Drug intelligence / Profile preview

rifapentine + moxifloxacin + pyrazinamide + isoniazid

Development stage
Unknown
Lead developer
National Institutes of Health Tuberculosis Trials Consortium
Modality
Small Molecules
Administration
Oral
01

Overview

This drug is a fixed-dose combination regimen consisting of four antibiotics—rifapentine, moxifloxacin, pyrazinamide, and isoniazid—used for the treatment of drug-susceptible pulmonary tuberculosis. Each component has a distinct mechanism of action targeting *Mycobacterium tuberculosis*: - **Rifapentine** inhibits DNA-dependent RNA polymerase in mycobacteria, blocking RNA synthesis. - **Moxifloxacin** is a fluoroquinolone that inhibits bacterial DNA gyrase and topoisomerase IV, interfering with DNA replication and repair. - **Pyrazinamide** disrupts membrane transport and energy production in *M. tuberculosis*, particularly effective against semi-dormant bacilli in acidic environments. - **Isoniazid** inhibits the synthesis of mycolic acids essential for the mycobacterial cell wall. The combination has been shown to be non-inferior to standard 6-month regimens (which use rifampin instead of rifapentine and ethambutol instead of moxifloxacin) when used as a 4-month daily regimen for pan-susceptible pulmonary TB[2][6][8]. This shortened course offers potential benefits in adherence and programmatic management.

Other names
HPMZ4-month rifapentine-moxifloxacin regimen
02

Targets

Topo IV (Bacterial Topoisomerase IV)rpoB (DNA-directed RNA polymerase subunit beta)MmpL3 (Mycobacterial membrane protein Large 3)FabI (Enoyl-acyl carrier protein reductase FabI)GyrA (DNA gyrase subunit A)

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