Sutezolid: A promising next enerationuberculosis agent

Kiran, Garlapati Usha and kumar, Loya Pavan and Mahesh, Maareedu and manikanta, Kankanala Uma Satya and Nehemiah, Gollamudi and kumar, Guntru Pavan (2025) Sutezolid: A promising next enerationuberculosis agent. World Journal of Biology Pharmacy and Health Sciences, 23 (2). pp. 348-355. ISSN 2582-5542

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.