ArticleClinical pharmacology in drug development2022
Effects of CYP3A Inhibition, CYP3A Induction, and Gastric Acid Reduction on the Pharmacokinetics of Ripretinib, a Switch Control KIT Tyrosine Kinase Inhibitor.
Article in Clinical pharmacology in drug development, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. It is linked to trial NCT06431451 (The Correlation Between Ripretinib Exposure and the Efficacy and Safety in Patients with Advanced Gastrointestinal Stromal Tumors), which is not on this map. Cited by 7 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.
The Correlation Between Ripretinib Exposure and the Efficacy and Safety in Patients with Advanced Gastrointestinal Stromal Tumors: an Observational Study
Who cites it
7 citing papers in PubMed, 10 citations in OpenAlex.
- Review
- Pharmacokinetics and Safety of Ripretinib in Participants with Hepatic Impairment: A Phase 1 Study.Advances in therapy · 2025Article
- Pharmacodynamics, pharmacokinetics, interactions with other drugs, toxicity and clinical effectiveness of proton pump inhibitors.Frontiers in pharmacology · 2025Review
- Negative outcomes associated with tyrosine kinase inhibitors during management of gastrointestinal stromal tumors: examination of data from the FDA adverse event reporting system.Frontiers in oncology · 2025Article
- Liquid chromatography-tandem mass spectrometry for the quantification of ripretinib and its metabolites DP-5439 in human plasma.Frontiers in pharmacology · 2024Article
- Effect of Verapamil, a P-glycoprotein-1 and Cytochrome P450 3A4 Inhibitor, on Pharmacokinetics and Metabolic Stability of Ripretinib: A Drug-Drug Interaction Study in Rats.European journal of drug metabolism and pharmacokinetics · 2023Article
- Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
5 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Ripretinib is a switch control KIT kinase inhibitor approved for treatment of adults with advanced gastrointestinal stromal tumors who received prior treatment with 3 or more kinase inhibitors, including imatinib. Ripretinib and its active metabolite (DP-5439) are cleared mainly via cytochrome P450 enzyme 3A4/5 (CYP3A4/5), and ripretinib solubility is pH-dependent, thus the drug-drug interaction potentials of ripretinib with itraconazole (strong CYP3A inhibitor), rifampin (strong CYP3A inducer), and pantoprazole (proton pump inhibitor) were each evaluated in open-label, fixed-sequence study designs. Overall, 20 participants received ripretinib 50 mg alone and with itraconazole 200 mg once daily, 24 participants received ripretinib 100 mg alone and with rifampin 600 mg once daily, and 25 participants received ripretinib 50 mg alone and with pantoprazole 40 mg once daily. Ripretinib exposure increased with concomitant itraconazole, with geometric least-squares (LS) mean ratios of ripretinib area under the concentration-time curve from 0 to ∞ (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.