Antibacterial activity of roxithromycin: a laboratory evaluation

Roxithromycin, formerly known as RU 28965 (9-[O [(2-methoxyethoxy)methyl]oxime]-erythromycin), is a novel 14 atom-membered semisynthetic macrolide with an antibacterial spectrum directed towards Gram-positive cocci and bacilli, Gram-negative cocci and some Parvobacteriaceae. The in vitro antibacterial activity of roxithromycin was compared with those of erythromycin and spiramycin against 275 clinical isolates by using 2-fold broth macro-dilution tests. The antibacterial spectrum of roxithromycin and erythromycin were qualitatively comparable (including the bacteriostatic type of activity and the profile of resistance), but minimal inhibitory concentrations of erythromycin were generally one half those of roxithromycin, except for Corynebacterium sp. and Bacteroides fragilis against which the new macrolide was more active. On the other hand, roxithromycin exhibited a superior in vivo antibacterial activity in laboratory animals, being up to six times more potent than erythromycin in curing experimentally infected mice. Roxithromycin showed high blood levels and long half-lives of elimination in rodents after oral administration, and its bioavailability amounted to 72% in mice and 85% in rats, compared to less than 10% for erythromycin. Roxithromycin was widely distributed throughout the body with a high degree of penetration into all tissues, particularly in the lungs.