摘要
有效治疗结核病(TB)与发病率和死亡率有关。结核病的多药耐药的发展阻碍了结核病患者的治疗,并需要长期的治疗。第二芳基喹啉类衍生物bedaquiline通过FDA加速审批被批准在2012十二月作为联合治疗的一部分用于治疗成人肺结核的人有效的治疗方法是不可用的。双环硝基咪唑类药物delamanid和它的同伴pretomanid抑制分枝菌酸的合成通过未知的机制。2013年十一月,Delamanid收到MDR-TB治疗由欧洲药品局有条件批准。然而,由于毒性问题这两种药物的使用是有限的。如果旨在减少治疗时间是追求以控制成本和提高病人的依从性,它是强制性的展示他们的非劣效性与更少月份治疗相比。三期III临床试验的最新的氟喹诺酮类药,加替沙星和莫西沙星物的疗效,已在为期四个月的药物敏感结核病治疗方案的研究。在所有三项研究中,经过两个月的观察痰培养转换率表明,氟喹诺酮类药物为基础的治疗可能较好。然而,这个特征并没有可靠地预测杀菌活性或复发的风险。换句话说,缩短治疗不劣于标准治疗。抗分枝杆菌的生存策略和减少治疗时间长度与抗结核药物,其他新的和强大的代理,以及肺结核疫苗,正处于紧张的临床研究的安全性和疗效评价中。
关键词: 抗结核药物研究
Current Medicinal Chemistry
Title:Human Tuberculosis. III. Current and Prospective Approaches in Anti-Tubercular Therapy
Volume: 23 Issue: 21
Author(s): Giampietro Sgaragli, Maria Frosini, Simona Saponara, Federico Corelli
Affiliation:
关键词: 抗结核药物研究
摘要: Ineffectively treated tuberculosis (TB) is associated with substantial morbidity and mortality. Cure of TB patients is hampered by the development of multidrug resistance in M. tuberculosis and the need of long-term treatment. The diarylquinoline derivative bedaquiline was approved in December 2012 under the accelerated-approval regulations of FDA as part of a combination therapy for treating adults with pulmonary MDR-TB for whom effective cures are not otherwise available. The bicyclic nitroimidazoles delamanid and its companion pretomanid inhibit mycolic acid synthesis via an unknown mechanism. In November 2013, delamanid received conditional approval by the European Medicines Agency for MDR-TB treatment. Use of both drugs, however, is limited owing to toxicity issues. If the aim to reduce treatment duration is pursued in order to limit costs and improve patient adherence, it is mandatory to demonstrate their noninferiority with fewer months of therapy. In three phase III clinical trials the efficacy of the most recent fluoroquinolones, gatifloxacin and moxifloxacin, has been investigated in a four-month treatment regimen of drug-susceptible TB. In all three studies, after two months the culture conversion rates of observed sputum indicated that fluoroquinolone-based therapies were likely to be superior. However, this feature did not reliably predict sterilizing activity or a risk of relapse. In other words, the shortened treatments were not noninferior to standard treatments. To counteract mycobacterial survival strategies and reduce the timelength of treatment with anti-TB drugs, other novel and powerful agents, as well as tuberculosis vaccines, are under intense clinical investigation for safety and efficacy assessment.
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Giampietro Sgaragli, Maria Frosini, Simona Saponara, Federico Corelli , Human Tuberculosis. III. Current and Prospective Approaches in Anti-Tubercular Therapy, Current Medicinal Chemistry 2016; 23 (21) . https://dx.doi.org/10.2174/0929867323666160504102636
DOI https://dx.doi.org/10.2174/0929867323666160504102636 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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