Drug intelligence / Profile preview

RX-05

Development stage
Discontinued
Lead developer
Melinta Therapeutics
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

RX-05 is a novel, next-generation macrolide antibiotic originally developed by Rib-X Pharmaceuticals (now Melinta Therapeutics). It was designed using a structure-based drug design platform to overcome common mechanisms of macrolide resistance, such as ribosomal methylation (encoded by *erm* genes) and efflux pumps (encoded by *mef* genes). RX-05 binds to the 50S ribosomal subunit, specifically targeting the peptidyl transferase center and the peptide exit tunnel to inhibit bacterial protein synthesis. It has demonstrated potent in vitro activity against a broad spectrum of Gram-positive pathogens, including methicillin-resistant *Staphylococcus aureus* (MRSA) and multi-drug resistant *Streptococcus pneumoniae*. The program was primarily investigated for indications such as community-acquired bacterial pneumonia (CABP) and complicated skin and soft tissue infections (cSSTI), but development appears to have been discontinued in favor of other candidates in the developer's pipeline.

02

Targets

Bacterial 50S ribosomal subunit

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