Expert Opinion on Therapeutic Patents最新文献_第10页

A patent review on aldehyde dehydrogenase inhibitors: an overview of small molecule inhibitors from the last decade. 醛脱氢酶抑制剂专利综述:近十年来小分子抑制剂的研究概况。

IF 6.6 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2023-10-01 Epub Date: 2024-01-10 DOI: 10.1080/13543776.2023.2287515

Biswajit Kundu, Malliga R Iyer

{"title":"A patent review on aldehyde dehydrogenase inhibitors: an overview of small molecule inhibitors from the last decade.","authors":"Biswajit Kundu, Malliga R Iyer","doi":"10.1080/13543776.2023.2287515","DOIUrl":"10.1080/13543776.2023.2287515","url":null,"abstract":"Introduction: Physiological and pathophysiological effects arising from detoxification of aldehydes in humans implicate the enzyme aldehyde dehydrogenase (ALDH) gene family comprising of 19 isoforms. The main function of this enzyme family is to metabolize reactive aldehydes to carboxylic acids. Dysregulation of ALDH activity has been associated with various diseases. Extensive research has since gone into studying ALHD isozymes, their structural biology and developing small-molecule inhibitors. Novel chemical strategies to enhance the selectivity of ALDH inhibitors have now appeared.Areas covered: A comprehensive review of patent literature related to aldehyde dehydrogenase inhibitors in the last decade and half (2007-2022) is provided.Expert opinion: Aldehyde dehydrogenase (ALDH) is an important enzyme that metabolizes reactive exogenous and endogenous aldehydes in the body through NAD(P)±dependent oxidation. Hence this family of enzymes possess important physiological as well as toxicological roles in human body. Significant efforts in the field have led to potent inhibitors with approved clinical agents for alcohol use disorder therapy. Further clinical translation of novel compounds targeting ALDH inhibition will validate the promised therapeutic potential in treating many human diseases.The scientific/patent literature has been searched on SciFinder-n, Reaxys, PubMed, Espacenet and Google Patents. The search terms used were 'ALDH inhibitors', 'Aldehyde Dehydrogenase Inhibitors'.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"651-668"},"PeriodicalIF":6.6,"publicationDate":"2023-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138458941","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

SREBP inhibitors: an updated patent review for 2008-present. SREBP 抑制剂：2008 年至今的最新专利回顾。

IF 6.6 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2023-10-01 Epub Date: 2024-01-10 DOI: 10.1080/13543776.2023.2291393

Zhenyu Peng, Leyuan Chen, Manjiang Wang, Xufan Yue, Huiqiang Wei, Feifei Xu, Wenbin Hou, Yiliang Li

{"title":"SREBP inhibitors: an updated patent review for 2008-present.","authors":"Zhenyu Peng, Leyuan Chen, Manjiang Wang, Xufan Yue, Huiqiang Wei, Feifei Xu, Wenbin Hou, Yiliang Li","doi":"10.1080/13543776.2023.2291393","DOIUrl":"10.1080/13543776.2023.2291393","url":null,"abstract":"Introduction: Sterol regulatory element-binding proteins (SREBPs) are a family of membrane-binding transcription factors that activate genes encoding enzymes required for cholesterol and unsaturated fatty acid synthesis. Overactivation of SREBP is related to the occurrence and development of diabetes, nonalcoholic fatty liver, tumor, and other diseases. In the past period, many SREBP inhibitors have been found.Areas covered: This manuscript is a patent review of SREBP inhibitors. We searched 2008 to date for all data from the US patent database (https://www.uspto.gov/) and the European patent database (https://www.epo.org/) with 'SREBP' and 'inhibitor' as keywords and analyzed the search results.Expert opinion: Both synthetic and natural SREBP inhibitors have been reported. Despite the lack of cocrystal structure of SREBP inhibitor, the mechanisms of several compounds have been clarified. Importantly, some SREBP inhibitors have been proved to have good activity in preclinical studies. As the characteristics of lipid metabolism reprogramming in cardio-cerebrovascular diseases and tumors are gradually revealed, more and more attention will be focused on SREBP.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"669-680"},"PeriodicalIF":6.6,"publicationDate":"2023-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138487059","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 matrix metalloproteinase (MMP) inhibitors (2021-present). 基质金属蛋白酶(MMP)抑制剂专利综述(2021年至今)

IF 6.6 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2023-10-01 Epub Date: 2024-01-10 DOI: 10.1080/13543776.2023.2284935

Suvankar Banerjee, Sandip Kumar Baidya, Nilanjan Adhikari, Tarun Jha

{"title":"An updated patent review of matrix metalloproteinase (MMP) inhibitors (2021-present).","authors":"Suvankar Banerjee, Sandip Kumar Baidya, Nilanjan Adhikari, Tarun Jha","doi":"10.1080/13543776.2023.2284935","DOIUrl":"10.1080/13543776.2023.2284935","url":null,"abstract":"Introduction: Matrix metalloproteinases (MMPs) are strongly interlinked with the progression and mechanisms of several life-threatening diseases including cancer. Thus, novel MMP inhibitors (MMPIs) as promising drug candidates can be effective in combating these diseases. However, no MMPIs are marketed to date due to poor pharmacokinetics and lower selectivity. Therefore, this review was performed to study the newer MMPIs patented after the COVID-19 period for an updated perspective on MMPIs.Areas covered: This review highlights patents related to MMPIs, and their therapeutic implications published between January 2021 and August 2023 available in the Google Patents, Patentscope, and Espacenet databases.Expert opinion: Despite various MMP-related patents disclosed up to 2020, newer patent applications in the post-COVID-19 period decreased a lot. Besides major MMPs, other isoforms (i.e. MMP-3 and MMP-7) have gained attention recently for drug development. This may open up newer dimensions targeting these MMPs for therapeutic advancements. The isoform selectivity and bioavailability are major concerns for effective MMPI development. Thus, adopting theoretical approaches and experimental methodologies can unveil the development of novel MMPIs with improved pharmacokinetic profiles. Nevertheless, the involvement of MMPs in cancer, and the mechanisms of such MMPs in other diseases should be extensively studied for novel MMPI development.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"631-649"},"PeriodicalIF":6.6,"publicationDate":"2023-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138046694","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

Nanoparticles in pancreatic cancer therapy: a detailed and elaborated review on patent literature. 纳米颗粒在胰腺癌治疗:专利文献的详细和详细的审查。

IF 6.6 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2023-10-01 Epub Date: 2024-01-10 DOI: 10.1080/13543776.2023.2287520

Mohini Singh, Bani Kumar Jana, Paulami Pal, Ishita Singha, Ananya Rajkumari, Pinky Chowrasia, Venessa Nath, Bhaskar Mazumder

{"title":"Nanoparticles in pancreatic cancer therapy: a detailed and elaborated review on patent literature.","authors":"Mohini Singh, Bani Kumar Jana, Paulami Pal, Ishita Singha, Ananya Rajkumari, Pinky Chowrasia, Venessa Nath, Bhaskar Mazumder","doi":"10.1080/13543776.2023.2287520","DOIUrl":"10.1080/13543776.2023.2287520","url":null,"abstract":"Introduction: Nanotechnology may open up new avenues for overcoming the challenges of pancreatic cancer therapy as a broad arsenal of anticancer medicines fail to realize their full therapeutic potential in pancreatic ductal adenocarcinoma due to the formation of multiple resistance mechanisms inside the tumor. Many studies have reported the successful use of various nano formulations in pancreatic cancer therapy.Areas covered: This review covers all the major nanotechnology-based patent litrature available on renowned patent data bases like Patentscope and Espacenet, through the time period of 2007-2022. This is an entirely patent centric review, and it includes both clinical and non-clinical data available on nanotechnology-based therapeutics and diagnostic tools for pancreatic cancer.Expert opinion: For the sake of understanding, the patents are categorized under various formulation-specific heads like metallic/non-metallic nanoparticles, polymeric nanoparticles, liposomes, carbon nanotubes, protein nanoparticles and liposomes. This distinguishes one specific nanoparticle type from another and makes this review a one-of-a-kind comprehensive patent compilation that has not been reported so far in the history of nanotechnological formulations in pancreatic cancer.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"681-699"},"PeriodicalIF":6.6,"publicationDate":"2023-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138290697","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 AKT inhibitors (2020 - present). Akt抑制剂的最新专利综述（2020年至今）。

IF 6.6 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2023-07-01 Epub Date: 2023-11-28 DOI: 10.1080/13543776.2023.2273895

Linjie Li, Yu Guo, Yang Lu, Yaping Xu, Yan Lu, Xiuping Zhu, Xiaowu Dong, Jinxin Che

{"title":"An updated patent review of AKT inhibitors (2020 - present).","authors":"Linjie Li, Yu Guo, Yang Lu, Yaping Xu, Yan Lu, Xiuping Zhu, Xiaowu Dong, Jinxin Che","doi":"10.1080/13543776.2023.2273895","DOIUrl":"10.1080/13543776.2023.2273895","url":null,"abstract":"Introduction: Protein kinase B (Akt), an essential protein in the PI3K/Akt/mTOR signaling pathway, plays a crucial role in tumor progression. Over the past two years, different types of Akt modulators have continued to emerge in the patent literature.Areas covered: This review focuses on the patent literature covering small molecule inhibitors, peptides, PROTACs, and antisense nucleic acids targetingAkt from 2020 to present. Also, we discuss the outcomes of several clinical trials, combination strategies for different mechanisms, and the application of Akt regulators in other non-oncology indications.Our search for relevant information was conducted using various databases, including the European Patent Office, SciFinder, andPubMed, from 01.2020 to 04.2023.Expert opinion: In recent years, some combination therapeutic strategies involvingAkt inhibitors have shown promising clinical outcomes. Future research can be directed toward developing new applications of Akt inhibitors, which may have implications for other diseases beyond cancer. New attempts suggest that targeting allosteric sites may be a potential solution to the problem of isoform selectivity.Furthermore, directly knocking out Akt protein by using the degraderssuggests a promising direction for future development.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"549-564"},"PeriodicalIF":6.6,"publicationDate":"2023-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"49676120","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

Type I inhibitors of tropomyosin receptor kinase (Trk): a 2020-2022 patent update. 原肌球蛋白受体激酶（Trk）的I型抑制剂：2020-2022年专利更新。

IF 6.6 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2023-07-01 Epub Date: 2023-11-06 DOI: 10.1080/13543776.2023.2262136

Carolin Jaworski, Petar Iliev, Carmen Wängler, Björn Wängler, Brent Page, Ralf Schirrmacher, Justin J Bailey

{"title":"Type I inhibitors of tropomyosin receptor kinase (Trk): a 2020-2022 patent update.","authors":"Carolin Jaworski, Petar Iliev, Carmen Wängler, Björn Wängler, Brent Page, Ralf Schirrmacher, Justin J Bailey","doi":"10.1080/13543776.2023.2262136","DOIUrl":"10.1080/13543776.2023.2262136","url":null,"abstract":"Introduction: Trk inhibitors are significant in the realm of personalized medicine as they target specific genetic alterations, such as NTRK gene fusions, leading to improved treatment outcomes for cancer patients. By tailoring the treatment to the genetic characteristics of the tumor rather than the tumor type, Trk inhibitors offer the potential for more effective and precise therapies, resulting in enhanced response rates and prolonged survival for patients with NTRK fusion-positive cancers.Areas covered: Patents covering type I inhibitors targeting the Trk family are discussed, building upon our prior review series on Trk inhibitors. Relevant patents were identified through the Web of Science database, Google, and Google Patents.Expert opinion: The field of Trk inhibitors has evolved significantly, as reflected in the current patent literature, which emphasizes the selective structural refinement of clinical champions. Efforts now concentrate on enhancing efficacy against on-target resistance mechanisms, with modifications made to improve potency, reduce toxicity, and enhance pharmacokinetics. Combination therapies show potential to address off-target resistance mechanisms and improve treatment outcomes. Challenges remain in accurately diagnosing NTRK gene alterations and integrating screening into routine clinical practice. Trk inhibitors have surpassed their conventional role of inhibition and are now seeing new applications in radiopharmaceutical development and as molecular targeting agents.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"503-521"},"PeriodicalIF":6.6,"publicationDate":"2023-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41147051","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

N-acetylgalactosamine delivery systems for RNA therapeutics: a patent perspective. 用于RNA治疗的N-乙酰氨基半乳糖递送系统：专利视角。

IF 6.6 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2023-07-01 Epub Date: 2023-11-28 DOI: 10.1080/13543776.2023.2277249

Hai-Long Zhang, Lansuo Wang

{"title":"N-acetylgalactosamine delivery systems for RNA therapeutics: a patent perspective.","authors":"Hai-Long Zhang, Lansuo Wang","doi":"10.1080/13543776.2023.2277249","DOIUrl":"10.1080/13543776.2023.2277249","url":null,"abstract":"Introduction: SiRNA molecules with a feature of good gene-silencing are critical for drug discovery and development based on RNA interference. GalNAc-RNA therapeutics is a rapid growing area in RNA therapeutics.Areas covered: This article provides patent landscape and modification feature of GalNAc-RNA therapeutics. The US-granted patents from January 2004 to April 2023 were retrieved and analyzed.Expert opinion: Globally, our study is the first one to holistically depict a map of modifications and therapeutic applications for GalNAc-RNA therapeutics by patent data analysis. The results showed there were 8 major modifications and 5 new emerged modifications for GalNAc-RNA therapeutic agents. Especially, the study provides recent new emerged modifications in sugar, base, and internucleotide linkage of GalNAc-RNA therapeutic agents, e.g. morpholino-type ring, 5-methylcytosine, and phosphorodithioates. In addition, our study systematically demonstrated major therapeutic applications for GalNAc-RNA therapeutics, including liver or gallbladder disorders, anticancer, antihyperlipidemics, and disorders of the nervous system etc.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"539-547"},"PeriodicalIF":6.6,"publicationDate":"2023-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"61561764","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

Therapeutic treatment strategies for the management of onychomycosis: a patent perspective. ONYCHOMCOSIS治疗策略：专利视角。

IF 6.6 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2023-07-01 Epub Date: 2023-11-28 DOI: 10.1080/13543776.2023.2268278

Snigdha Chakraborty, Sanshita, Inderbir Singh

{"title":"Therapeutic treatment strategies for the management of onychomycosis: a patent perspective.","authors":"Snigdha Chakraborty, Sanshita, Inderbir Singh","doi":"10.1080/13543776.2023.2268278","DOIUrl":"10.1080/13543776.2023.2268278","url":null,"abstract":"Introduction: Onychomycosis, a multifactorial fungal infection of the nails, shows a global prevalence of about 5.5% and is responsible for 50% of all nail infections. To develop effective management strategies, it is necessary to understand the etiology, pathophysiology, and risk factors of onychomycosis. Oral route of drug delivery is one of the routes utilized to deliver anti-fungal agents, but, has its own limitations like longer duration of treatment, increased adverse effects, and potential for drug interaction. The ungual route has received greater attention due to its localized, non- invasive action and improved patient compliance.Areas covered: This review comprehensively discusses conventional onychomycosis therapies and patented novel drug delivery systems for the management of onychomycosis including chemical permeation enhancers, non-particulate drug delivery systems, penetration enhancing devices etc., Databases such as PubMed, ResearchGate, and Google Patents were searched by using the keywords onychomycosis and trans-ungual drug delivery.Expert opinion: Enormous research has been conducted and is still ongoing to find the best possible novel drug delivery system for onychomycosis management. Approaches like incorporation of herbal constituents in nano-formulations, inkjet printing, laser devices, iontophoretic techniques, etc. can be employed to make safe and effective drug delivery systems which are regulatory compliant.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"613-630"},"PeriodicalIF":6.6,"publicationDate":"2023-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41128178","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 GLP-1 receptor agonists (2020-present). GLP-1受体激动剂的最新专利综述（2020至今）。

IF 6.6 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2023-07-01 Epub Date: 2023-11-28 DOI: 10.1080/13543776.2023.2274905

Weiwen Lu, Zhongbo Zhou, Neng Jiang, Jing Han

{"title":"An updated patent review of GLP-1 receptor agonists (2020-present).","authors":"Weiwen Lu, Zhongbo Zhou, Neng Jiang, Jing Han","doi":"10.1080/13543776.2023.2274905","DOIUrl":"10.1080/13543776.2023.2274905","url":null,"abstract":"Introduction: Type 2 diabetes (T2DM) and obesity present significant global health issues, requiring the development of long-lasting and highly effective pharmacotherapies. Although glucagon-like peptide-1 receptor agonists (GLP-1RAs) are commonly used for diabetes treatment, their potential for addressing obesity is still being explored.Areas covered: This review offers a comprehensive overview of recently published patents from January 2020 to July 2023, focusing on modified GLP-1RAs, small molecule GLP-1RAs, GLP-1 R-based multi-agonists, GLP-1RA-based fusion proteins, and combination therapies. The patents discussed pertain to the treatment and prevention of diabetes and obesity. Patent searches were conducted using the PATENTSCOPE database of the World Intellectual Property Organization, using the keywords GLP-1, GLP-1/GIP, GLP-1/GCG, and GLP-1/GCG/GIP.Expert opinion: In recent years, patents have emphasized two main goals for developing GLP-1RAs drugs: oral delivery and improved weight reduction effects. To address the growing demand for improved treatments, researchers have focused their efforts on developing GLP-1 R-based multi-agonists, orally administered GLP-1RAs, and combination therapies utilizing GLP-1RAs. These new approaches offer promising benefits, such as improved effectiveness by targeting multiple pathways and reduced side effects. Additionally, the development of new uses, oral forms, and long-lasting preparations will be crucial in shaping the future market potential of GLP-1 drugs.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"597-612"},"PeriodicalIF":6.6,"publicationDate":"2023-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"49689564","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 metallo-β-lactamase inhibitors (2020-2023). 金属-β-内酰胺酶抑制剂的最新专利综述（2020-2023）。

IF 6.6 2区医学

Expert Opinion on Therapeutic Patents Pub Date : 2023-07-01 Epub Date: 2023-11-06 DOI: 10.1080/13543776.2023.2262763

Elsa Denakpo, Thierry Naas, Bogdan I Iorga

{"title":"An updated patent review of metallo-β-lactamase inhibitors (2020-2023).","authors":"Elsa Denakpo, Thierry Naas, Bogdan I Iorga","doi":"10.1080/13543776.2023.2262763","DOIUrl":"10.1080/13543776.2023.2262763","url":null,"abstract":"Introduction: Metallo-β-lactamases (MBLs) are enzymes produced by bacteria that confer resistance to most β-lactam antibiotics, including carbapenems, which have the broadest spectrum of activity. This resistance mechanism poses a significant threat to public health as it drastically reduces treatment options for severe bacterial infections. Developing effective inhibitors against MBLs is crucial to restore susceptibility to β-lactam antibiotics.Areas covered: This review aims to provide an updated analysis of patents describing novel MBL inhibitors and their potential therapeutic applications that were filed between January 2020 and May 2023.Expert opinion: Significant advancements were made in the development of selective MBL inhibitors with zinc-binding and zinc-chelating mechanisms of action. Dual inhibitors, targeting simultaneously both serine-β-lactamases (SBLs) and MBLs, represent an interesting alternative approach that is increasingly pertinent for the treatment of infections involving multiple β-lactamases from different Ambler classes. Most examples of MBL-specific inhibitors were focused on the treatment of MBL-mediated infections in Enterobacterales, where IMP-1 was a more difficult target compared with VIM-1 or NDM-1, and much less on Pseudomonas aeruginosa or Acinetobacter baumannii, which are more challenging to address.","PeriodicalId":12314,"journal":{"name":"Expert Opinion on Therapeutic Patents","volume":" ","pages":"523-538"},"PeriodicalIF":6.6,"publicationDate":"2023-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41119008","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