Antituberculosis activity of clarithromycin (CLA), a macrolide antibio
tic, was investigated in vitro, in macrophages, and in C57BL/6 mice. C
LA showed high in vitro MICs (4 to > 16 mu g/ml) for several strains o
f Mycobacterium tuberculosis and caused slight enhancement of activity
of rifampin (RIF) against H37Rv but failed to increase the activity o
f either RIF or isoniazid (INH) against other strains, However, inside
J774A.1 macrophages, CLA showed high activity and was synergistic wit
h RIF against some strains of tubercle bacilli susceptible or resistan
t to INH and RIF. In the in vivo studies with a drug-susceptible strai
n (H37Rv), CLA protected mice from mortality due to tuberculosis for u
p to 8 weeks of observation, The CFU data for lungs and Spleens reveal
ed that the antituberculosis activity of CLA is inferior to those of I
NH and streptomycin, However, the activity of CLA when used alone or i
n combination was comparable to that of thiacetazone, indicating its p
otential usefulness as a secondary drug for the treatment of tuberculo
sis.