Telithromycin is a semi-synthetic erythromycin derivative. It belongs to the chemical family called ketolides, a group belonging to the macrolide-lincosamide-streptogramin (MLS) class. Telithromycin prevents bacterial growth by inhibiting bacterial protein synthesis. Similar to macrolides, telithromycin directly blocks translation of the bacterial 23S ribosomal RNA; however, unlike macrolides, telithromycin also blocks bacterial ribosomal assembly (mechanism not shown). Telithromycin binds to two sites on the 50S ribosomal subunit, domains II and V of the 23S rRNA, whereas macrolides bind only to domain V. The C11-12 carbamate side chain is thought to contribute to a higher binding affinity of telithromycin compared to erythromycin A. In erythromycin A-susceptible bacteria, telithromycin exhibits 10 times greater affinity than erythromycin. Its relative binding affinity is further increased to 25 times greater in macrolide-resistant bacteria strains. This is likely due to the additional binding site on domain II since macrolide resistance occurs as a result of alterations in the domain V binding site.

Telithromycin Pathway References