ArticleClinical pharmacokinetics2017
Target-Mediated Drug Disposition Pharmacokinetic-Pharmacodynamic Model of Bosentan and Endothelin-1.
Article in Clinical pharmacokinetics, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the 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.
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Who cites it
7 citing papers in PubMed, 14 citations in OpenAlex.
- Optimization of Dosing Regimens for Plasminogen Activation Inhibitor BT-114143 Using a Small Molecule TMDD Population PK and PD Model in Healthy Subjects.European journal of drug metabolism and pharmacokinetics · 2026Article
- Exact Formula of the Total Quasi-Steady State Approximation in Competitive Target-Mediated Drug Disposition.Computational and structural biotechnology journal · 2026Article
- The Possible effect of Bosentan on the methotrexate-induced salivary gland changes in male rats: histological and Immunohistochemical study.Toxicology research · 2025Article
- Modelling hemodynamics regulation in rats and dogs to facilitate drugs safety risk assessment.Frontiers in pharmacology · 2024Article
- Incorporating Pharmacological Target-Mediated Drug Disposition (TMDD) in a Whole-Body Physiologically Based Pharmacokinetic (PBPK) Model of Linagliptin in Rat and Scale-up to Human.The AAPS journal · 2020Article
- Predicting Clinical Effects of CYP3A4 Modulators on Abemaciclib and Active Metabolites Exposure Using Physiologically Based Pharmacokinetic Modeling.Journal of clinical pharmacology · 2020Article
- Target-Mediated Population Pharmacokinetic Modeling of Endothelin Receptor Antagonists.Pharmaceutical research · 2019Article
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 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
BACKGROUND AND
objectivesBosentan is a competitive antagonist on endothelin receptor A and B (ET
methodsPK/PD data from 70 young male Caucasian subjects were analyzed after single i.v. administration of 10, 50, 250, 500, and 750 mg of bosentan. Population analyses, simulations, and evaluation were performed using a non-linear mixed-effects modeling approach.
resultsThe PK of bosentan was best described by a two-compartment, target-mediated drug disposition (TMDD) model. ET-1 plasma and urine profiles were successfully integrated into the bosentan two-compartment, TMDD model encompassing competition for the same receptor. A multiple-peak phenomenon of bosentan plasma concentrations after i.v. administration was best described by a diurnal expression or reappearance of ET receptors on the cell surface. Blood pressure was best described by an E
conclusionThe developed competitive PK/PD model of bosentan and ET-1 after i.v. administration provides a first step towards understanding the complex PK properties of bosentan and offers a valuable tool for future PK/PD research.
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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.