Sutezolid: A promising next generation tuberculosis agent

Sutezolid (PNU-100480) is an advanced oxazolidinone antibiotic that shows strong effectiveness against Mycobacterium tuberculosis, including those tough multidrug-resistant (MDR) and extensively drug-resistant (XDR) strains. It works by blocking bacterial protein synthesis, specifically by attaching to the 23S rRNA of the 50S ribosomal subunit, which messes with translation and the formation of essential proteins. Both preclinical and clinical studies have shown that it has better intracellular bactericidal activity compared to linezolid, with impressive penetration into lung tissue and macrophages. Its active metabolite, PNU-101603 (M1), boosts its effectiveness outside the cells. With a favorable safety profile, hepatic metabolism, and a half-life of 4 to 6 hours, it shows promise for shorter and more effective TB treatment regimens. Ongoing Phase II trials are set to confirm its effectiveness against both drug-sensitive and resistant TB, as well as latent and CNS infections.

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Publication Details

Journal
World Journal of Biology Pharmacy and Health Sciences
Published
2025-08-28
DOI
https://doi.org/10.30574/wjbphs.2025.23.2.0769
Primary Topic
Sesquiterpenes and Asteraceae Studies
Type
article
Field-Weighted Citation Impact
0.00
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article

Sutezolid: A promising next generation tuberculosis agent

M. S. Mahesh, Gundu Ramachandra Kumar, Lalit Kumar, Garlapati Usha Kiran et al.
World Journal of Biology Pharmacy and Health Sciences
Sesquiterpenes and Asteraceae Studies
article

Sutezolid: A promising next generation tuberculosis agent

M. S. Mahesh, Gundu Ramachandra Kumar, Lalit Kumar, Garlapati Usha Kiran, Kankanala Uma Satya manikanta, Gollamudi Nehemiah
article en

Abstract

Sutezolid (PNU-100480) is an advanced oxazolidinone antibiotic that shows strong effectiveness against Mycobacterium tuberculosis, including those tough multidrug-resistant (MDR) and extensively drug-resistant (XDR) strains. It works by blocking bacterial protein synthesis, specifically by attaching to the 23S rRNA of the 50S ribosomal subunit, which messes with translation and the formation of essential proteins. Both preclinical and clinical studies have shown that it has better intracellular bactericidal activity compared to linezolid, with impressive penetration into lung tissue and macrophages. Its active metabolite, PNU-101603 (M1), boosts its effectiveness outside the cells. With a favorable safety profile, hepatic metabolism, and a half-life of 4 to 6 hours, it shows promise for shorter and more effective TB treatment regimens. Ongoing Phase II trials are set to confirm its effectiveness against both drug-sensitive and resistant TB, as well as latent and CNS infections.

World Journal of Biology Pharmacy and Health SciencesVol. 23(2)
Openalex Percentile: Top 72%
Sesquiterpenes and Asteraceae Studies
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