Drug intelligence / Profile preview

bedaquinoline + linezolid + moxifloxacin + cycloserine

Development stage
Unknown
Lead developer
Johnson & Johnson
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

This is a combination regimen consisting of four antibiotics—bedaquinoline, linezolid, moxifloxacin, and cycloserine—used primarily for the treatment of multidrug-resistant tuberculosis (MDR-TB) and extensively drug-resistant tuberculosis (XDR-TB). Each component has a distinct mechanism of action targeting Mycobacterium tuberculosis: - **Bedaquinoline** is a diarylquinoline antibiotic that inhibits mycobacterial ATP synthase, disrupting energy production in the bacteria. - **Linezolid** is an oxazolidinone antibiotic that inhibits bacterial protein synthesis by binding to the 50S ribosomal subunit. - **Moxifloxacin** is a fluoroquinolone antibiotic that acts by inhibiting bacterial DNA gyrase (topoisomerase II) and topoisomerase IV, enzymes essential for DNA replication and repair[3][4]. - **Cycloserine** interferes with cell wall synthesis in mycobacteria by inhibiting enzymes involved in peptidoglycan formation. This combination targets multiple pathways within M. tuberculosis to maximize bactericidal activity and reduce the risk of resistance development. The regimen is typically reserved for cases where first-line anti-tuberculosis drugs are ineffective due to resistance.

02

Targets

AtpE (ATP synthase subunit c)Alr (Alanine racemase)Topo IV (Bacterial Topoisomerase IV)50S ribosomal peptidyl transferase center A-site region of 23S rRNADdlA (D-alanyl-D-alanine Synthetase)DNA gyraseAtpC (ATP synthase epsilon subunit)

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