Telithromycin (Ketek, HMR 3647, RU 66647) is a semisynthetic antibacterial agent belonging to a class of compounds called ketolides, which are a variation on the existing class of antibiotics known as macrolides like erythromycin, whose structure includes a 14-molecule ring. Telithromycin was developed by the French pharmaceutical company Roussel Uclaf S.A., prior to 1997.
Telithromycin appears to be effective against macrolide-resistant Streptococcus pneumoniae. The defining differentiating characteristic of the ketolides, as opposed to other macrolides, is the removal of the neutral sugar, L-cladinose from the 3-position of the macrolide ring and the subsequent oxidation of the 3-hydroxyl to a 3-keto functional group.
Telithromycin shows activity against Gram-positive and Gram-negative bacteria, as well as mycoplasma. Telithromycin is a bacterial protein synthesis inhibitor that interacts with peptidyl transferase site of the 50S ribosomal subunit. The main binding sites are with domains II and V of the 23S rRNA.
Telithromycin is sparingly soluble in water and has a solubility of approximately 30mg/ml in organic solvents such as DMSO, ethanol, and dimethyl formamide (should be purged with inert gas).
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