ArticlePharmacology research & perspectives2015
Effect of CYP3A perpetrators on ibrutinib exposure in healthy participants.
Article in Pharmacology research & perspectives, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 46 papers.
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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
46 citing papers in PubMed, 98 citations in OpenAlex.
- Trial
- Treatment of relapsed/refractory chronic lymphocytic leukemia/small lymphocytic lymphoma with the BTK inhibitor zanubrutinib: phase 2, single-arm, multicenter study.Journal of hematology & oncology · 2020Trial
- Itraconazole Increases Ibrutinib Exposure 10-Fold and Reduces Interindividual Variation-A Potentially Beneficial Drug-Drug Interaction.Clinical and translational science · 2020Trial
- Stable isotope-labelled intravenous microdose for absolute bioavailability and effect of grapefruit juice on ibrutinib in healthy adults.British journal of clinical pharmacology · 2016Trial
- Food Effects, Pharmacokinetic Drug-Drug Interactions, and Clinical Optimization of Oral Anticancer Agents.Pharmaceutics · 2026Review
- Fitness in CLL.Cancers · 2026Review
- Comparative Analysis of Isavuconazole DDIs With Other Azole Antifungal Drugs and PBPK Model-Informed Dosing Recommendations for Anticancer Drugs.CPT: pharmacometrics & systems pharmacology · 2025Article
- Outcomes following exposure to drug interactions with ibrutinib in patients with chronic lymphocytic leukaemia.British journal of haematology · 2025Article
- Pharmacogenetic Biomarkers of Ibrutinib Response and Toxicity in Chronic Lymphocytic Leukemia: Insights from an Observational Study.Pharmaceuticals (Basel, Switzerland) · 2025Article
- Building Confidence in Physiologically Based Pharmacokinetic Modeling of CYP3A Induction Mediated by Rifampin: An Industry Perspective.Clinical pharmacology and therapeutics · 2025Review
- High-performance PBPK model for predicting CYP3A4 induction-mediated drug interactions: a refined and validated approach.Frontiers in pharmacology · 2025Article
- Clinical Trial Data-Driven Risk Assessment of Drug-Drug Interactions: A Rapid and Accurate Decision-Making Tool.Clinical pharmacokinetics · 2024Article
- Managing novel therapies and concomitant medications in chronic lymphocytic leukemia: key challenges.Frontiers in pharmacology · 2024Review
- Epidemiology, clinical characteristics and potential mechanism of ibrutinib-induced ventricular arrhythmias.Frontiers in pharmacology · 2024Review
- Recommendations on the use of azole antifungals in hematology-oncology patients.Revista espanola de quimioterapia : publicacion oficial de la Sociedad Espanola de Quimioterapia · 2023Review
- Managing Ibrutinib-Intolerant Patients With B-Cell Malignancies.The oncologist · 2023Review
- Can Mechanistic Static Models for Drug-Drug Interactions Support Regulatory Filing for Study Waivers and Label Recommendations?Clinical pharmacokinetics · 2023Review
- Simultaneous Determination of Orelabrutinib, Zanubrutinib, Ibrutinib and Its Active Metabolite in Human Plasma Using LC-MS/MS.Molecules (Basel, Switzerland) · 2023Article
- Determining drug dose in the era of targeted therapies: playing it (un)safe?Blood cancer journal · 2022Review
- Boosting the oral bioavailability of anticancer drugs through intentional drug-drug interactions.Basic & clinical pharmacology & toxicology · 2022Review
Corrections and comments
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Authors and funding
10 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Ibrutinib (PCI-32765), a potent covalent inhibitor of Bruton's tyrosine kinase, has shown efficacy against a variety of B-cell malignancies. Given the prominent role of CYP3A in ibrutinib metabolism, effect of coadministration of CYP3A perpetrators with ibrutinib was evaluated in healthy adults. Ibrutinib (120 mg [Study 1, fasted], 560 mg [studies 2 (fasted), and 3 (nonfasted)]) was given alone and with ketoconazole [Study 1; 400 mg q.d.], rifampin [Study 2; 600 mg q.d.], and grapefruit juice [GFJ, Study 3]. Lower doses of ibrutinib were used together with CYP3A inhibitors [Study 1: 40 mg; Study 3: 140 mg], as safety precaution. Under fasted condition, ketoconazole increased ibrutinib dose-normalized (DN) exposure [DN-AUClast: 24-fold; DN-C max: 29-fold], rifampin decreased ibrutinib exposure [C max: 13-fold; AUClast: 10-fold]. Under nonfasted condition, GFJ caused a moderate increase [DN-C max: 3.5-fold; DN-AUC: 2.2-fold], most likely through inhibition of intestinal CYP3A. Half-life was not affected by CYP perpetrators indicating the interaction was mainly on first-pass extraction. All treatments were well-tolerated.
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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.