鹹鑰醖壓獵遞選艱餘(壓鏇鑰願糧網齋膚糧製) = 積簾鑰繭選壓醖壓觸襯鹹鹽艱範窪簾構齋願構 (選襯淵選夢積簾鹹壓遞 ) 更多	积极	2022-06-01
				Enpatoran 100 mg BID	齋鹹鑰醖壓獵遞選艱餘(壓鏇鑰願糧網齋膚糧製) = 築餘積顧鹹蓋醖製廠鹹鹹鹽艱範窪簾構齋願構 (選襯淵選夢積簾鹹壓遞 ) 更多
NCT03676322 (Pubmed) 人工标引	临床1期	自身免疫性疾病	96	M5049 (single-dose)	餘糧遞壓選鏇範夢願醖(築獵壓獵獵鹽製壓願顧) = 窪鬱願餘廠遞夢願願鑰窪遞鏇顧顧鏇壓獵窪遞 (憲艱窪網顧鹽艱範鹽淵 ) 更多	积极	2021-10-01
				M5049 (multiple-dose)	餘糧遞壓選鏇範夢願醖(築獵壓獵獵鹽製壓願顧) = 範顧廠積網窪蓋顧餘構窪遞鏇顧顧鏇壓獵窪遞 (憲艱窪網顧鹽艱範鹽淵 )