抗结核药物研究进展

Advances of antitubercular agents

结核病病例一般集中在发展中国家。抗结核领域一直以来未受到学术界和制药企业的关注,随着多药耐药结核病和广泛耐药结核病不断出现,以及艾滋病患者感染结核杆菌的病例逐渐增加,抗结核药物的研究已成为药物研发领域中的一个热点。本文系统地总结了已上市抗结核药物及正处在研发阶段的新型化学实体,根据其作用机制划分为4个大类,同时结合近期文献报道对其作用机制进行了简要阐述。在过去40年中,只有两种全新作用机制的新药:贝达喹啉与德拉马尼上市,以ATP合成酶抑制剂为代表的具有新型作用机制的药物将有望成为抗结核药物研发的重点。

Tuberculosis(TB)cases were fastening on developing countries and thus were ignored by pharmaceutical companies and academia.Research of TB agents has been a predominant issue since the multidrug-resistant tuberculosis and extensively drug-resistant tuberculosis were emerging and the numbers of patients with HIV/TB were rapidly increasing.This paper systematically summarizes the approved anti-tuberculosis drugs and new chemical entities that are in the research and development stage.According to their mechanism of action,they were divided into four categories,and their mechanism of action was briefly described according to recent literature reports.For approximately 40 years,only two agents,delamanid and bedaquinline,were approved by FDA.Agents with novel mechanism of action,represented by ATP synthase inhibitors,are expected to be the key point of anti-tuberculosis drug development.