ArticleThe Journal of infectious diseases2024
Relative Contributions of the Novel Diarylquinoline TBAJ-876 and its Active Metabolite to the Bactericidal Activity in a Murine Model of Tuberculosis.
Article in The Journal of infectious diseases, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Who cites it
4 citing papers in PubMed.
- Recent advances in antituberculosis drugs and therapeutics: from mechanistic breakthroughs to clinical translation.Molecular biomedicine · 2026Review
- One-Dose Efficacy of Long-Acting Sorfequiline in a Mouse Model of Tuberculosis Preventive Therapy.bioRxiv : the preprint server for biology · 2026Article
- Semi-Mechanistic Joint Population Pharmacokinetic Modeling of the Novel Antituberculosis Drug Sorfequiline and Its Metabolite M3 in Healthy Volunteers.CPT: pharmacometrics & systems pharmacology · 2026Article
- REVOLUTIONIZING TUBERCULOSIS REGIMEN DEVELOPMENT.Transactions of the American Clinical and Climatological Association · 2025Review
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Authors and funding
7 authors.
Funding
Abstract
backgroundTBAJ-876 is a next-generation diarylquinoline. In vivo, diarylquinoline metabolites are formed with activity against Mycobacterium tuberculosis. Species-specific differences in parent drug-to-metabolite ratios might impact the translational value of animal model-based predictions. This study investigates the contribution of TBAJ-876 and its major active metabolite, TBAJ-876-M3 (M3), to the total bactericidal activity in a mouse tuberculosis model.
methodsIn vitro activity of TBAJ-876 and M3 was investigated and compared to bedaquiline. Subsequently, a dose-response study was conducted in M. tuberculosis-infected BALB/c mice treated with TBAJ-876 (1.6/6.3/25 mg/kg) or M3 (3.1/12.5/50 mg/kg). Colony-forming units in the lungs and TBAJ-876 and M3 plasma concentrations were determined. M3's contribution to TBAJ-876's bactericidal activity was estimated based on M3 exposure following TBAJ-876 treatment and corresponding M3 activity observed in M3-treated animals.
resultsTBAJ-876 and M3 demonstrated profound bactericidal activity. Lungs of mice treated for 4 weeks with 50 mg/kg M3 were culture negative. Following TBAJ-876 treatment, M3 exposures were 2.2 to 3.6-fold higher than for TBAJ-876. TBAJ-876 activity was substantially attributable to M3, given its high exposure and potent activity.
conclusionsThese findings emphasize the need to consider metabolites and their potentially distinct exposure and activity profiles compared to parent drugs to enhance the translational value of mouse model-driven predictions.
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