What Is Telithromycin?

Telithromycin is the first antibacterial drug in the semisynthetic macrolide-lincophthalamide-streptomycin B (MLSB) family.

Telithromycin

Telithromycin is the first antibacterial drug in the semisynthetic macrolide-lincophthalamide-streptomycin B (MLSB) family.

Drug Name

Telithromycin

Foreign name

telithromycin

Main indications

Respiratory infections

Drug type

antibiotic

Telithromycin is one of the semi-synthetic macrocycles

The mechanism of action of telithromycin is similar to that of macrolide antibiotics, mainly by directly binding to the 50S subunit of bacterial ribosomes, inhibiting protein synthesis, and inhibiting its translation and assembly. Both telithromycin and macrolide antibiotics can bind to the nucleotides of the and V domains of the 23s ribosomal RNA, but the biggest difference is that telithromycin binds wild-type ribosomes more than erythromycin and carat Mycin is about 10 and 6 times stronger, respectively.

Clinically used to treat respiratory infections, including community-acquired pneumonia (CAP), acute exacerbation of chronic bronchitis (AECB), acute maxillary sinusitis (AMS), pharyngitis, and tonsillitis, etc.

According to industry experts, the next century will be the era of macrolide antibiotics. As a new class of drugs, ketolactones are derived from macrolide antibiotics. A keto group is introduced at the 3 position to replace the neutral sugar group, which improves the stability of the weak acid environment. Due to the structural change, the antibacterial effect of these drugs is enhanced, especially the antibacterial activity of those who are resistant to the pathogens of respiratory infections is significantly increased. Ketolactones have high antibacterial activity against Streptococcus pneumoniae, Group A / B hemolytic streptococcus, Streptococcus grass green, including those bacteria resistant to erythromycin, penicillin-insensitive Streptococcus pneumoniae still The drug is highly sensitive and superior to all macrolides, clindamycin and penicillin drugs.

The world's first and only ketolactone on the market is telithromycin, which was developed by Sanofi-Aventis. It was first marketed in Germany on October 15, 2001. Now available in the United States, United Kingdom, Belgium, Brazil, France, Ireland, Italy, Mexico, Spain, Canada, and Japan, and is mainly used in the following four indications: community-acquired pneumonia (CAP), acute bacterial sinusitis (ABS), acute bacterial infectious deterioration (ABECB) in patients with chronic bronchitis over 18 years of age, and tonsillitis / pharyngitis in patients over 12 years of age. It has been a model for ketolactones and has proven to be more effective against bacterial infections than other drugs, and has been used as a first-line treatment for community-acquired pneumonia. As soon as the product was launched in the United States, it created a good market performance with strong growth momentum. In 2005, sales tripled from $ 64 million in the previous year to $ 193 million.

Because ketolactone antibiotics are consistently favored by the industry, it is very likely that it will subtly affect the market share of the entire macrolide drug. However, it is inevitable that, for ketolactone drugs, although more and more drug-resistant bacteria are currently making their therapeutic status and importance increasingly prominent, other macrolide drugs that have mature market status The competition between azithromycin and low-priced generic drugs from Pfizer in the United States has limited the market expansion of such drugs to a certain extent.