Telithromycin is an ketolide used to treat community acquired pneumonia of mild to moderate severity. Telithromycin, a semi-synthetic erythromycin derivative, belongs to a new chemical class of antibiotics called ketolides.
- Mechanism
- Curator reviewed
Telithromycin acts by binding to domains II and V of 23S rRNA of the 50S ribosomal subunit. By binding at domain II, telithromycin retains activity against gram-positive cocci (e.g. Streptococcus pneumoniae) in the presence of resistance mediated by methylases (erm genes) that alter the binding site at domain V. Telithromycin may also inhibit the assembly of nascent ribosomal units. Compared to erythromycin A, telithromycin binds to the 23S rRNA with 10 times greater affinity in erythromycin-susceptible organisms and 25 times greater affinity in macrolide-resistant strains. This increased binding affinity may be conferred by the C11-12 carbamate side chain of telithromycin. The side chain appears to maintain binding at domain II in the presence of resistance mediated by alterations in domain V.
- Primary indication
- For the treatment of Pneumococcal infection, acute sinusitis, acute bacterial tonsillitis, acute bronchitis and bronchiolitis, lower respiratory tract infection and lobar (pneumococcal) pneumonia.Curator reviewed · 2 structured indications
- Formula / weight
- C43H65N5O10 · 812.018 g/mol (avg)
- First approval
- Canada, 2006 · United States, 2004
- Code names
- HMR 3647
- Brand names
Resolves to
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Which other approved drugs treat the same conditions as Telithromycin, and which companies have late-stage candidates in those indications?
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