title: Analysis of effects of MCB3681, the antibacterially active substance of prodrug MCB3837, on human resident microflora as proof of principle.
abstract: The water-soluble prodrug MCB3837 is rapidly converted to MCB3681, active against Gram-positive bacterial species, after intravenous infusion. The aim of this study was to prove the principle that MCB3681 is efficacious in vivo by demonstrating its effect on the resident microflora or colonizers of the human skin, nose, oropharynx and intestine. MCB3837 was infused at a daily dose of 6 mg/kg for 5 days. MCB3681 was active against clostridia, bifidobacteria, lactobacilli, enterococci and Staphylococcus aureus, thus proving the principle that MCB3681 is antibacterially efficacious in vivo without affecting the Gram-negative microflora.
authors.affiliation: Institute for Infection Medicine, University Medical Center Schleswig-Holstein, Kiel, Germany. Electronic address: adalhoff@t-online.de.
authors.forename: A
authors.initials: A
authors.lastname: Dalhoff
authors.affiliation: Department of Laboratory Medicine, Karolinska University Hospital, Karolinska Institutet, Stockholm, Sweden.
authors.forename: M-U
authors.initials: MU
authors.lastname: Rashid
authors.affiliation: Morphochem Aktiengesellschaft für kombinatorische Chemie, Munich, Germany.
authors.forename: T
authors.initials: T
authors.lastname: Kapsner
authors.affiliation: Department of Laboratory Medicine, Karolinska University Hospital, Karolinska Institutet, Stockholm, Sweden.
authors.forename: G
authors.initials: G
authors.lastname: Panagiotidis
authors.affiliation: Department of Laboratory Medicine, Karolinska University Hospital, Karolinska Institutet, Stockholm, Sweden.
authors.forename: A
authors.initials: A
authors.lastname: Weintraub
authors.affiliation: Department of Laboratory Medicine, Karolinska University Hospital, Karolinska Institutet, Stockholm, Sweden.
authors.forename: C E
authors.initials: CE
authors.lastname: Nord
mesh_terms: D000900:Anti-Bacterial Agents / Q000378:metabolism*; D006094:Gram-Positive Bacteria / Q000187:drug effects*; D064368:Healthy Volunteers; D006801:Humans; D007422:Intestines / Q000382:microbiology; D008297:Male; D064307:Microbiota / Q000187:drug effects*; D009666:Nose / Q000382:microbiology; D009960:Oropharynx / Q000382:microbiology; D012867:Skin / Q000382:microbiology
chemical_list: D000900:Anti-Bacterial Agents
keywords: Antibacterial effects; Clostridium spp.; Enterococcus spp.; MCB3681; Staphylococcus aureus