ArticleDrug metabolism and disposition: the biological fate of chemicals2010
Comparison of the drug-drug interactions potential of erlotinib and gefitinib via inhibition of UDP-glucuronosyltransferases.
Article in Drug metabolism and disposition: the biological fate of chemicals, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 37 papers, 2 of them syntheses that pooled it.
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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.
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Who cites it
37 citing papers in PubMed, 2 syntheses or guidelines pooled it, 109 citations in OpenAlex.
- Hepatotoxicity and efficacy associated with first- and new-generation EGFR-TKIs in patients with NSCLC: a systematic review and meta-analysis.BMC cancer · 2025Pooled it
- Comparison of Hepatotoxicity Associated With New BCR-ABL Tyrosine Kinase Inhibitors vs Imatinib Among Patients With Chronic Myeloid Leukemia: A Systematic Review and Meta-analysis.JAMA network open · 2021Pooled it
- Clinical Implications ofPharmaceutics · 2026Review
- Sesamin exhibits potential food-drug interactions through the inhibition of cytochrome P450s and human UDP-glucuronosyltransferasesRSC advances · 2026Article
- Mechanism-based inactivation of human aldehyde oxidase by erlotinib: Mechanistic insights from structural analogs and molecular docking.Molecular pharmacology · 2026Article
- Influence of genetic polymorphisms on gefitinib pharmacokinetics and adverse drug reactions in non-small cell lung cancer patients.Cancer metastasis reviews · 2025Review
- Predicting in vivo cannabinoid-drug interactions mediated via inhibition of UDP-glucuronosyltransferases using in vitro studies and physiologically based pharmacokinetic modeling and simulations.Drug metabolism and disposition: the biological fate of chemicals · 2025Article
- Evaluation of Luteolin Nanosuspensions on Pharmacokinetics of Atorvastatin: Drug-Drug Interactions Using Rat Models.International journal of nanomedicine · 2025Article
- Kinase Inhibitors FDA Approved 2018-2023: Drug Targets, Metabolic Pathways, and Drug-Induced Toxicities.Drug metabolism and disposition: the biological fate of chemicals · 2024Review
- Avapritinib Carries the Risk of Drug InteractionCurrent drug metabolism · 2024Article
- Prediction of Drug-Drug Interaction Between Dabrafenib and Irinotecan via UGT1A1-Mediated Glucuronidation.European journal of drug metabolism and pharmacokinetics · 2022Article
- Cabozantinib Carries the Risk of Drug-Drug InteractionsCurrent drug metabolism · 2022Article
- Review
- Drug-drug interaction of atazanavir on UGT1A1-mediated glucuronidation of molidustat in human.Basic & clinical pharmacology & toxicology · 2021Article
- Emerging roles for UDP-glucuronosyltransferases in drug resistance and cancer progression.British journal of cancer · 2020Review
- The pharmacokinetic interaction between irinotecan and sunitinib.Cancer chemotherapy and pharmacology · 2020Article
- The analysis of pharmacokinetic and pharmacogenomic impact on gefitinib efficacy in advanced non-small cell lung cancer patients: results from a prospective cohort study.Annals of translational medicine · 2019Article
- Recent progress and challenges in screening and characterization of UGT1A1 inhibitors.Acta pharmaceutica Sinica. B · 2019Review
- Comparative review of drug-drug interactions with epidermal growth factor receptor tyrosine kinase inhibitors for the treatment of non-small-cell lung cancer.OncoTargets and therapy · 2019Review
- Pharmacokinetics and disposition of anlotinib, an oral tyrosine kinase inhibitor, in experimental animal species.Acta pharmacologica Sinica · 2018Article
Corrections and comments
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
Abstract
We aimed to investigate and compare the effects of erlotinib and gefitinib on UDP-glucuronosyltransferase (UGT) activities and to quantitatively evaluate their drug-drug interaction (DDI) potential due to UGT inhibition. The inhibitory effects of erlotinib and gefitinib on UGTs were determined using high-performance liquid chromatography by measuring the formation rates for 4-methylumbelliferone (4-MU) glucuronide, imipramine N-glucuronide, and bilirubin glucuronides using recombinant human UGT isoforms and human liver microsomes (HLMs) in the absence or presence of erlotinib and gefitinib. Inhibition kinetic studies were conducted. Area under the curve (AUC) ratios were used to predict the risk of potential DDI in vivo. Erlotinib exhibited selective potent competitive inhibition against 4-MU glucuronidation by UGT1A1, and gefitinib demonstrated a wide range of inhibition against UGT-mediated 4-MU glucuronidation, particularly against UGT1A1, UGT1A7, UGT1A9, and UGT2B7. Erlotinib also exerted potent mixed inhibition against bilirubin glucuronidation in HLMs. We estimated that coadministration of erlotinib at 100 mg/day or higher doses may result in at least a 30% increase in the AUC of drugs predominantly cleared by UGT1A1. Thus, the coadministration of erlotinib with drugs primarily cleared by UGT1A1 may result in potential DDI. In contrast, gefitinib is unlikely to cause a clinically significant DDI through inhibition of glucuronidation.
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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.