生物活性

• 描述Retapamulin, a semisynthetic pleuromutilin derivative, is exclusively used for the topical short-term medication of impetigo and staphylococcal infections^[3]. Retapamulin MICs ranged from ≤ 0.015 to 0.12 μg/mL, showing the highest intrinsic activity among the topical antimicrobial drugs studied^[4]. Retapamulin inhibited all the isolates of MSSA (methicillin-susceptible Staphylococcus aureus) and MRSA (methicillin-resistant S. aureus) at 0.125 mg/L, but the 18 linezolid-resistant-MRSA strains proved resistant, with MICs over 32 mg/L^[5]. Retapamulin 1% ointment is a unique topical antibiotic formulation that may be a suitable option for the treatment of clinically infected AD (atopic dermatitis). Retapamulin 1% is effective for the treatment of atopic dermatitis infected with S aureus, and demonstrates efficacy against both methicillin-susceptible and methicillin-resistant strains^[6].
• 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
  NCT01397461	Impetigo	Phase 3	Completed	-	Germany ... more >> Georg Popp Augsburg, Germany Roland Aschoff Dresden, Germany Diamant Thaci Frankfurt/Main, Germany Klaus Chelius Köln, Germany Stephan Schilling Mahlow, Germany South Africa Ismail Mitha Benoni, South Africa Johan Lombaard Bloemfontein, South Africa Jan Fourie Dundee, South Africa Dawie Kruger George, South Africa Philip Nel Hatfield, South Africa Essack Mitha Johannesburg, South Africa J Trokis Kraaifontein, South Africa Mohammed Tayob Middelburg, South Africa Mashra Gani Port Elizabeth, South Africa Zelda Punt Port Elizabeth, South Africa Molefe Phayane Pretoria, South Africa Gail Todd Rondebosch, South Africa Yacoob Vahed Welkom, South Africa Christo van Dyk Worcester, South Africa Collapse <<
  NCT01397461	-	-	Completed	-	-
  NCT00133874	Skin Infections, Bacterial	Phase 3	Completed	-	-

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• 参考文献

• [1] Nalwade S, Reddy VR. A validated stability-indicating liquid chromatographic method for the determination of retapamulin in topical dosage form. J Chromatogr Sci. 2014 Mar;52(3):238-45.

  [2] Champney WS, Rodgers WK. Retapamulin inhibition of translation and 50S ribosomal subunit formation in Staphylococcus aureus cells. Antimicrob Agents Chemother. 2007 Sep;51(9):3385-7.

  [3] Sun F, Zhang H, Gonzales GB, et al. Unraveling the Metabolic Routes of Retapamulin: Insights into Drug Development of Pleuromutilins. Antimicrob Agents Chemother. 2018;62(4):e02388-17. Published 2018 Mar 27

  [4] Pérez-Trallero E, Tamayo E, Montes M, García-Arenzana JM, Iriarte V. in vitro activities of retapamulin and 16 other antimicrobial agents against recently obtained Streptococcus pyogenes isolates. Antimicrob Agents Chemother. 2011;55(5):2406–2408

  [5] Candel FJ, Morales G, Picazo JJ. in vitro activity of retapamulin against linezolid and methicillin-resistant Staphylococcus aureus isolates. Rev Esp Quimioter. 2011;24(3):127–130

  [6] Kircik LH. Efficacy and tolerability of retapamulin 1% ointment for the treatment of infected atopic dermatitis: a pilot study. J Drugs Dermatol. 2012;11(7):858–860

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