ArticleEuropean journal of drug metabolism and pharmacokinetics2020
Effect of Multiple-Dose Aprocitentan Administration on the Pharmacokinetics of Midazolam in Healthy Male Subjects.
Article in European journal of drug metabolism and pharmacokinetics, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers, 1 of them a synthesis that pooled it.
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.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
9 citing papers in PubMed, 1 synthesis or guideline pooled it, 20 citations in OpenAlex.
- Collecting Metabolite Pharmacokinetics in Drug-Drug Interaction Studies: A Review of Industry Practices and Data Utilization.Clinical pharmacokinetics · 2026Pooled it
- Arterial Hypertension: Novel Pharmacological Targets and Future Perspectives.Journal of clinical medicine · 2024Review
- Aprocitentan: First Approval.Drugs · 2024Review
- Population pharmacokinetics of the dual endothelin receptor antagonist aprocitentan in subjects with or without essential or resistant hypertension.Journal of pharmacokinetics and pharmacodynamics · 2024Article
- Aprocitentan: A new development of resistant hypertension.Journal of clinical hypertension (Greenwich, Conn.) · 2023Review
- Novel Dual Endothelin Inhibitors in the Management of Resistant Hypertension.Life (Basel, Switzerland) · 2023Review
- Endothelin Receptor Antagonists in Kidney Disease.International journal of molecular sciences · 2023Review
- Single-dose pharmacokinetics, safety, and tolerability of the dual endothelin receptor antagonist aprocitentan in subjects with moderate hepatic impairment.Scientific reports · 2022Article
- Aprocitentan, A Dual Endothelin Receptor Antagonist Under Development for the Treatment of Resistant Hypertension.Cardiology and therapy · 2021Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
2 authors at 1 institution in 1 country.
Funding
Abstract
backgroundAprocitentan is an orally active dual endothelin receptor antagonist that targets a novel pathway in the treatment of difficult-to-control (resistant) hypertension. The drug-drug interaction potential of aprocitentan on cytochrome P450 (CYP) 3A enzymes was investigated in this open-label, two-treatment single-sequence study.
objectivesThe primary and main secondary objectives were to study the pharmacokinetics of midazolam in the absence and presence of aprocitentan and the safety and tolerability of combined administration, respectively.
methodsNineteen healthy male subjects received a single dose of 8 mg midazolam. Thereafter, they started aprocitentan treatment (loading dose of 150 mg followed by 50 mg once daily) and received another single dose of midazolam with aprocitentan at steady state. Pharmacokinetics and tolerability of midazolam and its metabolite 1-hydroxy midazolam were assessed over 24 h after each midazolam administration.
resultsAt steady state, aprocitentan did not affect the area under the plasma concentration-time curve and maximum plasma concentration (C
conclusionAprocitentan does not alter the pharmacokinetics of midazolam to a clinically relevant extent and was well tolerated when administered concomitantly. Therefore, aprocitentan can be administered together with drugs that are substrates of CYP3A without dose adjustments.
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Registered trials
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