生物活性

• 描述Nadifloxacin, a new fluoroquinolone with anti-Propionibacterium acnes activity and additional anti-inflammatory activity, is approved for use in acne. Topical nadifloxacin is effective, tolerable, and safe for mild or moderate facial acne. Its clinical effectiveness is comparable to clindamycin when used as add-on therapy to benzoyl peroxide^[3]. Nadifloxacin has potential as a topical agent for short-term treatment of skin infections^[2]. PHMB/nadifloxacin (polymer polyhexamethylene biguanide, PHMB) nanoparticles are effective against intracellular bacteria and could be further developed for the treatment of skin and soft tissue infections^[4]. LC-EC cultured with nadifloxacin at 10 microg/ml or more significantly suppressed the antigen-presenting function of LC (Langerhans cells) for T cells. The ability of MHC class II+ keratinocytes to present a superantigen to T cells was suppressed by preincubation of keratinocytes with 30 microg/ml or more of nadifloxacin. Nadifloxacin downmodulates cutaneous immunity by interfering with the antigen-presenting ability of epidermal cells^[5].
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT01445301	Acne Vulgaris	Phase 3	Completed	-	Japan ... more >> GSK Investigational Site Chiba, Japan, 273-0046 GSK Investigational Site Hokkaido, Japan, 002-8022 GSK Investigational Site Hokkaido, Japan, 003-0833 GSK Investigational Site Hokkaido, Japan, 004-0074 GSK Investigational Site Hokkaido, Japan, 004-0876 GSK Investigational Site Hokkaido, Japan, 006-0022 GSK Investigational Site Hokkaido, Japan, 060-0063 GSK Investigational Site Hokkaido, Japan, 062-0042 GSK Investigational Site Hokkaido, Japan, 064-0915 GSK Investigational Site Hokkaido, Japan, 066-0021 GSK Investigational Site Hokkaido, Japan, 066-0064 GSK Investigational Site Hokkaido, Japan, 069-0813 GSK Investigational Site Hokkaido, Japan, 090-0832 GSK Investigational Site Hokkaido, Japan, 093-0016 GSK Investigational Site Kanagawa, Japan, 211-0063 GSK Investigational Site Kanagawa, Japan, 221-0825 GSK Investigational Site Osaka, Japan, 532-0026 GSK Investigational Site Osaka, Japan, 559-0017 GSK Investigational Site Osaka, Japan, 572-0838 GSK Investigational Site Osaka, Japan, 593-8324 GSK Investigational Site Saitama, Japan, 350-1305 GSK Investigational Site Tokyo, Japan, 111-0053 GSK Investigational Site Tokyo, Japan, 141-0031 GSK Investigational Site Tokyo, Japan, 150-0021 GSK Investigational Site Tokyo, Japan, 169-0075 GSK Investigational Site Tokyo, Japan, 194-0013 Collapse <<
  NCT00869492	Acne Vulgaris	Phase 3	Unknown	June 2009	Turkey ... more >> Marmara University school of medicine Istanbul, Turkey Collapse <<
  NCT00202891	Pyoderma	Phase 4	Withdrawn(No further local int... more >>erest in pursuing the study.) Collapse <<	-	-

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• 参考文献

• [1] Hosoda S, Komine M, et al. Nadifloxacin downregulates the production of matrix metalloproteinases in the human epidermal keratinocyte cell line HaCaT. J Dermatol. 2012 Oct;39(10):855-7.

  [2] Jacobs MR, Appelbaum PC. Nadifloxacin: a quinolone for topical treatment of skin infections and potential for systemic use of its active isomer, WCK 771. Expert Opin Pharmacother. 2006;7(14):1957–1966

  [3] Choudhury S, Chatterjee S, Sarkar DK, Dutta RN. Efficacy and safety of topical nadifloxacin and benzoyl peroxide versus clindamycin and benzoyl peroxide in acne vulgaris: A randomized controlled trial. Indian J Pharmacol. 2011;43(6):628–631

  [4] Kamaruzzaman NF, Pina MF, Chivu A, Good L. Polyhexamethylene Biguanide and Nadifloxacin Self-Assembled Nanoparticles: Antimicrobial Effects against Intracellular Methicillin-Resistant Staphylococcus aureus. Polymers (Basel). 2018;10(5):521. Published 2018 May 12

  [5] Murata K, Sugita K, Kobayashi M, Kabashima K, Tokura Y. Nadifloxacin downmodulates antigen-presenting functions of epidermal Langerhans cells and keratinocytes. J Dermatol Sci. 2006;42(2):91–99

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