Drug intelligence / Profile preview

moxifloxacin + rifabutin + para-aminosalicylic acid + pyrazinamide + ethambutol

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

Overview

This is a combination regimen consisting of five antibiotics—moxifloxacin, rifabutin, para-aminosalicylic acid (PAS), pyrazinamide, and ethambutol—used primarily for the treatment of drug-resistant tuberculosis (TB), including multidrug-resistant TB (MDR-TB). Each component targets Mycobacterium tuberculosis through distinct mechanisms: - **Moxifloxacin** is a fluoroquinolone that inhibits bacterial DNA gyrase and topoisomerase IV, enzymes essential for DNA replication and repair[3][4]. - **Rifabutin** is a rifamycin antibiotic that inhibits bacterial DNA-dependent RNA polymerase, suppressing RNA synthesis. - **Para-aminosalicylic acid** acts as an antimetabolite interfering with folic acid synthesis in mycobacteria. - **Pyrazinamide** is converted by mycobacterial pyrazinamidase to its active form, pyrazinoic acid; it disrupts membrane transport and energy production under acidic conditions within macrophages where M. tuberculosis resides[6][7][8][10]. - **Ethambutol** inhibits arabinosyl transferases involved in cell wall biosynthesis. This combination aims to maximize bactericidal activity while minimizing resistance development by attacking the pathogen at multiple metabolic points. It is typically reserved for cases where first-line agents are ineffective or not tolerated.

02

Targets

rpoB (DNA-directed RNA polymerase subunit beta)DHPS (Dihydropteroate synthase)Emb (Arabinofuranosyltransferase complex)Topo IV (Bacterial Topoisomerase IV)DNA gyrase

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