Disclosed is a method for treating a symptom of M. tuberculosis infection in a subject, comprising administering the patient with an effective amount of (3R,4S)-1-(4-fluorophenyl)-3-[(3S)-3-(4-fluorophenyl)-3-hydroxypropyl]-4-(4-hydroxyphenyl)zetidin-2-one (EZETIMIBE). In the preferred embodiments, EZETIMIBE is capable of significantly inhibiting the survival and proliferation of Mycobacterium tuberculosis in the monocytes. The anti-tuberculous effect of EZETIMIBE is partly through stimulating CD13 leading to monocytes activation and thus bacterial killing of Mycobacterium tuberculosis, and partly through depleting the intracellular nutrition necessary for the survival of Mycobacterium tuberculosis. It is also proved that EZETIMIBE is capable of directly killing Mycobacterium tuberculosis outside cells.