Trial reportClinical pharmacology in drug development2020
Effects of Strong CYP2C8 or CYP3A Inhibition and CYP3A Induction on the Pharmacokinetics of Brigatinib, an Oral Anaplastic Lymphoma Kinase Inhibitor, in Healthy Volunteers.
Trial report in Clinical pharmacology in drug development, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 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.
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Who cites it
18 citing papers in PubMed, 27 citations in OpenAlex.
- A Phase 1 Study to Assess the Relative Bioavailability of Brigatinib Administered as an Oral Solution Versus an Immediate-Release Tablet in Healthy Adults.Clinical pharmacology in drug development · 2026Trial
- Brigatinib Dose Rationale in Anaplastic Lymphoma Kinase-Positive Non-Small Cell Lung Cancer: Exposure-Response Analyses of Pivotal ALTA Study.CPT: pharmacometrics & systems pharmacology · 2020Trial
- Physiologically Based Pharmacokinetic Model of Brigatinib in Healthy Volunteers and Patients With Cancer.CPT: pharmacometrics & systems pharmacology · 2026Article
- Physiologically based pharmacokinetic model of two ALK inhibitors to inform drug and dosing regimens for brain metastasis patients.Frontiers in pharmacology · 2026Article
- Clinical Assessment of the Drug-Drug Interaction Potential of Omaveloxolone in Healthy Adult Participants.Journal of clinical pharmacology · 2025Article
- Tyrosine-kinase inhibitors for lung or breast cancer and drug-drug interactions: a clinical guide.Oncology reviews · 2025Review
- Cyp3a4-Mediated in vitro Metabolism and in vivo Disposition of Lorlatinib in Rats.Drug design, development and therapy · 2025Article
- Evaluation of the drug-drug interaction potential of brigatinib using a physiologically-based pharmacokinetic modeling approach.CPT: pharmacometrics & systems pharmacology · 2024Article
- Clinical Pharmacology of Brigatinib: A Next-Generation Anaplastic Lymphoma Kinase Inhibitor.Clinical pharmacokinetics · 2023Review
- Brigatinib pharmacokinetics in patients with chronic hepatic impairment.Investigational new drugs · 2023Article
- Involvement of Transporters in Intestinal Drug-Drug Interactions of Oral Targeted Anticancer Drugs Assessed by Changes in Drug Absorption Time.Pharmaceutics · 2022Article
- Current Insights on the Treatment of Anaplastic Lymphoma Kinase-Positive Metastatic Non-Small Cell Lung Cancer: Focus on Brigatinib.Clinical pharmacology : advances and applications · 2022Review
- Effect of severe renal impairment on the pharmacokinetics of brigatinib.Investigational new drugs · 2021Article
- Model-Based Comparative Analysis of Rifampicin and Rifabutin Drug-Drug Interaction Profile.Antimicrobial agents and chemotherapy · 2021Article
- Potential Drug Interactions of Repurposed COVID-19 Drugs with Lung Cancer Pharmacotherapies.Archives of medical research · 2021Review
- Head to head evaluation of second generation ALK inhibitors brigatinib and alectinib as first-line treatment for ALK+ NSCLC using anOncotarget · 2021Article
- Population Pharmacokinetics of Brigatinib in Healthy Volunteers and Patients With Cancer.Clinical pharmacokinetics · 2021Article
- Pharmacokinetic-Based Drug-Drug Interactions with Anaplastic Lymphoma Kinase Inhibitors: A Review.Drug design, development and therapy · 2020Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
8 authors at 4 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
In vitro data support involvement of cytochrome P450 (CYP)2C8 and CYP3A4 in the metabolism of the anaplastic lymphoma kinase inhibitor brigatinib. A 3-arm, open-label, randomized, single-dose, fixed-sequence crossover study was conducted to characterize the effects of the strong inhibitors gemfibrozil (of CYP2C8) and itraconazole (of CYP3A) and the strong inducer rifampin (of CYP3A) on the single-dose pharmacokinetics of brigatinib. Healthy subjects (n = 20 per arm) were administered a single dose of brigatinib (90 mg, arms 1 and 2; 180 mg, arm 3) alone in treatment period 1 and coadministered with multiple doses of gemfibrozil 600 mg twice daily (BID; arm 1), itraconazole 200 mg BID (arm 2), or rifampin 600 mg daily (QD; arm 3) in period 2. Compared with brigatinib alone, coadministration of gemfibrozil with brigatinib did not meaningfully affect brigatinib area under the plasma concentration-time curve (AUC
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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.