ArticleAntimicrobial agents and chemotherapy2005
Preclinical testing of the nitroimidazopyran PA-824 for activity against Mycobacterium tuberculosis in a series of in vitro and in vivo models.
Article in Antimicrobial agents and chemotherapy, 2005. The graph could read no effect estimate from its abstract, so it casts no vote on the map. It is linked to trial NCT01571414 (A Phase I, Three-Arm Safety, Tolerability, and Pharmacokinetic Interaction Study of PA-824, an Investigational Nitroimidazole for the Treatment of Tuberculosis, Together With Efavirenz, Ritonavir-Boosted Lopinavir, or Rifampin), which is not on this map. Cited by 135 papers.
What it found
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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.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
A Phase I, Three-Arm Safety, Tolerability, and Pharmacokinetic Interaction Study of PA-824, an Investigational Nitroimidazole for the Treatment of Tuberculosis, Together With Efavirenz, Ritonavir-Boosted Lopinavir, or Rifampin
Who cites it
135 citing papers in PubMed, 305 citations in OpenAlex.
- Phase I safety, pharmacokinetics, and pharmacogenetics study of the antituberculosis drug PA-824 with concomitant lopinavir-ritonavir, efavirenz, or rifampin.Antimicrobial agents and chemotherapy · 2014Trial
- Effect of a high-calorie, high-fat meal on the bioavailability and pharmacokinetics of PA-824 in healthy adult subjects.Antimicrobial agents and chemotherapy · 2013Trial
- Early bactericidal activity and pharmacokinetics of PA-824 in smear-positive tuberculosis patients.Antimicrobial agents and chemotherapy · 2010Trial
- Safety, tolerability, and pharmacokinetics of PA-824 in healthy subjects.Antimicrobial agents and chemotherapy · 2009Trial
- Assessment of the effects of the nitroimidazo-oxazine PA-824 on renal function in healthy subjects.Antimicrobial agents and chemotherapy · 2009Trial
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- Discovery and development of a new oxazolidinone with reduced toxicity for the treatment of tuberculosis.Nature medicine · 2026Article
- Same class, different activity: Delamanid and pretomanid have comparable bactericidal activity but pretomanid potently inhibitsbioRxiv : the preprint server for biology · 2025Article
- Mouse Models Uniformly Featuring Human-like Lesions Harboring Drug-tolerantbioRxiv : the preprint server for biology · 2025Article
- The Perspectives of Combining Antibiotics with Saponins-Herbal Excipients.Molecules (Basel, Switzerland) · 2025Review
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- β-Aminopropioamidoximes derivatives as potential antitubercular agents against anthropozoonotic infections caused byVeterinary world · 2025Article
- Structural and mechanistic study of a novel inhibitor analogue ofnpj drug discovery · 2025Article
- Assessment of tuberculosis drug efficacy using preclinical animal models and in vitro predictive techniques.npj antimicrobials and resistance · 2024Article
- PA-824 inhibits porcine epidemic diarrhea virus infectionJournal of virology · 2024Article
- Use of multiple pharmacodynamic measures to deconstruct the Nix-TB regimen in a short-course murine model of tuberculosis.Antimicrobial agents and chemotherapy · 2024Article
- Drug distribution and efficacy of the DprE1 inhibitor BTZ-043 in the C3HeB/FeJ mouse tuberculosis model.Antimicrobial agents and chemotherapy · 2023Article
- Advances in Diagnostics and Drug Discovery against Resistant and Latent Tuberculosis Infection.Pharmaceutics · 2023Review
- Inhalable Combination Powder Formulations for Treating Latent and Multidrug-Resistant Tuberculosis: Formulation and In Vitro Characterization.Pharmaceutics · 2023Article
75 more citing papers are in PubMed but not listed here.
Corrections and comments
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Authors and funding
9 authors at 2 institutions in 1 country.
Funding
Abstract
This study extends earlier reports regarding the in vitro and in vivo efficacies of the nitroimidazopyran PA-824 against Mycobacterium tuberculosis. PA-824 was tested in vitro against a broad panel of multidrug-resistant clinical isolates and was found to be highly active against all isolates (MIC<1 microg/ml). The activity of PA-824 against M. tuberculosis was also assessed grown under conditions of oxygen depletion. PA-824 showed significant activity at 2, 10, and 50 microg/ml, similar to that of metronidazole, in a dose-dependent manner. In a short-course mouse infection model, the efficacy of PA-824 at 50, 100, and 300 mg/kg of body weight formulated in methylcellulose or cyclodextrin/lecithin after nine oral treatments was compared with those of isoniazid, rifampin, and moxifloxacin. PA-824 at 100 mg/kg in cyclodextrin/lecithin was as active as moxifloxacin at 100 mg/kg and isoniazid at 25 mg/kg and was slightly more active than rifampin at 20 mg/kg. Long-term treatment with PA-824 at 100 mg/kg in cyclodextrin/lecithin reduced the bacterial load below 500 CFU in the lungs and spleen. No significant differences in activity between PA-824 and the other single drug treatments tested (isoniazid at 25 mg/kg, rifampin at 10 mg/kg, gatifloxacin at 100 mg/kg, and moxifloxacin at 100 mg/kg) could be observed. In summary, its good activity in in vivo models, as well as its activity against multidrug-resistant M. tuberculosis and against M. tuberculosis isolates in a potentially latent state, makes PA-824 an attractive drug candidate for the therapy of tuberculosis. These data indicate that there is significant potential for effective oral delivery of PA-824 for the treatment of tuberculosis.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.