Drug intelligence / Profile preview

radezolid

Development stage
Phase 2
Lead developer
Melinta Therapeutics
Modality
RNA-Targeting Small Molecules → Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Oral, Topical
01

Overview

Radezolid is a novel, second-generation oxazolidinone antibiotic developed for the treatment of serious multi-drug–resistant Gram-positive infections. It acts by inhibiting bacterial protein synthesis through binding to the 23S ribosomal RNA of the 50S subunit, thereby preventing formation of a functional 70S initiation complex essential for bacterial translation. Radezolid demonstrates potent activity against a range of Gram-positive bacteria, including methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococcus (VRE), and shows greater intracellular potency compared to linezolid. It has completed phase II clinical trials for community-acquired pneumonia and uncomplicated skin and skin structure infections. The drug is orally bioavailable, widely distributed in tissues, metabolized in the liver, and primarily excreted via the kidneys[3][5][6][7].

Other names
radezolid hydrochloride
02

Targets

PTC (50S ribosomal peptidyl transferase center)

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