Sequence Information

    • DRAMP ID

    • DRAMP18057

    • Name

    • MSI-78(Pexiganan, Locilex)

    • Sequence

    • GXGKFLKKAKKFGKAFVKLLKK

    • Description

    • Pexiganan is a broad-spectrum synthetic analogue of the African frog peptide magainin.

    • Activity

    • Antibacterial

    • Target Organism

      • Gram-positive bacteria:
        Staphylococcus aureus ATCC 29213 (MIC=8-16 μg/ml), Staphylococcus aureus ATCC 33591 (methicillin resistant) (MIC=16-32 μg/ml), Staphylococcus epidermidis ATCC 12228 (MIC=2-4 μg/ml), Enterococcus faecium ATCC 51559 (vancomycin resistant) (MIC=8 μg/ml), Enterococcus faecalis ATCC 29212 (MIC=64 μg/ml), Group A Streptococcus ATCC 49399 (MIC=4 μg/ml), Streptococcus pneumoniae ATCC 49619 (MIC=32 μg/ml), Streptococcus bovis ATCC 49133 (MIC=4 μg/ml), Bacillus cereus ATCC 11778 (MIC=8 μg/ml), Micrococcus luteus ATCC 4698 (MIC=2 μg/ml), Corynebacterium group A ATCC 49676 (MIC=2-4 μg/ml);
      • Gram-negative bacteria:
        Escherichia coli ATCC 25922 (MIC=8-16 μg/ml), Enterobacter cloacae ATCC 35030 (MIC=8 μg/ml), Proteus mirabilis ATCC 29245 (MIC>256 μg/ml), Serratia marcescens ATCC 8100 (MIC>256 μg/ml), Helicobacter pylori ATCC 43504 (MIC=2 μg/ml), Haemophilus influenzae ATCC 49247 (MIC=8 μg/ml), Pseudomonas aeruginosa ATCC 27853 (MIC=8-16 μg/ml), Bacteroides fragilis ATCC 90028 (MIC=2-4 μg/ml), eroides thetaiotaomicron ATCC 29741 (MIC=2-4 μg/ml), Clostridium difficile ATCC 43255 (MIC=4 μg/ml), Propionibacterium acnes ATCC 29399 (MIC=8 μg/ml), Veillonella parvula ATCC 10790 (MIC=8 μg/ml).

    • Reference

      • In vitro antibacterial properties of pexiganan, an analog of magainin. Antimicrob. Agents Chemother(1999).(PMID: 10103181)
      • Pexiganan acetate. Drugs (1998)
      • Potential of immunomodulatory host defense peptides as novel anti-infectives.Trends in Biotechnology(2009).(PMID: 19683819)

Clinical Information

    • Medical use

    • Infected diabetic foot ulcers

    • Company

    • Genaera (Plymouth, PA)

    • Stage of Development

    • Phase III(Failure)

    • Comments

    • Drug was refused FDA approval, on the basis that is was no more effective than conventional antibiotics. In part due to the high rate (75%) of spontaneous resolution of disease in controls

    • Clinical Trials

    • NCT01594762
    • NCT01590758
    • NCT00563394
    • NCT00563433