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Mass Balance Recovery, Absorption, Metabolism, and Excretion of Elinzanetant in Healthy Human Volunteers and in vitro Biotransformation.
Eur J Drug Metab Pharmacokinet
December 2024
Preclinical Development-Drug Metabolism and Pharmacokinetics, Bayer AG, Berlin, Germany.
Background: Elinzanetant is a dual neurokinin-1,3 receptor antagonist in development for the treatment of menopausal vasomotor symptoms. The objectives of these studies were to characterize the mass balance and biotransformation of elinzanetant.
Methods: In the clinical evaluation, whole blood, plasma, urine, and feces were collected from healthy fasted male volunteers (n = 6) following a single dose of 120 mg [C]-elinzanetant oral suspension for analysis of total radioactivity and metabolite profiling.
Dermal penetration of 2-phenoxyethanol in humans: in vivo metabolism and toxicokinetics.
Arch Toxicol
December 2024
Institute and Outpatient Clinic of Occupational, Social and Environmental Medicine, Friedrich-Alexander-Universität Erlangen-Nürnberg, Erlangen, Germany.
2-Phenoxyethanol (PhE) is an amphiphilic organic compound frequently used as a broad-spectrum preservative in cosmetic products and other consumer goods. PhE is also used as a biocidal component in occupational settings. A previous volunteer study by our working group following oral exposure to PhE showed that PhE is almost completely taken up into the human body followed by an extensive metabolization and fast urinary elimination.
View Article and Find Full Text PDFThe hemodynamic responses to enhanced external counterpulsation therapy in post-PCI patients with a multi-dimension 0/1D-3D model.
J Biomech
December 2024
Department of Cardiology, The Eighth Affiliated Hospital of Sun Yat-sen University, Shenzhen, Guangdong 518033, China; Guangdong Innovative Engineering and Technology Research Center for Assisted Circulation, Sun Yat-sen University, Shenzhen, Guangdong 518033, China. Electronic address:
Enhanced external counterpulsation (EECP) is widely utilized in rehabilitating patients after percutaneous coronary intervention (PCI) and has demonstrated efficacy in promoting cardiovascular function recovery. Although the precise mechanisms of the therapeutic effects remain elusive, it is widely postulated that the improvement of biomechanical environment induced by EECP plays a critical role. This study aimed to unravel the underlying mechanism through a numerical investigation of the in-stent biomechanical environment during EECP using an advanced multi-dimensional 0/1D-3D coupled model.
View Article and Find Full Text PDFCorrelation between hematological indicators in acclimatized high-altitude individuals and acute mountain sickness.
PeerJ
December 2024
Air Force Clinical College; The Fifth School of Clinical Medicine, Anhui Medical University, Hefei, China.
Background: The impact of acute mountain sickness (AMS) on individuals ascending to plateaus, soon after exposure to high altitudes, is well-documented. However, the specific relationship between AMS and alterations in blood parameters remains unclear.
Methods: A total of 40 healthy volunteers were recruited.
Concentric Ring Trajectory Sampling With k-Space Reordering Enables Assessment of Tissue-Specific T and T Relaxation for H-Labeled Substrates in the Human Brain at 7 T.
NMR Biomed
February 2025
High Field MR Center, Department of Biomedical Imaging and Image-Guided Therapy, Medical University of Vienna, Vienna, Austria.
Deuterium metabolic imaging (DMI) is an emerging Magnetic Resonance technique providing valuable insight into the dynamics of cellular glucose (Glc) metabolism of the human brain in vivo using deuterium-labeled (H) glucose as non-invasive tracer. Reliable concentration estimation of H-Glc and downstream synthesized neurotransmitters glutamate + glutamine (Glx) requires accurate knowledge of relaxation times, but so far tissue-specific T and T relaxation times (e.g.
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