Telithromycin new product overview

Novel azithromycin derivatives with the C-4″ bisamide side chains: synthesis and biological evaluation against gram-positive bacteria

“…Telithromycin, a typical example of ketolides, which is well known for excellent activity against resistant strains and lower inductivity of the erm gene encoding resistance, has been launched in the market. [4][5][6] It has been reported that the C-11,12 prolonged carbamate side chain of telithromycin can interact with a secondary ribosomal binding site A752 directly in domain II of the 23S rRNA in addition to the main interaction with A2058 in domain V, resulting in tighter binding to bacterial ribosomes and improved activity against erm-resistant organisms. 7 Another promising ketolide, cethromycin, 8 which can also interact with A752 through its C-6 prolonged side chain, is in last-stage development at present.…”

In vitro effects of penicillin and telithromycin on the expression of Streptococcus pneumoniae capsule

“…9 The growing resistance of S. pneumoniae to penicillin and other antimicrobial agents requires use of alternative effective drugs. More than 99% of penicillin-resistant S. pneumoniae isolates are currently susceptible to telithromycin 1,3 and suppression of capsule formation is an additional beneficial quality that might enhance the eradication of the organism. Further studies are warranted to evaluate the ability of telithromycin and other antimicrobials to suppress capsular formation by other pathogens.…”

“…1 Penicillin-resistant S. pneumoniae are also often resistant to other commonly prescribed antibiotics such as macrolides, some cephalosporins and trimethoprim-sulfamethoxazole, 2 but 99.5% are susceptible to telithromycin. 1,3 Telithromycin is the first ketolide antibacterial approved for the treatment of community-acquired respiratory tract infections. 3 The virulence of S. pneumoniae is partly attributed to its capsule, which enables it to escape phagocytosis.…”

“…1,3 Telithromycin is the first ketolide antibacterial approved for the treatment of community-acquired respiratory tract infections. 3 The virulence of S. pneumoniae is partly attributed to its capsule, which enables it to escape phagocytosis. 4 Interruption of capsule production in S. pneumoniae by the use of transposon mutagenesis renders the organism avirulent.…”

Antibacterial resistance patterns in Streptococcus pneumoniae isolated from elderly patients: PROTEKT years 1–5 (1999–2004)

“…The ketolide antibacterial telithromycin exhibits good in vitro activity against the common RTI pathogens (including S. pneumoniae isolates resistant to other antibacterials) as well as atypical/intracellular organisms [9]. Prospective Resistant Organism Tracking and Epidemiology for the Ketolide Telithromycin (PROTEKT) is an ongoing, longitudinal, international surveillance study established in 1999 to monitor the susceptibility of pathogens collected from patients with community-acquired RTIs to telithromycin and other antibacterials.…”