Drug intelligence / Profile preview

sutezolid + pyrazinamide

Development stage
Unknown
Lead developer
Sequella
Modality
Small Molecules
Administration
Oral
01

Overview

Sutezolid + pyrazinamide is an experimental combination therapy investigated for the treatment of tuberculosis (TB). Sutezolid (formerly PNU-100480) is a next-generation oxazolidinone antibiotic, a thiomorpholine analogue of linezolid, which inhibits bacterial protein synthesis by binding to the 23S ribosomal RNA of the 50S subunit. Pyrazinamide is a standard first-line antitubercular prodrug that is converted into pyrazinoic acid by the bacterial enzyme pyrazinamidase; its mechanism involves the disruption of bacterial cell membrane potential and transport functions, as well as the inhibition of targets such as ribosomal protein S1 (RpsA) and aspartate 1-decarboxylase (PanD). This combination has demonstrated synergistic activity in preclinical mouse models of TB, suggesting potential for shortening treatment duration and improving outcomes in both drug-susceptible and drug-resistant tuberculosis cases.

Other names
PNU-100480 + pyrazinamidePNU-100480 + PZA
02

Targets

Bacterial 50S ribosomal subunit

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