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PMC9159537 | core_pubmed_pmc | Laser-Induced Forward Transfer Printing on Microneedles for Transdermal Delivery of Gemcitabine | Laser-Induced Forward Transfer Printing on Microneedles for Transdermal Delivery of Gemcitabine Abstract Cancer treatment with chemotherapeutic drugs remains to be challenging to the physician due to limitations associated with lack of efficacy or high toxicities. Typically, chemotherapeutic drugs are administered intr... |
PMC8415216 | core_pubmed_pmc | Stability investigations of cytochrome P450 (CYP) enzymes immediately after death in a pig model support the applicability of postmortem hepatic CYP quantification | Stability investigations of cytochrome P450 (CYP) enzymes immediately after death in a pig model support the applicability of postmortem hepatic CYP quantification Abstract Abstract Quantification of drug‐metabolizing cytochrome P450 (CYP) isoforms using LC–MS/MS has been proposed as a potential way of estimating antem... |
PMC6362170 | core_pubmed_pmc | Assessment of the risk of QT-interval prolongation associated with potential drug-drug interactions in patients admitted to Intensive Care Units | Assessment of the risk of QT-interval prolongation associated with potential drug-drug interactions in patients admitted to Intensive Care Units Abstract Objectives To evaluate the relationship between drug interactions and QT-interval prolongation in patients admitted to a general intensive care unit (ICU). Methods Th... |
PMC12326965 | core_pubmed_pmc | Drug development studies supporting zileuton as a parenteral adjuvant to attenuate antibiotic-associated nephrotoxicity | Drug development studies supporting zileuton as a parenteral adjuvant to attenuate antibiotic-associated nephrotoxicity Abstract ABSTRACT Glycopeptide, polymyxin, and aminoglycoside antibiotics are among the most commonly used agents to treat drug-resistant bacterial infections; however, their clinical use is hindered ... |
PMC4216230 | core_pubmed_pmc | iTEP Nanoparticle-Delivered Salinomycin Displays an Enhanced Toxicity to Cancer Stem Cells in Orthotopic Breast Tumors | iTEP Nanoparticle-Delivered Salinomycin Displays an Enhanced Toxicity to Cancer Stem Cells in Orthotopic Breast Tumors Abstract Abstract Salinomycin (Sali) has selective toxicity to cancer stem cells (CSCs), a subpopulation of cancer cells that have been recently linked with tumor multidrug resistance (MDR). To utilize... |
PMC11413051 | core_pubmed_pmc | Randomized, double‐blind, phase 1a single‐ascending dose and food effect studies assessing safety and pharmacokinetics of EC5026 in healthy volunteers | Randomized, double‐blind, phase 1a single‐ascending dose and food effect studies assessing safety and pharmacokinetics of EC5026 in healthy volunteers Abstract Abstract Chronic pain represents a significant unmet medical need, affecting one‐fifth of the U.S. population. EC5026 is a small molecule inhibitor of the enzym... |
PMC8673549 | core_pubmed_pmc | Computational Approaches for Supporting Combination Therapy in the Post-Aducanumab Era in Alzheimer’s Disease | Computational Approaches for Supporting Combination Therapy in the Post-Aducanumab Era in Alzheimer’s Disease Abstract With the approval of aducanumab on the “Accelerated Approval Pathway” and the recognition of amyloid load as a surrogate marker, new successful therapeutic approaches will be driven by combination ther... |
PMC10339203 | core_pubmed_pmc | Discovery of ecnoglutide – A novel, long-acting, cAMP-biased glucagon-like peptide-1 (GLP-1) analog | Discovery of ecnoglutide – A novel, long-acting, cAMP-biased glucagon-like peptide-1 (GLP-1) analog Abstract Abstract Objective Glucagon-like peptide (GLP)-1 is an incretin hormone that acts after food intake to stimulate insulin production, enhance satiety, and promote weight loss. Here we describe the discovery and c... |
PMC5320518 | core_pubmed_pmc | Novel Liver-targeted conjugates of Glycogen Phosphorylase Inhibitor PSN-357 for the Treatment of Diabetes: Design, Synthesis, Pharmacokinetic and Pharmacological Evaluations | Novel Liver-targeted conjugates of Glycogen Phosphorylase Inhibitor PSN-357 for the Treatment of Diabetes: Design, Synthesis, Pharmacokinetic and Pharmacological Evaluations Abstract PSN-357 , an effective glycogen phosphorylase (GP) inhibitor for the treatment for type 2 diabetics, is hampered in its clinical use by t... |
PMC9027114 | core_pubmed_pmc | Pharmacokinetic/Pharmacodynamic Analysis and Dose Optimization of Cefmetazole and Flomoxef against Extended-Spectrum β-Lactamase-Producing Enterobacterales in Patients with Invasive Urinary Tract Infection Considering Renal Function | Pharmacokinetic/Pharmacodynamic Analysis and Dose Optimization of Cefmetazole and Flomoxef against Extended-Spectrum β-Lactamase-Producing Enterobacterales in Patients with Invasive Urinary Tract Infection Considering Renal Function Abstract Abstract The optimal regimens of cefmetazole and flomoxef for the treatment of... |
PMC8618961 | core_pubmed_pmc | Optimization of Personalized Amlodipine Dosing Strategies for Children Based on Pharmacokinetic Data from Chinese Male Adults and PBPK Modeling | Optimization of Personalized Amlodipine Dosing Strategies for Children Based on Pharmacokinetic Data from Chinese Male Adults and PBPK Modeling Abstract Abstract For children, a special population who are continuously developing, a reasonable dosing strategy is the key to clinical therapy. Accurate dose predictions can... |
PMC6028881 | core_pubmed_pmc | Pharmacokinetic and Pharmacodynamic Modelling to Characterize the Tolerability of Alternative Up-Titration Regimens of Roflumilast in Patients with Chronic Obstructive Pulmonary Disease | Pharmacokinetic and Pharmacodynamic Modelling to Characterize the Tolerability of Alternative Up-Titration Regimens of Roflumilast in Patients with Chronic Obstructive Pulmonary Disease Abstract Background In the OPTIMIZE study, 4 weeks of roflumilast 250 µg once daily before escalation to the approved 500 µg once dail... |
PMC10762902 | core_pubmed_pmc | Prediction of drug–drug interactions between roflumilast and CYP3A4/1A2 perpetrators using a physiologically-based pharmacokinetic (PBPK) approach | Prediction of drug–drug interactions between roflumilast and CYP3A4/1A2 perpetrators using a physiologically-based pharmacokinetic (PBPK) approach Abstract This study aimed to develop a physiologically-based pharmacokinetic (PBPK) model to predict changes in the pharmacokinetics (PK) and pharmacodynamics (PD, PDE4 inhi... |
PMC10668725 | core_pubmed_pmc | Role of a Real-Time TDM-Based Expert Clinical Pharmacological Advice Program in Optimizing the Early Pharmacokinetic/Pharmacodynamic Target Attainment of Continuous Infusion Beta-Lactams among Orthotopic Liver Transplant Recipients with Documented or Suspected Gram-Negative Infections | Role of a Real-Time TDM-Based Expert Clinical Pharmacological Advice Program in Optimizing the Early Pharmacokinetic/Pharmacodynamic Target Attainment of Continuous Infusion Beta-Lactams among Orthotopic Liver Transplant Recipients with Documented or Suspected Gram-Negative Infections Abstract Abstract (1) Objectives: ... |
PMC10180305 | core_pubmed_pmc | Stachydrine, a Bioactive Equilibrist for Synephrine, Identified from Four Citrus Chinese Herbs | Stachydrine, a Bioactive Equilibrist for Synephrine, Identified from Four Citrus Chinese Herbs Abstract Abstract Four Chinese herbs from the Citrus genus, namely Aurantii Fructus Immaturus ( Zhishi ), Aurantii Fructus ( Zhiqiao ), Citri Reticulatae Pericarpium Viride ( Qingpi ) and Citri Reticulatae Pericarpium ( Chenp... |
PMC6738372 | core_pubmed_pmc | Characterization of the Pharmacokinetics of Samidorphan in Healthy Volunteers: Absolute Bioavailability and the Effect of Food and Age | Characterization of the Pharmacokinetics of Samidorphan in Healthy Volunteers: Absolute Bioavailability and the Effect of Food and Age Abstract Abstract Background and Objectives Samidorphan (SAM) is a novel μ-opioid receptor antagonist. We report clinical pharmacokinetic (PK) properties of SAM following different rout... |
PMC12365897 | core_pubmed_pmc | First-in-human study of an EGFRvIII x CD3 T cell bispecific antibody in the treatment of newly diagnosed glioblastoma | First-in-human study of an EGFRvIII x CD3 T cell bispecific antibody in the treatment of newly diagnosed glioblastoma Abstract Abstract Background This first-in-human study evaluated EGFRvIII × CD3 TCB, a novel T cell bispecific antibody, in patients with newly diagnosed EGFRvIII-positive glioblastoma. Methods Patients... |
PMC11992657 | core_pubmed_pmc | Personalized parathyroid hormone therapy for hypoparathyroidism: Insights from pharmacokinetic‐pharmacodynamic modelling | Personalized parathyroid hormone therapy for hypoparathyroidism: Insights from pharmacokinetic‐pharmacodynamic modelling Abstract Aims A 42‐year‐old male developed chronic primary hypoparathyroidism after total thyroidectomy. Conventional therapy led to recurrent nephrolithiasis and therefore rhPTH(1‐84) (parathyroid h... |
PMC10819724 | core_pubmed_pmc | Meltdose Tacrolimus Population Pharmacokinetics and Limited Sampling Strategy Evaluation in Elderly Kidney Transplant Recipients | Meltdose Tacrolimus Population Pharmacokinetics and Limited Sampling Strategy Evaluation in Elderly Kidney Transplant Recipients Abstract Abstract Background: Meltdose tacrolimus (Envarsus ® ) has been marketed as a formulation achieving a more consistent tacrolimus exposure. Due to the narrow therapeutic window of tac... |
PMC10390775 | core_pubmed_pmc | CETP inhibitor evacetrapib enters mouse brain tissue | CETP inhibitor evacetrapib enters mouse brain tissue Abstract High levels of plasma cholesterol, especially high levels of low-density lipoprotein cholesterol (LDL-C), have been associated with an increased risk of Alzheimer’s disease. The cholesteryl ester transfer protein (CETP) in plasma distributes cholesteryl este... |
PMC9357557 | core_pubmed_pmc | Clinical Impact of Semaglutide, a Glucagon-Like Peptide-1 Receptor Agonist, on Obesity Management: A Review | Clinical Impact of Semaglutide, a Glucagon-Like Peptide-1 Receptor Agonist, on Obesity Management: A Review Abstract Abstract Purpose Obesity and overweight pose a threat to health and are more common than undernutrition among adults. It is categorized by fat accumulation and a body mass index (BMI) of > 30. A signific... |
PMC8810562 | core_pubmed_pmc | A protocol to inject ocular drug implants into mouse eyes | A protocol to inject ocular drug implants into mouse eyes Abstract Summary Ocular drug implants (ODIs) are beneficial for treating ocular diseases. However, the lack of a robust injection approach for small-eyed model organisms has been a major technical limitation in developing ODIs. Here, we present a cost-effective,... |
PMC11174535 | core_pubmed_pmc | A Comparison and Safety Evaluation of Micellar versus Standard Vitamin D 3 Oral Supplementation in a Randomized, Double-Blind Human Pilot Study | A Comparison and Safety Evaluation of Micellar versus Standard Vitamin D 3 Oral Supplementation in a Randomized, Double-Blind Human Pilot Study Abstract The aim of this pilot study was to evaluate and compare bioavailability and safety of two Vitamin D 3 formulations (softgels) in healthy adults, at single daily doses ... |
PMC10696171 | core_pubmed_pmc | Impact of sex on antidepressant discontinuation in groups of similar cytochrome P450 phenotypes | Impact of sex on antidepressant discontinuation in groups of similar cytochrome P450 phenotypes Abstract Abstract Introduction Although there are studies assessing reasons for antidepressant discontinuation, little is known about the impact of sex differences or cytochrome P450 phenotypes. Our objective is to assess di... |
PMC10680636 | core_pubmed_pmc | Levetiracetam Modulates Brain Metabolic Networks and Transcriptomic Signatures in the 5XFAD Mouse Model of Alzheimer’s disease | Levetiracetam Modulates Brain Metabolic Networks and Transcriptomic Signatures in the 5XFAD Mouse Model of Alzheimer’s disease Abstract Abstract INTRODUCTION: Subcritical epileptiform activity is associated with impaired cognitive function and is commonly seen in patients with Alzheimer’s disease (AD). The anti-convuls... |
PMC8359307 | core_pubmed_pmc | First‐in‐man study to investigate safety, pharmacokinetics and exploratory pharmacodynamics of HTL0018318, a novel M 1 ‐receptor partial agonist for the treatment of dementias | First‐in‐man study to investigate safety, pharmacokinetics and exploratory pharmacodynamics of HTL0018318, a novel M 1 ‐receptor partial agonist for the treatment of dementias Abstract Abstract Aims HTL0018318 is a selective M 1 receptor partial agonist currently under development for the symptomatic treatment of cogni... |
PMC12641084 | core_pubmed_pmc | Advancing Predictions of Oral Drug Absorption, CYP3A4 Induction, and Transporter‐Mediated Interactions Using a Human Primary Intestinal 3D Model ( EpiIntestinal™ ) | Advancing Predictions of Oral Drug Absorption, CYP3A4 Induction, and Transporter‐Mediated Interactions Using a Human Primary Intestinal 3D Model ( EpiIntestinal™ ) Abstract Accurate prediction of oral drug absorption in humans is essential for early drug development; however, physiologically relevant human models are l... |
PMC4171780 | core_pubmed_pmc | Pharmacokinetics of dexmedetomidine combined with therapeutic hypothermia in a piglet asphyxia model | Pharmacokinetics of dexmedetomidine combined with therapeutic hypothermia in a piglet asphyxia model Abstract Abstract Background The highly selective α 2 -adrenoreceptor agonist, dexmedetomidine, exerts neuroprotective, analgesic, anti-inflammatory and sympatholytic properties that may be beneficial for perinatal asph... |
PMC6096535 | core_pubmed_pmc | GP2015: An Etanercept Biosimilar | GP2015: An Etanercept Biosimilar Abstract Abstract GP2015 is the second biosimilar of the reference p75 TNF receptor-Fc fusion protein etanercept. It is approved for use in all indications for which reference etanercept is approved, including rheumatoid arthritis, juvenile idiopathic arthritis, psoriatic arthritis, ank... |
PMC9439990 | core_pubmed_pmc | First-in-Patient Phase I/II Study of Upacicalcet in Japanese Patients with Secondary Hyperparathyroidism Undergoing Hemodialysis: Pharmacokinetic and Pharmacodynamic Properties | First-in-Patient Phase I/II Study of Upacicalcet in Japanese Patients with Secondary Hyperparathyroidism Undergoing Hemodialysis: Pharmacokinetic and Pharmacodynamic Properties Abstract Objective Upacicalcet is a new renally excreted and injectable calcimimetic agent. We evaluated the pharmacokinetics, pharmacodynamics... |
PMC5869567 | core_pubmed_pmc | Rifampin modulation of xeno‐ and endobiotic conjugating enzyme mRNA expression and associated microRNAs in human hepatocytes | Rifampin modulation of xeno‐ and endobiotic conjugating enzyme mRNA expression and associated microRNAs in human hepatocytes Abstract Abstract Rifampin is a pleiotropic inducer of multiple drug metabolizing enzymes and transporters. This work utilized a global approach to evaluate rifampin effects on conjugating enzyme... |
PMC10811482 | core_pubmed_pmc | Quantitative Pharmacokinetics Reveal Impact of Lipid Composition on Microbubble and Nanoprogeny Shell Fate | Quantitative Pharmacokinetics Reveal Impact of Lipid Composition on Microbubble and Nanoprogeny Shell Fate Abstract Abstract Microbubble‐enabled focused ultrasound (MB‐FUS) has revolutionized nano and molecular drug delivery capabilities. Yet, the absence of longitudinal, systematic, quantitative studies of microbubble... |
PMC7577242 | core_pubmed_pmc | Cross-species/cross-modality physiologically based pharmacokinetics for biologics: 89Zr-labelled albumin-binding domain antibody GSK3128349 in humans | Cross-species/cross-modality physiologically based pharmacokinetics for biologics: 89Zr-labelled albumin-binding domain antibody GSK3128349 in humans Abstract ABSTRACT Two-pore physiologically-based pharmacokinetics (PBPK) for biologics describes the tissue distribution and elimination kinetics of soluble proteins as a... |
PMC3585395 | core_pubmed_pmc | Material Basis of Chinese Herbal Formulas Explored by Combining Pharmacokinetics with Network Pharmacology | Material Basis of Chinese Herbal Formulas Explored by Combining Pharmacokinetics with Network Pharmacology Abstract Abstract The clinical application of Traditional Chinese medicine (TCM), using several herbs in combination (called formulas), has a history of more than one thousand years. However, the bioactive compoun... |
PMC12497385 | core_pubmed_pmc | Computational Prediction of Tissue Iron Dynamics in Iron Deficiency Anemia Following Intravenous Ferric Carboxymaltose Therapy | Computational Prediction of Tissue Iron Dynamics in Iron Deficiency Anemia Following Intravenous Ferric Carboxymaltose Therapy Abstract Background Iron deficiency anemia (IDA) is a global public health concern. Intravenous iron therapy, particularly ferric carboxymaltose (FCM), is a cornerstone therapy for IDA treatmen... |
PMC12399395 | core_pubmed_pmc | Mesenchymal stem cell-derived extracellular vesicles: current advances in preparation and therapeutic applications for neurological disorders | Mesenchymal stem cell-derived extracellular vesicles: current advances in preparation and therapeutic applications for neurological disorders Abstract Extracellular vesicles (EVs), nanoscale vesicles released by various cell types, have garnered significant attention in regenerative medicine. Mesenchymal stem cell-deri... |
PMC12465766 | core_pubmed_pmc | A pilot study evaluating mid-point vancomycin concentrations to estimate pharmacokinetics and area under the curve: a prospective study | A pilot study evaluating mid-point vancomycin concentrations to estimate pharmacokinetics and area under the curve: a prospective study Abstract Background Guidelines recommend monitoring vancomycin by estimating the area under the curve (AUC 24 ) with two levels, peak and trough, preferably using Bayesian software. Ho... |
PMC4169708 | core_pubmed_pmc | Pulmonary Penetration of Piperacillin and Tazobactam in Critically Ill Patients | Pulmonary Penetration of Piperacillin and Tazobactam in Critically Ill Patients Abstract Abstract Pulmonary infections in critically ill patients are common and are associated with high morbidity and mortality. Piperacillin–tazobactam is a frequently used therapy in critically ill patients with pulmonary infection. Ant... |
PMC3873236 | core_pubmed_pmc | Pharmacokinetic drug–drug interactions between 1,4-dihydropyridine calcium channel blockers and statins: factors determining interaction strength and relevant clinical risk management | Pharmacokinetic drug–drug interactions between 1,4-dihydropyridine calcium channel blockers and statins: factors determining interaction strength and relevant clinical risk management Abstract Abstract Background Coadministration of 1,4-dihydropyridine calcium channel blockers (DHP-CCBs) with statins (or 3-hydroxy-3-me... |
PMC9298861 | core_pubmed_pmc | A model‐based simulation of glycaemic control and body weight when switching from semaglutide to 3.0‐ and 4.5‐mg doses of once‐weekly dulaglutide | A model‐based simulation of glycaemic control and body weight when switching from semaglutide to 3.0‐ and 4.5‐mg doses of once‐weekly dulaglutide Abstract Abstract Aim To evaluate HbA1c and body weight changes when semaglutide 0.5‐ or 1.0‐mg once‐weekly (QW) is switched to dulaglutide 3.0‐ or 4.5‐mg QW via exposure‐res... |
PMC12399212 | core_pubmed_pmc | FtsZ as a novel target for antibiotics development: Promises and challenges | FtsZ as a novel target for antibiotics development: Promises and challenges Abstract Abstract Filamenting temperature-sensitive mutant Z (FtsZ), a protein essential for bacterial cell division, is highly conserved across bacterial species but absent in humans, positioning it as a strategic target for the development of... |
PMC5096775 | core_pubmed_pmc | Supratherapeutic dose evaluation and effect of lesinurad on cardiac repolarization: a thorough QT/QTc study | Supratherapeutic dose evaluation and effect of lesinurad on cardiac repolarization: a thorough QT/QTc study Abstract Introduction Lesinurad is a selective uric acid reabsorption inhibitor approved in the United States and Europe for treatment of gout in combination with a xanthine oxidase inhibitor. A maximum tolerated... |
PMC6249601 | core_pubmed_pmc | Development of Clinical-Stage Human Monoclonal Antibodies That Treat Advanced Ebola Virus Disease in Nonhuman Primates | Development of Clinical-Stage Human Monoclonal Antibodies That Treat Advanced Ebola Virus Disease in Nonhuman Primates Abstract Abstract Background For most classes of drugs, rapid development of therapeutics to treat emerging infections is challenged by the timelines needed to identify compounds with the desired effic... |
PMC4669488 | core_pubmed_pmc | Content and activity of human liver microsomal protein and prediction of individual hepatic clearance in vivo | Content and activity of human liver microsomal protein and prediction of individual hepatic clearance in vivo Abstract Abstract The lack of information concerning individual variation in content and activity of human liver microsomal protein is one of the most important obstacles for designing personalized medicines. W... |
PMC3108131 | core_pubmed_pmc | Evaluating Pharmacokinetic and Pharmacodynamic Interactions with Computational Models in Supporting Cumulative Risk Assessment | Evaluating Pharmacokinetic and Pharmacodynamic Interactions with Computational Models in Supporting Cumulative Risk Assessment Abstract Simultaneous or sequential exposure to multiple chemicals may cause interactions in the pharmacokinetics (PK) and/or pharmacodynamics (PD) of the individual chemicals. Such interaction... |
PMC7199303 | core_pubmed_pmc | Simultaneous determination of itraconazole and its CYP3A4-mediated metabolites including N -desalkyl itraconazole in human plasma using liquid chromatography-tandem mass spectrometry and its clinical application | Simultaneous determination of itraconazole and its CYP3A4-mediated metabolites including N -desalkyl itraconazole in human plasma using liquid chromatography-tandem mass spectrometry and its clinical application Abstract Abstract Background Itraconazole (ITZ), a triazole antifungal agent, is metabolized to hydroxy-ITZ ... |
PMC4309345 | core_pubmed_pmc | Measurement of Glomerular Filtration Rate by Rapid Intravenous Injection of a Newly Developed Inulin Fraction | Measurement of Glomerular Filtration Rate by Rapid Intravenous Injection of a Newly Developed Inulin Fraction Abstract Abstract Objective: Since the conventional drip-infusion method for measuring inulin clearance (Cin) has problems related to its accuracy and performance, we explored a more accurate and concise method... |
PMC4054977 | core_pubmed_pmc | Monitoring Drug and Antidrug Levels: A Rational Approach in Rheumatoid Arthritis Patients Treated with Biologic Agents Who Experience Inadequate Response While Being on a Stable Biologic Treatment | Monitoring Drug and Antidrug Levels: A Rational Approach in Rheumatoid Arthritis Patients Treated with Biologic Agents Who Experience Inadequate Response While Being on a Stable Biologic Treatment Abstract Abstract Clinical response in patients with rheumatoid arthritis (RA) treated with biologic agents can be influenc... |
PMC11976151 | core_pubmed_pmc | Prediction of first-in-human dose for new composition bee venom based on allometric scaling and pharmacokinetic modeling approach | Prediction of first-in-human dose for new composition bee venom based on allometric scaling and pharmacokinetic modeling approach Abstract Abstract Bee venom is a traditional remedy used to treat conditions related to the nervous and musculoskeletal systems, as well as autoimmune diseases. Recently, we developed a new ... |
PMC4060085 | core_pubmed_pmc | Comparison of Piroxicam Pharmacokinetics and Anti-Inflammatory Effect in Rats after Intra-Articular and Intramuscular Administration | Comparison of Piroxicam Pharmacokinetics and Anti-Inflammatory Effect in Rats after Intra-Articular and Intramuscular Administration Abstract This study evaluated the pharmacokinetic profile and therapeutic efficacy of piroxicam (PX), a long acting non-steroidal anti-inflammatory drug for the treatment of arthritis, fo... |
PMC8533986 | core_pubmed_pmc | [ 99m Tc]Tc-DB15 in GRPR-Targeted Tumor Imaging with SPECT: From Preclinical Evaluation to the First Clinical Outcomes | [ 99m Tc]Tc-DB15 in GRPR-Targeted Tumor Imaging with SPECT: From Preclinical Evaluation to the First Clinical Outcomes Abstract Simple Summary Radiolabeled gastrin-releasing peptide receptor (GRPR)-antagonists have been proposed for diagnostic imaging and radionuclide therapy—theranostics—of human tumors, including pro... |
PMC11129706 | core_pubmed_pmc | Phase 1 Study of MK-5475, an Inhaled Soluble Guanylate Cyclase Stimulator, in Participants with Pulmonary Hypertension Associated with Chronic Obstructive Pulmonary Disease | Phase 1 Study of MK-5475, an Inhaled Soluble Guanylate Cyclase Stimulator, in Participants with Pulmonary Hypertension Associated with Chronic Obstructive Pulmonary Disease Abstract Purpose This phase 1 study ( NCT04370873 ) evaluated safety and pharmacokinetics/pharmacodynamics (PK/PD) of MK-5475 in participants with ... |
PMC5175493 | core_pubmed_pmc | Pharmacokinetics and Exposure-response Relationship of Golimumab in Patients with Moderately-to-Severely Active Ulcerative Colitis: Results from Phase 2/3 PURSUIT Induction and Maintenance Studies | Pharmacokinetics and Exposure-response Relationship of Golimumab in Patients with Moderately-to-Severely Active Ulcerative Colitis: Results from Phase 2/3 PURSUIT Induction and Maintenance Studies Abstract Abstract Background and Aims: To assess golimumab pharmacokinetics [PK] and exposure-response [ER] in adults with ... |
PMC8772458 | core_pubmed_pmc | Fine-tuned long-acting interleukin-2 superkine potentiates durable immune responses in mice and non-human primate | Fine-tuned long-acting interleukin-2 superkine potentiates durable immune responses in mice and non-human primate Abstract Background Recombinant human interleukin-2 (rhIL-2, aldesleukin) is Food and Drug Administration approved for the treatment of metastatic melanoma and renal cell carcinoma and has achieved durable ... |
PMC7319089 | core_pubmed_pmc | Multi-Component Comparative Pharmacokinetics in Rats After Oral Administration of Fructus aurantii Extract, Naringin, Neohesperidin, and Naringin-Neohesperidin | Multi-Component Comparative Pharmacokinetics in Rats After Oral Administration of Fructus aurantii Extract, Naringin, Neohesperidin, and Naringin-Neohesperidin Abstract Abstract Citrus × aurantium L., Chinese name: Fructus Aurantii (FA) has been largely used as Qi-invigorating herb in China for centuries. The main comp... |
PMC10233978 | core_pubmed_pmc | Metastatic lymph node targeted CTLA4 blockade: a potent intervention for local and distant metastases with minimal ICI-induced pneumonia | Metastatic lymph node targeted CTLA4 blockade: a potent intervention for local and distant metastases with minimal ICI-induced pneumonia Abstract Background Immune checkpoint blockade (ICB) elicits a strong and durable therapeutic response, but its application is limited by disparate responses and its associated immune... |
PMC9439993 | core_pubmed_pmc | Repository Describing the Anatomical, Physiological, and Biological Changes in an Obese Population to Inform Physiologically Based Pharmacokinetic Models | Repository Describing the Anatomical, Physiological, and Biological Changes in an Obese Population to Inform Physiologically Based Pharmacokinetic Models Abstract Abstract Background Obesity is associated with physiological changes that can affect drug pharmacokinetics. Obese individuals are underrepresented in clinica... |
PMC11928783 | core_pubmed_pmc | Vancomycin Population Pharmacokinetic Models in Non- Critically Ill Adults Patients: a scoping review | Vancomycin Population Pharmacokinetic Models in Non- Critically Ill Adults Patients: a scoping review Abstract Background Vancomycin is an effective first-line therapy primarily in methicillin-resistant Staphylococcus aureus (MRSA) infection and Clostridium difficile, however, it has been shown that its effectiveness a... |
PMC3663980 | core_pubmed_pmc | Pharmacometric Characterization of Dabigatran Hemodialysis | Pharmacometric Characterization of Dabigatran Hemodialysis Abstract Abstract Background Hemodialysis has been shown to be a useful method of decreasing dabigatran plasma levels in situations that require rapid elimination of this thrombin inhibitor. However, there is currently no clinical recommendation for the acceler... |
PMC12199126 | core_pubmed_pmc | The effect of severe renal impairment on the pharmacokinetics, safety and tolerability of balcinrenone | The effect of severe renal impairment on the pharmacokinetics, safety and tolerability of balcinrenone Abstract Aims The aim of this phase 1 trial was to assess the pharmacokinetics, safety and tolerability of balcinrenone (previously AZD9977) in participants with severe renal impairment vs . those with normal renal fu... |
PMC8156416 | core_pubmed_pmc | Streptozotocin-Induced Hyperglycemia Affects the Pharmacokinetics of Koumine and its Anti-Allodynic Action in a Rat Model of Diabetic Neuropathic Pain | Streptozotocin-Induced Hyperglycemia Affects the Pharmacokinetics of Koumine and its Anti-Allodynic Action in a Rat Model of Diabetic Neuropathic Pain Abstract Koumine (KM), the most abundant alkaloid in Gelsemium elegans , has anti-neuropathic, anti-inflammatory, and analgesic activities; thus, it has the potential to... |
PMC11768502 | core_pubmed_pmc | Nanoformulation of Spirooxindole and Methods for Treating Hepatocellular Carcinoma | Nanoformulation of Spirooxindole and Methods for Treating Hepatocellular Carcinoma Abstract Abstract Objectives: This in vivo study introduces a newly developed spirooxindole derivative that is deemed safe and effective as a potential targeted therapy for various cancers. Methods: Extensive in vivo investigations, incl... |
PMC7037795 | core_pubmed_pmc | Discovering the Major Antitussive, Expectorant, and Anti-Inflammatory Bioactive Constituents in Tussilago farfara L. Based on the Spectrum–Effect Relationship Combined with Chemometrics | Discovering the Major Antitussive, Expectorant, and Anti-Inflammatory Bioactive Constituents in Tussilago farfara L. Based on the Spectrum–Effect Relationship Combined with Chemometrics Abstract Farfarae Flos (FF) is the dried flower bud of Tussilago farfara L, which has antitussive, expectorant, and anti-inflammatory ... |
PMC7879135 | core_pubmed_pmc | Rifabutin pharmacokinetics and safety among TB/HIV-coinfected children receiving lopinavir/ritonavir-containing second-line ART | Rifabutin pharmacokinetics and safety among TB/HIV-coinfected children receiving lopinavir/ritonavir-containing second-line ART Abstract Abstract Background Treatment options are limited for TB/HIV-coinfected children who require PI-based ART. Rifabutin is the preferred rifamycin for adults on PIs, but the one study ev... |
PMC5851736 | core_pubmed_pmc | A comparison of the pharmacokinetic and pharmacodynamic properties of nitroglycerin according to the composition of the administration set | A comparison of the pharmacokinetic and pharmacodynamic properties of nitroglycerin according to the composition of the administration set Abstract Abstract Background: There is a risk of drug sorption into an intravenous administration set composed of polyvinyl chloride (PVC), polyurethane (PU), or polyolefin (PO). Th... |
PMC9871843 | core_pubmed_pmc | A Phase 1, open-label, crossover study evaluating the effect of a single dose of sodium zirconium cyclosilicate on the pharmacokinetics of tacrolimus and cyclosporin | A Phase 1, open-label, crossover study evaluating the effect of a single dose of sodium zirconium cyclosilicate on the pharmacokinetics of tacrolimus and cyclosporin Abstract ABSTRACT Background Sodium zirconium cyclosilicate (SZC) is an oral, highly selective potassium binder approved for the treatment of hyperkalaemi... |
PMC8530378 | core_pubmed_pmc | Comparison of: (2 S ,4 R )-4-[ 18 F]Fluoroglutamine, [ 11 C]Methionine, and 2-Deoxy-2-[ 18 F]Fluoro- D -Glucose and Two Small-Animal PET/CT Systems Imaging Rat Gliomas | Comparison of: (2 S ,4 R )-4-[ 18 F]Fluoroglutamine, [ 11 C]Methionine, and 2-Deoxy-2-[ 18 F]Fluoro- D -Glucose and Two Small-Animal PET/CT Systems Imaging Rat Gliomas Abstract Abstract Purpose The three positron emission tomography (PET) imaging compounds: (2 S ,4 R )-4-[ 18 F]Fluoroglutamine ([ 18 F]FGln), L -[methyl... |
PMC8266675 | core_pubmed_pmc | Cefiderocol Pharmacokinetics in a Patient Receiving Continuous Venovenous Hemodiafiltration | Cefiderocol Pharmacokinetics in a Patient Receiving Continuous Venovenous Hemodiafiltration Abstract Abstract Antimicrobial dosing in patients receiving continuous renal replacement therapy is a continued clinical challenge. We describe a case of a patient receiving cefiderocol 2 g intravenously every 8 hours as a 3-ho... |
PMC6431447 | core_pubmed_pmc | A New UPLC-MS/MS Method Validated for Quantification of Jervine in Rat Plasma and the Study of Its Pharmacokinetics in Rats | A New UPLC-MS/MS Method Validated for Quantification of Jervine in Rat Plasma and the Study of Its Pharmacokinetics in Rats Abstract The aim of this study was to develop an ultraperformance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) method to assess the concentration of jervine in rat plasma and its ph... |
PMC9973634 | core_pubmed_pmc | Lectin‐Like Oxidized Low‐Density Lipoprotein Receptor 1 Inhibition in Type 2 Diabetes: Phase 1 Results | Lectin‐Like Oxidized Low‐Density Lipoprotein Receptor 1 Inhibition in Type 2 Diabetes: Phase 1 Results Abstract Background Blockade of the lectin‐like oxidized low‐density lipoprotein receptor‐1 (LOX‐1) is a potentially attractive mechanism for lowering inflammatory and lipid risk in patients with atherosclerosis. This... |
PMC12310330 | core_pubmed_pmc | In vivo pharmacokinetics, therapeutic efficacy and immune response of bacteriophage vB_AbaSt_W16 against carbapenem-resistant Acinetobacter baumannii | In vivo pharmacokinetics, therapeutic efficacy and immune response of bacteriophage vB_AbaSt_W16 against carbapenem-resistant Acinetobacter baumannii Abstract Abstract Background The increasing prevalence of carbapenem-resistant Acinetobacter baumannii (CRAB) infections necessitates alternative therapeutic strategies. ... |
PMC11327779 | core_pubmed_pmc | Effect of Obesity on the Exposure of Long-acting Cabotegravir and Rilpivirine: A Modeling Study | Effect of Obesity on the Exposure of Long-acting Cabotegravir and Rilpivirine: A Modeling Study Abstract Abstract Background Obesity is increasingly prevalent among people with human immunodeficiency virus (HIV, PWH). Obesity can reduce drug exposure; however, limited data are available for long-acting (LA) antiretrovi... |
PMC9812563 | core_pubmed_pmc | Efficacy and safety of ciprofol-remifentanil versus propofol-remifentanil during fiberoptic bronchoscopy: A prospective, randomized, double-blind, non-inferiority trial | Efficacy and safety of ciprofol-remifentanil versus propofol-remifentanil during fiberoptic bronchoscopy: A prospective, randomized, double-blind, non-inferiority trial Abstract Objective: Ciprofol is a novel 2,6-disubstituted phenol derivative that has improved pharmacokinetic and pharmacodynamic properties compared w... |
PMC8075697 | core_pubmed_pmc | Pharmacokinetics of 10-Hydroxy Mesaconitine in Rat Plasma by Ultra-Performance Liquid Chromatography-Tandem Quadrupole Mass Spectrometry | Pharmacokinetics of 10-Hydroxy Mesaconitine in Rat Plasma by Ultra-Performance Liquid Chromatography-Tandem Quadrupole Mass Spectrometry Abstract Mesaconitine is the predominant active ingredient in Aconitum carmichaelii Debx. The compound 10-hydroxy mesaconitine is one known metabolite of mesaconitine and is toxic. In... |
PMC10960166 | core_pubmed_pmc | A Systematic Review and Comprehensive Evaluation of Human Intervention Studies to Unravel the Bioavailability of Hydroxycinnamic Acids | A Systematic Review and Comprehensive Evaluation of Human Intervention Studies to Unravel the Bioavailability of Hydroxycinnamic Acids Abstract Significance: Hydroxycinnamic acids (HCAs) are the main phenolic acids in the western diet. Harmonizing the available information on the absorption, distribution, metabolism, a... |
PMC6739279 | core_pubmed_pmc | Optimization of Cancer Treatment in the Frequency Domain | Optimization of Cancer Treatment in the Frequency Domain Abstract Abstract Thorough exploration of alternative dosing frequencies is often not performed in conventional pharmacometrics approaches. Quantitative systems pharmacology (QSP) can provide novel insights into optimal dosing regimen and drug behaviors which cou... |
PMC9483551 | core_pubmed_pmc | Unprescribed and unnoticed: Retrospective chart review of adverse events of interactions between antidepressants and over-the-counter drugs | Unprescribed and unnoticed: Retrospective chart review of adverse events of interactions between antidepressants and over-the-counter drugs Abstract Abstract Aim: To systematically evaluate prevalence and clinical characteristics of adverse effects of antidepressants and OTC drugs interactions in a retrospective chart ... |
PMC3093627 | core_pubmed_pmc | Evidence of active transport involvement in morphine transport via MDCKII and MDCK-PGP cell lines | Evidence of active transport involvement in morphine transport via MDCKII and MDCK-PGP cell lines Abstract Several transporters appear to be important in transporting various drugs. Many patients, who receive morphine as analgesic medication, also receive other medications with potency of changing morphine transport by... |
PMC3788801 | core_pubmed_pmc | Tissue Distribution and Efficacy of Gold Nanorods Coupled with Laser Induced Photoplasmonic Therapy in Ehrlich Carcinoma Solid Tumor Model | Tissue Distribution and Efficacy of Gold Nanorods Coupled with Laser Induced Photoplasmonic Therapy in Ehrlich Carcinoma Solid Tumor Model Abstract Abstract Gold nanorods (GNR) within tumor microregions are characterized by their ability to absorb near IR light and emit heat in what is called photoplasmonic effect. Yet... |
PMC10237648 | core_pubmed_pmc | Filter inference: A scalable nonlinear mixed effects inference approach for snapshot time series data | Filter inference: A scalable nonlinear mixed effects inference approach for snapshot time series data Abstract Abstract Variability is an intrinsic property of biological systems and is often at the heart of their complex behaviour. Examples range from cell-to-cell variability in cell signalling pathways to variability... |
PMC12124217 | core_pubmed_pmc | Beta-cyclodextrin formulation of a disulfide-bond disrupting agent for improved systemic exposure † | Beta-cyclodextrin formulation of a disulfide-bond disrupting agent for improved systemic exposure † Abstract Disulfide-bond disrupting agents (DDAs) are a class of cyclic thiosulfonates that have been shown to kill human epidermal growth factor receptor (HER) family-overexpressing breast cancer (BC) cells selectively a... |
PMC7850405 | core_pubmed_pmc | Pharmacokinetics and Toxicities of Oral Docetaxel Formulations Co-Administered with Ritonavir in Phase I Trials | Pharmacokinetics and Toxicities of Oral Docetaxel Formulations Co-Administered with Ritonavir in Phase I Trials Abstract Introduction Docetaxel is widely used as intravenous (IV) chemotherapy. Oral docetaxel is co-administered with the cytochrome P450 3A4 and P-glycoprotein inhibitor ritonavir to increase oral bioavail... |
PMC12154640 | core_pubmed_pmc | In-dwelling microfluidic device for precise and reliable intranasal drug delivery during freely-moving behavior | In-dwelling microfluidic device for precise and reliable intranasal drug delivery during freely-moving behavior Abstract Many substances/drugs are administered intranasally (IN). These include opioid overdose reversal drugs, anti-epileptic medications, migraine medications, hormone treatments, and medicines to treat/pr... |
PMC9705454 | core_pubmed_pmc | Pharmacokinetics of Glepaglutide, A Long-Acting Glucagon-Like Peptide-2 Analogue: A Study in Healthy Subjects | Pharmacokinetics of Glepaglutide, A Long-Acting Glucagon-Like Peptide-2 Analogue: A Study in Healthy Subjects Abstract Background and Objective Glepaglutide is a novel, long-acting, glucagon-like peptide-2 analogue in a stable aqueous formulation for subcutaneous dosing to treat patients with short bowel syndrome. This... |
PMC8596821 | core_pubmed_pmc | Safety, pharmacokinetics and pharmacodynamics of HTL0009936, a selective muscarinic M 1 ‐acetylcholine receptor agonist: A randomized cross‐over trial | Safety, pharmacokinetics and pharmacodynamics of HTL0009936, a selective muscarinic M 1 ‐acetylcholine receptor agonist: A randomized cross‐over trial Abstract Abstract Aims HTL0009936 is a selective M 1 muscarinic receptor agonist in development for cognitive dysfunction in Alzheimer's disease. Safety, tolerability an... |
PMC3045896 | core_pubmed_pmc | Pharmacokinetics of phenoxodiol, a novel isoflavone, following intravenous administration to patients with advanced cancer | Pharmacokinetics of phenoxodiol, a novel isoflavone, following intravenous administration to patients with advanced cancer Abstract Abstract Background Phenoxodiol is a novel isoflavone currently being studied in clinical trials for the treatment of cancer. This study reports the pharmacokinetics of phenoxodiol in pati... |
PMC12823464 | core_pubmed_pmc | Impact of Obesity and MASH on Zonal Hepatocellular Statin Exposure: Pharmacodynamic Insights From a Permeability‐Limited Multicompartment Liver Model | Impact of Obesity and MASH on Zonal Hepatocellular Statin Exposure: Pharmacodynamic Insights From a Permeability‐Limited Multicompartment Liver Model Abstract ABSTRACT Statins are frequently prescribed for hyperlipidemia, a common comorbidity in patients with obesity and/or metabolic dysfunction‐associated steatohepati... |
PMC12515196 | core_pubmed_pmc | Pharmacokinetics, efficacy and safety of palbociclib and fulvestrant in a patient with hormone receptor-positive, human epidermal growth factor receptor 2 negative metastatic breast cancer with end-stage renal disease undergoing hemodialysis: A case report | Pharmacokinetics, efficacy and safety of palbociclib and fulvestrant in a patient with hormone receptor-positive, human epidermal growth factor receptor 2 negative metastatic breast cancer with end-stage renal disease undergoing hemodialysis: A case report Abstract Palbociclib combined with fulvestrant is a standard tr... |
PMC10058863 | core_pubmed_pmc | Effective Treatments of UTI—Is Intravesical Therapy the Future? | Effective Treatments of UTI—Is Intravesical Therapy the Future? Abstract Abstract Urinary tract infection (UTI) afflicts millions of patients globally each year. While the majority of UTIs are successfully treated with orally administered antibiotics, the impact of oral antibiotics on the host microbiota is under close... |
PMC12193167 | core_pubmed_pmc | L-3-[ 18 F]-Fluoro-α-Methyl Tyrosine as a PET Tracer for Tumor Diagnosis: A Systematic Review from Mechanisms to Clinical Applications | L-3-[ 18 F]-Fluoro-α-Methyl Tyrosine as a PET Tracer for Tumor Diagnosis: A Systematic Review from Mechanisms to Clinical Applications Abstract L-3-[ 18 F]-fluoro-α-methyl tyrosine ([ 18 F]FAMT) is an amino acid positron emission tomography (PET) tracer with high specificity for malignant tumors through its selective t... |
PMC10374720 | core_pubmed_pmc | Operational characteristics of full random effects modelling (‘frem’) compared to stepwise covariate modelling (‘scm’) | Operational characteristics of full random effects modelling (‘frem’) compared to stepwise covariate modelling (‘scm’) Abstract Abstract An adequate covariate selection is a key step in population pharmacokinetic modelling. In this study, the automated stepwise covariate modelling technique (‘scm’) was compared to full... |
PMC10619324 | core_pubmed_pmc | Deep learning-enabled natural language processing to identify directional pharmacokinetic drug–drug interactions | Deep learning-enabled natural language processing to identify directional pharmacokinetic drug–drug interactions Abstract Abstract Background During drug development, it is essential to gather information about the change of clinical exposure of a drug (object) due to the pharmacokinetic (PK) drug-drug interactions (DD... |
PMC4403852 | core_pubmed_pmc | Pharmacokinetics of Repeated Sodium Salicylate Administration to Laying Hens: Evidence for Time Dependent Increase in Drug Elimination from Plasma and Eggs | Pharmacokinetics of Repeated Sodium Salicylate Administration to Laying Hens: Evidence for Time Dependent Increase in Drug Elimination from Plasma and Eggs Abstract Abstract Salicylates were the first non-steroid anti-inflammatory drugs (NSAIDs) to be used in any species and are still widely used in humans and livestoc... |
PMC7610245 | core_pubmed_pmc | Pharmacokinetic evaluation of two pirfenidone formulations in patients with idiopathic pulmonary fibrosis and chronic hypersensitivity pneumonitis | Pharmacokinetic evaluation of two pirfenidone formulations in patients with idiopathic pulmonary fibrosis and chronic hypersensitivity pneumonitis Abstract Idiopathic pulmonary fibrosis (IPF) is a progressive and fatal disease characterized by an abnormal activation of lung epithelium and fibroblasts, as well as an exc... |
PMC10338597 | core_pubmed_pmc | Antifungal Dosing in Critically Ill Patients on Extracorporeal Membrane Oxygenation | Antifungal Dosing in Critically Ill Patients on Extracorporeal Membrane Oxygenation Abstract Abstract Extracorporeal membrane oxygenation (ECMO) is an established advanced life support system, providing temporary cardiac and/or respiratory support in critically ill patients. Fungal infections are associated with increa... |
PMC12285561 | core_pubmed_pmc | A Phase 1, Open‐Label Study of the Pharmacokinetics of Ritlecitinib in Children Aged 6–12 Years With Alopecia Areata | A Phase 1, Open‐Label Study of the Pharmacokinetics of Ritlecitinib in Children Aged 6–12 Years With Alopecia Areata Abstract ABSTRACT Background Alopecia areata (AA) is an autoimmune disease characterized by hair loss that can negatively impact quality of life. AA has a significant pediatric prevalence; however, no sy... |
PMC11407298 | core_pubmed_pmc | Drug–drug interactions of icenticaftor (QBW251) with a 5‐probe cytochrome P450 cocktail and oral contraceptives | Drug–drug interactions of icenticaftor (QBW251) with a 5‐probe cytochrome P450 cocktail and oral contraceptives Abstract Abstract A drug–drug interaction (DDI) study was conducted to evaluate the effect of icenticaftor (QBW251) on the pharmacokinetics (PK) of a 5‐probe cytochrome P450 (CYP) substrate cocktail, guided b... |
PMC6157577 | core_pubmed_pmc | Glucosamine-paracetamol spray-dried solid dispersions with maximized intrinsic dissolution rate, bioavailability and decreased levels of in vivo toxic metabolites | Glucosamine-paracetamol spray-dried solid dispersions with maximized intrinsic dissolution rate, bioavailability and decreased levels of in vivo toxic metabolites Abstract Abstract Purpose This study is aimed at preparing and testing physicochemical, pharmacokinetic and levels of toxic metabolites of paracetamol and gl... |
PMC10315054 | core_pubmed_pmc | Mathematical pharmacodynamic modeling for antimicrobial assessment of ceftazidime/colistin versus gentamicin/meropenem combinations against carbapenem-resistant Pseudomonas aeruginosa biofilm | Mathematical pharmacodynamic modeling for antimicrobial assessment of ceftazidime/colistin versus gentamicin/meropenem combinations against carbapenem-resistant Pseudomonas aeruginosa biofilm Abstract Abstract Background Carbapenem-resistant Pseudomonas aeruginosa (CRPA) represents an escalating healthcare hazard with ... |
PMC9961670 | core_pubmed_pmc | Regulatory Requirements for the Development of Second-Entry Semisolid Topical Products in the European Union | Regulatory Requirements for the Development of Second-Entry Semisolid Topical Products in the European Union Abstract The development of second-entry topical products is hampered by several factors. The excipient composition should be similar to the reference product because excipients may also contribute to efficacy. ... |
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