ArticleBritish journal of clinical pharmacology2021
Evaluation of drug interaction potential of zanubrutinib with cocktail probes representative of CYP3A4, CYP2C9, CYP2C19, P-gp and BCRP.
Article in British journal of clinical pharmacology, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed, 21 citations in OpenAlex.
- Relative Bioavailability, Food Effect, and Bioequivalence Studies to Assess a New Zanubrutinib 160-mg Tablet: Results From 2 Phase 1 Studies in Healthy Volunteers.Clinical pharmacology in drug development · 2026Trial
- Effect of Rivoceranib 200 mg Once Daily on the Pharmacokinetics of a Cocktail Probe Substrate of Cytochrome P450 Enzymes: A Phase I Trial in Healthy Volunteers.Clinical pharmacokinetics · 2026Article
- Zanubrutinib in B-cell lymphomas: from clinical pharmacology to therapeutic application.European journal of clinical pharmacology · 2026Review
- Managing novel therapies and concomitant medications in chronic lymphocytic leukemia: key challenges.Frontiers in pharmacology · 2024Review
- Zanubrutinib: past, present, and future.Blood cancer journal · 2023Review
- Advancements in the Treatment of CLL: The Rise of Zanubrutinib as a Preferred Therapeutic Option.Cancers · 2023Review
- Coming of Age for BTK Inhibitor Therapy: A Review of Zanubrutinib in Waldenström Macroglobulinemia.Cells · 2022Review
- Use of modeling and simulation to predict the influence of triazole antifungal agents on the pharmacokinetics of zanubrutinib and acalabrutinib.Frontiers in pharmacology · 2022Article
- In vitro investigations into the roles of CYP450 enzymes and drug transporters in the drug interactions of zanubrutinib, a covalent Bruton's tyrosine kinase inhibitor.Pharmacology research & perspectives · 2021Article
- BTK Inhibitors in Chronic Lymphocytic Leukemia.Current hematologic malignancy reports · 2021Review
- Evaluation of drug interaction potential of zanubrutinib with cocktail probes representative of CYP3A4, CYP2C9, CYP2C19, P-gp and BCRP.British journal of clinical pharmacology · 2021Article
- Vascular Impact of Cancer Therapies: The Case of BTK (Bruton Tyrosine Kinase) Inhibitors.Circulation research · 2021Review
- Comprehensive PBPK model to predict drug interaction potential of Zanubrutinib as a victim or perpetrator.CPT: pharmacometrics & systems pharmacology · 2021Article
Corrections and comments
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Authors and funding
7 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
aimThis study aims to assess the potential effects of zanubrutinib on the activity of cytochrome P450 (CYP) enzymes and drug transporter proteins using a cocktail probe approach.
methodsPatients received single oral doses of probe drugs alone and after at least 8 days of treatment with zanubrutinib 160 mg twice daily in a single-sequence study in 18 healthy male volunteers. Simultaneous doses of 10 mg warfarin (CYP2C9) and 2 mg midazolam (CYP3A) were administered on Day 1 and Day 14, 0.25 mg digoxin (P-glycoprotein [P-gp]) and 10 mg rosuvastatin (breast cancer resistance protein [BCRP]) on Day 3 and Day 16, and 20 mg omeprazole (CYP2C19) on Day 5 and Day 18. Pharmacokinetic (PK) parameters were estimated from samples obtained up to 12 h post dose for zanubrutinib; 24 h for digoxin, omeprazole and midazolam; 48 h for rosuvastatin; and 144 h for warfarin.
resultsThe ratios (%) of geometric least squares means (90% confidence intervals) for the area under the concentration-time curve from time zero to the last quantifiable concentration in the presence/absence of zanubrutinib were 99.80% (97.41-102.2%) for S-warfarin; 52.52% (48.49-56.88%) for midazolam; 111.3% (103.8-119.3%) for digoxin; 89.45% (78.73-101.6%) for rosuvastatin; and 63.52% (57.40-70.30%) for omeprazole. Similar effects were observed for maximum plasma concentrations.
conclusionsZanubrutinib 320 mg total daily dose had minimal or no effect on the activity of CYP2C9, BCRP and P-gp, but decreased the systemic exposure of CYP3A and CYP2C19 substrates (mean reduction <50%).
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