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Article
Extending the dosing intervals of nivolumab: model-based simulations in unselected cancer patients
Reducing nivolumab dose intensity could increase patients’ life quality and decrease the financial burden while maintaining efficacy. The aims of this study were to develop a population PK model of nivolumab b...
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Article
Open AccessFasting upregulates the monocarboxylate transporter MCT1 at the rat blood-brain barrier through PPAR δ activation
The blood-brain barrier (BBB) is pivotal for the maintenance of brain homeostasis and it strictly regulates the cerebral transport of a wide range of endogenous compounds and drugs. While fasting is increasing...
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Article
A Minimal PBPK Model for Plasma and Cerebrospinal Fluid Pharmacokinetics of Trastuzumab after Intracerebroventricular Administration in Patients with HER2-Positive Brain Metastatic Localizations
Dosing regimens of trastuzumab administered by intracerebroventricular (icv) route to patients with HER2-positive brain localizations remain empirical. The objectives of this study were to describe pharmacokin...
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Article
Open AccessSolubility of lamotrigine in age-specific biorelevant media that simulated the fasted- and fed-conditions of the gastric and intestinal environments in pediatrics and adults: implications for traditional, re-formulated, modified, and new oral formulations
Lamotrigine is an effective antiseizure medication that can be used in the management of focal and generalized epilepsies in pediatric patients. This study was conducted to quantify and compare the solubility ...
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Article
Accelerating robust plausible virtual patient cohort generation by substituting ODE simulations with parameter space map**
The generation of plausible virtual patients (VPs) is an important step in most quantitative systems pharmacology (QSP) workflows, which requires time-intensive solving of ordinary differential equations (ODEs...
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Article
Open AccessExposure of human cerebral microvascular endothelial cells hCMEC/D3 to laminar shear stress induces vascular protective responses
Endothelial cells (ECs) are constantly submitted in vivo to hemodynamical forces derived from the blood circulation, including shear stress (SS). ECs are able to detect SS and consequently adapt their phenotyp...
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Chapter
Drug Metabolism at the Blood-Brain and Blood-CSF Barriers
Drug metabolism is in most cases a detoxication process allowing the organism to inactivate and eliminate foreign substances to which it is exposed. While the liver is the main site of drug metabolism, drug me...
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Article
Open AccessAssessment of brain delivery of a model ABCB1/ABCG2 substrate in patients with non-contrast-enhancing brain tumors with positron emission tomography
P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) are two efflux transporters expressed at the blood–brain barrier which effectively restrict the brain distribution of the majority of current...
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Article
Is the 3,4-methylendioxypyrovalerone/mephedrone combination responsible for enhanced stimulant effects? A rat study with investigation of the effect/concentration relationships
The use of synthetic cathinones as recreational drugs frequently sold in combination has been increasing exponentially. However, the consequences of combining cathinones on the resulting stimulant effects and ...
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Article
Open AccessIsolation and differential transcriptome of vascular smooth muscle cells and mid-capillary pericytes from the rat brain
Brain mural cells form a heterogeneous family which significantly contributes to the maintenance of the blood-brain barrier and regulation of the cerebral blood flow. Current procedures to isolate them cannot ...
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Article
Intravenous infusion for the controlled exposure to the dual ABCB1 and ABCG2 inhibitor elacridar in nonhuman primates
Elacridar (GF120918) is a highly potent inhibitor of both P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2), the main efflux transporters expressed at the blood-brain barrier (BBB). Elacridar...
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Article
Double or Simple Emulsion Process to Encapsulate Hydrophilic Oxytocin Peptide in PLA-PEG Nanoparticles
Oral drug delivery using NPs is a current strategy for poorly absorbed molecules. It offers significant improvement in terms of bioavailability. However, the encapsulation of proteins and peptides in polymeric...
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Article
Effect of Long-term In Vitro Lithium Exposure on mRNA Levels of Claudin-3, CYP1A1, ABCG2 and GSTM3 Genes in the hCMEC/D3 Human Brain Endothelial Cell Line
Lithium chloride (LiCl) has been shown to improve the tightness of brain endothelial cell monolayers in vitro by inhibition of the GSK-3β enzyme, activation of the Wnt/beta-catenin pathway and regulation of ti...
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Article
Open AccessExpression and function of Abcg4 in the mouse blood-brain barrier: role in restricting the brain entry of amyloid-β peptide
ABCG4 is an ATP-binding cassette transmembrane protein which has been shown, in vitro, to participate in the cellular efflux of desmosterol and amyloid-β peptide (Aβ). ABCG4 is highly expressed in the brain, but ...
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Article
RYGB and Drug Disposition: How to Do Better? Analysis of Pharmacokinetic Studies and Recommendations for Clinical Practice
An important issue in the follow-up of patients with bariatric surgery remains to determine whether their therapeutic management should be different after surgery. In this article, we first reviewed all pharma...
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Article
Open AccessTranslation in astrocyte distal processes sets molecular heterogeneity at the gliovascular interface
Astrocytes send out long processes that are terminated by endfeet at the vascular surface and regulate vascular functions as well as homeostasis at the vascular interface. To date, the astroglial mechanisms un...
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Article
Open AccessProceedings of Réanimation 2017, the French Intensive Care Society International Congress
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Article
Effect of a Roux-en-Y Gastric Bypass on the Pharmacokinetics of Oral Morphine Using a Population Approach
Obesity and opioid use for chronic pain in obese individuals are both important public health concerns. The pharmacokinetics of oral morphine after Roux-en-Y gastric bypass (RYGB) are unknown. Therefore, we ai...
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Chapter
Drug Metabolism at the Blood–Brain and Blood–CSF Barriers
Drug metabolism is in most cases a detoxification process allowing the organism to inactivate and eliminate foreign substances to which it is exposed. While the liver is the main site of drug metabolism, drug-...
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Article
Physiologically Based Pharmacokinetic Modelling of Drug Penetration Across the Blood–Brain Barrier—Towards a Mechanistic IVIVE-Based Approach
Predicting the penetration of drugs across the human blood–brain barrier (BBB) is a significant challenge during their development. A variety of in vitro systems representing the BBB have been described, but the ...