• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利:CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法,用中文像聊天一样搜索,搜遍4000万医学文献。AI智能推荐,让科研检索更轻松。

立即免费搜索

文件翻译

保留排版,准确专业,支持PDF/Word/PPT等文件格式,支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述,25分钟生成高质量综述,智能提取关键信息,辅助科研写作。

立即免费体验

呈现处于不同药物研发阶段的新型抗结核药物的化学类别:2010 - 2020年综述

Chemical Classes Presenting Novel Antituberculosis Agents Currently in Different Phases of Drug Development: A 2010-2020 Review.

作者信息

Angula Klaudia T, Legoabe Lesetja J, Beteck Richard M

机构信息

Centre of Excellence for Pharmaceutical Sciences (Pharmacen), North-West University, Potchefstroom 2520, South Africa.

出版信息

Pharmaceuticals (Basel). 2021 May 13;14(5):461. doi: 10.3390/ph14050461.

DOI:10.3390/ph14050461
PMID:34068171
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8152995/
Abstract

Tuberculosis (TB), caused by (Mtb), is a curable airborne disease currently treated using a drug regimen consisting of four drugs. Global TB control has been a persistent challenge for many decades due to the emergence of drug-resistant Mtb strains. The duration and complexity of TB treatment are the main issues leading to treatment failures. Other challenges faced by currently deployed TB regimens include drug-drug interactions, miss-matched pharmacokinetics parameters of drugs in a regimen, and lack of activity against slow replicating sub-population. These challenges underpin the continuous search for novel TB drugs and treatment regimens. This review summarizes new TB drugs/drug candidates under development with emphasis on their chemical classes, biological targets, mode of resistance generation, and pharmacokinetic properties. As effective TB treatment requires a combination of drugs, the issue of drug-drug interaction is, therefore, of great concern; herein, we have compiled drug-drug interaction reports, as well as efficacy reports for drug combinations studies involving antitubercular agents in clinical development.

摘要

由结核分枝杆菌(Mtb)引起的结核病(TB)是一种可治愈的空气传播疾病,目前使用由四种药物组成的治疗方案进行治疗。由于耐药Mtb菌株的出现,全球结核病控制几十年来一直是一项持续的挑战。结核病治疗的持续时间和复杂性是导致治疗失败的主要问题。目前采用的结核病治疗方案面临的其他挑战包括药物相互作用、治疗方案中药物的药代动力学参数不匹配以及对缓慢复制亚群缺乏活性。这些挑战促使人们不断寻找新型结核病药物和治疗方案。本综述总结了正在研发的新型结核病药物/候选药物,重点介绍了它们的化学类别、生物学靶点、耐药产生模式和药代动力学特性。由于有效的结核病治疗需要联合用药,因此药物相互作用问题备受关注;在此,我们汇编了药物相互作用报告以及涉及临床开发中抗结核药物的药物组合研究的疗效报告。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1a9a/8152995/76b2fb868d18/pharmaceuticals-14-00461-g013.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1a9a/8152995/dac41fb3aa2a/pharmaceuticals-14-00461-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1a9a/8152995/8a8727c8b5fa/pharmaceuticals-14-00461-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1a9a/8152995/ca4276c2b293/pharmaceuticals-14-00461-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1a9a/8152995/d06eab8a84db/pharmaceuticals-14-00461-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1a9a/8152995/46cf31d1a6be/pharmaceuticals-14-00461-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1a9a/8152995/386cbab242b4/pharmaceuticals-14-00461-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1a9a/8152995/fef72684fa3d/pharmaceuticals-14-00461-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1a9a/8152995/8bbf1b5da93c/pharmaceuticals-14-00461-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1a9a/8152995/38e5cb729d5b/pharmaceuticals-14-00461-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1a9a/8152995/0e9efb16cd80/pharmaceuticals-14-00461-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1a9a/8152995/7fa75aa38a27/pharmaceuticals-14-00461-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1a9a/8152995/85705c2c62a1/pharmaceuticals-14-00461-g011.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1a9a/8152995/e63bccd4d266/pharmaceuticals-14-00461-g012.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1a9a/8152995/76b2fb868d18/pharmaceuticals-14-00461-g013.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1a9a/8152995/dac41fb3aa2a/pharmaceuticals-14-00461-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1a9a/8152995/8a8727c8b5fa/pharmaceuticals-14-00461-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1a9a/8152995/ca4276c2b293/pharmaceuticals-14-00461-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1a9a/8152995/d06eab8a84db/pharmaceuticals-14-00461-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1a9a/8152995/46cf31d1a6be/pharmaceuticals-14-00461-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1a9a/8152995/386cbab242b4/pharmaceuticals-14-00461-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1a9a/8152995/fef72684fa3d/pharmaceuticals-14-00461-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1a9a/8152995/8bbf1b5da93c/pharmaceuticals-14-00461-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1a9a/8152995/38e5cb729d5b/pharmaceuticals-14-00461-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1a9a/8152995/0e9efb16cd80/pharmaceuticals-14-00461-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1a9a/8152995/7fa75aa38a27/pharmaceuticals-14-00461-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1a9a/8152995/85705c2c62a1/pharmaceuticals-14-00461-g011.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1a9a/8152995/e63bccd4d266/pharmaceuticals-14-00461-g012.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1a9a/8152995/76b2fb868d18/pharmaceuticals-14-00461-g013.jpg

相似文献

1
Chemical Classes Presenting Novel Antituberculosis Agents Currently in Different Phases of Drug Development: A 2010-2020 Review.呈现处于不同药物研发阶段的新型抗结核药物的化学类别:2010 - 2020年综述
Pharmaceuticals (Basel). 2021 May 13;14(5):461. doi: 10.3390/ph14050461.
2
[Development of antituberculous drugs: current status and future prospects].[抗结核药物的研发:现状与未来前景]
Kekkaku. 2006 Dec;81(12):753-74.
3
Editorial: Current status and perspective on drug targets in tubercle bacilli and drug design of antituberculous agents based on structure-activity relationship.社论:结核杆菌药物靶点的现状与展望以及基于构效关系的抗结核药物设计
Curr Pharm Des. 2014;20(27):4305-6. doi: 10.2174/1381612819666131118203915.
4
Tuberculosis结核病
5
Recent updates on drug resistance in Mycobacterium tuberculosis.结核分枝杆菌耐药性的最新研究进展。
J Appl Microbiol. 2020 Jun;128(6):1547-1567. doi: 10.1111/jam.14478. Epub 2019 Oct 29.
6
In vitro interaction profiles of the new antitubercular drugs bedaquiline and delamanid with moxifloxacin against clinical Mycobacterium tuberculosis isolates.新型抗结核药物贝达喹啉和德拉马尼与莫西沙星体外抗临床结核分枝杆菌分离株的相互作用特征。
J Glob Antimicrob Resist. 2019 Dec;19:348-353. doi: 10.1016/j.jgar.2019.06.013. Epub 2019 Jun 18.
7
Artificial intelligence enabled parabolic response surface platform identifies ultra-rapid near-universal TB drug treatment regimens comprising approved drugs.人工智能支持的抛物线响应面平台确定了包含已批准药物的超快速近通用结核病药物治疗方案。
PLoS One. 2019 May 10;14(5):e0215607. doi: 10.1371/journal.pone.0215607. eCollection 2019.
8
Delamanid: From discovery to its use for pulmonary multidrug-resistant tuberculosis (MDR-TB).地拉米定:从发现到用于治疗肺部耐多药结核病(MDR-TB)。
Tuberculosis (Edinb). 2018 Jul;111:20-30. doi: 10.1016/j.tube.2018.04.008. Epub 2018 May 3.
9
Tuberculosis drug development: progress, challenges, and the road ahead.结核病药物研发:进展、挑战与未来展望。
Tuberculosis (Edinb). 2010 May;90(3):162-7. doi: 10.1016/j.tube.2010.03.003. Epub 2010 Apr 9.
10
Bedaquiline and delamanid in tuberculosis.贝达喹啉与地拉米啶在结核病治疗中的应用
Expert Opin Pharmacother. 2015;16(15):2319-30. doi: 10.1517/14656566.2015.1080240. Epub 2015 Aug 19.

引用本文的文献

1
Population pharmacokinetic and exposure-response study of a novel anti-tuberculosis drug to inform its dosage design in phase III clinical trial.一种新型抗结核药物的群体药代动力学和暴露-反应研究,为其III期临床试验的剂量设计提供依据。
Eur J Pharm Sci. 2025 Sep 1;212:107160. doi: 10.1016/j.ejps.2025.107160. Epub 2025 Jun 8.
2
Innovative Strategies for Combating Multidrug-Resistant Tuberculosis: Advances in Drug Delivery Systems and Treatment.对抗耐多药结核病的创新策略:药物递送系统与治疗的进展
Microorganisms. 2025 Mar 24;13(4):722. doi: 10.3390/microorganisms13040722.
3
A Narrative Review of Bedaquiline and Delamanid: New Arsenals Against Multidrug-Resistant and Extensively Drug-Resistant Mycobacterium tuberculosis.

本文引用的文献

1
Pretomanid: The latest USFDA-approved anti-tuberculosis drug.贝达喹啉:最新获得美国 FDA 批准的抗结核药物。
Indian J Tuberc. 2021 Apr;68(2):287-291. doi: 10.1016/j.ijtb.2020.09.003. Epub 2020 Sep 6.
2
InhA inhibitors have activity against non-replicating Mycobacterium tuberculosis.InhA 抑制剂对非复制状态的结核分枝杆菌具有活性。
PLoS One. 2020 Nov 17;15(11):e0239354. doi: 10.1371/journal.pone.0239354. eCollection 2020.
3
TB47 and clofazimine form a highly synergistic sterilizing block in a second-line regimen for tuberculosis in mice.
贝达喹啉和德拉马尼的叙述性综述:针对耐多药和广泛耐药结核分枝杆菌的新武器。
J Clin Lab Anal. 2024 Aug;38(15-16):e25091. doi: 10.1002/jcla.25091.
4
Design, synthesis, anti-mycobacterial activity, molecular docking and ADME analysis of spiroquinoxaline-1,2,4-oxadiazoles via [3 + 2] cycloaddition reaction under ultrasound irradiation.超声辐射下通过[3 + 2]环加成反应设计、合成、抗分枝杆菌活性、分子对接及药物代谢动力学分析螺喹喔啉-1,2,4-恶二唑
Mol Divers. 2024 Dec;28(6):3979-3991. doi: 10.1007/s11030-023-10790-9. Epub 2024 Jan 23.
5
New nitazoxanide derivatives: design, synthesis, biological evaluation, and molecular docking studies as antibacterial and antimycobacterial agents.新型硝唑尼特衍生物:作为抗菌和抗分枝杆菌剂的设计、合成、生物学评价及分子对接研究
RSC Med Chem. 2023 Oct 10;14(12):2714-2730. doi: 10.1039/d3md00449j. eCollection 2023 Dec 13.
6
Bedaquiline Resistance and Molecular Characterization of Rifampicin-Resistant Isolates in Zhejiang, China.中国浙江地区耐利福平菌株的贝达喹啉耐药性及分子特征
Infect Drug Resist. 2023 Oct 31;16:6951-6963. doi: 10.2147/IDR.S429003. eCollection 2023.
7
Quinolone-3-amidoalkanol: A New Class of Potent and Broad-Spectrum Antimicrobial Agent.喹诺酮-3-酰胺醇:一类新型强效广谱抗菌剂。
ACS Omega. 2023 May 4;8(19):17086-17102. doi: 10.1021/acsomega.3c01406. eCollection 2023 May 16.
8
Machine Learning Prediction of Mycobacterial Cell Wall Permeability of Drugs and Drug-like Compounds.机器学习预测药物和类药化合物对分枝杆菌细胞壁的通透性。
Molecules. 2023 Jan 7;28(2):633. doi: 10.3390/molecules28020633.
9
Synthesis and Assessment of the In Vitro and Ex Vivo Activity of Salicylate Synthase (Mbti) Inhibitors as New Candidates for the Treatment of Mycobacterial Infections.水杨酸合酶(Mbti)抑制剂的体外和离体活性的合成与评估:作为治疗分枝杆菌感染的新候选药物
Pharmaceuticals (Basel). 2022 Aug 11;15(8):992. doi: 10.3390/ph15080992.
10
New Quinoline-Urea-Benzothiazole Hybrids as Promising Antitubercular Agents: Synthesis, In Vitro Antitubercular Activity, Cytotoxicity Studies, and In Silico ADME Profiling.新型喹啉-尿素-苯并噻唑杂化物作为有前景的抗结核药物:合成、体外抗结核活性、细胞毒性研究及计算机辅助ADME分析
Pharmaceuticals (Basel). 2022 May 5;15(5):576. doi: 10.3390/ph15050576.
替比培南和氯法齐明在二线结核治疗方案中对小鼠具有高度协同杀菌作用。
Biomed Pharmacother. 2020 Nov;131:110782. doi: 10.1016/j.biopha.2020.110782. Epub 2020 Sep 25.
4
Activity of Riminophenazines against Mycobacterium tuberculosis: A Review of Studies that Might be Contenders for Use as Antituberculosis Agents.利福喷丁类衍生物抗结核活性研究:有望成为抗结核药物的候选化合物。
ChemMedChem. 2020 Dec 3;15(23):2207-2219. doi: 10.1002/cmdc.202000580. Epub 2020 Oct 15.
5
[The main results of clinical trials of the efficacy, safety and pharmacokinetics of the perspective anti-tuberculosis drug makozinone (PBTZ169)].[新型抗结核药物马科齐农(PBTZ169)疗效、安全性及药代动力学的临床试验主要结果]
Ter Arkh. 2020 Apr 27;92(3):61-72. doi: 10.26442/00403660.2020.03.000621.
6
Tedizolid (torezolid) for the treatment of complicated skin and skin structure infections.替考拉宁(托罗佐利德)治疗复杂性皮肤和皮肤软组织感染。
Expert Rev Clin Pharmacol. 2020 Jun;13(6):577-592. doi: 10.1080/17512433.2020.1774362. Epub 2020 Jun 16.
7
New tuberculosis drug targets, their inhibitors, and potential therapeutic impact.新的结核病药物靶点、抑制剂及其潜在的治疗影响。
Transl Res. 2020 Jun;220:68-97. doi: 10.1016/j.trsl.2020.03.007. Epub 2020 Mar 16.
8
Synthetic Studies to Help Elucidate the Metabolism of the Preclinical Candidate TBAJ-876-A Less Toxic and More Potent Analogue of Bedaquiline.TBAJ-876-A 的合成研究——一种比贝达喹啉更具潜力、毒性更低的临床前候选药物的代谢阐明
Molecules. 2020 Mar 20;25(6):1423. doi: 10.3390/molecules25061423.
9
OPC-167832, a Novel Carbostyril Derivative with Potent Antituberculosis Activity as a DprE1 Inhibitor.新型碳氮唑衍生物 OPC-167832 作为 DprE1 抑制剂具有强大的抗结核活性。
Antimicrob Agents Chemother. 2020 May 21;64(6). doi: 10.1128/AAC.02020-19.
10
Treatment of Highly Drug-Resistant Pulmonary Tuberculosis.耐多药肺结核的治疗。
N Engl J Med. 2020 Mar 5;382(10):893-902. doi: 10.1056/NEJMoa1901814.