Search Results - "de Lange, Elizabeth C. M"
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Status of Metabolomic Measurement for Insights in Alzheimer's Disease Progression-What Is Missing?
Published in International journal of molecular sciences (01-03-2023)“…Alzheimer's disease (AD) is an aging-related neurodegenerative disease, leading to the progressive loss of memory and other cognitive functions. As there is…”
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The implications of target saturation for the use of drug–target residence time
Published in Nature reviews. Drug discovery (01-01-2019)Get full text
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Revisiting Cerebrospinal Fluid Flow Direction and Rate in Physiologically Based Pharmacokinetic Model
Published in Pharmaceutics (24-08-2022)“…The bidirectional pulsatile movement of cerebrospinal fluid (CSF), instead of the traditionally believed unidirectional and constant CSF circulation, has been…”
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Revisiting atenolol as a low passive permeability marker
Published in Fluids and barriers of the CNS (31-10-2017)“…Atenolol, a hydrophilic beta blocker, has been used as a model drug for studying passive permeability of biological membranes such as the blood-brain barrier…”
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The need for mathematical modelling of spatial drug distribution within the brain
Published in Fluids and barriers of the CNS (16-05-2019)“…The blood brain barrier (BBB) is the main barrier that separates the blood from the brain. Because of the BBB, the drug concentration-time profile in the brain…”
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Utility of CSF in translational neuroscience
Published in Journal of pharmacokinetics and pharmacodynamics (01-06-2013)“…Human cerebrospinal fluid (CSF) sampling is of high value as the only general applicable methodology to obtain information on free drug concentrations in…”
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A 3D brain unit model to further improve prediction of local drug distribution within the brain
Published in PloS one (23-09-2020)“…The development of drugs targeting the brain still faces a high failure rate. One of the reasons is a lack of quantitative understanding of the complex…”
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Physiologically Based Modeling Approach to Predict Dopamine D2 Receptor Occupancy of Antipsychotics in Brain: Translation From Rat to Human
Published in Journal of clinical pharmacology (01-05-2019)“…Receptor occupancy (RO) is a translational biomarker for assessing drug efficacy and safety. We aimed to apply a physiologically based pharmacokinetic (PBPK)…”
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A Generic Multi-Compartmental CNS Distribution Model Structure for 9 Drugs Allows Prediction of Human Brain Target Site Concentrations
Published in Pharmaceutical research (01-02-2017)“…Purpose Predicting target site drug concentration in the brain is of key importance for the successful development of drugs acting on the central nervous…”
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Next-generation biomarker discovery in Alzheimer's disease using metabolomics - from animal to human studies
Published in Bioanalysis (01-09-2018)“…Alzheimer's disease (AD) is a complex disease driven mainly by neuronal loss due to accumulation of intracellular neurofibrillary tangles and amyloid β…”
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Imaging Techniques in Alzheimer's Disease: A Review of Applications in Early Diagnosis and Longitudinal Monitoring
Published in International journal of molecular sciences (20-02-2021)“…Alzheimer's disease (AD) is a progressive neurodegenerative disorder affecting many individuals worldwide with no effective treatment to date. AD is…”
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Mechanism-based pharmacokinetic -pharmacodynamic modeling : Biophase distribution, receptor theory, and dynamical systems analysis
Published in Annual review of pharmacology and toxicology (01-01-2007)“…Mechanism-based PK-PD models differ from conventional PK-PD models in that they contain specific expressions to characterize, in a quantitative manner,…”
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The potential impact of CYP and UGT drug-metabolizing enzymes on brain target site drug exposure
Published in Drug metabolism reviews (01-02-2024)“…Drug metabolism is one of the critical determinants of drug disposition throughout the body. While traditionally associated with the liver, recent research has…”
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The Extension of the LeiCNS-PK3.0 Model in Combination with the “Handshake” Approach to Understand Brain Tumor Pathophysiology
Published in Pharmaceutical research (01-07-2022)“…Micrometastatic brain tumor cells, which cause recurrence of malignant brain tumors, are often protected by the intact blood–brain barrier (BBB). Therefore, it…”
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Emerging Insights for Translational Pharmacokinetic and Pharmacokinetic-Pharmacodynamic Studies: Towards Prediction of Nose-to-Brain Transport in Humans
Published in The AAPS journal (01-05-2015)“…To investigate the potential added value of intranasal drug administration, preclinical studies to date have typically used the area under the curve (AUC) in…”
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Non‐linear blood–brain barrier transport and dosing strategies influence receptor occupancy ratios of morphine and its metabolites in pain matrix
Published in British journal of pharmacology (01-10-2024)“…Background and Purpose Morphine is important for treatment of acute and chronic pain. However, there is high interpatient variability and often inadequate pain…”
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Microdialysis: the Key to Physiologically Based Model Prediction of Human CNS Target Site Concentrations
Published in The AAPS journal (01-07-2017)“…Despite the enormous research efforts that have been put into the development of central nervous system (CNS) drugs, the success rate in this area is still…”
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Using the LeiCNS-PK3.0 Physiologically-Based Pharmacokinetic Model to Predict Brain Extracellular Fluid Pharmacokinetics in Mice
Published in Pharmaceutical research (01-11-2023)“…Introduction The unbound brain extracelullar fluid (brain ECF ) to plasma steady state partition coefficient, K p,uu,BBB , values provide steady-state…”
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Drug Distribution in Brain and Cerebrospinal Fluids in Relation to IC50 Values in Aging and Alzheimer’s Disease, Using the Physiologically Based LeiCNS-PK3.0 Model
Published in Pharmaceutical research (01-07-2022)“…Background Very little knowledge exists on the impact of Alzheimer’s disease on the CNS target site pharmacokinetics (PK). Aim To predict the CNS PK of…”
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Potential Mechanisms Underlying Resistance to Dementia in Non-Demented Individuals with Alzheimer's Disease Neuropathology
Published in Journal of Alzheimer's disease (01-01-2022)“…Alzheimer's disease (AD) is the most common form of dementia and typically characterized by the accumulation of amyloid-β plaques and tau tangles…”
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