ArticleDrug metabolism and disposition: the biological fate of chemicals2011
CYP3A-mediated generation of aldehyde and hydrazine in atazanavir metabolism.
Article in Drug metabolism and disposition: the biological fate of chemicals, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed, 26 citations in OpenAlex.
- Rosiglitazone hepatotoxicity resulting from hepatic protein covalent binding derived from its aldehyde metabolite.Archives of toxicology · 2026Article
- Gut microbiota crosstalk mechanisms are key in pulmonary hypertension: The involvement of melatonin is instrumental too.Pulmonary circulation · 2023Review
- Metabolism of a Selective Serotonin and Norepinephrine Reuptake Inhibitor Duloxetine in Liver Microsomes and Mice.Drug metabolism and disposition: the biological fate of chemicals · 2022Article
- PharmGKB summary: atazanavir pathway, pharmacokinetics/pharmacodynamics.Pharmacogenetics and genomics · 2018Article
- Antiretroviral Drug Metabolism in Humanized PXR-CAR-CYP3A-NOG Mice.The Journal of pharmacology and experimental therapeutics · 2018Article
- A novel humanized mouse lacking murine P450 oxidoreductase for studying human drug metabolism.Nature communications · 2017Article
- A High Dose of Isoniazid Disturbs Endobiotic Homeostasis in Mouse Liver.Drug metabolism and disposition: the biological fate of chemicals · 2016Article
- Biotransformation of Cobicistat: Metabolic Pathways and Enzymes.Drug metabolism letters · 2016Article
- Meconium Atazanavir Concentrations and Early Language Outcomes in HIV-Exposed Uninfected Infants With Prenatal Atazanavir Exposure.Journal of acquired immune deficiency syndromes (1999) · 2015Article
- Metabolomics of bronchoalveolar lavage differentiate healthy HIV-1-infected subjects from controls.AIDS research and human retroviruses · 2014Article
- Bedaquiline metabolism: enzymes and novel metabolites.Drug metabolism and disposition: the biological fate of chemicals · 2014Article
- CPY3A4-mediated α-hydroxyaldehyde formation in saquinavir metabolism.Drug metabolism and disposition: the biological fate of chemicals · 2014Article
- Metabolomic screening and identification of the bioactivation pathways of ritonavir.Chemical research in toxicology · 2011Article
- Profiling the reactive metabolites of xenobiotics using metabolomic technologies.Chemical research in toxicology · 2011Article
Corrections and comments
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Authors and funding
4 authors at 2 institutions in 1 country.
Funding
Abstract
Atazanavir (ATV) is an antiretroviral drug of the protease inhibitor class. Multiple adverse effects of ATV have been reported in clinical practice, such as jaundice, nausea, abdominal pain, and headache. The exact mechanisms of ATV-related adverse effects are unknown. It is generally accepted that a predominant pathway of drug-induced toxicity is through the generation of reactive metabolites. Our current study was designed to explore reactive metabolites of ATV. We used a metabolomic approach to profile ATV metabolism in mice and human liver microsomes. We identified 5 known and 13 novel ATV metabolites. Three potential reactive metabolites were detected and characterized for the first time: one aromatic aldehyde, one α-hydroxyaldehyde, and one hydrazine. These potential reactive metabolites were primarily generated by CYP3A. Our results provide a clue for studies on ATV-related adverse effects from the aspect of metabolic activation. Further studies are suggested to illustrate the impact of these potential reactive metabolites on ATV-related adverse effects.
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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.