Trial reportDrug design, development and therapy2019
Single- and multiple-dose tolerability, safety, pharmacokinetics, and pharmacodynamics of the dual endothelin receptor antagonist aprocitentan in healthy adult and elderly subjects.
Trial report in Drug design, development and therapy, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 24 papers, 1 of them a synthesis that pooled it.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
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
24 citing papers in PubMed, 1 synthesis or guideline pooled it, 43 citations in OpenAlex.
- Efficacy and Safety of Aprocitentan in the Treatment of Hypertension: A Meta-Analysis of Evidence from Randomized Controlled Trials.Reviews in cardiovascular medicine · 2025Pooled it
- Effects of aprocitentan on prognostically relevant ambulatory blood pressure-derived variables in resistant hypertension.Journal of hypertension · 2026Trial
- Effects of the Dual Endothelin Receptor Antagonist Aprocitentan on Body Weight and Fluid Homeostasis in Healthy Subjects on a High Sodium Diet.Clinical pharmacology and therapeutics · 2021Trial
- Randomized Dose-Response Study of the New Dual Endothelin Receptor Antagonist Aprocitentan in Hypertension.Hypertension (Dallas, Tex. : 1979) · 2020Trial
- Resistant hypertension: Epidemiology, mechanisms and contemporary therapeutic strategies.Heart international · 2026Review
- Aprocitentan: An oral, once-daily antihypertensive therapy for resistant hypertension in adult patients.Heart international · 2026Review
- Research trends and performance of endothelin A receptor antagonist in kidney care: a bibliometric analysis.Renal failure · 2025Article
- Current Knowledge About Aprocitentan in Hypertension.International journal of molecular sciences · 2025Review
- Chinese Guidelines for the Prevention and Treatment of Hypertension (2024 revision).Journal of geriatric cardiology : JGC · 2025Article
- Structure-Property Relationships Reported for the New Drugs Approved in 2024.Mini reviews in medicinal chemistry · 2025Review
- Arterial Hypertension: Novel Pharmacological Targets and Future Perspectives.Journal of clinical medicine · 2024Review
- Aprocitentan: First Approval.Drugs · 2024Review
- Current and future strategies for targeting the endothelin pathway in cardiovascular disease.Nature cardiovascular research · 2023Review
- 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
- Endothelin receptor antagonists in kidney protection for diabetic kidney disease and beyond?Nephrology (Carlton, Vic.) · 2023Review
- Single-dose pharmacokinetics, safety, and tolerability of the dual endothelin receptor antagonist aprocitentan in subjects with moderate hepatic impairment.Scientific reports · 2022Article
- Aprocitentan: New insights.Frontiers in cardiovascular medicine · 2022Article
- A Population Pharmacokinetic Model of Macitentan and Its Active Metabolite Aprocitentan in Healthy Volunteers and Patients with Pulmonary Arterial Hypertension.Clinical pharmacokinetics · 2021Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
4 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
backgroundAprocitentan is an orally active, dual endothelin (ET) receptor antagonist developed for the treatment of hypertension in which, despite available treatments, a medical need exists for drugs with a new mechanism of action. SUBJECTS AND
methodsIn this study, the single- and multiple-dose tolerability, safety, pharmacokinetics (PK), and pharmacodynamics of up to 600 mg (single doses) and 100 mg once a day (qd; multiple doses) of aprocitentan were investigated in healthy male and female subjects. The effect of age on the tolerability and PK parameters was investigated at a dose of 100 mg qd.
resultsAprocitentan was well tolerated across all doses. No serious adverse events (AEs) occurred. The most frequently reported AE was headache. Small increases in body weight were recorded in subjects receiving 100 mg qd. Plasma concentration-time profiles of aprocitentan were similar after single- and multiple-dose administration, and support a qd dosing regimen based on a half-life of 44 hours. After multiple doses, PK was dose proportional. Accumulation at steady state, reached by Day 8, was 3-fold. Only minor differences in exposure between healthy females and males, healthy elderly and adult subjects, and fed and fasted conditions were observed. Plasma ET-1 concentrations, reflecting ET
conclusionAprocitentan was well tolerated in healthy subjects with a PK profile favorable for qd dosing.
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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.