贝达喹啉:更短更好的抗结核治疗方案的新希望。

Niccolò Riccardi, Filippo Del Puente, Federica Magnè, Lucia Taramasso, Antonio Di Biagio
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引用次数: 19

摘要

背景:2014年,估计有180万人死于结核分枝杆菌(MTB);此外,68万人患上了耐多药结核病。方法:现有的抗mdr和XDR治疗方案耗时长、费用高、需要高依从性,且药物不良事件发生率高,导致成功率低;此外,在过去50年里,只有两种新分子——贝达喹啉(BDQ)和delamanid被批准用于治疗耐多药结核病。结果:BDQ(专利号US 7,498,343B2)是一种二芳基喹啉类抗分枝杆菌药物,与结核分枝杆菌状态无关;事实上,它的功效是保守的复制和非复制的杆菌,尽管细胞外或细胞内的位置。BDQ已获得美国食品和药物管理局(FDA)批准,仅用于联合治疗肺部耐多药结核病(MDR-TB)的成人患者,当由于耐药或耐受性差而无法提供有效治疗时;然而,由于其高杀菌活性,BDQ可能在未来用于治疗肺外结核和结核分枝杆菌(MOTT)感染。结论:BDQ可能在更接近根除结核病和确保更高的护理保持率方面发挥重要作用,即使是在完全易感的MTB菌株和针对潜伏结核的非复制分枝杆菌,提供标准方案的替代方案。
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Bedaquiline: A New Hope for Shorter and Better Anti-Tuberculosis Regimens.

Background: In 2014, an estimated 1.8 million people died from Mycobacterium tuberculosis (MTB); moreover, 680,000 people developed multidrug-resistant TB (MDRTB).

Methods: Currently available anti-MDR and XDR regimens are long-lasting and expensive, need high adherence and are undermined by a high frequency of adverse drug events, thus leading to a low success rate; furthermore, in the last 50 years only two new molecules, bedaquiline (BDQ) and delamanid, have been approved and released for the treatment of MDR-TB.

Results: BDQ, patent number US 7,498,343B2, is a diarylquinoline anti-mycobacterial drug, active regardless of the state of MTB; in fact, its efficacy is conserved against replicating and non-replicating bacilli, despite extracellular or intracellular location. BDQ has been approved by the Food and Drug Administration (FDA) only for combination treatment of pulmonary multidrug-resistant tuberculosis (MDR-TB), in adult patients, when an effective treatment cannot be provided otherwise due to resistance or poor tolerability; however, due to high bactericidal activity, BDQ may be used in future to treat extrapulmonary tuberculosis and Mycobacterium other than tuberculosis (MOTT) infection.

Conclusion: BDQ may play a major role to get closer to TB eradication and to ensure higher retention in care, even in fully susceptible MTB strains and against non-replicating mycobacteria in latent-TB, providing an alternative to standard regimen.

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来源期刊
Recent patents on anti-infective drug discovery
Recent patents on anti-infective drug discovery Medicine-Pharmacology (medical)
CiteScore
2.40
自引率
0.00%
发文量
1
期刊介绍: Recent Patents on Anti-Infective Drug Discovery publishes review articles on recent patents in the field of anti-infective drug discovery e.g. novel bioactive compounds, analogs & targets. A selection of important and recent patents on anti-infective drug discovery is also included in the journal. The journal is essential reading for all researchers involved in anti-infective drug design and discovery.
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