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PMC8709051
core_pubmed_pmc
Formulation of Lipid-Based Tableted Spray-Congealed Microparticles for Sustained Release of Vildagliptin: In Vitro and In Vivo Studies
Formulation of Lipid-Based Tableted Spray-Congealed Microparticles for Sustained Release of Vildagliptin: In Vitro and In Vivo Studies Abstract Abstract Spray-congealing (SPC) technology was utilized to prepare lipid-based microparticles (MP) capable of sustaining the release of Vildagliptin (VG) for use as a once-dail...
PMC6153808
core_pubmed_pmc
Local Skin Inflammation in Cutaneous Leishmaniasis as a Source of Variable Pharmacokinetics and Therapeutic Efficacy of Liposomal Amphotericin B
Local Skin Inflammation in Cutaneous Leishmaniasis as a Source of Variable Pharmacokinetics and Therapeutic Efficacy of Liposomal Amphotericin B Abstract Disfiguring skin lesions caused by several species of the Leishmania parasite characterize cutaneous leishmaniasis (CL). Successful treatment of CL with intravenous (...
PMC10693922
core_pubmed_pmc
Thoracic Epidural Anesthesia After a Transversus Abdominis Plane Block With Liposomal Bupivacaine in a Patient With Chronic Opioid Use: A Case Report
Thoracic Epidural Anesthesia After a Transversus Abdominis Plane Block With Liposomal Bupivacaine in a Patient With Chronic Opioid Use: A Case Report Abstract Abstract Liposomal bupivacaine is a long-acting local anesthetic drug that provides extended analgesia. A 45-year-old man with metastatic colon cancer and an int...
PMC9388998
core_pubmed_pmc
Nanocarriers for effective delivery: modulation of innate immunity for the management of infections and the associated complications
Nanocarriers for effective delivery: modulation of innate immunity for the management of infections and the associated complications Abstract Innate immunity is the first line of defense against invading pathogens. Innate immune cells can recognize invading pathogens through recognizing pathogen-associated molecular pa...
PMC10818831
core_pubmed_pmc
The Use of Population Pharmacokinetics to Extrapolate Food Effects from Human Adults and Beagle Dogs to the Pediatric Population Illustrated with Paracetamol as a Test Case
The Use of Population Pharmacokinetics to Extrapolate Food Effects from Human Adults and Beagle Dogs to the Pediatric Population Illustrated with Paracetamol as a Test Case Abstract Abstract To date, food–drug interactions in the pediatric population remain understudied. The current food effect studies are mostly perfo...
PMC9905187
core_pubmed_pmc
Cabozantinib exposure–response analysis for the phase 3 CheckMate 9ER trial of nivolumab plus cabozantinib versus sunitinib in first-line advanced renal cell carcinoma
Cabozantinib exposure–response analysis for the phase 3 CheckMate 9ER trial of nivolumab plus cabozantinib versus sunitinib in first-line advanced renal cell carcinoma Abstract Abstract Purpose In the phase 3 CheckMate 9ER trial, intravenous nivolumab (240 mg every 2 weeks) plus oral cabozantinib (40 mg/day) improved p...
PMC10941576
core_pubmed_pmc
Virtual twins for model‐informed precision dosing of clozapine in patients with treatment‐resistant schizophrenia
Virtual twins for model‐informed precision dosing of clozapine in patients with treatment‐resistant schizophrenia Abstract Abstract Model‐informed precision dosing using virtual twins (MIPD‐VTs) is an emerging strategy to predict target drug concentrations in clinical practice. Using a high virtualization MIPD‐VT appro...
PMC10812549
core_pubmed_pmc
Endotoxin-Induced Sepsis on Ceftriaxone-Treated Rats’ Ventilatory Mechanics and Pharmacokinetics
Endotoxin-Induced Sepsis on Ceftriaxone-Treated Rats’ Ventilatory Mechanics and Pharmacokinetics Abstract Sepsis can trigger acute respiratory distress syndrome (ARDS), which can lead to a series of physiological changes, modifying the effectiveness of therapy and culminating in death. For all experiments, male Wistar ...
PMC3466827
core_pubmed_pmc
Monitoring of Anticoagulant Therapy in Heart Disease: Considerations for the Current Assays
Monitoring of Anticoagulant Therapy in Heart Disease: Considerations for the Current Assays Abstract Clinicians should be aware of new developments to familiarize themselves with pharmacokinetic and pharmacodynamic characteristics of new anticoagulant agents to appropriately and safely use them. For the moment, cardiol...
PMC12029500
core_pubmed_pmc
Comparative Evaluation of Cytotoxic and Apoptotic Effects of Natural Compounds in SH-SY5Y Neuroblastoma Cells in Relation to Their Physicochemical Properties
Comparative Evaluation of Cytotoxic and Apoptotic Effects of Natural Compounds in SH-SY5Y Neuroblastoma Cells in Relation to Their Physicochemical Properties Abstract Abstract The cytotoxic and apoptotic properties of four bioactive natural compounds, the prenylated α-pyronephloroglucinol heterodimer arzanol (ARZ), the...
PMC12520407
core_pubmed_pmc
Phytochemical profiling and GC-MS analysis of bioactive compounds in methanolic crude extract of Beta vulgaris (BV) root from Bangladesh
Phytochemical profiling and GC-MS analysis of bioactive compounds in methanolic crude extract of Beta vulgaris (BV) root from Bangladesh Abstract Abstract Beta vulgaris (BV) is distributed worldwide and has long been used as a culinary and in traditional medicine to treat diseases. The objective of the present study wa...
PMC5346141
core_pubmed_pmc
Effect of sildenafil on the activity of some antidepressant drugs and electroconvulsive shock treatment in the forced swim test in mice
Effect of sildenafil on the activity of some antidepressant drugs and electroconvulsive shock treatment in the forced swim test in mice Abstract Sildenafil, a potent and selective inhibitor of phosphodiesterase type 5, is used clinically to treat erectile dysfunction and pulmonary arterial hypertension. It is often tak...
PMC6441808
core_pubmed_pmc
Preparation, characterization, and in vivo evaluation of a polymorphic form of valnemulin hydrogen tartrate
Preparation, characterization, and in vivo evaluation of a polymorphic form of valnemulin hydrogen tartrate Abstract Abstract We prepared a polymorphic form of valnemulin hydrogen tartrate (Form I) to overcome the instability and irritating odor of valnemulin hydrochloride that affect its use in the production and appl...
PMC8847740
core_pubmed_pmc
A Model Perspective Explanation of the Long-Term Sustainability of a Fully Human BCMA-Targeting CAR (CT103A) T-Cell Immunotherapy
A Model Perspective Explanation of the Long-Term Sustainability of a Fully Human BCMA-Targeting CAR (CT103A) T-Cell Immunotherapy Abstract Different from canonical drugs, CAR T-cells are “living drugs”, which derived from patient’s own blood. Studies of the pharmacokinetics of CAR T-cells could improve our understandin...
PMC8054631
core_pubmed_pmc
Durability of VEGF Suppression With Intravitreal Aflibercept and Brolucizumab: Using Pharmacokinetic Modeling to Understand Clinical Outcomes
Durability of VEGF Suppression With Intravitreal Aflibercept and Brolucizumab: Using Pharmacokinetic Modeling to Understand Clinical Outcomes Abstract Purpose To investigate whether vascular endothelial growth factor (VEGF)–suppression durations contribute to our understanding of clinical trial outcomes by simulating v...
PMC6942017
core_pubmed_pmc
Model-Based Characterization of the Pharmacokinetics, Target Engagement Biomarkers, and Immunomodulatory Activity of PF-06342674, a Humanized mAb Against IL-7 Receptor-α, in Adults with Type 1 Diabetes
Model-Based Characterization of the Pharmacokinetics, Target Engagement Biomarkers, and Immunomodulatory Activity of PF-06342674, a Humanized mAb Against IL-7 Receptor-α, in Adults with Type 1 Diabetes Abstract IL-7 receptor-α (IL-7Rα) blockade has been shown to reverse autoimmune diabetes in the non-obese diabetic mou...
PMC7567554
core_pubmed_pmc
Pharmacokinetics and Bioequivalence of Two Formulations of Valsartan 80 mg Capsules: A Randomized, Single Dose, 4-Period Crossover Study in Healthy Chinese Volunteers Under Fasting and Fed Conditions
Pharmacokinetics and Bioequivalence of Two Formulations of Valsartan 80 mg Capsules: A Randomized, Single Dose, 4-Period Crossover Study in Healthy Chinese Volunteers Under Fasting and Fed Conditions Abstract Abstract Purpose To compare the bioequivalence of two formulations of valsartan (80 mg capsules) under fasting ...
PMC12930014
core_pubmed_pmc
Population pharmacokinetics and exposure–response analysis of durvalumab in patients with resectable stage II to IIIB (N2) NSCLC in the phase III AEGEAN study
Population pharmacokinetics and exposure–response analysis of durvalumab in patients with resectable stage II to IIIB (N2) NSCLC in the phase III AEGEAN study Abstract Aims In the AEGEAN study, perioperative durvalumab plus platinum‐based neoadjuvant chemotherapy for patients with resectable stage II to IIIB (N2) non‐s...
PMC9820866
core_pubmed_pmc
Bioanalytical Assay Strategies and Considerations for Measuring Cellular Kinetics
Bioanalytical Assay Strategies and Considerations for Measuring Cellular Kinetics Abstract Abstract A vast evolution of drug modalities has occurred over the last several decades. Novel modalities such as cell and gene therapies have proven to be efficacious for numerous clinical indications–primarily in rare disease a...
PMC12114491
core_pubmed_pmc
Auto-Induction in Oral Esketamine Treatment for Treatment-Resistant Depression: An Exploratory Study
Auto-Induction in Oral Esketamine Treatment for Treatment-Resistant Depression: An Exploratory Study Abstract Background: Esketamine is a rapidly acting antidepressant with robust efficacy in treatment-resistant depression (TRD). Diminishing therapeutic effects and attenuated side effects have been reported after long-...
PMC6358182
core_pubmed_pmc
Darunavir Population Pharmacokinetic Model Based on HIV Outpatient Data
Darunavir Population Pharmacokinetic Model Based on HIV Outpatient Data Abstract Supplemental Digital Content is Available in the Text. Key Words: pharmacokinetics, protease inhibitor, HIV-1 infection, therapeutic drug monitoring Abstract Background: Darunavir is a second-generation protease inhibitor and is registered...
PMC10820640
core_pubmed_pmc
An Intravenous Pharmacokinetic Study of Cannabidiol Solutions in Piglets through the Application of a Validated Ultra-High-Pressure Liquid Chromatography Coupled to Tandem Mass Spectrometry Method for the Simultaneous Quantification of CBD and Its Carboxylated Metabolite in Plasma
An Intravenous Pharmacokinetic Study of Cannabidiol Solutions in Piglets through the Application of a Validated Ultra-High-Pressure Liquid Chromatography Coupled to Tandem Mass Spectrometry Method for the Simultaneous Quantification of CBD and Its Carboxylated Metabolite in Plasma Abstract Cannabidiol (CBD) has multipl...
PMC8520754
core_pubmed_pmc
Easy and reliable maximum a posteriori Bayesian estimation of pharmacokinetic parameters with the open‐source R package mapbayr
Easy and reliable maximum a posteriori Bayesian estimation of pharmacokinetic parameters with the open‐source R package mapbayr Abstract Abstract Pharmacokinetic (PK) parameter estimation is a critical and complex step in the model‐informed precision dosing (MIPD) approach. The mapbayr package was developed to perform ...
PMC12250628
core_pubmed_pmc
Pharmacokinetics of Cannabidiol in Rat Brain Tissue After Single-Dose Administration of Different Formulations
Pharmacokinetics of Cannabidiol in Rat Brain Tissue After Single-Dose Administration of Different Formulations Abstract Cannabidiol (CBD), a phytocannabinoid commonly isolated from chemotype III Cannabis sativa plants, is known for its therapeutic potential. However, comprehensive information on its bioavailability is ...
PMC9472132
core_pubmed_pmc
Preclinical characterization and clinical translation of pharmacodynamic markers for MK-5890: a human CD27 activating antibody for cancer immunotherapy
Preclinical characterization and clinical translation of pharmacodynamic markers for MK-5890: a human CD27 activating antibody for cancer immunotherapy Abstract Abstract Background Immune checkpoint inhibitors (ICI) have radically changed cancer therapy, but most patients with cancer are unresponsive or relapse after t...
PMC5516312
core_pubmed_pmc
Inhibition of Toll-Like Receptor Signaling as a Promising Therapy for Inflammatory Diseases: A Journey from Molecular to Nano Therapeutics
Inhibition of Toll-Like Receptor Signaling as a Promising Therapy for Inflammatory Diseases: A Journey from Molecular to Nano Therapeutics Abstract The recognition of invading pathogens and endogenous molecules from damaged tissues by toll-like receptors (TLRs) triggers protective self-defense mechanisms. However, exce...
PMC9964951
core_pubmed_pmc
Topical Application of Linezolid–Loaded Chitosan Nanoparticles for the Treatment of Eye Infections
Topical Application of Linezolid–Loaded Chitosan Nanoparticles for the Treatment of Eye Infections Abstract Abstract Linezolid (LZ) loaded chitosan–nanoparticles (CSNPs) was developed by the ionic–gelation method using Tripolyphosphate–sodium as a crosslinker for topical application for the treatment of bacterial eye i...
PMC12629111
core_pubmed_pmc
Pharmacokinetics of lopinavir/ritonavir in second-line treatment of children with HIV in the CHAPAS-4 trial
Pharmacokinetics of lopinavir/ritonavir in second-line treatment of children with HIV in the CHAPAS-4 trial Abstract Abstract Objective: Lopinavir/ritonavir (LPV/r) remains a much used drug combination for treatment of children with HIV, but pharmacokinetic data when the adult formulation (LPV/r 200/50 mg) is used for ...
PMC8464813
core_pubmed_pmc
A Novel Carbon Dots/Thermo-Sensitive In Situ Gel for a Composite Ocular Drug Delivery System: Characterization, Ex-Vivo Imaging, and In Vivo Evaluation
A Novel Carbon Dots/Thermo-Sensitive In Situ Gel for a Composite Ocular Drug Delivery System: Characterization, Ex-Vivo Imaging, and In Vivo Evaluation Abstract Abstract We developed a potential composite ocular drug delivery system for the topical administration of diclofenac sodium (DS). The novel carbon dot CD C-HP ...
PMC11052801
core_pubmed_pmc
Population Pharmacodynamic Dose–Response Analysis of Serum Potassium Following Dosing with Sodium Zirconium Cyclosilicate
Population Pharmacodynamic Dose–Response Analysis of Serum Potassium Following Dosing with Sodium Zirconium Cyclosilicate Abstract Abstract Background Sodium zirconium cyclosilicate (SZC) is an approved oral treatment for hyperkalemia that selectively binds potassium (K + ) in the gastrointestinal tract and removes K +...
PMC6126112
core_pubmed_pmc
Erzhi Formula Extracts Reverse Renal Injury in Diabetic Nephropathy Rats by Protecting the Renal Podocytes
Erzhi Formula Extracts Reverse Renal Injury in Diabetic Nephropathy Rats by Protecting the Renal Podocytes Abstract Podocytes injury was a crucial factor resulting in diabetic nephropathy (DN). Erzhi formula extract (EZF) was a clinical effective Chinese medicine on DN, but its mechanism was unclear. In this study, the...
PMC6595371
core_pubmed_pmc
Pharmacokinetics, safety and tolerability of the novel β‐hCG derived immunomodulatory compound, EA‐230
Pharmacokinetics, safety and tolerability of the novel β‐hCG derived immunomodulatory compound, EA‐230 Abstract Abstract Aims EA‐230 is a newly developed synthetic linear tetrapeptide (AQGV) derived from the chorionic gonadotropin hormone (β‐hCG). We investigated the pharmacokinetics, safety and tolerability of EA‐230 ...
PMC6844228
core_pubmed_pmc
Development Of Novel Liposome-Encapsulated Combretastatin A4 Acylated Derivatives: Prodrug Approach For Improving Antitumor Efficacy
Development Of Novel Liposome-Encapsulated Combretastatin A4 Acylated Derivatives: Prodrug Approach For Improving Antitumor Efficacy Abstract Abstract Purpose The objective of the present study was to develop a liposomal drug delivery system based on combretastatin A4 (CA4) prodrugs modified with varying alkyl chains a...
PMC9144547
core_pubmed_pmc
Comparison of Paliperidone Palmitate from Different Crystallization Processes and Effect on Formulations In Vitro and In Vivo
Comparison of Paliperidone Palmitate from Different Crystallization Processes and Effect on Formulations In Vitro and In Vivo Abstract Abstract The quality of active pharmaceutical ingredients (APIs) is an important factor which can affect the safety and efficacy of pharmaceuticals. This study was designed to investiga...
PMC7683794
core_pubmed_pmc
Rejuveinix Shows a Favorable Clinical Safety Profile in Human Subjects and Exhibits Potent Preclinical Protective Activity in the Lipopolysaccharide-Galactosamine Mouse Model of Acute Respiratory Distress Syndrome and Multi‐Organ Failure
Rejuveinix Shows a Favorable Clinical Safety Profile in Human Subjects and Exhibits Potent Preclinical Protective Activity in the Lipopolysaccharide-Galactosamine Mouse Model of Acute Respiratory Distress Syndrome and Multi‐Organ Failure Abstract Background: New treatment platforms that can prevent acute respiratory di...
PMC8264498
core_pubmed_pmc
Pharmacokinetic Modeling of Morphine’s Effect on Plasma Concentrations of Ticagrelor and Its Metabolite in Healthy Volunteers
Pharmacokinetic Modeling of Morphine’s Effect on Plasma Concentrations of Ticagrelor and Its Metabolite in Healthy Volunteers Abstract This study aimed to build a mathematical model describing the pharmacokinetics of ticagrelor and its active metabolite (AR-C124910XX) in a stable setting with concomitant administration...
PMC9784852
core_pubmed_pmc
Oral Pharmacokinetics of Hydroxycinnamic Acids: An Updated Review
Oral Pharmacokinetics of Hydroxycinnamic Acids: An Updated Review Abstract Abstract Hydroxycinnamic acids (HCAs) such as caffeic acid (CA), chlorogenic acid (CGA), coumaric acid (COA) isomers, ferulic acid (FA) and rosmarinic acid (RA) are natural phenolic acids with widespread distribution in vegetal foods and well-do...
PMC8382995
core_pubmed_pmc
Advances in flux balance analysis by integrating machine learning and mechanism-based models
Advances in flux balance analysis by integrating machine learning and mechanism-based models Abstract The availability of multi-omics data sets and genome-scale metabolic models for various organisms provide a platform for modeling and analyzing genotype-to-phenotype relationships. Flux balance analysis is the main too...
PMC2912846
core_pubmed_pmc
Treatment of CoQ 10 Deficient Fibroblasts with Ubiquinone, CoQ Analogs, and Vitamin C: Time- and Compound-Dependent Effects
Treatment of CoQ 10 Deficient Fibroblasts with Ubiquinone, CoQ Analogs, and Vitamin C: Time- and Compound-Dependent Effects Abstract Background Coenzyme Q 10 (CoQ 10 ) and its analogs are used therapeutically by virtue of their functions as electron carriers, antioxidant compounds, or both. However, published studies s...
PMC5289534
core_pubmed_pmc
NNKTT120, an anti-iNKT cell monoclonal antibody, produces rapid and sustained iNKT cell depletion in adults with sickle cell disease
NNKTT120, an anti-iNKT cell monoclonal antibody, produces rapid and sustained iNKT cell depletion in adults with sickle cell disease Abstract Abstract Invariant NKT (iNKT) cells can be activated to stimulate a broad inflammatory response. In murine models of sickle cell disease (SCD), interruption of iNKT cell activity...
PMC10520114
core_pubmed_pmc
Population Pharmacokinetic Analysis Supports Initiation Treatment and Bridging from Sublingual Buprenorphine to Subcutaneous Administration of a Buprenorphine Depot (CAM2038) in the Treatment of Opioid Use Disorder
Population Pharmacokinetic Analysis Supports Initiation Treatment and Bridging from Sublingual Buprenorphine to Subcutaneous Administration of a Buprenorphine Depot (CAM2038) in the Treatment of Opioid Use Disorder Abstract Abstract Background and Objective In treating opioid use disorder (OUD), subcutaneous (SC) exten...
PMC6539736
core_pubmed_pmc
Physiologically‐Based Pharmacokinetic Models for CYP 1A2 Drug–Drug Interaction Prediction: A Modeling Network of Fluvoxamine, Theophylline, Caffeine, Rifampicin, and Midazolam
Physiologically‐Based Pharmacokinetic Models for CYP 1A2 Drug–Drug Interaction Prediction: A Modeling Network of Fluvoxamine, Theophylline, Caffeine, Rifampicin, and Midazolam Abstract This study provides whole‐body physiologically‐based pharmacokinetic models of the strong index cytochrome P450 ( CYP )1A2 inhibitor an...
PMC12637173
core_pubmed_pmc
Investigation on LASSBio‐1971 and LASSBio‐1974 Cellular Cytotoxic Mechanism and Their Comparative DMPK Profile
Investigation on LASSBio‐1971 and LASSBio‐1974 Cellular Cytotoxic Mechanism and Their Comparative DMPK Profile Abstract ABSTRACT Due to the arising of clinically relevant resistant EGFR‐related phenotype through innovative mechanisms, mainly EGFR L858R/T790M , the emergence of novel molecules with dual or multi‐target ...
PMC10723574
core_pubmed_pmc
Meropenem extraction by ex vivo extracorporeal life support circuits
Meropenem extraction by ex vivo extracorporeal life support circuits Abstract Background : Meropenem is a broad-spectrum carbapenem-type antibiotic commonly used to treat critically ill patients infected with extended-spectrum β-lactamase (ESBL)-producing Enterobacteriaceae. As many of these patients require extracorpo...
PMC6272519
core_pubmed_pmc
Pharmacokinetics and Tissue Distribution Study of Caudatin in Normal and Diethylnitrosamine-Induced Hepatocellular Carcinoma Model Rats
Pharmacokinetics and Tissue Distribution Study of Caudatin in Normal and Diethylnitrosamine-Induced Hepatocellular Carcinoma Model Rats Abstract Abstract Caudatin is a potential antitumor agent isolated from the traditional Chinese medicine “ baishouwu ”, which was the root tuber of Cynanchum auriculatum Royle ex Wight...
PMC12943293
core_pubmed_pmc
Drivers of Methotrexate Polyglutamate Concentration in Erythrocytes: Insights from Immune-Mediated Inflammatory Diseases and Pediatric Acute Lymphoblastic Leukemia
Drivers of Methotrexate Polyglutamate Concentration in Erythrocytes: Insights from Immune-Mediated Inflammatory Diseases and Pediatric Acute Lymphoblastic Leukemia Abstract Abstract Background/Objectives : Methotrexate (MTX) is a cornerstone drug used to treat immune-mediated inflammatory diseases (IMIDs) in low doses ...
PMC11926880
core_pubmed_pmc
Procognitive Potential of Neuroprotective Triazine 5-HT 6 Receptor Antagonists Tested on Chronic Activity In Vivo in Rats: Computer-Aided Insight into the Role of Chalcogen-Differences on the Pharmacological Profile
Procognitive Potential of Neuroprotective Triazine 5-HT 6 Receptor Antagonists Tested on Chronic Activity In Vivo in Rats: Computer-Aided Insight into the Role of Chalcogen-Differences on the Pharmacological Profile Abstract Among serotonin receptors, the 5-HT 6 subtype is an important protein target and its ligands ma...
PMC12463259
core_pubmed_pmc
Stochastic treatment regimes in climate-health research: Reassessing malaria risk under warming scenarios in Colombia
Stochastic treatment regimes in climate-health research: Reassessing malaria risk under warming scenarios in Colombia Abstract Malaria remains a significant public health challenge, mainly because climate change is altering transmission dynamics. This study investigates the relationship between rising temperatures and ...
PMC7767934
core_pubmed_pmc
Efficacy and safety of apalutamide in Japanese patients with nonmetastatic castration-resistant prostate cancer: a subgroup analysis of a randomized, double-blind, placebo-controlled, Phase-3 study
Efficacy and safety of apalutamide in Japanese patients with nonmetastatic castration-resistant prostate cancer: a subgroup analysis of a randomized, double-blind, placebo-controlled, Phase-3 study Abstract Abstract Background In the global Phase-3 Selective Prostate Androgen Receptor Targeting with ARN-509 study, apal...
PMC5559813
core_pubmed_pmc
Anti-nausea effects and pharmacokinetics of ondansetron, maropitant and metoclopramide in a low-dose cisplatin model of nausea and vomiting in the dog: a blinded crossover study
Anti-nausea effects and pharmacokinetics of ondansetron, maropitant and metoclopramide in a low-dose cisplatin model of nausea and vomiting in the dog: a blinded crossover study Abstract Abstract Background Nausea is a subjective sensation which is difficult to measure in non-verbal species. The aims of this study were...
PMC7235792
core_pubmed_pmc
Effect of the Most Relevant CYP3A4 and CYP3A5 Polymorphisms on the Pharmacokinetic Parameters of 10 CYP3A Substrates
Effect of the Most Relevant CYP3A4 and CYP3A5 Polymorphisms on the Pharmacokinetic Parameters of 10 CYP3A Substrates Abstract Abstract Several cytochrome P450 (CYP) CYP3A polymorphisms were associated with reduced enzyme function. We aimed to evaluate the influence of these alleles on the pharmacokinetic parameters (PK...
PMC11591679
core_pubmed_pmc
Collagen I Microfiber Promotes Brain Capillary Network Formation in Three–Dimensional Blood–Brain Barrier Microphysiological Systems
Collagen I Microfiber Promotes Brain Capillary Network Formation in Three–Dimensional Blood–Brain Barrier Microphysiological Systems Abstract Background: The blood–brain barrier (BBB) strictly regulates the penetration of substances into the brain, which, although important for maintaining brain homeostasis, may delay ...
PMC11250615
core_pubmed_pmc
Very low monomethyl fumarate exposure via human milk: a case report—a contribution from the ConcePTION project
Very low monomethyl fumarate exposure via human milk: a case report—a contribution from the ConcePTION project Abstract Introduction While breastfeeding is recommended, knowledge regarding medicine transfer to human milk and its safety for nursing infants is limited. Only one paper has previously described dimethyl fum...
PMC5849655
core_pubmed_pmc
In vitro studies and in silico predictions of fluconazole and CYP2C9 genetic polymorphism impact on siponimod metabolism and pharmacokinetics
In vitro studies and in silico predictions of fluconazole and CYP2C9 genetic polymorphism impact on siponimod metabolism and pharmacokinetics Abstract Abstract Purpose The purpose of the study is to investigate the enzyme(s) responsible for siponimod metabolism and to predict the inhibitory effects of fluconazole as we...
PMC9554867
core_pubmed_pmc
Adherence to metformin in adults with type 2 diabetes: a combined method approach
Adherence to metformin in adults with type 2 diabetes: a combined method approach Abstract Background Medication adherence, one of the most important aspects in the process of optimal medicines use, is unfortunately still a major challenge in modern healthcare, and further research is required into how adherence can be...
PMC7642756
core_pubmed_pmc
Detection and quantification of Covid-19 antiviral drugs in biological fluids and tissues
Detection and quantification of Covid-19 antiviral drugs in biological fluids and tissues Abstract Abstract Since coronavirus disease 2019 (COVID-19) started as a fast-spreading pandemic, causing a huge number of deaths worldwide, several therapeutic options have been tested to counteract or reduce the clinical symptom...
PMC11281481
core_pubmed_pmc
Safety and Efficacy of Antiviral Drugs and Vaccines in Pregnant Women: Insights from Physiologically Based Pharmacokinetic Modeling and Integration of Viral Infection Dynamics
Safety and Efficacy of Antiviral Drugs and Vaccines in Pregnant Women: Insights from Physiologically Based Pharmacokinetic Modeling and Integration of Viral Infection Dynamics Abstract Abstract Addressing the complexities of managing viral infections during pregnancy is essential for informed medical decision-making. T...
PMC12300890
core_pubmed_pmc
Marine-Derived Compounds: A New Horizon in Cancer, Renal, and Metabolic Disease Therapeutics
Marine-Derived Compounds: A New Horizon in Cancer, Renal, and Metabolic Disease Therapeutics Abstract Abstract Marine-derived compounds represent a rich source of structurally diverse molecules with therapeutic potential for cancer, renal disorders, metabolic-associated fatty liver disease (MAFLD), and atherosclerosis....
PMC12683522
core_pubmed_pmc
Bioequivalence of a single dose of two palbociclib formulations in healthy Chinese subjects under fasting conditions: a two-period crossover study with rabeprazole pre-treatment
Bioequivalence of a single dose of two palbociclib formulations in healthy Chinese subjects under fasting conditions: a two-period crossover study with rabeprazole pre-treatment Abstract Abstract Objectives This study assessed the pharmacokinetics, safety, and bioequivalence of generic and original palbociclib tablets ...
PMC9576339
core_pubmed_pmc
A Novel Dextran-Based Dual Drug Conjugate Targeted Tumors with High Biodistribution Ratio of Tumors to Normal Tissues
A Novel Dextran-Based Dual Drug Conjugate Targeted Tumors with High Biodistribution Ratio of Tumors to Normal Tissues Abstract Purpose Most chemotherapeutic agents possess poor water solubility and show more significant accumulations in normal tissues than in tumor tissues, resulting in serious side effects. To this en...
PMC3702484
core_pubmed_pmc
Comparison of capecitabine and 5-fluorouracil in chemoradiotherapy for locally advanced pancreatic cancer
Comparison of capecitabine and 5-fluorouracil in chemoradiotherapy for locally advanced pancreatic cancer Abstract Abstract Background Although capecitabine has theoretical advantages in the pharmacokinetics, such as higher intratumoral and lower systemic concentration, relative to bolus 5-fluorouracil (5-FU), outcomes...
PMC4260869
core_pubmed_pmc
Pharmacodynamic and Therapeutic Investigation of Focused Ultrasound-Induced Blood-Brain Barrier Opening for Enhanced Temozolomide Delivery in Glioma Treatment
Pharmacodynamic and Therapeutic Investigation of Focused Ultrasound-Induced Blood-Brain Barrier Opening for Enhanced Temozolomide Delivery in Glioma Treatment Abstract Abstract Focused ultrasound (FUS) exposure with the presence of microbubbles has been shown to transiently open the blood-brain barrier (BBB), and thus ...
PMC6143933
core_pubmed_pmc
An opportunity for clinical pharmacology trained physicians to improve patient drug safety: A retrospective analysis of adverse drug reactions in teenagers
An opportunity for clinical pharmacology trained physicians to improve patient drug safety: A retrospective analysis of adverse drug reactions in teenagers Abstract Background: Adverse drug reactions (ADRs) are a major cause of hospital admissions, prolonged hospital stays, morbidity, and drug-related mortality. In thi...
PMC6907258
core_pubmed_pmc
Development of a prognostic composite cytokine signature based on the correlation with nivolumab clearance: translational PK/PD analysis in patients with renal cell carcinoma
Development of a prognostic composite cytokine signature based on the correlation with nivolumab clearance: translational PK/PD analysis in patients with renal cell carcinoma Abstract Background Although several therapeutic options for patients with renal cell carcinoma (RCC) have been approved over recent years, inclu...
PMC12558385
core_pubmed_pmc
Current progress of 1,2,3-triazole hybrids as EGFR inhibitors for cancer therapy – a literature review
Current progress of 1,2,3-triazole hybrids as EGFR inhibitors for cancer therapy – a literature review Abstract Epidermal growth factor receptor (EGFR) is a validated oncogenic driver in numerous solid tumors, and resistance to first- and second-generation tyrosine kinase inhibitors continues to limit clinical outcomes...
PMC5883975
core_pubmed_pmc
Serum Triamcinolone Levels following Cervical Interlaminar Epidural Injection
Serum Triamcinolone Levels following Cervical Interlaminar Epidural Injection Abstract Abstract Background Cervical interlaminar epidural steroid injections (ESIs) are commonly performed procedures to treat painful cervical radiculopathy, but little is known about the systemic absorption and serum levels of steroids fo...
PMC7712059
core_pubmed_pmc
Modeling Invasive Aspergillosis: How Close Are Predicted Antifungal Targets?
Modeling Invasive Aspergillosis: How Close Are Predicted Antifungal Targets? Abstract Abstract Animal model systems are a critical component of the process of discovery and development of new antifungal agents for treatment and prevention of invasive aspergillosis. The persistently neutropenic rabbit model of invasive ...
PMC5874837
core_pubmed_pmc
Epinephrine in Anaphylaxis: Preclinical Study of Pharmacokinetics after Sublingual Administration of Taste-Masked Tablets for Potential Pediatric Use
Epinephrine in Anaphylaxis: Preclinical Study of Pharmacokinetics after Sublingual Administration of Taste-Masked Tablets for Potential Pediatric Use Abstract Abstract Epinephrine is a life-saving treatment in anaphylaxis. In community settings, a first-aid dose of epinephrine is injected from an auto-injector (EAI). N...
PMC12539412
core_pubmed_pmc
Population Pharmacokinetic and Pharmacodynamic Modeling Analysis of rhIL-7-hyFc, a Hybrid Fc-Fused Long-Acting Interleukin-7, to Support Optimal Dosing Regimens in Patients with Solid Cancer
Population Pharmacokinetic and Pharmacodynamic Modeling Analysis of rhIL-7-hyFc, a Hybrid Fc-Fused Long-Acting Interleukin-7, to Support Optimal Dosing Regimens in Patients with Solid Cancer Abstract Purpose rhIL-7-hyFc (Efineptakin alfa) is a novel, long-acting recombinant human interleukin-7 developed to enhance immu...
PMC9621318
core_pubmed_pmc
Machine learning advances the integration of covariates in population pharmacokinetic models: Valproic acid as an example
Machine learning advances the integration of covariates in population pharmacokinetic models: Valproic acid as an example Abstract Abstract Background and Aim: Many studies associated with the combination of machine learning (ML) and pharmacometrics have appeared in recent years. ML can be used as an initial step for f...
PMC11546339
core_pubmed_pmc
Conformational Plasticity Enhances the Brain Penetration of a Metabolically Stable, Dual-Functional Opioid-Peptide CycloAnt
Conformational Plasticity Enhances the Brain Penetration of a Metabolically Stable, Dual-Functional Opioid-Peptide CycloAnt Abstract Abstract CycloAnt is an opioid peptide that produces potent and efficacious antinociception with significantly reduced side effects upon systemic administration in mice. To verify its CNS...
PMC3573743
core_pubmed_pmc
In vitro and in vivo properties of a fully human IgG1 monoclonal antibody that combats multidrug resistant Pseudomonas aeruginosa
In vitro and in vivo properties of a fully human IgG1 monoclonal antibody that combats multidrug resistant Pseudomonas aeruginosa Abstract The development of an anti-bacterial drug in the form of a monoclonal antibody (mAb) targeting an exposed virulence factor, represents an innovative therapeutic strategy. Consequent...
PMC10014062
core_pubmed_pmc
Gene expression databases for physiologically based pharmacokinetic modeling of humans and animal species
Gene expression databases for physiologically based pharmacokinetic modeling of humans and animal species Abstract Abstract In drug research, developing a sound understanding of the key mechanistic drivers of pharmacokinetics (PK) for new molecular entities is essential for human PK and dose predictions. Here, characte...
PMC3990489
core_pubmed_pmc
Impact of Different Oseltamivir Regimens on Treating Influenza A Virus Infection and Resistance Emergence: Insights from a Modelling Study
Impact of Different Oseltamivir Regimens on Treating Influenza A Virus Infection and Resistance Emergence: Insights from a Modelling Study Abstract Several studies have proven oseltamivir to be efficient in reducing influenza viral titer and symptom intensity. However, the usefulness of oseltamivir can be compromised b...
PMC8844171
core_pubmed_pmc
Safety, Pharmacokinetics and Pharmacodynamics of DS-1040, in Combination with Thrombectomy, in Japanese Patients with Acute Ischemic Stroke
Safety, Pharmacokinetics and Pharmacodynamics of DS-1040, in Combination with Thrombectomy, in Japanese Patients with Acute Ischemic Stroke Abstract Abstract Background and Objectives DS-1040 is a novel inhibitor of the activated form of thrombin-activatable fibrinolysis inhibitor that may have therapeutic potential in...
PMC8227119
core_pubmed_pmc
Urinary Elimination of Ecdysterone and Its Metabolites Following a Single-Dose Administration in Humans
Urinary Elimination of Ecdysterone and Its Metabolites Following a Single-Dose Administration in Humans Abstract Abstract Ecdysterone is a phytosteroid widely discussed for its various pharmacological, growth-promoting, and anabolic effects, mediated by the activation of estrogen receptor beta (ERbeta). Performance-enh...
PMC5496343
core_pubmed_pmc
Effect of pharmacogenetics on plasma lumefantrine pharmacokinetics and malaria treatment outcome in pregnant women
Effect of pharmacogenetics on plasma lumefantrine pharmacokinetics and malaria treatment outcome in pregnant women Abstract Background Pregnancy has considerable effects on the pharmacokinetic properties of drugs used to treat uncomplicated Plasmodium falciparum malaria. The role of pharmacogenetic variation on anti-ma...
PMC10304583
core_pubmed_pmc
Effects of Temperature on the Pharmacokinetics, Tissue Residues, and Withdrawal Times of Doxycycline in Rainbow Trout ( Oncorhynchus mykiss ) following Oral Administration
Effects of Temperature on the Pharmacokinetics, Tissue Residues, and Withdrawal Times of Doxycycline in Rainbow Trout ( Oncorhynchus mykiss ) following Oral Administration Abstract Abstract Simple Summary Doxycycline, an approved aquacultural antibiotic, is extensively used in the treatment of bacterial diseases in fis...
PMC11945303
core_pubmed_pmc
Safety, pharmacokinetics, and pharmacodynamics of MK-6194, an IL-2 mutein designed to selectively activate regulatory T cells: single ascending dose and multiple ascending dose trial data
Safety, pharmacokinetics, and pharmacodynamics of MK-6194, an IL-2 mutein designed to selectively activate regulatory T cells: single ascending dose and multiple ascending dose trial data Abstract Abstract MK-6194, an interleukin-2 mutein designed to selectively activate regulatory T cells (Tregs), was evaluated for sa...
PMC9047675
core_pubmed_pmc
Omadacycline pharmacokinetics and soft-tissue penetration in diabetic patients with wound infections and healthy volunteers using in vivo microdialysis
Omadacycline pharmacokinetics and soft-tissue penetration in diabetic patients with wound infections and healthy volunteers using in vivo microdialysis Abstract Abstract Objectives We assessed the plasma and soft-tissue pharmacokinetic exposure of omadacycline in infected patients with diabetic foot infection (DFI) and...
PMC11770492
core_pubmed_pmc
Pharmacokinetics of difloxacin after single intravenous, oral and intramuscular administration in pigeons
Pharmacokinetics of difloxacin after single intravenous, oral and intramuscular administration in pigeons Abstract This study aimed to investigate the pharmacokinetics of difloxacin in pigeons following oral ( PO ), intramuscular ( IM ), and intravenous ( IV ) administration. Thirty pigeons were randomly divided into t...
PMC10927247
core_pubmed_pmc
Hypoxia‐activated ADCC‐enhanced humanized anti‐CD147 antibody for liver cancer imaging and targeted therapy with improved selectivity
Hypoxia‐activated ADCC‐enhanced humanized anti‐CD147 antibody for liver cancer imaging and targeted therapy with improved selectivity Abstract Abstract Therapeutic antibodies (Abs) improve the clinical outcome of cancer patients. However, on‐target off‐tumor toxicity limits Ab‐based therapeutics. Cluster of differentia...
PMC10582665
core_pubmed_pmc
A randomized, placebo‐controlled study to evaluate safety and pharmacokinetics of ART‐001 with a novel oral pediatric formulation in healthy subjects
A randomized, placebo‐controlled study to evaluate safety and pharmacokinetics of ART‐001 with a novel oral pediatric formulation in healthy subjects Abstract Abstract ART‐001 is an orally available selective PI3Kα inhibitor currently being developed for the treatment of slow‐flow vascular malformations (SFVMs). ART‐00...
PMC9241727
core_pubmed_pmc
Evaluating Mono- and Combination Therapy of Meropenem and Amikacin against Pseudomonas aeruginosa Bacteremia in the Hollow-Fiber Infection Model
Evaluating Mono- and Combination Therapy of Meropenem and Amikacin against Pseudomonas aeruginosa Bacteremia in the Hollow-Fiber Infection Model Abstract ABSTRACT Debate continues as to the role of combination antibiotic therapy for the management of Pseudomonas aeruginosa infections. We studied the extent of bacterial...
PMC12823310
core_pubmed_pmc
Integrating Population Approaches With Physiologically Based Pharmacokinetic Models: A Novel Framework for Parameter Estimation
Integrating Population Approaches With Physiologically Based Pharmacokinetic Models: A Novel Framework for Parameter Estimation Abstract ABSTRACT Physiologically Based Pharmacokinetic (PBPK) modeling is a powerful tool in drug development that integrates drug‐specific information with physiological parameters to predic...
PMC11313610
core_pubmed_pmc
Clinical Significance and Patterns of Potential Drug–Drug Interactions in Cardiovascular Patients: Focus on Low-Dose Aspirin and Angiotensin-Converting Enzyme Inhibitors
Clinical Significance and Patterns of Potential Drug–Drug Interactions in Cardiovascular Patients: Focus on Low-Dose Aspirin and Angiotensin-Converting Enzyme Inhibitors Abstract Objective : This study assessed the patterns and clinical significance of potential drug–drug interactions (pDDIs) in patients with diseases ...
PMC12486823
core_pubmed_pmc
Safety, pharmacokinetics, and pharmacodynamics of human interferon-α2b spray in healthy participants
Safety, pharmacokinetics, and pharmacodynamics of human interferon-α2b spray in healthy participants Abstract ABSTRACT The safety, pharmacokinetics (PK), and pharmacodynamics (PD) of multiple doses of human interferon (IFN)-α2b spray administered via nasal and oropharyngeal routes were evaluated in a randomized, double...
PMC12127131
core_pubmed_pmc
In Silico, In Vitro, and In Vivo Investigations of Anticancer Properties of a Novel Platinum (II) Complex and Its PLGA Encapsulated Form
In Silico, In Vitro, and In Vivo Investigations of Anticancer Properties of a Novel Platinum (II) Complex and Its PLGA Encapsulated Form Abstract Abstract In recent years, the development of multinuclear platinum complexes has introduced a new era in platinum-based chemotherapy, offering improved cytotoxicity and the a...
PMC7067890
core_pubmed_pmc
Processing and Polyherbal Formulation of Tetradium ruticarpum (A. Juss.) Hartley: Phytochemistry, Pharmacokinetics, and Toxicity
Processing and Polyherbal Formulation of Tetradium ruticarpum (A. Juss.) Hartley: Phytochemistry, Pharmacokinetics, and Toxicity Abstract Herbal medicine is a major part of traditional Chinese medicine (TCM), which is evolved as a system of medical practice from ancient China. The use of herbal medicine is mainly based...
PMC7004020
core_pubmed_pmc
Open‐label study to investigate the safety and efficacy of adjunctive perampanel in pediatric patients (4 to <12 years) with inadequately controlled focal seizures or generalized tonic‐clonic seizures
Open‐label study to investigate the safety and efficacy of adjunctive perampanel in pediatric patients (4 to <12 years) with inadequately controlled focal seizures or generalized tonic‐clonic seizures Abstract Abstract Objective Study 311 ( NCT02849626 ) was a global, multicenter, open‐label, single‐arm study that asse...
PMC7363835
core_pubmed_pmc
The effect of the VKORC1 promoter variant on warfarin responsiveness in the Saudi WArfarin Pharmacogenetic (SWAP) cohort
The effect of the VKORC1 promoter variant on warfarin responsiveness in the Saudi WArfarin Pharmacogenetic (SWAP) cohort Abstract Abstract Warfarin is a frequently prescribed oral anticoagulant with a narrow therapeutic index, requiring careful dosing and monitoring. However, patients respond with significant inter-ind...
PMC12445756
core_pubmed_pmc
Impact of ageing on sevoflurane’s hypnotic potency and induction kinetics during wash-in period: A prospective observational study
Impact of ageing on sevoflurane’s hypnotic potency and induction kinetics during wash-in period: A prospective observational study Abstract Abstract Background and Aims: The age-dependent decline in sevoflurane’s minimum alveolar concentration is well established. However, the relationship between ageing and its hypnot...
PMC11074935
core_pubmed_pmc
Factors contributing to variability in metformin concentration in polycystic ovary syndrome
Factors contributing to variability in metformin concentration in polycystic ovary syndrome Abstract Aim To investigate the factors affecting metformin concentrations after chronic administration in patients with polycystic ovary syndrome (PCOS), focusing on the pharmacokinetic variability and its implications for pers...
PMC4133921
core_pubmed_pmc
Basic Aspects of the Pharmacodynamics of Tolperisone, A Widely Applicable Centrally Acting Muscle Relaxant
Basic Aspects of the Pharmacodynamics of Tolperisone, A Widely Applicable Centrally Acting Muscle Relaxant Abstract Abstract Tolperisone (2-methyl-1-(4-methylphenyl)-3-piperidin-1-ylpropan-1-one hydro-chloride) was introduced in the clinical practice more than forty years ago and is still evaluated as a widely applicab...
PMC6334931
core_pubmed_pmc
Preclinical toxicity and pharmacokinetics of a new orally bioavailable flubendazole formulation and the impact for clinical trials and risk/benefit to patients
Preclinical toxicity and pharmacokinetics of a new orally bioavailable flubendazole formulation and the impact for clinical trials and risk/benefit to patients Abstract Abstract Background Flubendazole, originally developed to treat infections with intestinal nematodes, has been shown to be efficacious in animal models...
PMC9790930
core_pubmed_pmc
A randomized, double-blind, placebo-controlled phase I trial of inhalation treatment of recombinant TFF2-IFN protein: A multifunctional candidate for the treatment of COVID-19
A randomized, double-blind, placebo-controlled phase I trial of inhalation treatment of recombinant TFF2-IFN protein: A multifunctional candidate for the treatment of COVID-19 Abstract Background and Objectives: Coronavirus disease 2019 (COVID-19) has caused global pandemics in the last 3 years, and the development of ...
PMC5424195
core_pubmed_pmc
Ex Vivo and In Vivo Characterization of Interpolymeric Blend/Nanoenabled Gastroretentive Levodopa Delivery Systems
Ex Vivo and In Vivo Characterization of Interpolymeric Blend/Nanoenabled Gastroretentive Levodopa Delivery Systems Abstract Abstract One approach for delivery of narrow absorption window drugs is to formulate gastroretentive drug delivery systems. This study was undertaken to provide insight into in vivo performances o...
PMC5762083
core_pubmed_pmc
Local Radiotherapy Affects Drug Pharmacokinetics—Exploration of a Neglected but Significant Uncertainty of Cancer Therapy
Local Radiotherapy Affects Drug Pharmacokinetics—Exploration of a Neglected but Significant Uncertainty of Cancer Therapy Abstract Abstract Purpose: Concurrent chemoradiation therapy is the mainstay of treatment for many types of malignancies. However, concurrent chemoradiation therapy is associated with a greater numb...
PMC11015086
core_pubmed_pmc
Population pharmacokinetic modeling of oral brepocitinib in healthy volunteers and patients with immuno‐inflammatory diseases
Population pharmacokinetic modeling of oral brepocitinib in healthy volunteers and patients with immuno‐inflammatory diseases Abstract Abstract The objective of this population pharmacokinetic (PK) analysis was to characterize the concentration–time profile of brepocitinib plasma concentration after single‐ and multipl...
PMC12960560
core_pubmed_pmc
Effects of sleeve gastrectomy on rivaroxaban pharmacokinetics, efficacy, and safety
Effects of sleeve gastrectomy on rivaroxaban pharmacokinetics, efficacy, and safety Abstract Abstract Background Thromboembolic events are potentially serious complications in patients undergoing bariatric surgery. Several studies have investigated the use of rivaroxaban in patients undergoing bariatric surgery. Furthe...