ArticleAntimicrobial agents and chemotherapy2014
Comparative study of the effects of antituberculosis drugs and antiretroviral drugs on cytochrome P450 3A4 and P-glycoprotein.
Article in Antimicrobial agents and chemotherapy, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. It is linked to trial NCT03827811 (Pharmacometrics to Advance Novel Regimens for Drug-resistant Tuberculosis), which is not on this map. Cited by 22 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.
Pharmacometrics to Advance Novel Regimens for Drug-resistant Tuberculosis
Who cites it
22 citing papers in PubMed, 35 citations in OpenAlex.
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- Pharmacokinetics of anti-Mycobacterium avium-intracellulare disease drugs in silkworms.Scientific reports · 2024Article
- Clofazimine as a substitute for rifampicin improves efficacy ofAntimicrobial agents and chemotherapy · 2024Article
- PBPK Modeling of Azithromycin Systemic Exposure in a Roux-en-Y Gastric Bypass Surgery Patient Population.Pharmaceutics · 2023Article
- Clofazimine for the treatment of tuberculosis.Frontiers in pharmacology · 2023Review
- Coadministration of bedaquiline and pyrifazimine reduce exposure to toxic metabolite N-desmethyl bedaquiline.Frontiers in pharmacology · 2023Article
- Advancing personalized medicine for tuberculosis through the application of immune profiling.Frontiers in cellular and infection microbiology · 2023Review
- New and Repurposed Drugs for the Treatment of Active Tuberculosis: An Update for Clinicians.Respiration; international review of thoracic diseases · 2023Review
- Physiologically Based Pharmacokinetic Modeling To Guide Management of Drug Interactions between Elexacaftor-Tezacaftor-Ivacaftor and Antibiotics for the Treatment of Nontuberculous Mycobacteria.Antimicrobial agents and chemotherapy · 2022Article
- Pharmacokinetics and Adverse Effects of Clofazimine in the Treatment of Pulmonary Non-Tuberculous Mycobacterial Infection.Antimicrobial agents and chemotherapy · 2022Observational
- Characterization of Clofazimine as a Potential Substrate of Drug Transporter.Antimicrobial agents and chemotherapy · 2022Article
- Predicting Drug-Drug Interactions between Rifampicin and Ritonavir-Boosted Atazanavir Using PBPK Modelling.Clinical pharmacokinetics · 2022Article
- Candidate Proficiency Test Chemicals to Address Industrial Chemical Applicability Domains forFrontiers in toxicology · 2022Review
- Prediction of potential drug interactions between repurposed COVID-19 and antitubercular drugs: an integrational approach of drug information software and computational techniques data.Therapeutic advances in drug safety · 2021Article
- Clofazimine pharmacokinetics in patients with TB: dosing implications.The Journal of antimicrobial chemotherapy · 2020Article
- Safety implications of combined antiretroviral and anti-tuberculosis drugs.Expert opinion on drug safety · 2020Review
- Validation of in vitro methods for human cytochrome P450 enzyme induction: Outcome of a multi-laboratory study.Toxicology in vitro : an international journal published in association with BIBRA · 2019Article
- Dually Acting Nonclassical 1,4-Dihydropyridines Promote the Anti-Tuberculosis (Tb) Activities of Clofazimine.Molecules (Basel, Switzerland) · 2019Article
- Effect of rifampin with bio-enhancer in the treatment of newly diagnosed sputum positive pulmonary tuberculosis patients: A double-center study.Journal of clinical tuberculosis and other mycobacterial diseases · 2018Article
- Impact of Clofazimine Dosing on Treatment Shortening of the First-Line Regimen in a Mouse Model of Tuberculosis.Antimicrobial agents and chemotherapy · 2018Article
Corrections and comments
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Authors and funding
2 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Predicting drug-drug interactions (DDIs) related to cytochrome P450 (CYP), such as CYP3A4 and one of the major drug transporters, P-glycoprotein (P-gp), is crucial in the development of future chemotherapeutic regimens to treat tuberculosis (TB) and TB/AIDS coinfection cases. We evaluated the effects of 30 anti-TB drugs, novel candidates, macrolides, and representative antiretroviral drugs on human CYP3A4 activity using a commercially available screening kit for CYP3A4 inhibitors and a human hepatocyte, HepaRG. Moreover, in order to estimate the interactions of these drugs with human P-gp, screening for substrates was performed. For some substrates, P-gp inhibition tests were carried out using P-gp-expressing MDCK cells. As a result, almost all the compounds showed the expected effects on human CYP3A4 both in the in vitro screening and in HepaRG cells. Importantly, the unproven mechanisms of DDIs caused by WHO group 5 drugs, thioamides, and p-aminosalicylic acid were elucidated. Intriguingly, clofazimine (CFZ) exhibited weak inductive effects on CYP3A4 at >0.25 μM in HepaRG cells, while an inhibitory effect was observed at 1.69 μM in the in vitro screening, suggesting that CFZ autoinduces CYP3A4 in the human liver. Our method, based on one of the pharmacokinetics parameters in humans, provides more practical information associated with not only DDIs but also with drug metabolism.
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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.