ArticleNature communications2025
The clinical-stage drug BTZ-043 accumulates in murine tuberculosis lesions and efficiently acts against Mycobacterium tuberculosis.
Article in Nature communications, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed.
- Population pharmacokinetics and exposure-response relationship of the antituberculosis drug BTZ-043.The Journal of antimicrobial chemotherapy · 2025Trial
- Human prostaglandin reductases dearomatize and inactivate benzothiazinone antitubercular drugs.EMBO molecular medicine · 2026Article
- Small is big: growing impact of small molecule mass spectrometry in infectious disease drug development.mSphere · 2026Review
- Applications and technical challenges of MALDI mass spectrometry imaging in microbial ecosystems and metabolic network research.Archives of microbiology · 2026Review
- Bacterial cell envelope-targeting antibiotics.Nature reviews. Microbiology · 2026Review
- Advancing Tuberculosis Treatment with Next-Generation Drugs and Smart Delivery Systems.Pharmaceutics · 2026Review
- Levofloxacin-Catalase-PLGA Nanoparticles Potentiate Sonodynamic Therapy to Alleviate BCG-Induced Tuberculous Granulomas via PI3K/Akt/VEGF Pathway Suppression in Rats.International journal of nanomedicine · 2026Article
- Analysis of risk factors for latent tuberculosis infection among type 2 diabetics: a hospital-based multicenter cross-sectional study.Frontiers in cellular and infection microbiology · 2026Article
- New drugs for the management of tuberculosis.Current opinion in infectious diseases · 2025Review
- Low-level BTZ-043 resistance inIJTLD open · 2025Article
- First-in-human study of the benzothiazinone and DprE1 inhibitor BTZ-043, a novel drug candidate for the treatment of Tuberculosis.JAC-antimicrobial resistance · 2025Article
- Translational Modeling of BTZ-043 to Predict Phase 2A Efficacy and Evaluate Drug-Drug Interactions With Bedaquiline, Pretomanid, and Linezolid in Murine Models.The Journal of infectious diseases · 2025Article
- A Comparative Pharmacokinetics Study of Orally and Intranasally Administered 8-Nitro-1,3-benzothiazin-4-one (BTZ043) Amorphous Drug Nanoparticles.ACS pharmacology & translational science · 2024Article
Corrections and comments
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Authors and funding
24 authors.
Funding
Abstract
The development of granulomas with central necrosis harboring Mycobacterium tuberculosis (Mtb) is the hallmark of human tuberculosis (TB). New anti-TB therapies need to effectively penetrate the cellular and necrotic compartments of these lesions and reach sufficient concentrations to eliminate Mtb. BTZ-043 is a novel antibiotic showing good bactericidal activity in humans in a phase IIa trial. Here, we report on lesional BTZ-043 concentrations severalfold above the minimal-inhibitory-concentration and the substantial local efficacy of BTZ-043 in interleukin-13-overexpressing mice, which mimic human TB pathology of granuloma necrosis. High-resolution MALDI imaging further reveals that BTZ-043 diffuses and accumulates in the cellular compartment, and fully penetrates the necrotic center. This is the first study that visualizes an efficient penetration and accumulation of a clinical-stage TB drug in human-like centrally necrotizing granulomas and that also determines its lesional activity. Our results most likely predict a substantial bactericidal effect of BTZ-043 at these hard-to-reach sites in TB patients.
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