Telithromycin, the first of the ketolide antimicrobials, has been specifica
lly designed to provide potent activity against common and atypical/intrace
llular or cell-associated respiratory pahtogens, including those that are r
esistant to beta -lactams and/or macrolide-lincosamide-streptogramin(B) (ML
SB) antimicrobials. Against Gram-positive cocci, telithromycin possesses mo
re potent activity in vitro and in vivo than the macrolides clarithromycin
and azithromycin. It retains its activity against erm-(MLSB) or mef-mediate
d macrolide-resistant Streptococcus pneumoniae and Streptococcus pyogenes a
nd against Staphylococcus aureus resistant to macrolides through inducible
MLSB mechanisms. Telithromycin also possesses high activity against the Gra
m-negative pathogens Haemophilus influenzae and Moraxella catarrhalis, rega
rdless of beta -lactamase production. In vitro, it shows similar activity t
o azithromycin against H. influenzae, while in vivo its activity against H.
influenzae is higher than that of azithromycin. Telithromycin's spectrum o
f activity also extends to the atypical, intracellular and cell-associated
pathogens Legionella pneumophila, Mycoplasma pneumoniae and Chlamydia pneum
oniae. In vitro, telithromycin does not induce MLSB resistance and it shows
low potential to select for resistance or cross-resistance to other antimi
crobials. These characteristics indicate that telithromycin will have an im
portant clinical role in the empirical treatment of community-acquired resp
iratory tract infections.