ArticleAntimicrobial agents and chemotherapy2010
In vitro interactions between new antitubercular drug candidates SQ109 and TMC207.
Article in Antimicrobial agents and chemotherapy, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 49 papers.
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Who cites it
49 citing papers in PubMed, 132 citations in OpenAlex.
- Integrated computational and experimental approaches for drug repurposing targeting key Mycobacterium tuberculosis proteins.Molecular diversity · 2026Article
- Physiologic recovery of Mycobacterium tuberculosis from drug injury: A molecular study of post antibiotic effect in vitro and in vivo.PLoS pathogens · 2026Article
- Assessing the efficacy of combined treatment using bedaquiline against clinical isolates of multidrug-resistant Mycobacterium tuberculosis in vitro and the macrophage model.BMC microbiology · 2026Article
- Investigating the unbinding mechanisms and kinetics of MmpL3 inhibitors: A computational study.Protein science : a publication of the Protein Society · 2025Article
- Evolution of Small Molecule Inhibitors ofJournal of medicinal chemistry · 2025Article
- Revolutionizing tuberculosis treatment: Breakthroughs, challenges, and hope on the horizon.Acta pharmaceutica Sinica. B · 2025Review
- Inhibitor binding and disruption of coupled motions in MmpL3 protein: Unraveling the mechanism of trehalose monomycolate transport.Protein science : a publication of the Protein Society · 2024Article
- Deciphering the possible role of MmpL7 efflux pump in SQ109 resistance in Mycobacterium tuberculosis.Annals of clinical microbiology and antimicrobials · 2024Article
- S288T mutation altering MmpL3 periplasmic domain channel and H-bond network: a novel dual drug resistance mechanism.Journal of molecular modeling · 2024Article
- Discovery of anti-infective compounds againstFrontiers in microbiology · 2024Article
- The implication of Mycobacterium tuberculosis-mediated metabolism of targeted xenobiotics.Nature reviews. Chemistry · 2023Review
- The pathogenic mechanism of Mycobacterium tuberculosis: implication for new drug development.Molecular biomedicine · 2022Review
- NSC19723, a Thiacetazone-Like Benzaldehyde Thiosemicarbazone Improves the Efficacy of TB DrugsMicrobiology spectrum · 2022Article
- Pharmacokinetics and Target Attainment of SQ109 in Plasma and Human-Like Tuberculosis Lesions in Rabbits.Antimicrobial agents and chemotherapy · 2021Article
- Hydroxylation of Antitubercular Drug Candidate, SQ109, by Mycobacterial Cytochrome P450.International journal of molecular sciences · 2020Article
- Multiple Mutations in Mycobacterium tuberculosis MmpL3 Increase Resistance to MmpL3 Inhibitors.mSphere · 2020Article
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- Bioenergetics of Mycobacterium: An Emerging Landscape for Drug Discovery.Pathogens (Basel, Switzerland) · 2018Review
- Revisiting Activation of and Mechanism of Resistance to Compound IQG-607 in Mycobacterium tuberculosis.Antimicrobial agents and chemotherapy · 2018Article
Corrections and comments
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The in vitro interactions of two new antitubercular drugs, SQ109 and TMC207, with each other and with rifampin (RIF) were evaluated. The combination of SQ109 with TMC207 (i) improved an already excellent TMC207 MIC for M. tuberculosis H37Rv by 4- to 8-fold, (ii) improved the rate of killing of bacteria over the rate of killing by each single drug, and (iii) enhanced the drug postantibiotic effect by 4 h. In no instance did we observe antagonistic activities with the combination of SQ109 and TMC207. Rifampin activates cytochrome P450 genes to reduce the area under the curve (AUC) for TMC207 in humans. The presence of RIF in three-drug combinations did not affect the synergistic activities of SQ109 and TMC207, and SQ109 also dramatically decreased the MIC of RIF. SQ109 was active by itself, and both its activity was improved by and it improved the in vitro activities of both RIF and TMC207.
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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.