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Topical retapamulin in the management of infected traumatic skin lesions
Ribhi Shawar1, Nicole Scangarella-Oman, Marybeth Dalessandro
1Infectious Disease Center for Excellence in Drug Discovery, GlaxoSmithKline, Collegeville, PA, USA;
Abstract:
Retapamulin is a novel semisynthetic pleuromutilin antibiotic specifically designed for use as a topical agent. The unique mode of action by which retapamulin selectively inhibits bacterial protein synthesis differentiates it from other nonpleuromutilin antibacterial agents that target the ribosome or ribosomal factors, minimizing the potential for target-specific cross-resistance with other antibacterial classes in current use. In vitro studies show that retapamulin has high potency against the Gram-positive bacteria (Staphylococcus aureus, Streptococcus pyogenes, and coagulase-negative staphylococci) commonly found in skin and skin-structure infections (SSSIs), including S. aureus strains with resistance to agents such as macrolides, fusidic acid, or mupirocin, and other less common organisms associated with SSSIs, anaerobes, and common respiratory tract pathogens. Clinical studies have shown that twice-daily topical retapamulin for 5 days is comparable to 10 days of oral cephalexin in the treatment of secondarily infected traumatic lesions. A 1% concentration of retapamulin ointment has been approved for clinical use as an easily applied treatment with a short, convenient dosing regimen for impetigo. Given the novel mode of action, low potential for cross-resistance with established antibacterial agents, and high in vitro potency against many bacterial pathogens commonly recovered from SSSIs, retapamulin is a valuable enhancement over existing therapeutic options.
Insights
Retapamulin is a novel topical antibiotic that inhibits bacterial protein synthesis. It effectively treats skin infections, including those resistant to other drugs, offering a convenient alternative.
Area of Science:
- Microbiology
- Pharmacology
- Dermatology
Background:
- Retapamulin is a novel semisynthetic pleuromutilin antibiotic developed for topical application.
- Its unique mechanism of action inhibits bacterial protein synthesis, distinct from other ribosome-targeting agents.
- This minimizes potential cross-resistance with existing antibacterial classes.
Purpose of the Study:
- To evaluate the efficacy and safety of retapamulin as a topical agent for skin and skin-structure infections (SSSIs).
- To assess its activity against common Gram-positive pathogens, including antibiotic-resistant strains.
- To compare retapamulin's effectiveness with standard oral treatments for specific SSSIs.
Main Methods:
- In vitro studies assessed retapamulin's potency against various bacterial pathogens.
- Clinical trials compared topical retapamulin (twice-daily for 5 days) with oral cephalexin (10 days) for secondarily infected traumatic lesions.
- Approved clinical use involves a 1% retapamulin ointment for impetigo.
Main Results:
- Retapamulin demonstrated high in vitro potency against Staphylococcus aureus, Streptococcus pyogenes, and coagulase-negative staphylococci.
- It showed efficacy against S. aureus strains resistant to macrolides, fusidic acid, or mupirocin.
- Clinical studies found topical retapamulin comparable to oral cephalexin for treating infected traumatic lesions.
Conclusions:
- Retapamulin offers a novel mechanism of action with low cross-resistance potential.
- It is highly effective against key pathogens causing SSSIs.
- Retapamulin represents a valuable topical treatment option for impetigo and other skin infections.
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