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A step closer to medicinal product harmonisation: EMA PMS becomes the next focus of IDMP efforts 离药品统一又近了一步：EMA PMS成为IDMP工作的下一个重点。
IF 6.5 2区 医学
Drug Discovery Today Pub Date : 2025-07-01 DOI: 10.1016/j.drudis.2025.104410
Michiel Stam
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引用次数: 0
Computational approaches to DMPK: A realistic assessment of current methods and their practical impact. Part I: Physicochemical and in vitro properties DMPK的计算方法：对当前方法及其实际影响的现实评估。第一部分：理化和体外特性。
IF 6.5 2区 医学
Drug Discovery Today Pub Date : 2025-06-30 DOI: 10.1016/j.drudis.2025.104422
Koichi Handa , Mariko Hirano , Michiharu Kageyama , Andreas Bender
{"title":"Computational approaches to DMPK: A realistic assessment of current methods and their practical impact. Part I: Physicochemical and in vitro properties","authors":"Koichi Handa ,&nbsp;Mariko Hirano ,&nbsp;Michiharu Kageyama ,&nbsp;Andreas Bender","doi":"10.1016/j.drudis.2025.104422","DOIUrl":"10.1016/j.drudis.2025.104422","url":null,"abstract":"<div><div>Artificial intelligence and computational approaches have received considerable interest in recent years, and here we assess their real-world utility in drug discovery projects. We review recent <em>in silico</em> models in the area of drug metabolism and pharmacokinetics (DMPK), especially for physicochemical properties (pKa and logD) and <em>in vitro</em> assays [solubility (DMSO, Dried-DMSO, Powder), permeability (PAMPA, Caco-2, MDCK), metabolic stability (liver microsome, hepatocyte), and protein binding (plasma, microsome, brain)]. We discuss which are currently fit for purpose (and which are not), bridging both computational and experimental aspects in the early drug discovery stages. The review includes diverse aspects of obtaining data and model generation, as well as modeler/experimentalist interplay.</div></div>","PeriodicalId":301,"journal":{"name":"Drug Discovery Today","volume":"30 8","pages":"Article 104422"},"PeriodicalIF":6.5,"publicationDate":"2025-06-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144551549","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Back to gene therapy: bringing the EU regulation into the future 回到基因治疗：将欧盟监管带入未来。
IF 6.5 2区 医学
Drug Discovery Today Pub Date : 2025-06-30 DOI: 10.1016/j.drudis.2025.104424
Umberto M. Musazzi , Paolo Rocco , Sara Manellari , Sara Azari , Giulio Pompilio , Paola Minghetti
{"title":"Back to gene therapy: bringing the EU regulation into the future","authors":"Umberto M. Musazzi ,&nbsp;Paolo Rocco ,&nbsp;Sara Manellari ,&nbsp;Sara Azari ,&nbsp;Giulio Pompilio ,&nbsp;Paola Minghetti","doi":"10.1016/j.drudis.2025.104424","DOIUrl":"10.1016/j.drudis.2025.104424","url":null,"abstract":"<div><div>The current European framework for Advanced Therapy Medicinal Products (ATMPs), which also covers gene therapies, was established in 2007 at the dawn of the biotechnology era in the pharmaceutical sector. However, its inherent limitations have been revealed by the new frontiers enabled by the scientific and technological advances of the past few decades, particularly in the areas of innovative gene therapeutics (e.g., CRISPR/Cas9–RNA complexes), manufacturing technologies, and delivery systems. Here, we contribute to the scientific discussion on how to reduce regulatory uncertainty in the qualification of medicinal products with a different mechanism of action (e.g., editing the host genome or regulating gene expression), and on rationalizing regulatory support and incentives for the most complex therapies in terms of mechanism of action and manufacturing process.</div></div>","PeriodicalId":301,"journal":{"name":"Drug Discovery Today","volume":"30 8","pages":"Article 104424"},"PeriodicalIF":6.5,"publicationDate":"2025-06-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144551548","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Lysine lactylation: Regulatory mechanisms, role in health and disease, and its therapeutic potential 赖氨酸乳酸化：调节机制，在健康和疾病中的作用，及其治疗潜力。
IF 6.5 2区 医学
Drug Discovery Today Pub Date : 2025-06-30 DOI: 10.1016/j.drudis.2025.104420
Xu Yan , Guangming Zhang , Huayuan Wei , Lin Yang , Xijuan Jiang
{"title":"Lysine lactylation: Regulatory mechanisms, role in health and disease, and its therapeutic potential","authors":"Xu Yan ,&nbsp;Guangming Zhang ,&nbsp;Huayuan Wei ,&nbsp;Lin Yang ,&nbsp;Xijuan Jiang","doi":"10.1016/j.drudis.2025.104420","DOIUrl":"10.1016/j.drudis.2025.104420","url":null,"abstract":"<div><div>Lysine lactylation of (Kla), a novel post-translational modification, is prevalent in various diseases and has garnered increasing attention. Kla has diverse roles in diseases, exhibiting both beneficial and detrimental effects depending on the context and modification site. This review focuses on the emerging therapeutic potential of Kla in various diseases. We discuss recent studies that have underscored the therapeutic potential of Kla and its inhibitors in treating diverse disorders. We also explore potential therapeutic strategies targeting Kla and its substrates, providing a scientific basis and roadmap for subsequent research and drug development.</div></div>","PeriodicalId":301,"journal":{"name":"Drug Discovery Today","volume":"30 8","pages":"Article 104420"},"PeriodicalIF":6.5,"publicationDate":"2025-06-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144551551","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Experts hail regulatory impact assessment as ripe for GenAI transformation, to streamline product change control 专家们称赞监管影响评估对GenAI转型来说已经成熟，可以简化产品变更控制。
IF 6.5 2区 医学
Drug Discovery Today Pub Date : 2025-06-30 DOI: 10.1016/j.drudis.2025.104423
Agnes Cwienczek
{"title":"Experts hail regulatory impact assessment as ripe for GenAI transformation, to streamline product change control","authors":"Agnes Cwienczek","doi":"10.1016/j.drudis.2025.104423","DOIUrl":"10.1016/j.drudis.2025.104423","url":null,"abstract":"","PeriodicalId":301,"journal":{"name":"Drug Discovery Today","volume":"30 8","pages":"Article 104423"},"PeriodicalIF":6.5,"publicationDate":"2025-06-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144551550","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
CPPsite3: An updated large repository of experimentally validated cell-penetrating peptides CPPsite3：一个经过实验验证的细胞穿透肽更新的大型储存库。
IF 6.5 2区 医学
Drug Discovery Today Pub Date : 2025-06-27 DOI: 10.1016/j.drudis.2025.104421
Nisha Bajiya , Sohana Najrin , Pankaj Kumar , Shubham Choudhury , Ritu Tomer , Gajendra P.S. Raghava
{"title":"CPPsite3: An updated large repository of experimentally validated cell-penetrating peptides","authors":"Nisha Bajiya ,&nbsp;Sohana Najrin ,&nbsp;Pankaj Kumar ,&nbsp;Shubham Choudhury ,&nbsp;Ritu Tomer ,&nbsp;Gajendra P.S. Raghava","doi":"10.1016/j.drudis.2025.104421","DOIUrl":"10.1016/j.drudis.2025.104421","url":null,"abstract":"<div><div>Over the past two decades, cell-penetrating peptides (CPPs) have emerged as key intracellular drug delivery vehicles. This review provides a systematic overview of advancements in CPP research, encompassing both experimental techniques and computational resources crucial for their discovery. Our primary focus is on CPPsite3, a meticulously curated repository that currently houses 6788 entries, representing 4285 unique CPPs. This updated version builds upon CPPsite and CPPsite2, both of which have been extensively utilized by the scientific community for designing CPPs and developing robust prediction methods. Furthermore, we explore the clinical applications of CPPs, specifically highlighting those currently undergoing clinical use. This comprehensive review aims to be a vital resource for the drug delivery research community.</div></div>","PeriodicalId":301,"journal":{"name":"Drug Discovery Today","volume":"30 8","pages":"Article 104421"},"PeriodicalIF":6.5,"publicationDate":"2025-06-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144525778","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Rediscovering nitroxoline: a metal-chelating agent bridging infection and cancer 重新发现硝基喹啉：一种桥接感染和癌症的金属螯合剂。
IF 6.5 2区 医学
Drug Discovery Today Pub Date : 2025-06-26 DOI: 10.1016/j.drudis.2025.104419
Praveen Papareddy , Sophie R.M. Mielke , Marlowe Graham , Dennis Bachmann , Ewgenij Proschak , Thomas A. Wichelhaus , Kerstin Sander , Heiko Herwald
{"title":"Rediscovering nitroxoline: a metal-chelating agent bridging infection and cancer","authors":"Praveen Papareddy ,&nbsp;Sophie R.M. Mielke ,&nbsp;Marlowe Graham ,&nbsp;Dennis Bachmann ,&nbsp;Ewgenij Proschak ,&nbsp;Thomas A. Wichelhaus ,&nbsp;Kerstin Sander ,&nbsp;Heiko Herwald","doi":"10.1016/j.drudis.2025.104419","DOIUrl":"10.1016/j.drudis.2025.104419","url":null,"abstract":"<div><div>Nitroxoline, a legacy antimicrobial agent, is gaining attention for its potential repurposing in infectious diseases and oncology. Its broad-spectrum activity, including biofilm disruption and metal-chelating properties, supports diverse therapeutic applications. However, its systemic use is limited by rapid urinary excretion, short plasma half-life, and limited tissue distribution. In this review, we summarize recent advances in understanding the mechanisms of action, cross-kingdom activity, and anticancer effects of nitroxoline. Despite encouraging preclinical data, clinical translation is constrained by pharmacokinetic (PK) and regulatory challenges. As interest in repurposing established drugs grows, nitroxoline presents a compelling candidate for integration into modern therapeutic strategies across infectious and neoplastic disease domains.</div></div>","PeriodicalId":301,"journal":{"name":"Drug Discovery Today","volume":"30 8","pages":"Article 104419"},"PeriodicalIF":6.5,"publicationDate":"2025-06-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144525779","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
The discovery of medicines: drug testing on humans and the development of medical ethics before the 20th century 药物的发现：20世纪以前的人体药物试验和医学伦理的发展。
IF 6.5 2区 医学
Drug Discovery Today Pub Date : 2025-06-24 DOI: 10.1016/j.drudis.2025.104418
Agnieszka M. Polak , Katarzyna Karska , Mariola Drozd
{"title":"The discovery of medicines: drug testing on humans and the development of medical ethics before the 20th century","authors":"Agnieszka M. Polak ,&nbsp;Katarzyna Karska ,&nbsp;Mariola Drozd","doi":"10.1016/j.drudis.2025.104418","DOIUrl":"10.1016/j.drudis.2025.104418","url":null,"abstract":"<div><div>In this article, we review the historical approach to the discovery of medicines, human drug testing, and the development of medical ethics. We cover the period from prehistoric times until 1906, when the Pure Food and Drug Act was introduced in response to the poor quality of food products and medicines. In the first part of the article, we discuss the period before the 16th century when drug testing relied on observation, trial and error, prescriptions and recipes, and the first use of pharmacopoeias to ensure medication safety. The second part focuses on the 19th century which was marked, on the one hand, by pharmacological advancements and the rise of the pharmaceutical industry, and, on the other, by the need for the introduction of safety guidelines.</div></div>","PeriodicalId":301,"journal":{"name":"Drug Discovery Today","volume":"30 8","pages":"Article 104418"},"PeriodicalIF":6.5,"publicationDate":"2025-06-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144504339","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Transitioning to regulatory harmonisation for medicines: a comparison between Africa and Europe 向药品监管协调过渡：非洲和欧洲之间的比较。
IF 6.5 2区 医学
Drug Discovery Today Pub Date : 2025-06-23 DOI: 10.1016/j.drudis.2025.104416
Kirti Narsai , Hubert G.M. Leufkens , Francine Brinkhuis , Aukje K. Mantel-Teeuwisse , Hendrika A. van den Ham
{"title":"Transitioning to regulatory harmonisation for medicines: a comparison between Africa and Europe","authors":"Kirti Narsai ,&nbsp;Hubert G.M. Leufkens ,&nbsp;Francine Brinkhuis ,&nbsp;Aukje K. Mantel-Teeuwisse ,&nbsp;Hendrika A. van den Ham","doi":"10.1016/j.drudis.2025.104416","DOIUrl":"10.1016/j.drudis.2025.104416","url":null,"abstract":"<div><div>The harmonisation of medicines regulation has varied across regions. Europe began over 50 years ago, whereas Africa started only recently through regional initiatives. We compared regulatory developments in both regions, examining stakeholder influence, philosophy, funding, and systems. Key differences included legislation (common binding legislation was essential to success in Europe), economics, disease patterns, and industrial policy, while protecting health and work-sharing were common goals. Disease outbreaks drove African manufacturing and regulatory strengthening, whereas European harmonisation followed the formation of the European Union. The establishment of the European Medicines Agency in 1995 was crucial, but an African Medicines Agency remains in progress. Both regions require national support for supranational bodies. Africa has advanced in regulation recently, while Europe strengthens its system. Future health challenges require continued harmonisation efforts.</div></div>","PeriodicalId":301,"journal":{"name":"Drug Discovery Today","volume":"30 8","pages":"Article 104416"},"PeriodicalIF":6.5,"publicationDate":"2025-06-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144493212","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
ADAM10: Function insights, disease implications, and promise of therapeutic targeting ADAM10：功能洞察、疾病意义和治疗靶向前景。
IF 6.5 2区 医学
Drug Discovery Today Pub Date : 2025-06-20 DOI: 10.1016/j.drudis.2025.104414
Wenqian Zhang , Youhua Xu , Junjiang Fu
{"title":"ADAM10: Function insights, disease implications, and promise of therapeutic targeting","authors":"Wenqian Zhang ,&nbsp;Youhua Xu ,&nbsp;Junjiang Fu","doi":"10.1016/j.drudis.2025.104414","DOIUrl":"10.1016/j.drudis.2025.104414","url":null,"abstract":"<div><div>As a sheddase, ADAM10 plays a critical role in various physiological and pathological processes because of its widespread distribution and proteolytic functions. Dysregulation of ADAM10 is associated with multiple diseases, including cancer. Despite significant research, a comprehensive synthesis of its structural characteristics, activation mechanisms, regulatory pathways, and involvement in disease remains lacking. This review provides an in-depth analysis of ADAM10, focusing on its molecular structure, mechanisms of activation and regulation, and roles in normal physiology and disease, particularly cancer. By elucidating ADAM10’s interactions and pathways, this review aims to identify potential therapeutic targets and strategies to modulate its activity in disease contexts, offering insights for researchers and clinicians.</div></div>","PeriodicalId":301,"journal":{"name":"Drug Discovery Today","volume":"30 8","pages":"Article 104414"},"PeriodicalIF":6.5,"publicationDate":"2025-06-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144367756","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
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