Comparative activities of LY 333328, a new glycopeptide, against penicillin-susceptible and -resistant pneumococci

Abstract

Microdilution MIC testing was used to test the susceptibility of 202 pneumococci to LY 333328 and six other agents. LY 333328 was the most active glycopeptide (MIC at which 90% of the pneumococci were inhibited [MIC90], 0.008 microgram/ml), followed by teicoplanin (MIC90, 0.06 microgram/ml) and vancomycin (MIC90, 0.5 microgram/ml). Rifampin resistance was seen in some penicillin-resistant strains. The MICs of imipenem and ceftriaxone rose with those of penicillin. Time-kill testing confirmed the excellent antipneumococcal activity of LY 333328.

Telavancin: A novel lipoglycopeptide antimicrobial agent

“…Oritavancin (Targanta), a semisynthetic glycopeptide derived from a vancomycin analogue, has shown promise against MRSA, as well as potential activity against vancomycinresistant strains of staphylococci and enterococci. 24,25,[80][81][82][83][84][85][86][87] Oritavancin displays concentration-dependent bactericidal activity and has an extended half-life allowing administration every 24 or 48 hours. [88][89][90][91] Oritavancin is currently in Phase III clinical trials, and, although no formally published clinical trials are available, meeting presentations suggest that it is effective in the treatment of skin and softtissue infections.…”

Class-dependent relevance of tissue distribution in the interpretation of anti-infective pharmacokinetic/pharmacodynamic indices

“…This antibiotic class works by forming hydrogen bonds with bacterial cell wall intermediate peptides, thereby inhibiting peptidoglycan synthesis [99]. As characteristic for antibiotics that inhibit cell wall synthesis, the glycopeptides mainly display time-dependent killing in vitro [100][101][102][103][104]. However, oritavancin and dalbavancin have been shown to display bactericidal concentration-dependent activity in vitro [103,105].…”

Mechanism of action of oritavancin and related glycopeptide antibiotics

“… b See lettered footnotes for cited references: (a) [19,71,73,76–78,89,137–144], (b) [19,21,71,73,74,76–78,89,137–142], (c) [72–74,76–78,84,89,138,140,141,145], (d) [73,76–78,89,93,140,145], (e) [73,76–79,140,141], (f) [73,76,77,141], (g) [73,76,77,140], (h) [73], (i) [73,77], (j) [73,77,82], (k) [82], (l) [77,82]. …”