Expert Opinion on Therapeutic Patents最新文献

Glycogen synthase kinase 3β (GSK-3β) inhibitors - a patent update (2019-2024). 糖原合成酶激酶3β (GSK-3β)抑制剂-专利更新（2019-2024）。

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2025-07-23 DOI: 10.1080/13543776.2025.2536003

Swanand Vinayak Joshi, Devandla Soujanya, Manchella Sai Supriya, Venkata Madhavi Yaddanapudi, Srinivas Nanduri

{"title":"Glycogen synthase kinase 3β (GSK-3β) inhibitors - a patent update (2019-2024).","authors":"Swanand Vinayak Joshi, Devandla Soujanya, Manchella Sai Supriya, Venkata Madhavi Yaddanapudi, Srinivas Nanduri","doi":"10.1080/13543776.2025.2536003","DOIUrl":"10.1080/13543776.2025.2536003","url":null,"abstract":"Introduction: Glycogen synthase kinase-3β (GSK-3β) is a proline-directed serine/threonine kinase identified over 40 years ago. It is the key enzyme involved in glycogen biosynthesis and is expressed in all human tissues. Overexpression of GSK-3β is linked to several diseases, including diabetes mellitus, neurodegenerative disorders such as Alzheimer's disease, and cancer. Owing to its critical role in the pathophysiology of these diseases, GSK-3β has emerged as a validated and potential target for therapeutic intervention. In recent years, significant progress has been made in developing novel GSK-3 inhibitors. Some of these new inhibitors have shown promising results in treating some of these diseases.Areas covered: This review covers patent literature on various GSK-3β inhibitors published between 2019 and 2024. This review also discusses the recent clinical developmental status of some of the promising GSK-3 inhibitors.Expert opinion: Although many heterocyclic compounds from natural as well as synthetic origin have shown promising inhibitory effects against GSK-3β, most of them have not yet progressed to the development stage. However, a critical review of their structures and biological profiles reveals significant potential for further development.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"1-13"},"PeriodicalIF":5.4,"publicationDate":"2025-07-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144689697","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

Overcoming triple mutant EGFR-tyrosine kinase barriers in the therapeutics of non-small cell lung cancer: a patent review on fourth-generation inhibitors (2017-2024). 克服非小细胞肺癌治疗中三重突变egfr -酪氨酸激酶屏障：第四代抑制剂专利审查（2017-2024）。

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2025-07-22 DOI: 10.1080/13543776.2025.2536006

Narendra R Nagpure, Harun M Patel

{"title":"Overcoming triple mutant EGFR-tyrosine kinase barriers in the therapeutics of non-small cell lung cancer: a patent review on fourth-generation inhibitors (2017-2024).","authors":"Narendra R Nagpure, Harun M Patel","doi":"10.1080/13543776.2025.2536006","DOIUrl":"10.1080/13543776.2025.2536006","url":null,"abstract":"Introduction: Non-small cell lung cancer (NSCLC) remains a leading cause of cancer mortality, with epidermal growth factor receptor (EGFR) mutations being the primary driver of tumor progression. This review highlights the significance of fourth-generation EGFR tyrosine kinase inhibitors (EGFR-TKIs) in addressing acquired resistance mechanisms, such as the C797S mutation, which compromises the efficacy of third-generation inhibitors like Osimertinib and explores their potential to revolutionize NSCLC treatment through enhanced molecular specificity.Areas covered: This review covers the latest progress in patented fourth-generation EGFR-TKIs and their clinical trial status for the treatment of NSCLC from 2017 to the present.Expert opinion: Osimertinib, a third-generation EGFR inhibitor, revolutionized treatment for T790M mutations but is limited by resistance from C797S mutations. Fourth-generation EGFR inhibitors, incorporating scaffolds like aminopyrimidine and quinazoline, are designed to selectively target resistant EGFR variants, including L858R/T790M/C797S. Preclinical trials highlight the potential of sulfonyl and phosphine oxide-based compounds for their potency, selectivity, and favorable pharmacokinetics. Promising clinical trials with inhibitors like BDTX-1535, JIN-A02, and HS-10504 could redefine NSCLC treatment, with future success likely relying on innovative strategies, such as combination therapies, to combat resistance and enhance efficacy.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"1-21"},"PeriodicalIF":5.4,"publicationDate":"2025-07-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144642192","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

Recent advances in tropomyosin receptor kinase (TRK) inhibitors: a 2023-2024 patent landscape review. 原肌球蛋白受体激酶（TRK）抑制剂的最新进展：2023-2024年专利回顾

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2025-07-10 DOI: 10.1080/13543776.2025.2529217

Minh Le, Elena Timakova, Ralf Schirrmacher, Justin J Bailey

{"title":"Recent advances in tropomyosin receptor kinase (TRK) inhibitors: a 2023-2024 patent landscape review.","authors":"Minh Le, Elena Timakova, Ralf Schirrmacher, Justin J Bailey","doi":"10.1080/13543776.2025.2529217","DOIUrl":"10.1080/13543776.2025.2529217","url":null,"abstract":"Introduction: The rise of tissue-agnostic therapies has revolutionized cancer treatment, with therapies targeting NTRK fusions leading the way. TRK inhibitors like larotrectinib and entrectinib marked a paradigm shift - prioritizing molecular alterations over the tumor's anatomical location. Acquired resistance remains a significant challenge, with next-generation inhibitors and combination strategies at the forefront of efforts to enhance the clinical efficacy of TRK-targeted therapies.Areas covered: This review discusses patents published in 2023 and 2024 covering inhibitors of the TRK family, extending our ongoing review series on TRK inhibitors. Patent searches were conducted using the key word 'TRK*' and 'inhibitor' in Google Patents database to identify novel TRK-targeting inhibitors and therapeutic strategies.Expert opinion: Ongoing advancements in TRK inhibitor development, combination therapies, and precision diagnostics continue to elevate the potential of treatment outcomes. Recent patent filings reflect the expanding promise of TRK inhibitors for NTRK fusion-driven cancers. However, widespread adoption of high-throughput screening remains crucial unlocking their full therapeutic value and delivering truly precision-guided care. Combination therapies with TRK inhibitors are emerging as a key strategy to enhance efficacy and overcome resistance. The FDA's recent approval of repotrectinib underscores progress in the TRK inhibitor landscape, while highlighting the continued need for innovation.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"1-14"},"PeriodicalIF":5.4,"publicationDate":"2025-07-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144567337","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

An updated patent review of small molecule KCNT1 inhibitors (2022-2024). 小分子KCNT1抑制剂的最新专利审查（2022 - 2024）。

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2025-07-01 Epub Date: 2025-05-21 DOI: 10.1080/13543776.2025.2504460

Paul K Peprah, Kyle A Emmitte

{"title":"An updated patent review of small molecule KCNT1 inhibitors (2022-2024).","authors":"Paul K Peprah, Kyle A Emmitte","doi":"10.1080/13543776.2025.2504460","DOIUrl":"10.1080/13543776.2025.2504460","url":null,"abstract":"Introduction: Gain-of-function mutations in KCNT1 channels has been associated with severe childhood epilepsies. KCNT1 channels are sodium activated potassium channels in the CNS involved in neuronal excitability. Substantial efforts have been made by several groups to discover novel small molecule KCNT1 inhibitors to validate this approach as a therapeutic strategy for the treatment of KCNT1-related epilepsies.Areas covered: This review focuses on 10 published international patent applications from Praxis Precision Medicine that disclose novel small molecule KCNT1 inhibitors for the treatment of KCNT1-related neurological disorders. Features of compounds that contribute to KCNT1 inhibition and published in applications between 2022 and 2024 are discussed. Applications were identified and obtained through the online database, Patentscope, provided by the World Intellectual Property Organization (WIPO) using the search term 'KCNT1 inhibitors.'Expert opinion: Tremendous progress has been made toward the discovery of small molecule inhibitors of KCNT1 channels; however, much work remains to reach a viable therapeutic. Areas of work that will be critically important include further in vivo studies for efficacy, safety, and development of PK/PD relationships. Studies to better understand the binding of known ligands and determine the structural features that govern modulation of the channel are also much needed.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"775-794"},"PeriodicalIF":5.4,"publicationDate":"2025-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144076644","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

Small-molecule RNA ligands: a patent review (2018-2024). 小分子RNA配体：专利审查（2018-2024）。

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2025-07-01 Epub Date: 2025-04-16 DOI: 10.1080/13543776.2025.2492759

Elia Ravegnini, Andrea Trabocchi, Elena Lenci

{"title":"Small-molecule RNA ligands: a patent review (2018-2024).","authors":"Elia Ravegnini, Andrea Trabocchi, Elena Lenci","doi":"10.1080/13543776.2025.2492759","DOIUrl":"10.1080/13543776.2025.2492759","url":null,"abstract":"Introduction: Targeting three-dimensional RNA structures with traditional drug-like small molecules is gaining wide attention in both the academia and the pharmaceutical industries, due to their good oral bioavailability, cheap production cost, and the possibility of fine-tuning ADMET properties, which represent a powerful alternative to the current RNA-targeted therapies, including ASO and siRNA. As RNAs are involved in nearly all the physiological and pathological processes, small molecules RNA ligands can have a plethora of different therapeutic applications, spanning from cancer to infectious and neurological diseases.Areas covered: This review describes patents concerning small molecules RNA ligands published within January 2018 and October 2024, searched through Espacenet, Patentscope, and Google Patents databases.Expert opinion: The number of patents that has been released in the last few years demonstrates the relevance of targeting RNA structures for the development of next generation chemotherapeutic agents and antiviral/antibacterial drugs, even though this field is still in its infancy and many issues still need to be resolved, in particular related to selectivity. An emerging approach to considerably limiting side effects is presented by RIBOTAC derivatives, as promoting a selective RNase-L mediated RNA degradation allows to significantly reduce the dose of the compound.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"675-693"},"PeriodicalIF":5.4,"publicationDate":"2025-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143964166","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

Quorum sensing inhibitors (QSIs): a patent review (2019-2023). 群体感应抑制剂（qsi）：专利审查（2019-2023）。

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2025-07-01 Epub Date: 2025-04-16 DOI: 10.1080/13543776.2025.2491382

Chiara Spaggiari, Clementine Yamukujije, Marco Pieroni, Giannamaria Annunziato

{"title":"Quorum sensing inhibitors (QSIs): a patent review (2019-2023).","authors":"Chiara Spaggiari, Clementine Yamukujije, Marco Pieroni, Giannamaria Annunziato","doi":"10.1080/13543776.2025.2491382","DOIUrl":"10.1080/13543776.2025.2491382","url":null,"abstract":"Introduction: The collective behavior of bacteria is regulated by Quorum Sensing (QS), in which bacteria release chemical signals and express virulence genes in a cell density-dependent manner. Quorum Sensing inhibitors (QSIs) are a large class of natural and synthetic compounds that have the potential to competitively inhibit the Quorum Sensing (QS) systems of several pathogens blocking their virulence mechanisms. They are considered promising compounds to deal with antimicrobial resistance, providing an opportunity to develop new drugs against these targets.Areas covered: The present review represents a comprehensive analysis of patents and patent applications available on Espacenet and Google Patent, from 2019 to 2023 referring to the therapeutic use of Quorum Sensing inhibitors.Expert opinion: Unlike classical antibiotics, which target the basic cellular metabolic processes, QSIs provide a promising alternative to attenuating virulence and pathogenicity without putting selective pressure on bacteria. The general belief is that QSIs pose no or little selective pressure on bacteria since these do not affect their growth. To date, QSIs are seen as the most promising alternative to traditional antibiotics. The next big step in this area of research is its succession to the clinical stage.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"657-673"},"PeriodicalIF":5.4,"publicationDate":"2025-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143981871","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

Novel inhibitors of STAT3: an updated patent review (2022-present). STAT3的新型抑制剂：更新的专利审查（2022年至今）。

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2025-07-01 Epub Date: 2025-04-22 DOI: 10.1080/13543776.2025.2494857

Keting Bao, Peiran Li, Dingding Gao

{"title":"Novel inhibitors of STAT3: an updated patent review (2022-present).","authors":"Keting Bao, Peiran Li, Dingding Gao","doi":"10.1080/13543776.2025.2494857","DOIUrl":"10.1080/13543776.2025.2494857","url":null,"abstract":"Introduction: Signal transducer and activator of transcription 3 (STAT3), a member of the STAT protein family, serves as both a signal transducer and a transcription factor. Previous studies have highlighted its pivotal roles in regulating cell proliferation, differentiation, apoptosis, as well as immune and inflammatory responses. Consequently, targeting STAT3 has emerged as a promising therapeutic strategy for addressing related diseases.Areas covered: This review offers a comprehensive summary of the progress in discovering STAT3 inhibitors, with a focus on their structural diversity and structure-activity relationships as presented in patent literature from 2022 to the present.Expert opinion: Over the past decades, significant progress has transformed STAT3 into a target of interest for drug development. Despite these advances, no STAT3-targeting drugs have successfully progressed through late-phase clinical trials, largely due to challenges such as limited selectivity and undesirable side effects. These obstacles highlight the inherent complexity of developing safe and effective STAT3 inhibitors. Nevertheless, STAT3 remains a highly promising therapeutic target, and ongoing advancements in this field hold the potential to unlock novel strategies for addressing STAT3-related diseases.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"695-717"},"PeriodicalIF":5.4,"publicationDate":"2025-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144005104","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

A patent review of IDO1 inhibitors for cancer (2023 - present): an update. 用于癌症的IDO1抑制剂的专利审查（2023年至今）：更新。

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2025-07-01 Epub Date: 2025-05-25 DOI: 10.1080/13543776.2025.2510641

Hanyue Qiu, Yiheng Yin, Ziyu Qin, Dongdong Li, Pengfei Wang

{"title":"A patent review of IDO1 inhibitors for cancer (2023 - present): an update.","authors":"Hanyue Qiu, Yiheng Yin, Ziyu Qin, Dongdong Li, Pengfei Wang","doi":"10.1080/13543776.2025.2510641","DOIUrl":"10.1080/13543776.2025.2510641","url":null,"abstract":"Introduction: Indoleamine 2,3-dioxygenase 1 (IDO1) is a promising target in cancer immunotherapy, yet its application faces significant challenges due to complex mechanisms of action. Recent advancements in IDO1 inhibitors aim to tackle these issues, potentially paving the way for successful therapeutic development.Areas covered: This review highlights patent publications (2023-2024) related to IDO1 inhibitors with potential anti-cancer applications, sourced from Espacenet and Google Scholar.Expert opinion: IDO1 exhibits complex mechanisms of action and variable expression across different cancer types, presenting both challenges and opportunities. Its intricate mechanisms in tumor development and immune evasion pose significant challenges for translating IDO1 inhibitors into clinical drugs. However, recent advancements in AI-guided drug design, combination therapies, and improved drug delivery methods offer promising insights for enhancing IDO1 inhibitors, although further data is warranted. Despite these challenges, the increasing availability of IDO1 crystal structures and a deeper understanding of its biological roles support ongoing trials that combine IDO1 inhibitors with other therapies. These developments hold potential for improving therapeutic outcomes in cancer treatment. Moreover, the growing interest in applying IDO1 inhibitors to other diseases could stimulate further research and development of new IDO1 inhibitors, potentially benefiting their application in cancer therapy as well.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"719-733"},"PeriodicalIF":5.4,"publicationDate":"2025-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144141809","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

A patent review of anti-coronavirus agents targeting the spike-ACE2 interaction (2019-present). 针对刺突- ace2相互作用的抗冠状病毒药物专利审查（2019年至今）

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2025-07-01 Epub Date: 2025-04-24 DOI: 10.1080/13543776.2025.2494860

Xing Huang, Heng Gao, Jiwei Zhang, Peng Zhan, Xinyong Liu

{"title":"A patent review of anti-coronavirus agents targeting the spike-ACE2 interaction (2019-present).","authors":"Xing Huang, Heng Gao, Jiwei Zhang, Peng Zhan, Xinyong Liu","doi":"10.1080/13543776.2025.2494860","DOIUrl":"10.1080/13543776.2025.2494860","url":null,"abstract":"Introduction: The Angiotensin-converting enzyme 2 (ACE2) receptor, crucial for coronavirus recognition of host cells, is a key target for therapeutic intervention against SARS-CoV-2 and related coronaviruses. Therefore, thoroughly investigating the interaction mechanism between ACE2 and the Spike protein (S protein), as well as developing targeted inhibitors based on this mechanism, is vital for effectively controlling the spread of SARS-CoV-2 and preventing potential future pandemics caused by other coronaviruses.Areas covered: This article comprehensively reviews the mechanisms underlying ACE2-S protein interaction that facilitate SARS-CoV-2 entry into host cells. It also analyzes the patent landscape regarding inhibitors targeting the ACE2-S interface since 2019.Expert opinion: In the 5 years since the outbreak of SARS-CoV-2, numerous methods and design strategies have been employed to develop innovative therapeutics against coronaviruses. Among these approaches, inhibitors targeting both the ACE2 receptor and the S protein have gained significant interest due to their potential in blocking various coronaviruses. Despite facing challenges similar to other protein-protein interaction inhibitors, progress has been made in developing these inhibitors through virtual screening, covalent protein binding, and peptide modification strategies. However, obstacles persist in clinical translation, necessitating a multidisciplinary strategy that integrates state-of-the-art methodologies to optimize S-ACE2 interface-targeted drug discovery.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"735-746"},"PeriodicalIF":5.4,"publicationDate":"2025-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143990595","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

A patent review of IDH1 inhibitors (2018-present). IDH1抑制剂专利审查（2018年至今）。

IF 5.4 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2025-07-01 Epub Date: 2025-05-07 DOI: 10.1080/13543776.2025.2500959

Qing Liang, Fei Wen, Peilin Wang, Yitong Jiang, Yuting Geng, Xiaoming Zha

{"title":"A patent review of IDH1 inhibitors (2018-present).","authors":"Qing Liang, Fei Wen, Peilin Wang, Yitong Jiang, Yuting Geng, Xiaoming Zha","doi":"10.1080/13543776.2025.2500959","DOIUrl":"10.1080/13543776.2025.2500959","url":null,"abstract":"Introduction: isocitrate dehydrogenase 1 (IDH1), a key metabolic enzyme in the cytosol, catalyzes the oxidative decarboxylation of isocitrate to produce α-ketoglutarate (α-KG) and NADPH in the TCA cycle. Pan-cancer studies have demonstrated that IDH1 exhibits a higher mutation frequency and is implicated in a broader range of cancer types, indicating its potential as a promising anti-tumor target.Areas covered: We summarized patents from 2018 to the present that identify novel molecules, compounds, formulations, and methods for inhibiting mIDH1. The literature was retrieved from Web of Science and PubMed. Patent information was obtained via the State Intellectual Property Office's Patent Search and Analysis platform. Clinical data were sourced from the Cortellis Drug Discovery Intelligence database. The date of the most recent search was .Expert opinion: Due to multiple signaling pathway dysregulations and compensatory pathways in solid tumor, monotherapies targeting mutant IDH1 (mIDH1) often fail to achieve desired therapeutic outcomes. Consequently, the combination of mIDH1 inhibitors with other therapeutic agents can enhance the efficacy of antitumor treatments and mitigate the risk of drug resistance. Moreover, the development of novel dual or multiple inhibitors and functional molecules targeting mIDH1 May represent a more promising approach.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"747-774"},"PeriodicalIF":5.4,"publicationDate":"2025-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143995051","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