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The global status of bioequivalence trials: a comprehensive clinical trial landscape analysis based on the Trialtrove database. 生物等效性试验的全球现状：基于 Trialtrove 数据库的临床试验综合分析。
IF 6.5 2区 医学
Drug Discovery Today Pub Date : 2024-11-06 DOI: 10.1016/j.drudis.2024.104223
Xiuxin Zhong, Shaojing Lin, Mingxia Deng, Ling Guan
{"title":"The global status of bioequivalence trials: a comprehensive clinical trial landscape analysis based on the Trialtrove database.","authors":"Xiuxin Zhong, Shaojing Lin, Mingxia Deng, Ling Guan","doi":"10.1016/j.drudis.2024.104223","DOIUrl":"https://doi.org/10.1016/j.drudis.2024.104223","url":null,"abstract":"","PeriodicalId":301,"journal":{"name":"Drug Discovery Today","volume":null,"pages":null},"PeriodicalIF":6.5,"publicationDate":"2024-11-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142602410","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
Pharma innovation: how evolutionary economics is shaping the future of pharma R&D. 医药创新：进化经济学如何塑造医药研发的未来。
IF 6.5 2区 医学
Drug Discovery Today Pub Date : 2024-11-05 DOI: 10.1016/j.drudis.2024.104222
Alexander Schuhmacher
{"title":"Pharma innovation: how evolutionary economics is shaping the future of pharma R&D.","authors":"Alexander Schuhmacher","doi":"10.1016/j.drudis.2024.104222","DOIUrl":"https://doi.org/10.1016/j.drudis.2024.104222","url":null,"abstract":"<p><p>This paper describes the theory of evolutionary economics in the context of pharmaceutical R&D. In this context, the R&D productivity crisis acts as a key selection mechanism, and R&D, technology and industry trends provide mechanisms of variation. Drawing on today's prevailing business model among leading pharmaceutical companies, the biotech-leveraged pharma company (BIPCO), I propose two new value creation logics: the technology-investigating pharma company (TIPCO) and the asset-integrating pharma company (AIPCO). Although some companies already share aspects of these business models, it is not yet clear, in terms of evolutionary economics, what the ultimate outcome of the evolutionary process in pharma R&D will be.</p>","PeriodicalId":301,"journal":{"name":"Drug Discovery Today","volume":null,"pages":null},"PeriodicalIF":6.5,"publicationDate":"2024-11-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142602393","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
Advances in molecular glues: exploring chemical space and design principles for targeted protein degradation 分子胶的进展：探索定向降解蛋白质的化学空间和设计原则。
IF 6.5 2区 医学
Drug Discovery Today Pub Date : 2024-11-01 DOI: 10.1016/j.drudis.2024.104205
Hemant Kumar S , Muthukumaran Venkatachalapathy , Ramesh Sistla , Vasanthanathan Poongavanam
{"title":"Advances in molecular glues: exploring chemical space and design principles for targeted protein degradation","authors":"Hemant Kumar S ,&nbsp;Muthukumaran Venkatachalapathy ,&nbsp;Ramesh Sistla ,&nbsp;Vasanthanathan Poongavanam","doi":"10.1016/j.drudis.2024.104205","DOIUrl":"10.1016/j.drudis.2024.104205","url":null,"abstract":"<div><div>The discovery of the E3 ligase cereblon (CRBN) as the target of thalidomide and its analogs revolutionized the field of targeted protein degradation (TPD). This ubiquitin-mediated degradation pathway was first harnessed by bivalent degraders. Recently, the emergence of low-molecular-weight molecular glue degraders (MGDs) has expanded the TPD landscape, because MGDs operate via the same mechanism while offering attractive physicochemical properties that are consistent with small-molecule therapeutics. This review delves into the discovery and advancement of MGDs, with case studies on cyclin K and the zinc finger protein IKZF2, highlighting the design principles, biological assays and therapeutic applications. Additionally, it examines the chemical space of molecular glues and outlines the collaborative efforts that are fueling innovation in this field.</div></div>","PeriodicalId":301,"journal":{"name":"Drug Discovery Today","volume":null,"pages":null},"PeriodicalIF":6.5,"publicationDate":"2024-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142405788","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Comprehensive analysis of acetylcholinesterase inhibitor and reactivator complexes: implications for drug design and antidote development. 乙酰胆碱酯酶抑制剂和再激活剂复合物的综合分析：对药物设计和解毒剂开发的影响。
IF 6.5 2区 医学
Drug Discovery Today Pub Date : 2024-10-29 DOI: 10.1016/j.drudis.2024.104217
Weronika Bagrowska, Angelika Karasewicz, Artur Góra
{"title":"Comprehensive analysis of acetylcholinesterase inhibitor and reactivator complexes: implications for drug design and antidote development.","authors":"Weronika Bagrowska, Angelika Karasewicz, Artur Góra","doi":"10.1016/j.drudis.2024.104217","DOIUrl":"10.1016/j.drudis.2024.104217","url":null,"abstract":"<p><p>The main function of acetylcholinesterase (AChE) is to regulate the levels of one of the most important neurotransmitters: acetylcholine. This makes AChE an ideal molecular target for the treatment of neurodegenerative diseases and dementia (such as Alzheimer's disease), as well as for the neutralisation of natural toxins (e.g., venom peptides) and chemical warfare agents. The significance of AChE inhibitors in slowing the progression of dementia, as well as the role of reactivators in treating poisoned individuals, is reflected in several co-crystallised complexes deposited in the Protein Data Bank. In this study, we analysed all deposited AChE-small-molecule complexes to gain insights into compound binding and to provide guidance for the future design of therapeutic drugs and new antidotes.</p>","PeriodicalId":301,"journal":{"name":"Drug Discovery Today","volume":null,"pages":null},"PeriodicalIF":6.5,"publicationDate":"2024-10-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142542503","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
Metabolic reprogramming in KRAS-mutant cancers: Proven targetable vulnerabilities and potential therapeutic strategies. KRAS突变癌症的代谢重编程：已证实的靶向弱点和潜在的治疗策略。
IF 6.5 2区 医学
Drug Discovery Today Pub Date : 2024-10-29 DOI: 10.1016/j.drudis.2024.104220
Ruilin Wu, Hong Zhu, Qiaojun He, Tao Yuan, Bo Yang
{"title":"Metabolic reprogramming in KRAS-mutant cancers: Proven targetable vulnerabilities and potential therapeutic strategies.","authors":"Ruilin Wu, Hong Zhu, Qiaojun He, Tao Yuan, Bo Yang","doi":"10.1016/j.drudis.2024.104220","DOIUrl":"10.1016/j.drudis.2024.104220","url":null,"abstract":"<p><p>Kras (Ki-ras2 Kirsten rat sarcoma viral oncogene homolog), one of the most frequently mutated oncogenes in the human genome, is considered 'untargetable'. Although specific KRAS<sup>G12C</sup> inhibitors have been developed, their overall impact is limited, highlighting the need for further research on targeting KRAS-mutant cancers. Metabolic abnormalities are key hallmarks of cancer, with KRAS-driven tumors exhibiting traits like glycolysis upregulation, glutamine addiction, lipid droplet accumulation, highly active macropinocytosis, and metabolic reprogramming-associated tumor microenvironment remodeling. Targeting these unique metabolic characteristics offers a promising strategy for new cancer treatments. This review summarizes recent advances in our understanding of the metabolic network in KRAS-mutated tumor cells, discusses potential targetable vulnerabilities, and outlines clinical developments in relevant therapies, while also addressing challenges to improve strategies against these aggressive cancers.</p>","PeriodicalId":301,"journal":{"name":"Drug Discovery Today","volume":null,"pages":null},"PeriodicalIF":6.5,"publicationDate":"2024-10-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142556738","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
How to nurture natural products to create new therapeutics: Strategic innovations and molecule-to-medicinal insights into therapeutic advancements. 如何培育天然产品以创造新疗法：战略创新和从分子到药物的治疗进展见解。
IF 6.5 2区 医学
Drug Discovery Today Pub Date : 2024-10-29 DOI: 10.1016/j.drudis.2024.104221
Ayan Acharya, Mithilesh Nagpure, Nibedita Roy, Vaibhav Gupta, Soumyadeep Patranabis, Sankar K Guchhait
{"title":"How to nurture natural products to create new therapeutics: Strategic innovations and molecule-to-medicinal insights into therapeutic advancements.","authors":"Ayan Acharya, Mithilesh Nagpure, Nibedita Roy, Vaibhav Gupta, Soumyadeep Patranabis, Sankar K Guchhait","doi":"10.1016/j.drudis.2024.104221","DOIUrl":"10.1016/j.drudis.2024.104221","url":null,"abstract":"<p><p>Natural products (NPs) are privileged structures interacting with biomacromolecular targets and exhibiting biological effects important for human health. In this review, we have presented NP-inspired strategic innovations that are promising for addressing preclinical and clinical challenges. An analysis of 'molecule-to-medicinal' properties for improvement of P3 and absorption, distribution, metabolism, excretion, and toxicity (ADMET) profiles has been illustrated. The strategies include chemical evolution through knowledge of structure-medicinal properties, truncation of NPs to avoid molecular obesity, pseudo-NPs, selection of common structural features of NPs, medicinophore installation, scaffold hopping, and induced proximity. Molecule-to-medicinal property analysis can guide the development of 'nature-to-new' chemical therapeutics. Coupled with scientific advances and innovations in instrumentation, these strategies hold great potential for enhancing drug design and discovery.</p>","PeriodicalId":301,"journal":{"name":"Drug Discovery Today","volume":null,"pages":null},"PeriodicalIF":6.5,"publicationDate":"2024-10-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142556737","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
Green synthesis of metal nanocarriers: A perspective for targeting glioblastoma. 金属纳米载体的绿色合成：靶向胶质母细胞瘤的前景。
IF 6.5 2区 医学
Drug Discovery Today Pub Date : 2024-10-29 DOI: 10.1016/j.drudis.2024.104219
Taskeen F Docrat, Ali O E Eltahir, Ahmed A Hussein, Jeanine L Marnewick
{"title":"Green synthesis of metal nanocarriers: A perspective for targeting glioblastoma.","authors":"Taskeen F Docrat, Ali O E Eltahir, Ahmed A Hussein, Jeanine L Marnewick","doi":"10.1016/j.drudis.2024.104219","DOIUrl":"10.1016/j.drudis.2024.104219","url":null,"abstract":"<p><p>Glioblastoma, the most aggressive brain cancer, is challenging to treat owing to the difficulty of crossing the blood-brain barrier, high recurrence rates and significant mortality. This review highlights the potential of green synthesis methods in developing metal nanoparticles (MNPs) as a sustainable solution for drug delivery systems targeting glioblastoma. We explore the unique properties and modes of action of MNPs synthesised through eco-friendly processes by focusing on their bioavailability and precision in brain targeting, and discuss the potential of MNPs to target glioblastoma at the molecular level. Integrating green synthesis into cancer therapeutics represents a novel paradigm shift towards treatments with higher efficacy and lower environmental impact, offering hope in the fight against glioblastoma.</p>","PeriodicalId":301,"journal":{"name":"Drug Discovery Today","volume":null,"pages":null},"PeriodicalIF":6.5,"publicationDate":"2024-10-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142542504","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
Elevating life science R&D success with AI: a framework 利用人工智能提升生命科学研发的成功率：一个框架。
IF 6.5 2区 医学
Drug Discovery Today Pub Date : 2024-10-22 DOI: 10.1016/j.drudis.2024.104211
Ben Sidders
{"title":"Elevating life science R&D success with AI: a framework","authors":"Ben Sidders","doi":"10.1016/j.drudis.2024.104211","DOIUrl":"10.1016/j.drudis.2024.104211","url":null,"abstract":"","PeriodicalId":301,"journal":{"name":"Drug Discovery Today","volume":null,"pages":null},"PeriodicalIF":6.5,"publicationDate":"2024-10-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142491946","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
Drugs from drugs: New chemical insights into a mature concept 从药物中提取药物：对成熟概念的新化学见解。
IF 6.5 2区 医学
Drug Discovery Today Pub Date : 2024-10-22 DOI: 10.1016/j.drudis.2024.104212
Eloy Lozano Baró , Federica Catti , Carolina Estarellas , Ouldouz Ghashghaei , Rodolfo Lavilla
{"title":"Drugs from drugs: New chemical insights into a mature concept","authors":"Eloy Lozano Baró ,&nbsp;Federica Catti ,&nbsp;Carolina Estarellas ,&nbsp;Ouldouz Ghashghaei ,&nbsp;Rodolfo Lavilla","doi":"10.1016/j.drudis.2024.104212","DOIUrl":"10.1016/j.drudis.2024.104212","url":null,"abstract":"<div><div>Developing new drugs from marketed ones is a well-established and successful approach in drug discovery. We offer a unified view of this field, focusing on the new chemical aspects of the involved approaches: (a) chemical transformation of the original drugs (late-stage modifications, molecular editing), (b) prodrug strategies, and (c) repurposing as a tool to develop new hits/leads. Special focus is placed on the molecular structure of the drugs and their synthetic feasibility. The combination of experimental advances and new computational approaches, including artificial intelligence methods, paves the way for the evolution of the drugs from drugs concept.</div></div>","PeriodicalId":301,"journal":{"name":"Drug Discovery Today","volume":null,"pages":null},"PeriodicalIF":6.5,"publicationDate":"2024-10-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142491945","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
The identification of essential cellular genes is critical for validating drug targets 鉴定重要的细胞基因对于验证药物靶点至关重要。
IF 6.5 2区 医学
Drug Discovery Today Pub Date : 2024-10-18 DOI: 10.1016/j.drudis.2024.104215
Ting Xu , Shuang Wang , Tingting Ma , Yawen Dong , Charles R. Ashby Jr , Ge-Fei Hao
{"title":"The identification of essential cellular genes is critical for validating drug targets","authors":"Ting Xu ,&nbsp;Shuang Wang ,&nbsp;Tingting Ma ,&nbsp;Yawen Dong ,&nbsp;Charles R. Ashby Jr ,&nbsp;Ge-Fei Hao","doi":"10.1016/j.drudis.2024.104215","DOIUrl":"10.1016/j.drudis.2024.104215","url":null,"abstract":"<div><div>Accurately identifying biological targets is crucial for advancing treatment options. Essential genes, vital for cell or organism survival, hold promise as potential drug targets in disease treatment. Although many studies have sought to identify essential genes as therapeutic targets in medicine and bioinformatics, systematic reviews on their relationship with drug targets are relatively rare. This work presents a comprehensive analysis to aid in identifying essential genes as potential targets for drug discovery, encompassing their relevance, identification methods, successful case studies, and challenges. This work will facilitate the identification of essential genes as therapeutic targets, thereby boosting new drug development.</div></div>","PeriodicalId":301,"journal":{"name":"Drug Discovery Today","volume":null,"pages":null},"PeriodicalIF":6.5,"publicationDate":"2024-10-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142454529","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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