New progress in the fundamental studies of anti-tuberculotic fluoroquinolones
LIU Ming-liang
FENG Lian-shun
CHAI Yun
GUO Hui-yuan
XIAO Chun-ling
Abstract：The rising incidence of tuberculosis (TB) infection due to the emergence of drug resistant TB, especially multi-drug resistant TB (MDR-TB) as well as the association of TB and HIV/AIDS since 1980s, presents a global heath problem. Fluoroquinolones are characterized by their favorable pharmacokinetic profiles and relatively low incidence of mycobacterial resistance at the present time, and no cross-resistance with other classes of anti-myco-bacterial agents has been reported. Therefore, they have been recommended as second-line agents by the WHO to treat MDR-TB and TB in patients who have intolerance to first-line anti-TB drugs. The newly marketed 8-methoxy flu-oroquinolones gatifloxacin and moxifloxacin have greatly improved the activity against M. tuberculosis, and may be a-ble to reduce the length of therapy owing to activity against non-replicating bacilli. However, like other anti-TB drugs, modern clinical trials of fluoroquinolones could not be carried out alone due to ethics. Therefore, the funda-mental studies in the anti-TB activities undoubtedly play an important role in guiding clinicians to use fluoroquinolo-nes rationally. New progress in the fundamental studies of anti-tuberculotic fluoroquinolones is reviewed, including mechanisms of action and resistance, structure-activity relationships, in vitro and in vivo anti-tuberculous activity, pharmacokinetics and clinical tests.
Keywords：fluoroquinolonesmechanisms of action and resistancestructure-activity relationshipsanti-tuberculous activitypharmacokineticsclinical research
Publication Date：2010-01-01
Online Publishing Date：2026-08-14(First online date of this platform, not the publication date of the document)
Pages：9( 190-198 )