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首页> 外文期刊>International Journal of Basic & Clinical Pharmacology >Bedaquiline: a new weapon against MDR and XDR-TB
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Bedaquiline: a new weapon against MDR and XDR-TB

机译：Bedaquiline：对抗耐多药和广泛耐药结核的新武器

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Multidrug-resistant tuberculosis (MDR-TB) is a global public health problem. It requires treatment with combination therapy consisting of four to six drugs including combinations of bactericidal and bacteriostatic drugs, usually for a period of 2 years. There is alarming rise in MDR and XDR-TB all over the world and better treatment options are needed to control the global MDR-TB and XDR-TB epidemic. Drugs which can shorten the treatment duration and which are free from serious adverse effects are urgently needed. Bedaquiline (TMC-207) is a newly FDA approved anti-TB drug, having unique mechanism of action i.e. causes inhibition of the proton pump activity of the ATP synthase in M. tuberculosis and targets the energy metabolism. It is found to active within macrophages, and is a promising agent in shortening the duration of anti- TB treatment. It is metabolized by CYP3A4, so interactions with inducers and inhibitors of this enzyme are expected. It has shown promising results in preclinical and clinical studies and it seems to be a good option for MDR and XDR-TB. Adverse effects reported in various studies were of mild nature except nausea which was the most commonly associated. Few cases of prolongation of QT intervals were reported, so it demands careful monitoring and use of bedaquiline as a reserve drug for patients in whom conventional regimens are not effective. Currently it is approved as part of combination therapy in adults of ≥18 year with pulmonary MDR-TB. Long term studies are needed to explore its full safety profile.
机译：耐多药结核病（MDR-TB）是全球性的公共卫生问题。它需要使用由四到六种药物组成的联合疗法进行治疗，包括杀菌和抑菌药物的组合，通常为期2年。全世界耐多药和广泛耐药结核病的上升令人震惊，因此需要更好的治疗方案来控制全球耐多药结核和广泛耐药结核病的流行。迫切需要能够缩短治疗时间并且没有严重不良反应的药物。 Bedaquiline（TMC-207）是FDA新批准的抗结核药物，具有独特的作用机制，即抑制结核分枝杆菌ATP合酶的质子泵活性，并靶向能量代谢。发现它在巨噬细胞中有活性，并且是缩短抗结核病治疗时间的有前途的药物。它通过CYP3A4代谢，因此预期与该酶的诱导剂和抑制剂发生相互作用。在临床前和临床研究中已显示出令人鼓舞的结果，对于MDR和XDR-TB来说似乎是一个不错的选择。除恶心是最常见的相关疾病外，各种研究报告的不良反应均为轻度性质。据报道很少有延长QT间隔的病例，因此，对于常规治疗无效的患者，需要仔细监测和使用苯达喹啉作为储备药物。目前，它已被批准作为18岁以上肺部MDR-TB合并治疗的一部分。需要进行长期研究以探索其完整的安全性。

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