Drug intelligence / Profile preview

telithromycin

Development stage
Approved
Lead developer
Sanofi
Modality
Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Oral
01

Overview

Telithromycin is a semi-synthetic ketolide antibiotic, structurally related to the macrolide class but distinguished by modifications that enhance its activity against certain resistant bacteria. It was developed as the first clinically used ketolide and is primarily indicated for the treatment of community-acquired pneumonia (CAP) caused by susceptible strains of bacteria, including multidrug-resistant Streptococcus pneumoniae. Telithromycin acts by binding to domains II and V of 23S rRNA within the 50S subunit of bacterial ribosomes, thereby inhibiting protein synthesis and exerting bactericidal effects. This dual-domain binding confers increased efficacy against macrolide-resistant organisms compared to older macrolides. The drug was originally approved for broader respiratory indications but is now restricted due to safety concerns, particularly hepatotoxicity and life-threatening exacerbations in patients with myasthenia gravis. Telithromycin is administered orally as tablets[1][2][3][4][5].

Brand names
KetekKetek Pak
Other names
telitromicinatelithromycineLevviax
02

Targets

PTC (50S ribosomal peptidyl transferase center)

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