Drug intelligence / Profile preview

retapamulin

Development stage
Phase 4
Lead developer
GSK
Modality
Small Molecules
Administration
Topical
01

Overview

Retapamulin is a topical antibiotic in the pleuromutilin class, developed for the treatment of skin infections such as impetigo caused by methicillin-susceptible *Staphylococcus aureus* and *Streptococcus pyogenes*. It works by selectively inhibiting bacterial protein synthesis through binding to a unique site on the 50S subunit of the bacterial ribosome (specifically at domain V of 23S rRNA near the peptidyl transferase center and P-site), thereby blocking peptidyl transfer, preventing P-site interactions, and inhibiting formation of active 50S ribosomal subunits. This mechanism is distinct from other protein synthesis inhibitors and reduces cross-resistance with other antibiotic classes. Retapamulin does not affect mammalian ribosomes and is used topically due to low systemic absorption. Developed by GlaxoSmithKline (GSK) and manufactured by GSK.

Brand names
AltabaxAltargo
Other names
retapamulina
02

Targets

Bacterial 50S ribosomal subunit

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