Injectible Antibiotic Shows Potent Activity

The results of in vitro studies and human clinical studies of a new injectable antibiotic showed low potential for drug resistance as well as potent in vitro activity for serious infections caused by Gram-positive bacteria. These results were presented at the annual European Congress of Clinical Microbiology and Infectious Diseases (ECCMID), held in Copenhagen (Denmark) in April 2005.

A study designed to evaluate the potential of the antibiotic for development of resistance to the new drug, called telavancin, among a collection of Staphylocaccus aureus revealed that telavancin has a low potential for resistant mutant selection. The compound exhibited potent in vitro activity across a broad spectrum of Gram-positive organisms, including vancomycin-intermediate S aureus and vancomycin-resistant S aureus strains. Another study showed excellent penetration of the drug in plasma and skin blister fluid, achieving concentrations well above those shown to be bactericidal against S aureus, including methicillin-resistant strains. Still another study of the drug used in hemodialysis subjects concluded that a dosage reduction is recommended for patients with moderate-to-severe renal impairment.

Televancin is a novel lipoglycopeptide discovered by Theravance (So. San Francisco, CA, USA) through the application of multivalent drug design in a program dedicated to finding new antibiotics for serious infections due to S aureus and other Gram-positive pathogens. Televance has a unique multifunctional mechanism of action that the company believes speeds bacterial killing and reduces the risks of inducing resistance. The compound is currently in phase III study for the treatment of complicated skin and skin structure infections and hospital-acquired pneumonia. At higher, clinically achievable concentrations, direct effects on bacterial plasma membrane function, such as membrane potential depolarization and increased permeability, were observed.




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