Nadifloxacin

Nadifloxacin (OPC7251) is a broad-spectrum quinolone antibiotic. Nadifloxacin inhibits bacterial DNA gyrase and topoisomerase IV, interfering with DNA replication. It also suppresses the production of proinflammatory cytokines (such as IL-1α, IL-6, and IL-8). Nadifloxacin exhibits antibacterial activity against various pathogens, including Propionibacterium acnes and Staphylococcus aureus. Nadifloxacin also exhibits anti-inflammatory activity. Nadifloxacin can be used in the research of skin infections such as acne vulgaris, folliculitis, and impetigo^{[1][2][3][4][5]}. In Vitro:Nadifloxacin shows potent activity against Propionibacterium acnes isolated from acne vulgaris, with MIC₉₀ of 0.39 µg/mL^[1].
Nadifloxacin shows activity against clinical isolates of Propionibacterium acnes, Propionibacterium granulosum, Staphylococcus aureus and coagulase-negative staphylococci, with MIC₅₀s of 0.25, 0.125, 0.03, 0.06 mg/L, respectively^[3].
Nadifloxacin (3-30 μg/mL; up to 24 h) inhibits the production of IL-12 and IFN-γ by human peripheral blood mononuclear cells stimulated with heat-killed Propionibacterium acnes, and also inhibits the production of IL-1α, IL-6, IL-8 and GM-CSF by human epidermal keratinocytes treated with IFN-γ plus IL-1β^[4].
In Vivo:Nadifloxacin (1% cream; topical application) shows antimicrobial activity in experimental subcutaneous infections in mice caused by P. acnes, S. epidermidis and S. aureus^[3].
Nadifloxacin (7.4 mg/kg; topical application) reaches detectable cutaneous concentrations in the dorsal skin of male SD rats, with concentrations of 82.3 μg/g wet tissue at 4 h and 6.7 μg/g wet tissue at 24 h^[4].