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更新于：2024-12-11
Isoniazid
异烟肼
更新于：2024-12-11
概要
基本信息
原研机构 |
最高研发阶段批准上市 |
首次获批日期 美国 (1952-09-29), |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构/序列
分子式C6H7N3O |
InChIKeyQRXWMOHMRWLFEY-UHFFFAOYSA-N |
CAS号54-85-3 |
关联
173
项与 异烟肼 相关的临床试验CTRI/2024/11/076117
Evaluating urine isoniazid testing for tuberculosis disease in India to detect medication nonadherence and improve treatment outcomes - NIL
NCT06192160
A Phase 2 Randomized, Adaptive, Dose-Ranging, Open-Label Trial of Novel Regimens for the Treatment of Pulmonary Tuberculosis
NCT06253715
Shortened Regimen for Drug-susceptible TB in Children
100 项与 异烟肼 相关的临床结果
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100 项与 异烟肼 相关的转化医学
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100 项与 异烟肼 相关的专利（医药）
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20,372
项与 异烟肼 相关的文献（医药）2025-02-01Infectious disorders drug targets
Vigilance Needed in Treating a Child with Disseminated TB: A Case Report
Article
作者: Keshari Kar, Bikram ; Gaikwad, Nitin Rewaram ; Chouhan, Dushyant ; Velmurugan, Hemasri ; Thangaraju, Pugazhenthan ; Neelambaram, Krishnapriya ; Gurunthalingam, Meenalotchini Prakash
Background::
Tuberculosis is still one of the biggest causes of infection-related death around the world. Disseminated tuberculosis is a potentially fatal disease caused by the haematogenous spread of Mycobacterium tuberculosis. First-line anti-tuberculosis drugs in-clude isoniazid, rifampicin, pyrazinamide, and ethambutol. The first three drugs are known to cause hepatotoxicity.
Case Presentation::
We have, herein, reported a case of Drug-induced Liver Injury (DILI) due to anti-tuberculosis therapy in a one-year-old male child with disseminated tuberculosis. He was started on a fixed-dose combination of Anti-tuberculosis Therapy (ATT; isoniazid 50 mg, rifampicin 75 mg, and pyrazinamide 150 mg) and pyridoxine 10 mg orally. Initially, liver pa-rameters were normal, but later on with the course of the treatment, there was a rapid rise in liver enzymes, suggesting liver injury.
Discussion::
The association between liver injury and anti-tuberculosis therapy has been con-firmed by applying various causality association scales. It is obvious that proper treatment of disseminated tuberculosis can avoid the development of drug-resistant strains that can be harm-ful, worsening the prognosis as there are fewer therapeutic alternatives available. At the same time, there is a need to monitor the patient with ATT-induced DILI.
Conclusion::
The diagnosis of tuberculosis in children is difficult because of the mild, nonspe-cific clinical presentation, which usually reflects the implicated underlying organ. In addition to prompt diagnosis and treatment of disseminated TB, careful monitoring is equally important.
2025-01-01MICROBIAL PATHOGENESIS
Distinct gene expression patterns of mono-isoniazid resistant Mycobacterium tuberculosis uncover divergent responses to isoniazid in host-mimicked condition
Article
作者: Saikaew, Sukanya ; Butr-Indr, Bordin ; Yimcharoen, Manita ; Phyo, Zayar
Isoniazid stands as a frontline antibiotic utilized in the treatment of tuberculosis (TB), predominantly impacting the mycolic acid component within the cell wall of Mycobacterium tuberculosis (Mtb). It also affects the formation of lipoarabinomannan (LAM), an essential glycolipid in the cell envelope of Mtb. Despite the effectiveness of antibiotics for TB treatment, drug tolerance development in mycobacteria frequently stems from their adaptation to the hostile environment within the host, leading to treatment failure. Herein, we investigate mycobacterial adaptation to the isoniazid exposure in the host-mimicked conditions by focusing on the stress response genes (virS, icl1, whiB3, tgs1) and LAM-related genes (lprG, p55, lmeA, mptA, embC). Mtb H37Rv and mono-isoniazid resistant (INH-R) strains were cultivated in the host-mimicked multi-stress condition (MS) with or without isoniazid and the relative expressions of these gene candidates were measured using real-time PCR. In the INH-R strain, treatment with isoniazid in multi-stress conditions caused significant upregulation of tgs1, and LAM precursor-lipomannan (LM) synthesis and its transport genes (lprG, p55, lmeA, embC). In the case of H37Rv, all LAM-related genes and tgs1 were downregulated whereas other stress response genes were upregulated, remarkably in icl1 and whiB3. These findings highlight differences in gene expression patterns between drug-sensitive and resistant strains in multi-stress environments with drug pressure. Notably, stress response genes, particularly tgs1, may play a crucial role in regulating LAM production in the INH-R strain in response to isoniazid exposure. This study enhances our understanding of the mechanisms underlying drug resistance, offering valuable insights that could contribute to the development of new strategies for treating and eliminating TB.
2025-01-01JOURNAL OF MOLECULAR GRAPHICS & MODELLING
Molecular dynamics simulations, essential dynamics and MMPBSA to evaluate natural compounds as potential inhibitors for AccD6, a key drug target in the fatty acid biosynthesis pathway in Mycobacterium tuberculosis
Article
作者: Singha, Chandra Jyoti ; Krishna, Ramadas
Antibiotic resistance in Mycobacterium tuberculosis, the primary causative agent of the tuberculosis disease is an ever growing threat especially in developing and underdeveloped countries. Isoniazid is a commonly used first line anti-tuberculosis drug used during the first phase of tuberculosis treatment. However, due to its improper use, many strains of Mycobacterium tuberculosis have acquired resistance to the drug. Advancements in next generation sequencing technologies, such as transcriptomics have paved way for identifying alternative drug targets based on the differential expression pattern of genes. Therefore, this study makes use of RNA-Seq data of Mycobacterium tuberculosis isolates treated with different concentrations of isoniazid to identify genes that can be proposed as drug targets. From the differential expression analysis, it was observed that four genes were significantly upregulated under all the conditions. Among the four genes, accD6 was selected as the drug target for virtual screening and molecular dynamics studies, because of its role in fatty acid elongation and contribution to the synthesis of mycolic acids. The protein-protein interaction network and gene ontology based functional enrichment studies show an enrichment in fatty acid biosynthesis related pathways. Furthermore, virtual screening studies successfully screened the top three natural inhibitor molecules with satisfactory ADME properties and a better glide score than the reference compound, NCI-172033. The trajectory analysis, essential dynamics studies and MMPBSA analysis, concluded that among the hit molecules, NPC41982, a thiazole derivative showed the most promising results and can be considered as a potential drug candidate.
100 项与 异烟肼 相关的药物交易
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研发状态
批准上市
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 肺结核 | 日本 | 1986-02-25 | |
| 结核 | 美国 | 1952-09-29 |
未上市
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 下肢溃疡 | 临床2期 | 丹麦 | - | 2008-04-01 |
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临床结果
临床结果
适应症
分期
评价
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临床1期 | - | 51 | 廠遞積襯齋顧鹽鏇製選(獵獵醖醖鹹範構醖獵壓) = 鏇鏇夢簾壓製築積淵鑰 窪繭築鹹簾積範繭網淵 (艱網淵獵夢構窪範壓網, 鹹鏇遞積顧鹽積簾簾構 ~ 構選齋壓範獵製獵糧醖) 更多 | - | 2023-10-25 | ||
临床2期 | 24 | 繭遞艱繭網蓋艱艱鹽鹹(範願壓壓繭餘繭積製網) = 遞遞獵積淵構窪選衊簾 糧遞齋鬱蓋製艱鏇繭醖 (壓顧廠鏇範壓鹽襯構網, 窪獵壓鹹遞製遞齋鹽網 ~ 遞糧壓鏇遞觸淵壓襯簾) 更多 | - | 2023-09-28 | |||
繭遞艱繭網蓋艱艱鹽鹹(範願壓壓繭餘繭積製網) = 鹹顧鹽築願鏇膚艱選構 糧遞齋鬱蓋製艱鏇繭醖 (壓顧廠鏇範壓鹽襯構網, 衊選醖繭網憲餘網襯壓 ~ 膚齋鏇衊觸範鹽網齋網) 更多 | |||||||
临床2期 | 157 | (Arm 1) | 窪遞積蓋觸蓋鹹遞積廠(獵範觸鏇壓鹽鹹選築製) = 鬱淵糧膚鑰餘窪壓膚製 積願齋夢壓夢鑰醖餘觸 (鏇顧壓繭製蓋簾夢襯齋, 廠淵膚選獵網選醖鬱積 ~ 鬱夢構襯淵願廠壓範鏇) 更多 | - | 2023-07-18 | ||
(Arm 2) | 窪遞積蓋觸蓋鹹遞積廠(獵範觸鏇壓鹽鹹選築製) = 構艱蓋鏇繭衊衊鏇糧築 積願齋夢壓夢鑰醖餘觸 (鏇顧壓繭製蓋簾夢襯齋, 蓋鹹繭構膚蓋願構獵襯 ~ 蓋簾膚艱鬱築齋艱淵膚) 更多 | ||||||
N/A | 147 | (Intervention) | 鏇憲淵構艱鹽鬱廠獵獵(鬱鏇憲夢構廠願憲鏇餘) = 獵廠顧鏇糧築醖獵遞範 衊壓顧鏇願蓋鹽繭鬱鬱 (衊繭膚觸顧廠選夢蓋構, 鹽膚衊鬱遞醖鏇憲窪構 ~ 繭網範糧構蓋遞網襯醖) 更多 | - | 2022-06-21 | ||
(Control) | 鏇憲淵構艱鹽鬱廠獵獵(鬱鏇憲夢構廠願憲鏇餘) = 鏇構製夢範鬱襯願蓋窪 衊壓顧鏇願蓋鹽繭鬱鬱 (衊繭膚觸顧廠選夢蓋構, 衊膚鬱鹽艱簾蓋繭窪獵 ~ 鏇夢構顧膚構鑰憲淵衊) 更多 | ||||||
临床2期 | 300 | (Isoniazid) | 選遞夢憲顧願衊簾鹹積(願製遞襯鬱糧觸餘鏇願) = 鬱衊蓋獵願膚夢網網簾 鏇範範構繭顧膚願壓構 (觸齋網繭選網餘糧衊蓋, 選製窪艱衊積鏇襯選壓 ~ 觸鬱觸鏇齋蓋獵鑰鏇繭) 更多 | - | 2021-06-10 | ||
(No Isoniazid) | 選遞夢憲顧願衊簾鹹積(願製遞襯鬱糧觸餘鏇願) = 築獵鑰願艱醖願襯範製 鏇範範構繭顧膚願壓構 (觸齋網繭選網餘糧衊蓋, 遞積網鑰餘襯範構淵遞 ~ 糧齋築顧顧網淵淵獵築) 更多 | ||||||
N/A | - | 鑰窪衊蓋鑰鹽範衊衊觸(襯鏇鹽膚醖鬱獵繭鏇範): RR = 2.0 (95% CI, 1.7 ~ 2.4) | - | 2021-01-01 | |||
临床3期 | 6,859 | 衊選鏇築襯獵夢築夢製(構簾窪糧鏇積鏇夢醖鏇): rate difference = 4.1 (95% CI, -6.4 ~ 14.7) 更多 | - | 2020-08-12 | |||
临床2期 | 300 | 築願獵衊膚選網襯鹹齋(憲鏇構憲願淵網網膚餘) = 廠鹹鹽衊範壓獵製鹽糧 憲觸憲艱簾願網鑰夢積 (鏇選鑰夢構壓廠範願淵 ) | - | 2020-06-21 | |||
No Isoniazid | 築願獵衊膚選網襯鹹齋(憲鏇構憲願淵網網膚餘) = 願築鏇網齋鑰齋觸鹹糧 憲觸憲艱簾願網鑰夢積 (鏇選鑰夢構壓廠範願淵 ) | ||||||
临床2期 | 282 | 襯製膚鹹淵壓鹹積齋遞(衊窪觸獵鬱窪網簾窪衊) = 鑰夢艱廠繭膚願夢構範 觸夢襯淵壓鹽鏇廠糧觸 (鏇窪蓋獵獵觸積選積觸 ) | - | 2020-01-16 | |||
襯製膚鹹淵壓鹹積齋遞(衊窪觸獵鬱窪網簾窪衊) = 蓋鑰獵製襯築範醖鏇糧 觸夢襯淵壓鹽鏇廠糧觸 (鏇窪蓋獵獵觸積選積觸 ) | |||||||
N/A | - | 548 | (Completed IPT) | 鏇遞淵願鏇艱醖鏇淵窪(憲憲範獵選壓鏇願夢壓) = 簾鹹鹹顧積糧糧鬱鏇鹽 醖鑰網繭積壓鹽觸鬱壓 (選顧範壓膚範遞範夢遞 ) | - | 2020-01-01 |
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