>>SOUTH SAN FRANCISCO, Calif., April 7 /PRNewswire-FirstCall/ -- Theravance, Inc. (Nasdaq: THRX - News) announced today that results from a series of in vitro studies as well as human clinical studies with the investigational antibiotic telavancin were presented at the 15th European Congress of Clinical Microbiology and Infectious Diseases (ECCMID) in Copenhagen, April 2-5, 2005.
Among the highlights of the telavancin studies presented at ECCMID were:
-- A study designed to evaluate the potential for development of resistance to telavancin among a collection of S. aureus (including strains of MRSA) and vancomycin-sensitive and -resistant enterococci (VSE and VRE, respectively). Based on the observation that the maximum increase in telavancin MIC was less than or equal to 4-fold for most organisms following continuous exposure for 20 consecutive passages, the authors concluded that telavancin possesses a low potential for resistant mutant selection.
-- A baseline assessment of telavancin's activity against a collection of 101 Gram-positive bacterial isolates, including resistant phenotypes. The compound exhibited potent in vitro activity across a broad spectrum of Gram-positive organisms, including vancomycin-intermediate S. aureus (VISA) and vancomycin-resistant S. aureus (VRSA) strains.
-- Results of a Phase 1 clinical study of the steady state pharmacokinetic profile of telavancin in plasma and skin blister fluid in healthy volunteers that showed excellent penetration, achieving local concentrations well above those shown to be bactericidal against S. aureus, including methicillin-resistant strains (MRSA).
-- Results of a Phase 1 clinical study of the single-dose pharmacokinetics of telavancin in subjects maintained on hemodialysis compared to healthy subjects, demonstrating reduced clearance in these patients, minimal removal of telavancin by hemodialysis, and good tolerability in the hemodialysis subjects. Consistent with previously reported data from this study, the authors concluded that a dosage reduction is recommended for patients with moderate to severe renal impairment, including those on hemodialysis.
Telavancin, a rapidly bactericidal injectable antibiotic, is a novel lipoglycopeptide that was discovered by Theravance through the application of multivalent drug design in a research program dedicated to finding new antibiotics for serious infections due to Staphylococcus aureus (including multi-drug resistant strains) and other Gram-positive pathogens. Previously presented data demonstrated that telavancin has a unique multifunctional mechanism of action that the company believes speeds bacterial killing and reduces the risks of inducing resistance. This antibacterial activity results from interaction with D-Ala-D-Ala-containing peptidoglycan intermediates that leads, at submicromolar concentrations, to inhibition of the transglycosylation step of peptidoglycan synthesis during cell wall synthesis. Also, at higher, clinically-achievable concentrations, direct effects on bacterial plasma membrane function, such as membrane potential depolarization and increased permeability, are observed. Telavancin is currently in Phase 3 studies for the treatment of complicated skin and skin structure infections (cSSSI) and Hospital-Acquired Pneumonia (HAP).<<
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Cheers, Tuck |
