Drug intelligence / Profile preview

rifampicin + pyrazinamide + ethambutol

Development stage
Phase 3
Modality
Small Molecules
Administration
Oral
01

Overview

rifampicin + pyrazinamide + ethambutol (commonly referred to as the REZ or RZE regimen) is a three-drug antimycobacterial combination regimen used for the treatment of tuberculosis, particularly in patients with isoniazid-resistant tuberculosis (Hr-TB) or those who cannot tolerate isoniazid. The regimen consists of three first-line antitubercular agents with distinct mechanisms of action to prevent the development of drug resistance. Rifampicin is a rifamycin antibiotic that inhibits bacterial DNA-directed RNA polymerase, thereby blocking RNA transcription. Pyrazinamide is a prodrug converted to pyrazinoic acid, which targets aspartate decarboxylase (PanD) and ribosomal protein S1 (RpsA), disrupting coenzyme A synthesis and trans-translation. Ethambutol is a bacteriostatic agent that inhibits arabinosyl transferases, disrupting mycobacterial cell wall synthesis. This combination is typically administered orally as separate tablets over a period of 6 to 9 months.

Other names
REZREZ regimenRZERZE regimenrifampicin, pyrazinamide, and ethambutolrifampin + pyrazinamide + ethambutolrifampin, pyrazinamide, and ethambutol
02

Targets

Aspartate decarboxylaserpoB (DNA-directed RNA polymerase subunit beta)embA (Arabinosyltransferase A)embB (Arabinosyltransferase EmbB)EmbC (Mycobacterium avium complex arabinosyltransferase EmbC)

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