フィダキソマイシン

危険有害性情報のコード(GHS)

• 絵表示(GHS)

  

• 注意喚起語

  Warning

• 危険有害性情報

  H315：皮膚刺激

  H319：強い眼刺激

  H335：呼吸器への刺激のおそれ

• 注意書き

  P280：保護手袋/保護衣/保護眼鏡/保護面を着用するこ と。

  P305+P351+P338：眼に入った場合：水で数分間注意深く洗うこと。次にコ ンタクトレンズを着用していて容易に外せる場合は外す こと。その後も洗浄を続けること。

  P321：特別な処置が必要である（このラベルの．．． を見よ）。

フィダキソマイシン 価格

フィダキソマイシン 化学特性,用途語,生産方法

• 外観

  白色～うすい黄色粉末～結晶

• 効能

  抗生物質, タンパク質合成阻害薬

• 商品名

  ダフクリア (アステラス製薬)

• 説明

  Fidaxomicin (OPT-80) was approved by the U.S. FDA in May 2011 for the treatment of Clostridium difficile-associated diarrhea (CDAD), joining metronidazole and vancomycin as drugs recommended for treatment of C. difficile infections (CDI). Fidaxomicin, also known as lipiarmycin and tiacumicin, is an 18-membered macrolide natural product that was first reported in mid-1970s and is produced by fermentation. Fidaxomicin and its primary metabolite OP-1118, which results from hydrolysis of the isobutyryl ester, are narrowspectrum antibacterial agents with activity against gram-positive aerobic and anaerobic organisms, but not against gram-negative organisms. Fidaxomicin and OP-1118 exert their antibacterial activity by inhibiting bacterial RNA polymerase, thereby inhibiting bacterial protein synthesis.
  The MIC90 (minimum inhibitory concentration to kill 90% of bacteria) for fidaxomicin against C.difficile is 0.125–0.25 μg/mL; OP- 1118 is 4- to 16-fold less potent than the parent compound. Fidaxomicin has been reported to spare native intestinal flora such as Bacteroides spp. and as such, may prevent selection of drug-resistant bacteria. Fidaxomicin is bactericidal to C. difficile and has a low propensity for resistance development with no cross-resistance to existing antibiotics. Fidaxomicin shows minimal systemic absorption following oral administration in preclinical studies and humans.

• 使用

  Fidaxomicin is a recently marketed antibiotic with a confusing history dating back to its original isolation in 1975. Fidaxomicin is the major analogue of a family of macrocyclic lactones, isolated independently by three different groups from cultures belonging to three different genera (Actinoplanes, Dactylosporangium and Micromonospora) known as lipiarmycin A3, tiacumicin B and clostomicin B1, respectively. Fidaxomicin is a narrow spectrum antibiotic with excellent activity against Gram positive bacteria, notably Clostridium difficile. Fidaxomicin acts in the gastrointestinal tract without undue disruption to gut microbial flora.

• 定義

  ChEBI: An 18-membered macrolide that is a fermentation product obtained from the Actinomycete Dactylosporangium aurantiacum. A narrow spectrum antibiotic used for treatment of Clostridium difficile-related infections.

• 応用例（製薬）

  Formerly known as difimicin. An 18-membered macrocyclic compound related to the tiacumicin group of antibiotics rather than conventional macrolides. It is active against staphylococci (MIC 0.5–2 mg/L) and most anaerobic Grampositive bacilli and cocci, but Gram-negative bacilli, including Gram-negative anaerobes, are resistant. It is very poorly absorbed when given orally and most interest surrounds its activity against C. difficile (MIC 0.12–0.25 mg/L). Such data as are presently available from clinical trials suggest that it is as safe and effective in the treatment of C. difficile-associated diarrhea as vancomycin.

フィダキソマイシン 生産企業

Global(275)Suppliers

フィダキソマイシン スペクトルデータ(¹HNMR)

873857-62-6, フィダキソマイシン キーワード