Drug intelligence / Profile preview

bedaquiline + linezolid + levofloxacin + clofazimine + cycloserine

Development stage
Preclinical
Lead developer
Janssen Pharmaceutical
Modality
Small Molecules
Administration
Oral
01

Overview

This is a combination regimen of five drugs used for the treatment of drug-resistant tuberculosis (DR-TB), particularly multidrug-resistant tuberculosis (MDR-TB) and extensively drug-resistant tuberculosis (XDR-TB). The regimen combines: - Bedaquiline: A diarylquinoline that inhibits mycobacterial adenosine triphosphate (ATP) synthase - Linezolid: An oxazolidinone antibiotic that inhibits protein synthesis - Levofloxacin: A fluoroquinolone antibiotic that inhibits DNA gyrase - Clofazimine: A riminophenazine antibiotic with antimycobacterial properties - Cycloserine: An antibiotic that inhibits cell wall synthesis This all-oral regimen represents an approach to treating highly resistant forms of tuberculosis without injectable agents, which have traditionally been associated with significant adverse effects.

02

Targets

PTC (50S ribosomal peptidyl transferase center)AtpC (ATP synthase epsilon subunit)DdlA (D-alanyl-D-alanine Synthetase)Alr (Alanine racemase)DNA gyraseTopo IV (Bacterial Topoisomerase IV)Mycobacterial membrane and respiratory redox systemAtpE (Mycobacterial F1Fo ATP synthase subunit c)

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