title: In-vitro and in-vivo antibacterial activity of BI 397, a new semi-synthetic glycopeptide antibiotic.
abstract: BI 397 (formerly A-A-1) is a semisynthetic derivative of the teicoplanin-like glycopeptide A40926. It was more active in vitro against staphylococci (including some teicoplanin-resistant strains) than teicoplanin and vancomycin. Against streptococci (including penicillin-resistant strains) BI 397 has activity comparable with that of teicoplanin and better than vancomycin. BI 397, when administered to rats by the i.v. route, gives high and long lasting blood levels. It shows excellent activity in models of acute septicaemia in immunocompetent and neutropenic mice. In a rat staphylococcal endocarditis model it is as effective as teicoplanin and vancomycin at reducing bacterial loads in the heart, but at lower dosages and with a reduced number of daily treatments compared with the two glycopeptide controls. BI 397 is highly efficacious in clearing penicillin-susceptible and -resistant pneumococci from lungs of immunocompetent and neutropenic rats. The data from these studies show that BI 397 combines an excellent in-vitro antibacterial activity with favourable pharmacokinetic behaviour resulting in potent in-vivo activity.
authors.affiliation: Biosearch Italia S.p.A., Gerenzano (Varese), Italy. gcandiani@biosearch.it
authors.forename: G
authors.initials: G
authors.lastname: Candiani
authors.forename: M
authors.initials: M
authors.lastname: Abbondi
authors.forename: M
authors.initials: M
authors.lastname: Borgonovi
authors.forename: G
authors.initials: G
authors.lastname: Romanò
authors.forename: F
authors.initials: F
authors.lastname: Parenti
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000627:therapeutic use*; D004697:Endocarditis, Bacterial / Q000188:drug therapy / Q000382:microbiology; D005260:Female; D006094:Gram-Positive Bacteria / Q000187:drug effects* / Q000302:isolation & purification; D016908:Gram-Positive Bacterial Infections / Q000188:drug therapy* / Q000382:microbiology; D006801:Humans; D016867:Immunocompromised Host; D051379:Mice; D008826:Microbial Sensitivity Tests; D011018:Pneumonia, Pneumococcal / Q000188:drug therapy / Q000382:microbiology; D051381:Rats; D018805:Sepsis / Q000188:drug therapy / Q000382:microbiology; D017334:Teicoplanin / Q000494:pharmacology / Q000031:analogs & derivatives; D014640:Vancomycin / Q000494:pharmacology
chemical_list: D000900:Anti-Bacterial Agents; D017334:Teicoplanin; D014640:Vancomycin; C469289:dalbavancin