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PMC11975203
core_pubmed_pmc
Evaluation of the Effect of Momelotinib on Cardiac Repolarization: A Thorough QT Study
Evaluation of the Effect of Momelotinib on Cardiac Repolarization: A Thorough QT Study Abstract Abstract A randomized, partially blinded, placebo‐controlled, crossover study in 48 healthy adults assessed the effect of momelotinib on the heart rate‐corrected QT interval (QTc) using the Fridericia formula (QTcF). QTc was...
PMC12107230
core_pubmed_pmc
Therapeutic drug monitoring for antimicrobial agents for people living with HIV (TAP)
Therapeutic drug monitoring for antimicrobial agents for people living with HIV (TAP) Abstract Background Antimicrobial resistance (AMR) is a growing health concern, particularly in Africa, and is predicted to become the leading cause of death after cancer by 2050. Factors like overuse or inappropriate use of antibioti...
PMC3262391
core_pubmed_pmc
Two-way pharmacokinetic interaction studies between saxagliptin and cytochrome P450 substrates or inhibitors: simvastatin, diltiazem extended-release, and ketoconazole
Two-way pharmacokinetic interaction studies between saxagliptin and cytochrome P450 substrates or inhibitors: simvastatin, diltiazem extended-release, and ketoconazole Abstract Background Many medicines, including several cholesterol-lowering agents (eg, lovastatin, simvastatin), antihypertensives (eg, diltiazem, nifed...
PMC11098160
core_pubmed_pmc
Model‐based meta‐analysis to quantify the effects of short interfering RNA therapeutics on hepatitis B surface antigen turnover in hepatitis B‐infected mice
Model‐based meta‐analysis to quantify the effects of short interfering RNA therapeutics on hepatitis B surface antigen turnover in hepatitis B‐infected mice Abstract Abstract The objective of this study was to compare the efficacy of short interfering RNA therapeutics (siRNAs) in reducing hepatitis B surface antigen (H...
PMC10583248
core_pubmed_pmc
Population pharmacokinetics of apixaban in a real‐life hospitalized population from the OptimAT study
Population pharmacokinetics of apixaban in a real‐life hospitalized population from the OptimAT study Abstract Abstract This study aimed to characterize apixaban pharmacokinetics (PKs) and its variability in a real‐world clinical setting of hospitalized patients using a population PK (PopPK) approach. Model‐based simul...
PMC11659111
core_pubmed_pmc
Efflux and uptake transport and gut microbial reactivation of raloxifene glucuronides
Efflux and uptake transport and gut microbial reactivation of raloxifene glucuronides Abstract Abstract Raloxifene has low bioavailability due to extensive glucuronidation in the intestine and the liver, and its pharmacokinetics is associated with high intra‐ and interindividual variability. Some of this variability co...
PMC5061948
core_pubmed_pmc
Pharmacokinetic, Pharmacogenetic, and Other Factors Influencing CNS Penetration of Antiretrovirals
Pharmacokinetic, Pharmacogenetic, and Other Factors Influencing CNS Penetration of Antiretrovirals Abstract Abstract Neurological complications associated with the human immunodeficiency virus (HIV) are a matter of great concern. While antiretroviral (ARV) drugs are the cornerstone of HIV treatment and typically produc...
PMC7307240
core_pubmed_pmc
A multicenter, phase I, pharmacokinetic study of osimertinib in cancer patients with normal renal function or severe renal impairment
A multicenter, phase I, pharmacokinetic study of osimertinib in cancer patients with normal renal function or severe renal impairment Abstract Abstract Osimertinib is a third‐generation, irreversible, oral epidermal growth factor receptor (EGFR)‐tyrosine kinase inhibitor (TKI) that potently and selectively inhibits bot...
PMC11733924
core_pubmed_pmc
A Dynamic Breathing Lung Chip for Precise Evaluation of Inhaled Drug Efficacy and Airway Epithelial Responses
A Dynamic Breathing Lung Chip for Precise Evaluation of Inhaled Drug Efficacy and Airway Epithelial Responses Abstract Inhaled therapy has become a crucial treatment option for respiratory diseases like asthma, cystic fibrosis, and chronic obstructive pulmonary disease (COPD), delivering drugs directly to bronchial and...
PMC7891593
core_pubmed_pmc
Exposure–Response Analyses of Anaplastic Lymphoma Kinase Inhibitors Crizotinib and Alectinib in Non‐Small Cell Lung Cancer Patients
Exposure–Response Analyses of Anaplastic Lymphoma Kinase Inhibitors Crizotinib and Alectinib in Non‐Small Cell Lung Cancer Patients Abstract Abstract Crizotinib and alectinib are anaplastic lymphoma kinase (ALK)‐inhibitors indicated for the treatment of ALK‐positive metastatic non‐small cell lung cancer (NSCLC). At the...
PMC5026379
core_pubmed_pmc
A Liver-Centric Multiscale Modeling Framework for Xenobiotics
A Liver-Centric Multiscale Modeling Framework for Xenobiotics Abstract We describe a multi-scale, liver-centric in silico modeling framework for acetaminophen pharmacology and metabolism. We focus on a computational model to characterize whole body uptake and clearance, liver transport and phase I and phase II metaboli...
PMC10326127
core_pubmed_pmc
A case report of typhlitis during novel use of ropidoxuridine–capecitabine–radiotherapy for treatment-naïve rectal cancer
A case report of typhlitis during novel use of ropidoxuridine–capecitabine–radiotherapy for treatment-naïve rectal cancer Abstract Background Rectal carcinomas are tumors that arise from the last 12 cm of the large intestine closest to the anus. They generally have a modest prognosis exacerbated by a high local recurre...
PMC8448008
core_pubmed_pmc
Obesity in inflammatory bowel disease: A review of its role in the pathogenesis, natural history, and treatment of IBD
Obesity in inflammatory bowel disease: A review of its role in the pathogenesis, natural history, and treatment of IBD Abstract In contrast to previous perceptions that inflammatory bowel disease (IBD) patients are generally malnourished and underweight, there is mounting evidence to suggest that rates of obesity in IB...
PMC5805504
core_pubmed_pmc
Preclinical assessment of galunisertib (LY2157299 monohydrate), a first-in-class transforming growth factor-β receptor type I inhibitor
Preclinical assessment of galunisertib (LY2157299 monohydrate), a first-in-class transforming growth factor-β receptor type I inhibitor Abstract Transforming growth factor-β (TGFβ) is an important driver of tumor growth via intrinsic and extrinsic mechanisms, and is therefore an attractive target for developing cancer ...
PMC7379497
core_pubmed_pmc
Pharmacokinetics of harpagoside in horses after intragastric administration of a Devil's claw (Harpagophytum procumbens) extract
Pharmacokinetics of harpagoside in horses after intragastric administration of a Devil's claw (Harpagophytum procumbens) extract Abstract Abstract Devil's claw is used for the treatment of inflammatory symptoms and degenerative disorders in horses since many years, but without the substantive pharmacokinetic data. The ...
PMC7143261
core_pubmed_pmc
Bioavailability of Melatonin from Lentil Sprouts and Its Role in the Plasmatic Antioxidant Status in Rats
Bioavailability of Melatonin from Lentil Sprouts and Its Role in the Plasmatic Antioxidant Status in Rats Abstract Melatonin is a multifunctional antioxidant neurohormone found in plant foods such as lentil sprouts. We aim to evaluate the effect of lentil sprout intake on the plasmatic levels of melatonin and metabolic...
PMC3418170
core_pubmed_pmc
Improved biological properties and hypouricemic effects of uricase from Candida utilis loaded in novel alkaline enzymosomes
Improved biological properties and hypouricemic effects of uricase from Candida utilis loaded in novel alkaline enzymosomes Abstract Objective: Previous studies on various enzymosomes (functional lipid vesicles encapsulating an enzyme) have been mostly carried out in vitro and have focused on preserving catalytic activ...
PMC8744811
core_pubmed_pmc
Anticonvulsive Effects and Pharmacokinetic Profile of Cannabidiol (CBD) in the Pentylenetetrazol (PTZ) or N-Methyl-D-Aspartate (NMDA) Models of Seizures in Infantile Rats
Anticonvulsive Effects and Pharmacokinetic Profile of Cannabidiol (CBD) in the Pentylenetetrazol (PTZ) or N-Methyl-D-Aspartate (NMDA) Models of Seizures in Infantile Rats Abstract In spite of use of cannabidiol (CBD), a non-psychoactive cannabinoid, in pediatric patients with epilepsy, preclinical studies on its effect...
PMC6567967
core_pubmed_pmc
Research tools for extrapolating the disposition and pharmacokinetics of nanomaterials from preclinical animals to humans
Research tools for extrapolating the disposition and pharmacokinetics of nanomaterials from preclinical animals to humans Abstract A critical step in the translational science of nanomaterials from preclinical animal studies to humans is the comprehensive investigation of their disposition (or ADME) and pharmacokinetic...
PMC8587571
core_pubmed_pmc
Mollusc-Derived Brominated Indoles for the Selective Inhibition of Cyclooxygenase: A Computational Expedition
Mollusc-Derived Brominated Indoles for the Selective Inhibition of Cyclooxygenase: A Computational Expedition Abstract Abstract Inflammation plays an important role in different chronic diseases. Brominated indoles derived from the Australian marine mollusk Dicathais orbita ( D. orbita ) are of interest for their anti-...
PMC11693714
core_pubmed_pmc
Comparative immunogenicity assessment of biosimilar natalizumab to its reference medicine: a matching immunogenicity profile
Comparative immunogenicity assessment of biosimilar natalizumab to its reference medicine: a matching immunogenicity profile Abstract Background Biosimilar natalizumab (biosim-NTZ) is the first biosimilar monoclonal antibody of reference natalizumab (ref-NTZ) for treatment of relapsing forms of multiple sclerosis (MS)....
PMC4148169
core_pubmed_pmc
4-Aminopyridyl-Based CYP51 Inhibitors as Anti- Trypanosoma cruzi Drug Leads with Improved Pharmacokinetic Profile and in Vivo Potency
4-Aminopyridyl-Based CYP51 Inhibitors as Anti- Trypanosoma cruzi Drug Leads with Improved Pharmacokinetic Profile and in Vivo Potency Abstract Abstract CYP51 is a P450 enzyme involved in the biosynthesis of the sterol components of eukaryotic cell membranes. CYP51 inhibitors have been developed to treat infections caus...
PMC11775036
core_pubmed_pmc
Effects of zuranolone on next-day simulated driving in healthy adults
Effects of zuranolone on next-day simulated driving in healthy adults Abstract Rationale Zuranolone is an oral positive allosteric modulator of GABA A receptors. Due to its central nervous system (CNS) activity, zuranolone may impact activities requiring complex cognition, including driving. Objective Evaluate the effe...
PMC3506575
core_pubmed_pmc
GLP2-2G-XTEN: A Pharmaceutical Protein with Improved Serum Half-Life and Efficacy in a Rat Crohn’s Disease Model
GLP2-2G-XTEN: A Pharmaceutical Protein with Improved Serum Half-Life and Efficacy in a Rat Crohn’s Disease Model Abstract Objectives Glucagon-like peptide 2 (GLP2) is an intestinal growth factor that has been shown to stimulate intestinal growth and reduce disease severity in preclinical models of short bowel syndrome ...
PMC9334058
core_pubmed_pmc
In-Depth Study of Thymus vulgaris Essential Oil: Towards Understanding the Antibacterial Target Mechanism and Toxicological and Pharmacological Aspects
In-Depth Study of Thymus vulgaris Essential Oil: Towards Understanding the Antibacterial Target Mechanism and Toxicological and Pharmacological Aspects Abstract Abstract Questions have been raised apropos the emerging problem of microbial resistance, which may pose a great hazard to the human health. Among biosafe comp...
PMC11136808
core_pubmed_pmc
A population pharmacokinetics model of balovaptan to support dose selection in adult and pediatric populations
A population pharmacokinetics model of balovaptan to support dose selection in adult and pediatric populations Abstract Balovaptan is a brain-penetrating vasopressin receptor 1a antagonist previously investigated for the core symptoms of autism spectrum disorder (ASD). A population pharmacokinetic (PK) model of balovap...
PMC12564590
core_pubmed_pmc
Exploring the Anticancer Potential of Coriolus versicolor in Breast Cancer: A Review
Exploring the Anticancer Potential of Coriolus versicolor in Breast Cancer: A Review Abstract Breast cancer remains a leading cause of morbidity and mortality among women globally, with increasing incidence projected in the coming years. Despite advances in standard oncologic therapies, there is a growing interest in s...
PMC2890358
core_pubmed_pmc
Dose-Response Effects of Insulin Glargine in Type 2 Diabetes
Dose-Response Effects of Insulin Glargine in Type 2 Diabetes Abstract Abstract OBJECTIVE To determine the pharmacokinetic and pharmacodynamic dose-response effects of insulin glargine administered subcutaneously in individuals with type 2 diabetes. RESEARCH DESIGN AND METHODS Twenty obese type 2 diabetic individuals (1...
PMC10199278
core_pubmed_pmc
Drug repositioning targeting glutaminase reveals drug candidates for the treatment of Alzheimer’s disease patients
Drug repositioning targeting glutaminase reveals drug candidates for the treatment of Alzheimer’s disease patients Abstract Abstract Background Despite numerous clinical trials and decades of endeavour, there is still no effective cure for Alzheimer's disease. Computational drug repositioning approaches may be employed...
PMC9428304
core_pubmed_pmc
Rotational intraperitoneal pressurized aerosol chemotherapy with paclitaxel and cisplatin: pharmacokinetics, tissue concentrations, and toxicities in a pig model
Rotational intraperitoneal pressurized aerosol chemotherapy with paclitaxel and cisplatin: pharmacokinetics, tissue concentrations, and toxicities in a pig model Abstract Objective We used paclitaxel and cisplatin, known to be effective in intraperitoneal chemotherapy, in a novel prototype of rotational intraperitoneal...
PMC10351292
core_pubmed_pmc
SuPreme Study: a protocol to study the neuroprotective potential of sulfate among very/extremely preterm infants
SuPreme Study: a protocol to study the neuroprotective potential of sulfate among very/extremely preterm infants Abstract Introduction Antenatal maternal magnesium sulfate (MgSO 4 ) administration is a proven efficacious neuroprotective treatment reducing the risk of cerebral palsy (CP) among infants born preterm. Iden...
PMC10789662
core_pubmed_pmc
Advancing Subcutaneous Dosing Regimens for Biotherapeutics: Clinical Strategies for Expedited Market Access
Advancing Subcutaneous Dosing Regimens for Biotherapeutics: Clinical Strategies for Expedited Market Access Abstract Abstract In recent years, subcutaneous administration of biotherapeutics has made significant progress. The self-administration market for rheumatoid arthritis has witnessed the introduction of additiona...
PMC5383603
core_pubmed_pmc
Effects of CYP2C19 Genetic Polymorphisms on PK/PD Responses of Omeprazole in Korean Healthy Volunteers
Effects of CYP2C19 Genetic Polymorphisms on PK/PD Responses of Omeprazole in Korean Healthy Volunteers Abstract The aim of this study was to examine the effects of CYP2C19*2 and *3 genetic polymorphisms on omeprazole pharmacokinetic (PK) and pharmacodynamic (PD) responses. Twenty-four healthy Korean volunteers were enr...
PMC9966787
core_pubmed_pmc
Integrated Computational Approaches for Inhibiting Sex Hormone-Binding Globulin in Male Infertility by Screening Potent Phytochemicals
Integrated Computational Approaches for Inhibiting Sex Hormone-Binding Globulin in Male Infertility by Screening Potent Phytochemicals Abstract Male infertility is significantly influenced by the plasma-protein sex hormone-binding globulin (SHBG). Male infertility, erectile dysfunction, prostate cancer, and several oth...
PMC12276709
core_pubmed_pmc
Modeling of pharmacokinetic/pharmacodynamic parameters in regular intermittent intravenous infusion and translational application of the models in personalized antibiotics dosing
Modeling of pharmacokinetic/pharmacodynamic parameters in regular intermittent intravenous infusion and translational application of the models in personalized antibiotics dosing Abstract Objective Quantitative calculation models for the ratio of daily area under the concentration–time curve (AUC 24 ) to the minimum in...
PMC8251565
core_pubmed_pmc
Survival assessment of the extended‐wear insulin infusion set featuring lantern technology in adults with type 1 diabetes by the glucose clamp technique
Survival assessment of the extended‐wear insulin infusion set featuring lantern technology in adults with type 1 diabetes by the glucose clamp technique Abstract Abstract Maintaining good glycaemic control with the same infusion set for longer than 3 days may improve the quality of life of insulin pump users. The aim o...
PMC7858623
core_pubmed_pmc
Cyclodextrin-based host-guest complexes loaded with regorafenib for colorectal cancer treatment
Cyclodextrin-based host-guest complexes loaded with regorafenib for colorectal cancer treatment Abstract Abstract The malignancy of colorectal cancer (CRC) is connected with inflammation and tumor-associated macrophages (TAMs), but effective therapeutics for CRC are limited. To integrate therapeutic targeting with tumo...
PMC6969165
core_pubmed_pmc
Large-scale Analyses of Disease Biomarkers and Apremilast Pharmacodynamic Effects
Large-scale Analyses of Disease Biomarkers and Apremilast Pharmacodynamic Effects Abstract Abstract Finding biomarkers that provide shared link between disease severity, drug-induced pharmacodynamic effects and response status in human trials can provide number of values for patient benefits: elucidating current therap...
PMC5762979
core_pubmed_pmc
Evaluation of GalNAc-siRNA Conjugate Activity in Pre-clinical Animal Models with Reduced Asialoglycoprotein Receptor Expression
Evaluation of GalNAc-siRNA Conjugate Activity in Pre-clinical Animal Models with Reduced Asialoglycoprotein Receptor Expression Abstract The hepatocyte-specific asialoglycoprotein receptor (ASGPR) is an ideal candidate for targeted drug delivery to the liver due to its high capacity for substrate clearance from circula...
PMC11098907
core_pubmed_pmc
Dose-dependent effect of lamotrigine on quetiapine serum concentration in patients using instant release tablets
Dose-dependent effect of lamotrigine on quetiapine serum concentration in patients using instant release tablets Abstract Abstract Purpose Lamotrigine was previously reported to reduce serum concentration of quetiapine. The aim of this study was to investigate whether lamotrigine dose or quetiapine formulation was of i...
PMC4147042
core_pubmed_pmc
Statistical Power Calculations for Mixed Pharmacokinetic Study Designs Using a Population Approach
Statistical Power Calculations for Mixed Pharmacokinetic Study Designs Using a Population Approach Abstract Simultaneous modelling of dense and sparse pharmacokinetic data is possible with a population approach. To determine the number of individuals required to detect the effect of a covariate, simulation-based power ...
PMC6554016
core_pubmed_pmc
The daily practice of direct oral anticoagulant use in patients with atrial fibrillation; an observational cohort study
The daily practice of direct oral anticoagulant use in patients with atrial fibrillation; an observational cohort study Abstract Background Direct oral anticoagulants (DOACs) are administered in fixed doses without monitoring. There is still little published data on the impact of the absence of monitoring on adherence ...
PMC3681568
core_pubmed_pmc
Why do hypertensive patients of African ancestry respond better to calcium blockers and diuretics than to ACE inhibitors and β-adrenergic blockers? A systematic review
Why do hypertensive patients of African ancestry respond better to calcium blockers and diuretics than to ACE inhibitors and β-adrenergic blockers? A systematic review Abstract Abstract Background Clinicians are encouraged to take an individualized approach when treating hypertension in patients of African ancestry, bu...
PMC4208492
core_pubmed_pmc
Optimizing antimicrobial therapy in critically ill patients
Optimizing antimicrobial therapy in critically ill patients Abstract Abstract Critically ill patients with infection in the intensive care unit (ICU) would certainly benefit from timely bacterial identification and effective antimicrobial treatment. Diagnostic techniques have clearly improved in the last years and allo...
PMC5934856
core_pubmed_pmc
In vitro antineoplastic effects of auranofin in canine lymphoma cells
In vitro antineoplastic effects of auranofin in canine lymphoma cells Abstract Background The orally available gold complex auranofin (AF) has been used in humans, primarily as an antirheumatic/immunomodulatory agent. It has been safely administered to healthy dogs to establish pharmacokinetic parameters for oral admin...
PMC4767720
core_pubmed_pmc
Effects of CYP3A4 Inhibitors Ketoconazole and Verapamil and the CYP3A4 Inducer Rifampicin on the Pharmacokinetic Parameters of Fostamatinib: Results from In Vitro and Phase I Clinical Studies
Effects of CYP3A4 Inhibitors Ketoconazole and Verapamil and the CYP3A4 Inducer Rifampicin on the Pharmacokinetic Parameters of Fostamatinib: Results from In Vitro and Phase I Clinical Studies Abstract Background Fostamatinib (R788) is a spleen tyrosine kinase (SYK) inhibitor. The active metabolite of fostamatinib, R406...
PMC8857346
core_pubmed_pmc
Use of a Novel EEG-Based Objective Test, the Cognalyzer ® , in Quantifying the Strength and Determining the Action Time of Cannabis Psychoactive Effects and Factors that May Influence Them Within an Observational Study Framework
Use of a Novel EEG-Based Objective Test, the Cognalyzer ® , in Quantifying the Strength and Determining the Action Time of Cannabis Psychoactive Effects and Factors that May Influence Them Within an Observational Study Framework Abstract Introduction Current methods to detect recent delta-9-tetrahydrocannabinol (THC) u...
PMC4853014
core_pubmed_pmc
Development and evaluation of vitamin E d -α-tocopheryl polyethylene glycol 1000 succinate-mixed polymeric phospholipid micelles of berberine as an anticancer nanopharmaceutical
Development and evaluation of vitamin E d -α-tocopheryl polyethylene glycol 1000 succinate-mixed polymeric phospholipid micelles of berberine as an anticancer nanopharmaceutical Abstract Abstract Berberine (Brb) is an active alkaloid occurring in various common plant species, with well-recognized potential for cancer t...
PMC5111764
core_pubmed_pmc
Pharmacokinetics and Pharmacodynamics of Omarigliptin, a Once‐Weekly Dipeptidyl Peptidase‐4 (DPP‐4) Inhibitor, After Single and Multiple Doses in Healthy Subjects
Pharmacokinetics and Pharmacodynamics of Omarigliptin, a Once‐Weekly Dipeptidyl Peptidase‐4 (DPP‐4) Inhibitor, After Single and Multiple Doses in Healthy Subjects Abstract Abstract The pharmacokinetics (PK) and pharmacodynamics (PD) of omarigliptin, a novel once‐weekly DPP‐4 inhibitor, were assessed following single an...
PMC4312629
core_pubmed_pmc
Pharmacokinetics of Etravirine Combined with Atazanavir/Ritonavir and a Nucleoside Reverse Transcriptase Inhibitor in Antiretroviral Treatment-Experienced, HIV-1-Infected Patients
Pharmacokinetics of Etravirine Combined with Atazanavir/Ritonavir and a Nucleoside Reverse Transcriptase Inhibitor in Antiretroviral Treatment-Experienced, HIV-1-Infected Patients Abstract Abstract Objectives . TEACH ( NCT00896051 ) was a randomized, open-label, two-arm Phase II trial to investigate the pharmacokinetic...
PMC10525765
core_pubmed_pmc
Impact of Continuous Kidney Replacement Therapy and Hemoadsorption with CytoSorb on Antimicrobial Drug Removal in Critically Ill Children with Septic Shock: A Single-Center Prospective Study on a Pediatric Cohort
Impact of Continuous Kidney Replacement Therapy and Hemoadsorption with CytoSorb on Antimicrobial Drug Removal in Critically Ill Children with Septic Shock: A Single-Center Prospective Study on a Pediatric Cohort Abstract Abstract Background: Extracorporeal therapies (ET) are increasingly used in pediatric settings as ...
PMC10012935
core_pubmed_pmc
Blueprint for antibody biologics developability
Blueprint for antibody biologics developability Abstract ABSTRACT Large-molecule antibody biologics have revolutionized medicine owing to their superior target specificity, pharmacokinetic and pharmacodynamic properties, safety and toxicity profiles, and amenability to versatile engineering. In this review, we focus on...
PMC11181026
core_pubmed_pmc
Translational PK/PD and the first-in-human dose selection of a PD1/IL15: an engineered recombinant targeted cytokine for cancer immunotherapy
Translational PK/PD and the first-in-human dose selection of a PD1/IL15: an engineered recombinant targeted cytokine for cancer immunotherapy Abstract Introduction Interleukin 15 (IL-15) is a potential anticancer agent and numerous engineered IL-15 agonists are currently under clinical investigation. Selective targetin...
PMC12519141
core_pubmed_pmc
Distribution of fluralaner in plasma and liver in broiler breeder hens and roosters following the administration of fluralaner (Bravecto®) via medicated drinking water
Distribution of fluralaner in plasma and liver in broiler breeder hens and roosters following the administration of fluralaner (Bravecto®) via medicated drinking water Abstract Highlight • Transcutol V was useful to enhance the water solubility of fluralaner. • 0.2 % (V/V) Transcutol V was tolerated by old broiler bree...
PMC3666986
core_pubmed_pmc
Similar Results in Children with Asthma for Steady State Pharmacokinetic Parameters of Ciclesonide Inhaled with or without Spacer
Similar Results in Children with Asthma for Steady State Pharmacokinetic Parameters of Ciclesonide Inhaled with or without Spacer Abstract Background: Ciclesonide is an inhaled corticosteroid administered by a metered dose inhaler (MDI) to treat bronchial asthma. After inhalation, the inactive ciclesonide is converted ...
PMC10731752
core_pubmed_pmc
Drug-related problems and associated factors among patients with kidney dysfunction at a tertiary hospital in southwestern Uganda: a prospective observational study
Drug-related problems and associated factors among patients with kidney dysfunction at a tertiary hospital in southwestern Uganda: a prospective observational study Abstract Abstract Background Kidney dysfunction is a common, progressive condition that is increasingly becoming a global public health issue. Because the ...
PMC8316236
core_pubmed_pmc
Mechanistic physiology-based pharmacokinetic modeling to elucidate vincristine-induced peripheral neuropathy following treatment with novel kinase inhibitors
Mechanistic physiology-based pharmacokinetic modeling to elucidate vincristine-induced peripheral neuropathy following treatment with novel kinase inhibitors Abstract Abstract Purpose Limited information is available regarding the drug–drug interaction (DDI) potential of molecular targeted agents and rituximab plus cyc...
PMC9828399
core_pubmed_pmc
Population PK and PD Analysis of Domagrozumab in Pediatric Patients with Duchenne Muscular Dystrophy
Population PK and PD Analysis of Domagrozumab in Pediatric Patients with Duchenne Muscular Dystrophy Abstract Abstract Myostatin, a negative regulator of skeletal muscle growth, is a therapeutic target in muscle‐wasting diseases. Domagrozumab, a humanized recombinant monoclonal antibody, binds myostatin and inhibits ac...
PMC12135532
core_pubmed_pmc
Population pharmacokinetics of intravenous fosfomycin: dose optimization for critically ill patients with and without kidney replacement therapy
Population pharmacokinetics of intravenous fosfomycin: dose optimization for critically ill patients with and without kidney replacement therapy Abstract ABSTRACT We investigated the pharmacokinetics (PK) of intravenous fosfomycin in critically ill patients undergoing different types of kidney replacement therapy (KRT)...
PMC9861162
core_pubmed_pmc
Prospective Prediction of Dapaconazole Clinical Drug–Drug Interactions Using an In Vitro to In Vivo Extrapolation Equation and PBPK Modeling
Prospective Prediction of Dapaconazole Clinical Drug–Drug Interactions Using an In Vitro to In Vivo Extrapolation Equation and PBPK Modeling Abstract This study predicted dapaconazole clinical drug–drug interactions (DDIs) over the main Cytochrome P450 (CYP) isoenzymes using static (in vitro to in vivo extrapolation eq...
PMC10106747
core_pubmed_pmc
Addressing maternal medication use during breastfeeding using clinical resources and a novel physiologically based pharmacokinetic model-derived metric: A qualitative study
Addressing maternal medication use during breastfeeding using clinical resources and a novel physiologically based pharmacokinetic model-derived metric: A qualitative study Abstract Introduction Breastfeeding has major benefits to the maternal-infant dyad and yet healthcare providers have expressed uncertainty about ad...
PMC5321807
core_pubmed_pmc
Population Pharmacokinetics Modeling of Unbound Efavirenz, Atazanavir, and Ritonavir in HIV‐Infected Subjects With Aging Biomarkers
Population Pharmacokinetics Modeling of Unbound Efavirenz, Atazanavir, and Ritonavir in HIV‐Infected Subjects With Aging Biomarkers Abstract Unbound drug is the pharmacodynamically relevant concentration. This study aimed to determine if chronologic age or markers of biologic aging, such as the frailty phenotype and p1...
PMC3383947
core_pubmed_pmc
Population pharmacokinetic analysis of 17-dimethylaminoethylamino-17-demethoxygeldanamycin (17-DMAG) in adult patients with solid tumors
Population pharmacokinetic analysis of 17-dimethylaminoethylamino-17-demethoxygeldanamycin (17-DMAG) in adult patients with solid tumors Abstract Purpose To identify sources of exposure variability for the tumor growth inhibitor 17-dimethylaminoethylamino-17-demethoxygeldanamycin (17-DMAG) using a population pharmacoki...
PMC8832337
core_pubmed_pmc
Rituximab Concentration Varies in Patients With Different Lymphoma Subtypes and Correlates With Clinical Outcome
Rituximab Concentration Varies in Patients With Different Lymphoma Subtypes and Correlates With Clinical Outcome Abstract Individual variations in concentrations of rituximab in different B cell non-Hodgkin’s lymphoma subtypes and their relevance to efficacy were still unclear. From 2016 to 2021, a prospective clinical...
PMC8074779
core_pubmed_pmc
The multiple faces of ketamine in anaesthesia and analgesia
The multiple faces of ketamine in anaesthesia and analgesia Abstract Abstract Objective Ketamine is an anaesthetic agent with a unique dissociative profile and pharmacological effects ranging from the induction and maintenance of anaesthesia to analgesia and sedation, depending on the dose. This article provides inform...
PMC8487314
core_pubmed_pmc
Open-label phase 3 study of intravenous golimumab in patients with polyarticular juvenile idiopathic arthritis
Open-label phase 3 study of intravenous golimumab in patients with polyarticular juvenile idiopathic arthritis Abstract Abstract Objectives To assess efficacy, pharmacokinetics (PK) and safety of intravenous (i.v.) golimumab in patients with polyarticular-course JIA (pc-JIA). Methods Children aged 2 to <18 years with a...
PMC10961409
core_pubmed_pmc
Evaluation of physical variables, thermal nociceptive threshold testing and pharmacokinetics during placement of transdermal buprenorphine matrix-type patch in healthy adult horses
Evaluation of physical variables, thermal nociceptive threshold testing and pharmacokinetics during placement of transdermal buprenorphine matrix-type patch in healthy adult horses Abstract Background Matrix type transdermal buprenorphine patches have not been investigated in horses and may provide an effective means o...
PMC7674781
core_pubmed_pmc
The Pharmacokinetics of Doxycycline in Channel Catfish ( Ictalurus punctatus ) Following Intravenous and Oral Administrations
The Pharmacokinetics of Doxycycline in Channel Catfish ( Ictalurus punctatus ) Following Intravenous and Oral Administrations Abstract Abstract The objective of this study was to investigate the bioavailability (BA) and pharmacokinetics (PK) of doxycycline (DC) in channel catfish ( Ictalurus punctatus ) following a sin...
PMC11762061
core_pubmed_pmc
Safety, Tolerability and Pharmacokinetic-Pharmacodynamic Relationship of NX210c Peptide in Healthy Elderly Volunteers: Randomized, Placebo-Controlled, Double-Blind, Multiple Ascending Dose Study
Safety, Tolerability and Pharmacokinetic-Pharmacodynamic Relationship of NX210c Peptide in Healthy Elderly Volunteers: Randomized, Placebo-Controlled, Double-Blind, Multiple Ascending Dose Study Abstract Abstract Introduction Blood-brain barrier (BBB) integrity is fundamental to brain homeostasis, enabling control of s...
PMC2928215
core_pubmed_pmc
Compliance assessment of ambulatory Alzheimer patients to aid therapeutic decisions by healthcare professionals
Compliance assessment of ambulatory Alzheimer patients to aid therapeutic decisions by healthcare professionals Abstract Abstract Background Compliance represents a major determinant for the effectiveness of pharmacotherapy. Compliance reports summarising electronically compiled compliance data qualify healthcare needs...
PMC3599209
core_pubmed_pmc
Body Surface Area Predicts Plasma Oxaliplatin and Pharmacokinetic Advantage in Hyperthermic Intraoperative Intraperitoneal Chemotherapy
Body Surface Area Predicts Plasma Oxaliplatin and Pharmacokinetic Advantage in Hyperthermic Intraoperative Intraperitoneal Chemotherapy Abstract Background Hyperthermic intraoperative intraperitoneal chemotherapy (HIPEC) is used to treat peritoneal surface-spreading malignancies to maximize local drug concentrations wh...
PMC9907915
core_pubmed_pmc
In-silico studies of inhibitory compounds against protease enzymes of SARS-CoV-2
In-silico studies of inhibitory compounds against protease enzymes of SARS-CoV-2 Abstract Abstract In December 2019, a COVID-19 outbreak caused by SARS-CoV-2 raised worldwide health concerns. In this case, molecular docking and drug repurposing computational approaches were engaged to check the efficiency of plant-base...
PMC10831339
core_pubmed_pmc
Paclitaxel plus Eftilagimod Alpha, a Soluble LAG-3 Protein, in Metastatic, HR + Breast Cancer: Results from AIPAC, a Randomized, Placebo Controlled Phase IIb Trial
Paclitaxel plus Eftilagimod Alpha, a Soluble LAG-3 Protein, in Metastatic, HR + Breast Cancer: Results from AIPAC, a Randomized, Placebo Controlled Phase IIb Trial Abstract Abstract Purpose: Eftilagimod alpha (efti), a soluble lymphocyte activation gene (LAG-3) protein and MHC class II agonist, enhances innate and adap...
PMC9808715
core_pubmed_pmc
Lack of Clinical Relevance of Bilastine-Food Interaction in Healthy Volunteers: A Wheal and Flare Study
Lack of Clinical Relevance of Bilastine-Food Interaction in Healthy Volunteers: A Wheal and Flare Study Abstract Abstract Introduction The aim of this study was to compare the pharmacodynamic activity of bilastine administered under fasting and fed conditions in healthy volunteers. Methods In this randomized, open-labe...
PMC11503958
core_pubmed_pmc
Imaging-Assisted Antisense Oligonucleotide Delivery for Tumor-Targeted Gene Therapy
Imaging-Assisted Antisense Oligonucleotide Delivery for Tumor-Targeted Gene Therapy Abstract Antisense oligonucleotide (ASO) represents a class of practical tools for targeting undruggable oncogenes with several candidates currently undergoing clinical investigation. The advancement of antisense therapeutics necessitat...
PMC5980459
core_pubmed_pmc
Pharmacokinetics and efficacy of intravenous famotidine in adult cattle
Pharmacokinetics and efficacy of intravenous famotidine in adult cattle Abstract Background Abomasal ulceration is recognized in neonatal and adult cattle, but research regarding treatment is limited. Histamine‐2 receptor antagonists (H 2 RA), such as famotidine, are used clinically with little evidence‐based research ...
PMC11129016
core_pubmed_pmc
Thromboembolic prevention in athletes: management of anticoagulation in sports players affected by atrial fibrillation
Thromboembolic prevention in athletes: management of anticoagulation in sports players affected by atrial fibrillation Abstract Abstract Atrial fibrillation (AF) is a common cardiac arrhythmia that poses a significant risk of stroke and thromboembolic events. Anticoagulation therapy is essential for preventing stroke i...
PMC6804073
core_pubmed_pmc
Interaction Effects between Doxorubicin and Hernandezine on the Pharmacokinetics by Liquid Chromatography Coupled with Mass Spectrometry
Interaction Effects between Doxorubicin and Hernandezine on the Pharmacokinetics by Liquid Chromatography Coupled with Mass Spectrometry Abstract Abstract Doxorubicin (DOX) is an effective anti-tumor drug widely used in clinics. Hernandezine (HER), isolated from a Chinese medicinal herb, has a selective inhibitory effe...
PMC7714761
core_pubmed_pmc
Understanding Volume Kinetics: The Role of Pharmacokinetic Modeling and Analysis in Fluid Therapy
Understanding Volume Kinetics: The Role of Pharmacokinetic Modeling and Analysis in Fluid Therapy Abstract Fluid therapy is a rapidly evolving yet imprecise clinical practice based upon broad assumptions, species-to-species extrapolations, obsolete experimental evidence, and individual preferences. Although widely reco...
PMC12232703
core_pubmed_pmc
Herb-drug interactions in oncology: pharmacodynamic/pharmacokinetic mechanisms and risk prediction
Herb-drug interactions in oncology: pharmacodynamic/pharmacokinetic mechanisms and risk prediction Abstract The prevalence of herbal medicines has gained widespread, particularly among cancer patients seeking adjunctive therapies. Co-administered with anticancer drugs (ACDs) frequently, herbal medicines result in incre...
PMC7354398
core_pubmed_pmc
The Edoxaban Hokusai VTE PEDIATRICS Study: An open‐label, multicenter, randomized study of edoxaban for pediatric venous thromboembolic disease
The Edoxaban Hokusai VTE PEDIATRICS Study: An open‐label, multicenter, randomized study of edoxaban for pediatric venous thromboembolic disease Abstract Abstract Background Little evidence is available for treatment of pediatric venous thromboembolism (VTE). Large randomized controlled trials are challenging in childre...
PMC2880414
core_pubmed_pmc
Non-compartment model to compartment model pharmacokinetics transformation meta-analysis – a multivariate nonlinear mixed model
Non-compartment model to compartment model pharmacokinetics transformation meta-analysis – a multivariate nonlinear mixed model Abstract Abstract Background To fulfill the model based drug development, the very first step is usually a model establishment from published literatures. Pharmacokinetics model is the central...
PMC9348130
core_pubmed_pmc
Development of novel ultra-sensitive IL-11 target engagement assays to support mechanistic PK/PD modeling for an anti-IL-11 antibody therapeutic
Development of novel ultra-sensitive IL-11 target engagement assays to support mechanistic PK/PD modeling for an anti-IL-11 antibody therapeutic Abstract ABSTRACT An in-house antibody generation campaign identified a diverse, high affinity set of anti-interleukin-11 (IL-11) monoclonal antibodies (mAbs) to enable succes...
PMC11897560
core_pubmed_pmc
Monte Carlo simulation to optimize polymyxin B dosing regimens for the treatment of Gram-negative bacteremia
Monte Carlo simulation to optimize polymyxin B dosing regimens for the treatment of Gram-negative bacteremia Abstract Objective This study aimed to predict and evaluate the efficacy of various polymyxin B dosing regimens for Gram-negative bacteremia using Monte Carlo simulation, with a specific focus on assessing the e...
PMC9266449
core_pubmed_pmc
Dried Blood Spots as Matrix for Evaluation of Valproate Levels and the Immediate and Delayed Metabolomic Changes Induced by Single Valproate Dose Treatment
Dried Blood Spots as Matrix for Evaluation of Valproate Levels and the Immediate and Delayed Metabolomic Changes Induced by Single Valproate Dose Treatment Abstract Abstract The immediate and delayed metabolic changes in rats treated with valproate (VPA), a drug used for the treatment of epilepsy, were profiled. An est...
PMC6831770
core_pubmed_pmc
Effect of Pterostilbene, a Natural Analog of Resveratrol, on the Activity of some Antiepileptic Drugs in the Acute Seizure Tests in Mice
Effect of Pterostilbene, a Natural Analog of Resveratrol, on the Activity of some Antiepileptic Drugs in the Acute Seizure Tests in Mice Abstract Pterostilbene (PTE), a natural analog of resveratrol, is available both as a diet ingredient and a dietary supplement. The present study was undertaken to assess the effect o...
PMC4407414
core_pubmed_pmc
Increased systemic exposures of artemether and dihydroartemisinin in infants under 5 kg with uncomplicated Plasmodium falciparum malaria treated with artemether-lumefantrine (Coartem®)
Increased systemic exposures of artemether and dihydroartemisinin in infants under 5 kg with uncomplicated Plasmodium falciparum malaria treated with artemether-lumefantrine (Coartem®) Abstract Abstract Background Artemether-lumefantrine (AL) dispersible formulation was developed for the treatment of uncomplicated Plas...
PMC6901793
core_pubmed_pmc
Status of Recombinant Factor VIII Concentrate Treatment for Hemophilia A in Italy: Characteristics and Clinical Benefits
Status of Recombinant Factor VIII Concentrate Treatment for Hemophilia A in Italy: Characteristics and Clinical Benefits Abstract Abstract The current interest in recombinant factor VIII (rFVIII) products stems from the fact that they offer a technological solution to prolonging the half-life of and reducing the risk o...
PMC8417876
core_pubmed_pmc
Pharmacodynamics and Pharmacokinetics of Injectable Pimobendan and Its Metabolite, O-Desmethyl-Pimobendan, in Healthy Dogs
Pharmacodynamics and Pharmacokinetics of Injectable Pimobendan and Its Metabolite, O-Desmethyl-Pimobendan, in Healthy Dogs Abstract Objectives: This study was designed to thoroughly evaluate the effects of bolus pimobendan at a dose of 0.15 mg/kg on cardiac functions, hemodynamics, and electrocardiographic parameters t...
PMC10014699
core_pubmed_pmc
The randomized, single‐ and multiple‐ ascending dose studies of the safety, tolerability, pharmacokinetics of CSPCHA115 in healthy Chinese subjects
The randomized, single‐ and multiple‐ ascending dose studies of the safety, tolerability, pharmacokinetics of CSPCHA115 in healthy Chinese subjects Abstract Abstract CSPCHA115 is a highly selective and potent antagonist of chemoattractant receptor‐homologous molecule expressed on TH2 cells (CRTH2). This study aimed to ...
PMC11859694
core_pubmed_pmc
Bioconjugation of Podophyllotoxin and Nanosystems: Approaches for Boosting Its Biopharmaceutical and Antitumoral Profile
Bioconjugation of Podophyllotoxin and Nanosystems: Approaches for Boosting Its Biopharmaceutical and Antitumoral Profile Abstract Abstract Podophyllotoxin is a natural compound belonging to the lignan family and is well-known for its great antitumor activity. However, it shows several limitations, such as severe side e...
PMC9026419
core_pubmed_pmc
Repeated-Dose Pharmacodynamics of Pimobendan in Healthy Cats
Repeated-Dose Pharmacodynamics of Pimobendan in Healthy Cats Abstract Abstract Simple Summary The dosing of pimobendan in cats is determined with reference to the effects of a single dose, although pimobendan is normally administered in repeated doses. In this study, the pharmacodynamics of repeated and multiple-dose p...
PMC12816428
core_pubmed_pmc
Model‐Informed Deep Q‐Networks to Guide Infliximab Dosing in Pediatric Crohn’s Disease
Model‐Informed Deep Q‐Networks to Guide Infliximab Dosing in Pediatric Crohn’s Disease Abstract Abstract Model‐informed precision dosing (MIPD) utilizes pharmacokinetic/pharmacodynamic (PK/PD) models to optimize drug therapy. However, conventional MIPD often requires manual simulation and regimen selection, which are t...
PMC8267123
core_pubmed_pmc
Preoperative histogram parameters of dynamic contrast‐enhanced MRI as a potential imaging biomarker for assessing the expression of Ki‐67 in prostate cancer
Preoperative histogram parameters of dynamic contrast‐enhanced MRI as a potential imaging biomarker for assessing the expression of Ki‐67 in prostate cancer Abstract Abstract Purpose To investigate whether preoperative histogram parameters of dynamic contrast‐enhanced MRI (DCE‐MRI) can assess the expression of Ki‐67 in...
PMC9060532
core_pubmed_pmc
Pharmacokinetic profile and metabolite identification of bornyl caffeate and caffeic acid in rats by high performance liquid chromatography coupled with mass spectrometry †
Pharmacokinetic profile and metabolite identification of bornyl caffeate and caffeic acid in rats by high performance liquid chromatography coupled with mass spectrometry † Abstract Bornyl caffeate was initially discovered as a bioactive compound in medicinal plants. Despite the promising pharmacological activities inc...
PMC4203516
core_pubmed_pmc
Combined MTOR and autophagy inhibition
Combined MTOR and autophagy inhibition Abstract The combination of temsirolimus (TEM), an MTOR inhibitor, and hydroxychloroquine (HCQ), an autophagy inhibitor, augments cell death in preclinical models. This phase 1 dose-escalation study evaluated the maximum tolerated dose (MTD), safety, preliminary activity, pharmaco...
PMC11836065
core_pubmed_pmc
Associations of long-term exposure to nitrogen oxides with all-cause and cause-specific mortality
Associations of long-term exposure to nitrogen oxides with all-cause and cause-specific mortality Abstract Associations between long-term exposure to nitrogen oxides (NO x ) and cause-specific mortality remain insufficiently explored. This study utilizes data from 502,040 participants registered in the UK Biobank. Time...
PMC7066271
core_pubmed_pmc
A drug–drug interaction study of a novel, selective urate reabsorption inhibitor dotinurad and the non-steroidal anti-inflammatory drug oxaprozin in healthy adult males
A drug–drug interaction study of a novel, selective urate reabsorption inhibitor dotinurad and the non-steroidal anti-inflammatory drug oxaprozin in healthy adult males Abstract Background Dotinurad is a novel, selective urate reabsorption inhibitor, which reduces serum uric acid levels by inhibiting the urate transpor...
PMC8021041
core_pubmed_pmc
Knowledge, Perception, and Antibiotic Prescribing Practice in the Intensive Care Unit: Findings from the Malaysian Public Setting
Knowledge, Perception, and Antibiotic Prescribing Practice in the Intensive Care Unit: Findings from the Malaysian Public Setting Abstract A BSTRACT Introduction: Approach to managing infection in the intensive care unit (ICU) often varies between institutions and not many readily adapt to available local guidelines de...
PMC12256690
core_pubmed_pmc
Use of Model‐Based Meta‐Analysis to Inform the Design of Early Clinical Trials of Anti‐Amyloid Beta Therapies in Alzheimer's Disease
Use of Model‐Based Meta‐Analysis to Inform the Design of Early Clinical Trials of Anti‐Amyloid Beta Therapies in Alzheimer's Disease Abstract ABSTRACT To inform an efficient development of new investigational anti‐amyloid beta (anti‐Aβ) monoclonal antibodies (mAbs), a modeling‐and‐simulation‐based strategy was proposed...