ArticleClinical and translational science2022
Effect of enzalutamide on PK of P-gp and BCRP substrates in cancer patients: CYP450 induction may not always predict overall effect on transporters.
Article in Clinical and translational science, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. It is linked to trial NCT04094519 (A Phase 1 Open-label Study to Evaluate the Effect of Multiple Doses of Enzalutamide on the Pharmacokinetics of Substrates of P-glycoprotein), which is not on this map. Cited by 11 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.
A Phase 1 Open-label Study to Evaluate the Effect of Multiple Doses of Enzalutamide on the Pharmacokinetics of Substrates of P-glycoprotein (Digoxin) and Breast Cancer Resistant Protein (Rosuvastatin) in Male Subjects With Prostate Cancer
Who cites it
11 citing papers in PubMed, 15 citations in OpenAlex.
- Population Pharmacokinetics Analysis of Talazoparib and Enzalutamide Combination Therapy for Patients With Metastatic Castration-Resistant Prostate Cancer.Journal of clinical pharmacology · 2026Trial
- Nutraceuticals in Uro-Oncology: A Structured Expert Review and Precision-Oriented Framework.Nutrients · 2026Review
- [Androgen receptor-targeted therapies - avoid clinically relevant interactions].Aktuelle Urologie · 2026Review
- Effect of Enzalutamide on Morphine Exposure in Patients with Prostate Cancer.Clinical pharmacokinetics · 2026Article
- Effect of enzalutamide on anticoagulant therapy with edoxaban in patients with prostate cancer.British journal of clinical pharmacology · 2026Article
- Managing Drug Interactions with Enzalutamide in Patients with Prostate Cancer: A Podcast.Drug safety · 2026Article
- Cardiac glycosides: Looking beyond heart failure and atrial fibrillation.Indian journal of pharmacology · 2025Article
- Pharmacokinetic Interactions Between Abiraterone, Apalutamide, Darolutamide or Enzalutamide and Antithrombotic Drugs: Prediction of Clinical Events and Review of Pharmacological Information.Cardiovascular drugs and therapy · 2024Review
- Enzalutamide: Understanding and Managing Drug Interactions to Improve Patient Safety and Drug Efficacy.Drug safety · 2024Review
- Physiologically-based pharmacokinetic modeling to predict drug-drug interaction of enzalutamide with combined P-gp and CYP3A substrates.Journal of pharmacokinetics and pharmacodynamics · 2023Article
- Effect of enzalutamide on PK of P-gp and BCRP substrates in cancer patients: CYP450 induction may not always predict overall effect on transporters.Clinical and translational science · 2022Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
9 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Drug-drug interaction (DDI) is an important consideration for clinical decision making in prostate cancer treatment. The objective of this study was to evaluate the effect of enzalutamide, an oral androgen receptor inhibitor, on the pharmacokinetics (PK) of digoxin (P-glycoprotein [P-gp] probe substrate) and rosuvastatin (breast cancer resistance protein [BCRP] probe substrate) in men with metastatic castration-resistant prostate cancer (mCRPC). This was a phase I, open-label, fixed-sequence, crossover study (NCT04094519). Eligible men with mCRPC received a single dose of transporter probe cocktail containing 0.25 mg digoxin and 10 mg rosuvastatin plus enzalutamide placebo-to-match on day 1. On day 8, patients started 160 mg enzalutamide once daily through day 71. On day 64, patients also received a single dose of the cocktail. The primary end points were digoxin and rosuvastatin plasma maximum concentration (C
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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.