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PMC11258351 | core_pubmed_pmc | PK/PD investigation of antiviral host matriptase/TMPRSS2 inhibitors in cell models | PK/PD investigation of antiviral host matriptase/TMPRSS2 inhibitors in cell models Abstract Abstract Certain corona- and influenza viruses utilize type II transmembrane serine proteases for cell entry, making these enzymes potential drug targets for the treatment of viral respiratory infections. In this study, the cyto... |
PMC5064154 | core_pubmed_pmc | Concentration-Dependent Synergy and Antagonism of Linezolid and Moxifloxacin in the Treatment of Childhood Tuberculosis: The Dynamic Duo | Concentration-Dependent Synergy and Antagonism of Linezolid and Moxifloxacin in the Treatment of Childhood Tuberculosis: The Dynamic Duo Abstract Background. No treatment regimens have been specifically designed for children, in whom tuberculosis is predominantly intracellular. Given their activity as monotherapy and t... |
PMC9237996 | core_pubmed_pmc | Comparing the Liver Safety Profiles of 4 Next-Generation CGRP Receptor Antagonists to the Hepatotoxic CGRP Inhibitor Telcagepant Using Quantitative Systems Toxicology Modeling | Comparing the Liver Safety Profiles of 4 Next-Generation CGRP Receptor Antagonists to the Hepatotoxic CGRP Inhibitor Telcagepant Using Quantitative Systems Toxicology Modeling Abstract Abstract Calcitonin gene-related peptide (CGRP) signaling inhibitors have shown efficacy in both the acute and preventive treatment of ... |
PMC12424064 | core_pubmed_pmc | Population Pharmacokinetics and Exposure–Response Analysis of Serplulimab in Small Cell Lung Cancer Patients | Population Pharmacokinetics and Exposure–Response Analysis of Serplulimab in Small Cell Lung Cancer Patients Abstract ABSTRACT While PD‐L1 antibodies have demonstrated efficacy in small cell lung cancer, the therapeutic benefits remain limited. To address this unmet medical need, serplulimab was developed as an innovat... |
PMC10635337 | core_pubmed_pmc | Pharmacokinetic/Pharmacodynamic Target Attainment of Tigecycline in Patients with Hepatic Impairment in a Real-World Setting | Pharmacokinetic/Pharmacodynamic Target Attainment of Tigecycline in Patients with Hepatic Impairment in a Real-World Setting Abstract Background: This study aimed to investigate the pharmacokinetic/pharmacodynamic (PK/PD) target attainment of various tigecycline dosing regimens in real-world patients with impaired live... |
PMC12381602 | core_pubmed_pmc | Spotlight commentary: Treatment of multidrug‐resistant Gram‐negative infections in the era of growing antimicrobial resistance | Spotlight commentary: Treatment of multidrug‐resistant Gram‐negative infections in the era of growing antimicrobial resistance Results KEY FINDINGS AND CLINICAL IMPLICATIONS In recent years, several new beta‐lactams, such as ceftazidime/avibactam, ceftolozane/tazobactam, meropenem/vaborbactam, imipenem/relebactam, cefi... |
PMC9303355 | core_pubmed_pmc | Pharmacokinetic and pharmacodynamic equivalence of Biocon's biosimilar Insulin‐R with the US ‐licensed Humulin® R formulation in healthy subjects: Results from the RHINE ‐1 ( Recombinant Human INsulin Equivalence‐1 ) study | Pharmacokinetic and pharmacodynamic equivalence of Biocon's biosimilar Insulin‐R with the US ‐licensed Humulin® R formulation in healthy subjects: Results from the RHINE ‐1 ( Recombinant Human INsulin Equivalence‐1 ) study Abstract Abstract Aim To establish equivalence in the pharmacokinetic (PK) and pharmacodynamic (P... |
PMC8388457 | core_pubmed_pmc | Evaluation of a Tasteless Enrofloxacin Pharmaceutical Preparation for Cats. Naive Pooled-Sample Approach to Study Its Pharmacokinetics | Evaluation of a Tasteless Enrofloxacin Pharmaceutical Preparation for Cats. Naive Pooled-Sample Approach to Study Its Pharmacokinetics Abstract Abstract Simple Summary Enrofloxacin has low oral bioavailability in cats. Additionally, its unpleasant taste is linked to profuse salivation and vomiting, and the cat’s refusa... |
PMC12931723 | core_pubmed_pmc | A modelling framework to characterize the impact of antibiotics on the gut microbiota diversity | A modelling framework to characterize the impact of antibiotics on the gut microbiota diversity Abstract ABSTRACT Metagenomic sequencing deepened our knowledge about the role of the intestinal microbiota in human health, and several studies with various methodologies explored its dynamics during antibiotic treatments. ... |
PMC10718298 | core_pubmed_pmc | Exploring Route-Specific Pharmacokinetics of PFAS in Mice by Coupling in Vivo Tests and Physiologically Based Toxicokinetic Models | Exploring Route-Specific Pharmacokinetics of PFAS in Mice by Coupling in Vivo Tests and Physiologically Based Toxicokinetic Models Abstract Abstract Background: Oral ingestion, inhalation, and skin contact are important exposure routes for humans to uptake per- and polyfluoroalkyl substances (PFAS). However, nasal and ... |
PMC7762146 | core_pubmed_pmc | Exploring the Multifaceted Therapeutic Potential of Withaferin A and Its Derivatives | Exploring the Multifaceted Therapeutic Potential of Withaferin A and Its Derivatives Abstract Withaferin A (WA), a manifold studied, C28-steroidal lactone withanolide found in Withania somnifera . Given its unique beneficial effects, it has gathered attention in the era of modern science. Cancer, being considered a “ho... |
PMC8205585 | core_pubmed_pmc | Development and Validation of a UPLC-MS/MS Method for the Quantitative Determination and Pharmacokinetic Analysis of Cirsimarin in Rat Plasma | Development and Validation of a UPLC-MS/MS Method for the Quantitative Determination and Pharmacokinetic Analysis of Cirsimarin in Rat Plasma Abstract Cirsimarin is a bioactive antilipogenic flavonoid isolated from the cotyledons of Abrus precatorius and represents one of the most abundant flavonoids present in this pl... |
PMC9552737 | core_pubmed_pmc | Development of immunohistochemistry for detecting fluvoxamine in rat tissues using newly prepared monoclonal antibody: its precise localization in small intestine, kidney, and liver of rats | Development of immunohistochemistry for detecting fluvoxamine in rat tissues using newly prepared monoclonal antibody: its precise localization in small intestine, kidney, and liver of rats Abstract A monoclonal antibody (mAb) was produced against a fluvoxamine (FLV)-bovine serum albumin conjugate that was specific to ... |
PMC9843174 | core_pubmed_pmc | Phase Ib open-label, multicenter study of pixatimod, an activator of TLR9, in combination with nivolumab in subjects with microsatellite-stable metastatic colorectal cancer, metastatic pancreatic ductal adenocarcinoma and other solid tumors | Phase Ib open-label, multicenter study of pixatimod, an activator of TLR9, in combination with nivolumab in subjects with microsatellite-stable metastatic colorectal cancer, metastatic pancreatic ductal adenocarcinoma and other solid tumors Abstract Abstract Background Pixatimod is a unique activator of the Toll-like R... |
PMC7038275 | core_pubmed_pmc | Differential Impact of Nevirapine on Artemether-Lumefantrine Pharmacokinetics in Individuals Stratified by CYP2B6 c.516G>T Genotypes | Differential Impact of Nevirapine on Artemether-Lumefantrine Pharmacokinetics in Individuals Stratified by CYP2B6 c.516G>T Genotypes Abstract There is an increased recognition of the need to identify and quantify the impact of genetic polymorphisms on drug-drug interactions. This study investigated the pharmacogenetics... |
PMC4392966 | core_pubmed_pmc | Pharmacodynamics Must Inform Statistics: An Example from a Cocaine Dependence Pharmacotherapy Trial | Pharmacodynamics Must Inform Statistics: An Example from a Cocaine Dependence Pharmacotherapy Trial Abstract Background. There is no FDA-approved medication for cocaine dependence or consensus on the statistical approach for analyzing data from cocaine dependence pharmacotherapy trials. The goal of this paper is to ill... |
PMC3154497 | core_pubmed_pmc | Clinical Pharmacology of Chemotherapy Agents in Older People with Cancer | Clinical Pharmacology of Chemotherapy Agents in Older People with Cancer Abstract Populations around the world are aging, and the associated increase in cancer incidence has led to the recognition of the importance of geriatric oncology. Chronological age is a poor determinant of pharmacological response to cancer chem... |
PMC6430889 | core_pubmed_pmc | Pharmacokinetics and pharmacodynamics of intravenous esomeprazole at 2 different dosages in dogs | Pharmacokinetics and pharmacodynamics of intravenous esomeprazole at 2 different dosages in dogs Abstract Background Although the demand for esomeprazole is increasing in veterinary medicine, the pharmacokinetics (PK) and pharmacodynamics of esomeprazole have been described in only a few studies. Objective To determine... |
PMC11646943 | core_pubmed_pmc | Global sensitivity analysis of Open Systems Pharmacology Suite physiologically based pharmacokinetic models | Global sensitivity analysis of Open Systems Pharmacology Suite physiologically based pharmacokinetic models Abstract Abstract Sensitivity analyses are important components of physiologically based pharmacokinetic (PBPK) model development and are required by regulatory agencies for PBPK submissions. They assess the impa... |
PMC12081410 | core_pubmed_pmc | Bioactive compound combinations from Rhodiola tangutica alleviate pulmonary vascular remodeling in high-altitude pulmonary hypertension rats through the PI3K–AKT pathway | Bioactive compound combinations from Rhodiola tangutica alleviate pulmonary vascular remodeling in high-altitude pulmonary hypertension rats through the PI3K–AKT pathway Abstract Background Hypoxia-induced pulmonary vascular remodeling is central to the development of high-altitude pulmonary hypertension (HAPH). Rhodio... |
PMC6151756 | core_pubmed_pmc | Novel Anti-Tuberculosis Nanodelivery Formulation of Ethambutol with Graphene Oxide | Novel Anti-Tuberculosis Nanodelivery Formulation of Ethambutol with Graphene Oxide Abstract Abstract Tuberculosis (TB) is a bacterial disease responsible for millions of infections and preventable deaths each year. Its treatment is complicated by patients’ noncompliance due to dosing frequency, lengthy treatment, and a... |
PMC8944228 | core_pubmed_pmc | Chronic Behavioral Manipulation via Orally Delivered Chemogenetic Actuator in Macaques | Chronic Behavioral Manipulation via Orally Delivered Chemogenetic Actuator in Macaques Abstract Abstract The chemogenetic technology referred to as designer receptors exclusively activated by designer drugs (DREADDs) offers reversible means to control neuronal activity for investigating its functional correlation with ... |
PMC12930023 | core_pubmed_pmc | Population pharmacokinetics of lumefantrine in pregnant and non‐pregnant women with uncomplicated Plasmodium falciparum malaria in Western Kenya | Population pharmacokinetics of lumefantrine in pregnant and non‐pregnant women with uncomplicated Plasmodium falciparum malaria in Western Kenya Abstract Aim This study intends to assess the pharmacokinetic properties and treatment response of lumefantrine in pregnant and non‐pregnant women with uncomplicated Plasmodiu... |
PMC10894853 | core_pubmed_pmc | Distribution and elimination kinetics of midazolam and metabolites after post-resuscitation care: a prospective observational study | Distribution and elimination kinetics of midazolam and metabolites after post-resuscitation care: a prospective observational study Abstract Abstract Administration of sedatives for post-resuscitation care can complicate the determination of the optimal timing to avoid inappropriate, pessimistic prognostications. This ... |
PMC12672762 | core_pubmed_pmc | From pharmacokinetic-guided FVIII prophylaxis to low-dose Emicizumab prophylaxis: a pilot study revealed a flush of hope | From pharmacokinetic-guided FVIII prophylaxis to low-dose Emicizumab prophylaxis: a pilot study revealed a flush of hope Abstract Limited studies investigated the low dose emicizumab prophylaxis, especially in patients switched from pharmacokinetic (PK)-guided FVIII prophylaxis. A retrospective study was conducted amon... |
PMC11616243 | core_pubmed_pmc | RSM01, a novel respiratory syncytial virus monoclonal antibody: preclinical characterization and results of a first-in-human, randomised clinical trial | RSM01, a novel respiratory syncytial virus monoclonal antibody: preclinical characterization and results of a first-in-human, randomised clinical trial Abstract Abstract Background Respiratory syncytial virus (RSV) is a leading cause of lower respiratory tract disease among infants and young children worldwide, especia... |
PMC7406860 | core_pubmed_pmc | Redox Imbalance and Oxidative DNA Damage During Isoniazid Treatment of HIV-Associated Tuberculosis: A Clinical and Translational Pharmacokinetic Study | Redox Imbalance and Oxidative DNA Damage During Isoniazid Treatment of HIV-Associated Tuberculosis: A Clinical and Translational Pharmacokinetic Study Abstract Background The potential for hepatotoxicity during isoniazid-based tuberculosis (TB) treatment presents a major challenge for TB control programs worldwide. We ... |
PMC9862189 | core_pubmed_pmc | In Silico Identification of 1-DTP Inhibitors of Corynebacterium diphtheriae Using Phytochemicals from Andrographis paniculata | In Silico Identification of 1-DTP Inhibitors of Corynebacterium diphtheriae Using Phytochemicals from Andrographis paniculata Abstract Abstract A number of phytochemicals have been identified as promising drug molecules against a variety of diseases using an in-silico approach. The current research uses this approach t... |
PMC9502275 | core_pubmed_pmc | Understanding the Pharmacology of COVID-19 mRNA Vaccines: Playing Dice with the Spike? | Understanding the Pharmacology of COVID-19 mRNA Vaccines: Playing Dice with the Spike? Abstract Coronavirus disease-19 (COVID-19) mRNA vaccines are the mainstays of mass vaccination campaigns in most Western countries. However, the emergency conditions in which their development took place made it impossible to fully c... |
PMC7722752 | core_pubmed_pmc | First-in-human Phase 1 open label study of the BET inhibitor ODM-207 in patients with selected solid tumours | First-in-human Phase 1 open label study of the BET inhibitor ODM-207 in patients with selected solid tumours Abstract Abstract Background Bromodomain and extra-terminal domain (BET) proteins are reported to be epigenetic anti-cancer drug targets. This first-in-human study evaluated the safety, pharmacokinetics and prel... |
PMC8719395 | core_pubmed_pmc | Biologic TNF-α inhibitors reduce microgliosis, neuronal loss, and tau phosphorylation in a transgenic mouse model of tauopathy | Biologic TNF-α inhibitors reduce microgliosis, neuronal loss, and tau phosphorylation in a transgenic mouse model of tauopathy Abstract Background Tumor necrosis factor-α (TNF-α) plays a central role in Alzheimer’s disease (AD) pathology, making biologic TNF-α inhibitors (TNFIs), including etanercept, viable therapeuti... |
PMC9017614 | core_pubmed_pmc | Preserved pharmacokinetics and pharmacodynamics of insulin degludec and liraglutide when administered as insulin degludec/liraglutide in a Chinese population | Preserved pharmacokinetics and pharmacodynamics of insulin degludec and liraglutide when administered as insulin degludec/liraglutide in a Chinese population Abstract Abstract We report the findings of a single‐dose, randomized, three‐period cross‐over, clinical trial in healthy Chinese individuals ( n = 24) comparing ... |
PMC8416757 | core_pubmed_pmc | Dynamic Modeling of Mitochondrial Membrane Potential Upon Exposure to Mitochondrial Inhibitors | Dynamic Modeling of Mitochondrial Membrane Potential Upon Exposure to Mitochondrial Inhibitors Abstract Mitochondria are the main bioenergetic organelles of cells. Exposure to chemicals targeting mitochondria therefore generally results in the development of toxicity. The cellular response to perturbations in cellular ... |
PMC9842843 | core_pubmed_pmc | Synthesis and preclinical evaluation of novel 99m Tc-labeled PSMA ligands for radioguided surgery of prostate cancer | Synthesis and preclinical evaluation of novel 99m Tc-labeled PSMA ligands for radioguided surgery of prostate cancer Abstract Abstract Background Radioguided surgery (RGS) has recently emerged as a valuable new tool in the management of recurrent prostate cancer (PCa). After preoperative injection of a 99m Tc-labeled p... |
PMC9042341 | core_pubmed_pmc | Prediction of Corresponding Dose of Transdermal Blonanserin to Oral Dose Based on Dopamine D 2 Receptor Occupancy | Prediction of Corresponding Dose of Transdermal Blonanserin to Oral Dose Based on Dopamine D 2 Receptor Occupancy Abstract Abstract Background/Purpose Blonanserin is an atypical antipsychotic, a potent selective antagonist of dopamine D 2 receptor (D 2 ), prescribed as oral formulations in patients with schizophrenia. ... |
PMC6034581 | core_pubmed_pmc | A Novel Flavonoid Composition Targets Androgen Receptor Signaling and Inhibits Prostate Cancer Growth in Preclinical Models 1 2 | A Novel Flavonoid Composition Targets Androgen Receptor Signaling and Inhibits Prostate Cancer Growth in Preclinical Models 1 2 Abstract The high prevalence and long latency period of prostate cancer (PCa) provide a unique opportunity to control disease progression with dietary and nutraceutical approaches. We develope... |
PMC8523013 | core_pubmed_pmc | Sedation Effects Produced by a Ciprofol Initial Infusion or Bolus Dose Followed by Continuous Maintenance Infusion in Healthy Subjects: A Phase 1 Trial | Sedation Effects Produced by a Ciprofol Initial Infusion or Bolus Dose Followed by Continuous Maintenance Infusion in Healthy Subjects: A Phase 1 Trial Abstract Abstract Introduction The effects of continuous infusions of ciprofol on its pharmacodynamic and pharmacokinetic properties and safety profiles in healthy Chin... |
PMC7555336 | core_pubmed_pmc | Self-Report for Measuring and Predicting Medication Adherence: Experts’ Experience in Predicting Adherence in Stable Psychiatric Outpatients and in Pharmacokinetics | Self-Report for Measuring and Predicting Medication Adherence: Experts’ Experience in Predicting Adherence in Stable Psychiatric Outpatients and in Pharmacokinetics Abstract The Problem Poor adherence to appropriately prescribed medication is a global challenge for psychiatrists. Prior Studies Measuring adherence is co... |
PMC12744204 | core_pubmed_pmc | Optimizing Cardiovascular Treatment in Non-Small Cell Lung Cancer: A Comprehensive Computational Approach for Assessment of Drug-Drug Interactions Between Tyrosine Kinase Inhibitors and Cardiovascular Drugs | Optimizing Cardiovascular Treatment in Non-Small Cell Lung Cancer: A Comprehensive Computational Approach for Assessment of Drug-Drug Interactions Between Tyrosine Kinase Inhibitors and Cardiovascular Drugs Abstract Background As lung cancer treatment has progressed, there has been an increase in awareness of the short... |
PMC8861132 | core_pubmed_pmc | R-etodolac is a more potent Wnt signaling inhibitor than enantiomer, S-etodolac | R-etodolac is a more potent Wnt signaling inhibitor than enantiomer, S-etodolac Abstract Etodolac is an FDA-approved nonsteroidal anti-inflammatory drug (NSAID) used to treat a variety of inflammatory diseases. The drug is administered as a racemate (50/50 mixture of R- and S- enantiomers), however, studies have shown ... |
PMC4501448 | core_pubmed_pmc | Differential benefit risk assessment of DOACs in the treatment of venous thromboembolism: focus on dabigatran | Differential benefit risk assessment of DOACs in the treatment of venous thromboembolism: focus on dabigatran Abstract Abstract Venous thromboembolism includes deep vein thrombosis and pulmonary embolism and is a serious medical condition that requires anticoagulation as part of treatment. Currently, standard therapy c... |
PMC10662790 | core_pubmed_pmc | Intranasal Oxytocin in Pediatric Populations: Exploring the Potential for Reducing Irritability and Modulating Neural Responses: A Mini Review | Intranasal Oxytocin in Pediatric Populations: Exploring the Potential for Reducing Irritability and Modulating Neural Responses: A Mini Review Abstract Endogenous neuropeptide Oxytocin (OXT) plays a crucial role in modulating pro-social behavior and the neural response to social/emotional stimuli. Intranasal administra... |
PMC10432875 | core_pubmed_pmc | Pharmacokinetic and pharmacodynamic drug–drug interactions between evogliptin and empagliflozin or dapagliflozin in healthy male volunteers | Pharmacokinetic and pharmacodynamic drug–drug interactions between evogliptin and empagliflozin or dapagliflozin in healthy male volunteers Abstract Abstract Evogliptin (EV) is a novel dipeptidyl peptidase‐4 inhibitor (DPP4i) for glycemic control in patients with type 2 diabetes mellitus (T2DM). This study evaluated th... |
PMC12190732 | core_pubmed_pmc | Pharmacokinetics and Ex Vivo Activity of 7-Methylxanthine, an Inhibitor of Monosodium Urate Crystallization | Pharmacokinetics and Ex Vivo Activity of 7-Methylxanthine, an Inhibitor of Monosodium Urate Crystallization Abstract Abstract Background/Objectives: 7-Methylxanthine (7-MX) is a naturally occurring metabolite of caffeine and theobromine that can inhibit the crystallization of monosodium urate (MSU) and may be useful fo... |
PMC12567947 | core_pubmed_pmc | Analytical Methods for the Determination of Diamorphine (Heroin) in Biological Matrices: A Review | Analytical Methods for the Determination of Diamorphine (Heroin) in Biological Matrices: A Review Abstract Diamorphine (DIM, heroin) is a semi-synthetic opioid that undergoes rapid conversion to 6-monoacetylmorphine and morphine, producing short-lived biomarkers that are difficult to capture during the process. This re... |
PMC10135361 | core_pubmed_pmc | The Current Status and Future Perspectives of Beta-Lactam Therapeutic Drug Monitoring in Critically Ill Patients | The Current Status and Future Perspectives of Beta-Lactam Therapeutic Drug Monitoring in Critically Ill Patients Abstract Beta-lactams (BL) are the first line agents for the antibiotic management of critically ill patients with sepsis or septic shock. BL are hydrophilic antibiotics particularly subject to unpredictable... |
PMC10726570 | core_pubmed_pmc | In vivo study of newly developed albumin-conjugated urate oxidase for gout treatment | In vivo study of newly developed albumin-conjugated urate oxidase for gout treatment Abstract Background Exogenously providing engineered Uox with enhanced half-life is one of the important urate-lowering treatments for gout. The potential of PAT101, a recombinant human albumin (rHA)-conjugated variant, was evaluated a... |
PMC7049619 | core_pubmed_pmc | Synthesis and biological evaluation of a series of 2-(((5-akly/aryl-1 H -pyrazol-3-yl)methyl)thio)-5-alkyl-6-(cyclohexylmethyl)-pyrimidin-4(3 H )-ones as potential HIV-1 inhibitors | Synthesis and biological evaluation of a series of 2-(((5-akly/aryl-1 H -pyrazol-3-yl)methyl)thio)-5-alkyl-6-(cyclohexylmethyl)-pyrimidin-4(3 H )-ones as potential HIV-1 inhibitors Abstract Abstract A series of 2-(((5-akly/aryl-1 H -pyrazol-3-yl)methyl)thio)-5-alkyl-6-(cyclohexylmethyl)-pyrimidin-4(3 H )-ones were synt... |
PMC10161560 | core_pubmed_pmc | Uncovering the Fate and Risks of Intravenously Injected Prussian Blue Nanoparticles in mice by an Integrated Methodology of Toxicology, Pharmacokinetics, Proteomics, and Metabolomics | Uncovering the Fate and Risks of Intravenously Injected Prussian Blue Nanoparticles in mice by an Integrated Methodology of Toxicology, Pharmacokinetics, Proteomics, and Metabolomics Abstract Abstract Background Prussian blue (PB) nanoparticles (NPs) have been intensively investigated for medical applications, but an i... |
PMC9207296 | core_pubmed_pmc | Photoacoustic imaging reveals mechanisms of rapid-acting insulin formulations dynamics at the injection site | Photoacoustic imaging reveals mechanisms of rapid-acting insulin formulations dynamics at the injection site Abstract Abstract Objective Ultra-rapid insulin formulations control postprandial hyperglycemia; however, inadequate understanding of injection site absorption mechanisms is limiting further advancement. We used... |
PMC5656813 | core_pubmed_pmc | Efficacy, Safety, Pharmacokinetics, and Pharmacodynamics of Filgotinib, a Selective JAK‐1 Inhibitor, After Short‐Term Treatment of Rheumatoid Arthritis: Results of Two Randomized Phase IIa Trials | Efficacy, Safety, Pharmacokinetics, and Pharmacodynamics of Filgotinib, a Selective JAK‐1 Inhibitor, After Short‐Term Treatment of Rheumatoid Arthritis: Results of Two Randomized Phase IIa Trials Abstract Objective JAK inhibitors have shown efficacy in rheumatoid arthritis (RA). We undertook this study to test our hypo... |
PMC11807728 | core_pubmed_pmc | Understanding Drug Interactions in Antiplatelet Therapy for Atherosclerotic Vascular Disease: A Systematic Review | Understanding Drug Interactions in Antiplatelet Therapy for Atherosclerotic Vascular Disease: A Systematic Review Abstract ABSTRACT Background Antiplatelet drugs are a cornerstone in managing atherosclerotic vascular disease (ASVD). However, their interactions with other medications present significant challenges to tr... |
PMC8224453 | core_pubmed_pmc | A New PqsR Inverse Agonist Potentiates Tobramycin Efficacy to Eradicate Pseudomonas aeruginosa Biofilms | A New PqsR Inverse Agonist Potentiates Tobramycin Efficacy to Eradicate Pseudomonas aeruginosa Biofilms Abstract Abstract Pseudomonas aeruginosa (PA) infections can be notoriously difficult to treat and are often accompanied by the development of antimicrobial resistance (AMR). Quorum sensing inhibitors (QSI) acting on... |
PMC6556870 | core_pubmed_pmc | Pharmacokinetics of the SABRE agent 4,6-d 2 -nicotinamide and also nicotinamide in rats following oral and intravenous administration | Pharmacokinetics of the SABRE agent 4,6-d 2 -nicotinamide and also nicotinamide in rats following oral and intravenous administration Abstract Abstract To prepare the way for using the isotopically labelled SABRE hyperpolarized 4,6-d 2 -nicotinamide as an MRI agent in humans we have performed an in-vivo study to measur... |
PMC3960627 | core_pubmed_pmc | Prediction of tumour response induced by chemotherapy using modelling of CA-125 kinetics in recurrent ovarian cancer patients | Prediction of tumour response induced by chemotherapy using modelling of CA-125 kinetics in recurrent ovarian cancer patients Abstract Abstract Background: The main objective of the present study was to establish the relationships between CA-125 kinetics and tumour size changes during treatment. Methods: The data from ... |
PMC4870510 | core_pubmed_pmc | Liquid Crystalline Nanoparticles as an Ophthalmic Delivery System for Tetrandrine: Development, Characterization, and In Vitro and In Vivo Evaluation | Liquid Crystalline Nanoparticles as an Ophthalmic Delivery System for Tetrandrine: Development, Characterization, and In Vitro and In Vivo Evaluation Abstract The purpose of this study was to develop novel liquid crystalline nanoparticles (LCNPs) that display improved pre-ocular residence time and ocular bioavailabilit... |
PMC6847991 | core_pubmed_pmc | Improving The Oral Absorption Of Nintedanib By A Self-Microemulsion Drug Delivery System: Preparation And In Vitro/In Vivo Evaluation | Improving The Oral Absorption Of Nintedanib By A Self-Microemulsion Drug Delivery System: Preparation And In Vitro/In Vivo Evaluation Abstract Abstract Objective Nintedanib (NDNB) is a triple receptor tyrosine kinase inhibitor with poor solubility in neutral conditions and low bioavailability. A self-microemulsifying d... |
PMC4330923 | core_pubmed_pmc | Year in review 2013: critical care - respiratory infections | Year in review 2013: critical care - respiratory infections Abstract Abstract Infectious complications, particularly in the respiratory tract of critically ill patients, are related to increased mortality. Severe infection is part of a multiple system illness and female patients with severe sepsis have a worse prognosi... |
PMC11415018 | core_pubmed_pmc | Bioanalysis of free antisense oligonucleotide payload from antibody–oligonucleotide conjugate by hybridization LC-MS/MS | Bioanalysis of free antisense oligonucleotide payload from antibody–oligonucleotide conjugate by hybridization LC-MS/MS Abstract Abstract Background: Antisense oligonucleotides (ASOs) have been conjugated to various moieties, such as peptides, antibodies or Fab regions of antibodies, to enhance their delivery to target... |
PMC2807935 | core_pubmed_pmc | Absorption and distribution of etoricoxib in plasma, CSF, and wound tissue in patients following hip surgery—a pilot study | Absorption and distribution of etoricoxib in plasma, CSF, and wound tissue in patients following hip surgery—a pilot study Abstract Abstract The perioperative administration of selective cyclooxygenase-2 (COX-2)-inhibitors to avoid postoperative pain is an attractive option: they show favorable gastro-intestinal tolera... |
PMC3882305 | core_pubmed_pmc | Pharmacokinetics and 48-week Safety and Antiviral Activity of Fosamprenavir-containing Regimens in HIV-infected 2- to 18-year-old Children | Pharmacokinetics and 48-week Safety and Antiviral Activity of Fosamprenavir-containing Regimens in HIV-infected 2- to 18-year-old Children Abstract Supplemental Digital Content is available in the text. Background: Pharmacokinetics, safety and antiviral activity of twice-daily fosamprenavir with or without ritonavir we... |
PMC10113450 | core_pubmed_pmc | Effects of bariatric surgery on drug pharmacokinetics—Preclinical studies | Effects of bariatric surgery on drug pharmacokinetics—Preclinical studies Abstract Abstract With the rising worldwide obesity rates, bariatric surgeries are increasing. Although the surgery offers an effective treatment option for weight loss, the procedure causes dramatic physiological and metabolic changes. Animal mo... |
PMC6331755 | core_pubmed_pmc | Development of an HPLC–MS/MS method for the determination of ceftolozane/tazobactam in bronchoalveolar lavage fluid | Development of an HPLC–MS/MS method for the determination of ceftolozane/tazobactam in bronchoalveolar lavage fluid Abstract Abstract Aim: We describe the validation of an HPLC–MS/MS method to analyze ceftolozane and tazobactam simultaneously in saline matrixes. Materials & methods: An Agilent 1260 HPLC interfaced to a... |
PMC9913351 | core_pubmed_pmc | Computational Approach to Drug Penetration across the Blood-Brain and Blood-Milk Barrier Using Chromatographic Descriptors | Computational Approach to Drug Penetration across the Blood-Brain and Blood-Milk Barrier Using Chromatographic Descriptors Abstract Abstract Drug penetration through biological barriers is an important aspect of pharmacokinetics. Although the structure of the blood-brain and blood-milk barriers is different, a connecti... |
PMC7140522 | core_pubmed_pmc | The Pyrazolo[3,4-d]pyrimidine Derivative, SCO-201, Reverses Multidrug Resistance Mediated by ABCG2/BCRP | The Pyrazolo[3,4-d]pyrimidine Derivative, SCO-201, Reverses Multidrug Resistance Mediated by ABCG2/BCRP Abstract Abstract ATP-binding cassette (ABC) transporters, such as breast cancer resistance protein (BCRP), are key players in resistance to multiple anti-cancer drugs, leading to cancer treatment failure and cancer-... |
PMC7691079 | core_pubmed_pmc | Pharmacodynamic and pharmacokinetic behavior of landiolol during dobutamine challenge in healthy adults | Pharmacodynamic and pharmacokinetic behavior of landiolol during dobutamine challenge in healthy adults Abstract Background To study the pharmacokinetic and -dynamic behavior of landiolol in the presence of dobutamine in healthy subjects of European ancestry. Methods We conducted a single-center, prospective randomized... |
PMC6021259 | core_pubmed_pmc | Translational inhibition of APP by Posiphen: Efficacy, pharmacodynamics, and pharmacokinetics in the APP/PS1 mouse | Translational inhibition of APP by Posiphen: Efficacy, pharmacodynamics, and pharmacokinetics in the APP/PS1 mouse Abstract Introduction Translational inhibition of amyloid precursor protein (APP) by Posiphen has been shown to reduce APP and its fragments in cell culture, animal models, and mildly cognitively impaired ... |
PMC12396558 | core_pubmed_pmc | Suprachoroidal Injection of Topotecan for Retinoblastoma: A Preclinical Study | Suprachoroidal Injection of Topotecan for Retinoblastoma: A Preclinical Study Abstract Abstract Purpose To assess whether levels of topotecan that are expected to be therapeutic against retinoblastoma tumors can be achieved within the retina and choroid by suprachoroidal injection (SCI) and to assess toxicity and safet... |
PMC11228576 | core_pubmed_pmc | Design, synthesis, and in vitro and in silico studies of morpholine derived thiazoles as bovine carbonic anhydrase-II inhibitors † | Design, synthesis, and in vitro and in silico studies of morpholine derived thiazoles as bovine carbonic anhydrase-II inhibitors † Abstract Abstract Carbonic anhydrase CA-II enzyme is essential for maintaining homeostasis in several processes, including respiration, lipogenesis, gluconeogenesis, calcification, bone res... |
PMC4310326 | core_pubmed_pmc | Bioavailability of everolimus administered as a single 5 mg tablet versus five 1 mg tablets: a randomized, open-label, two-way crossover study of healthy volunteers | Bioavailability of everolimus administered as a single 5 mg tablet versus five 1 mg tablets: a randomized, open-label, two-way crossover study of healthy volunteers Abstract Background The mammalian target of rapamycin (mTOR) inhibitor everolimus has a well-established pharmacokinetics profile. We conducted a randomize... |
PMC9177239 | core_pubmed_pmc | Phase I Study of Safety, Tolerability, and Efficacy of Tebentafusp Using a Step-Up Dosing Regimen and Expansion in Patients With Metastatic Uveal Melanoma | Phase I Study of Safety, Tolerability, and Efficacy of Tebentafusp Using a Step-Up Dosing Regimen and Expansion in Patients With Metastatic Uveal Melanoma Abstract PURPOSE This phase I study aimed to define the recommended phase II dose (RP2D) of tebentafusp, a first-in-class T-cell receptor/anti-CD3 bispecific protein... |
PMC8976035 | core_pubmed_pmc | Pharmacodynamic, pharmacokinetic, and phase 1a study of bisthianostat, a novel histone deacetylase inhibitor, for the treatment of relapsed or refractory multiple myeloma | Pharmacodynamic, pharmacokinetic, and phase 1a study of bisthianostat, a novel histone deacetylase inhibitor, for the treatment of relapsed or refractory multiple myeloma Abstract Abstract HDAC inhibitors (HDACis) have been intensively studied for their roles and potential as drug targets in T-cell lymphomas and other ... |
PMC10600534 | core_pubmed_pmc | Biliary excretion and pharmacokinetics of several fluoroquinolones after intravenous injection in rabbits | Biliary excretion and pharmacokinetics of several fluoroquinolones after intravenous injection in rabbits Abstract Abstract The aim of this study was to measure the concentrations of enrofloxacin (ERFX) and other fluoroquinolones; orbifloxacin (OBFX), marbofloxacin (MBFX), and ofloxacin (OFLX) in the plasma and bile of... |
PMC7803984 | core_pubmed_pmc | Evaluation for pharmacokinetic exposure of cytotoxic anticancer drugs in elderly patients receiving (R-)CHOP therapy | Evaluation for pharmacokinetic exposure of cytotoxic anticancer drugs in elderly patients receiving (R-)CHOP therapy Abstract (R-)miniCHOP therapy, which delivers approximately half-doses of the (R-)CHOP regimen, has shown efficacy and safety in patients who are more than 80 years old. This study aimed to compare the a... |
PMC12823294 | core_pubmed_pmc | Evaluating the Impact of Intestinal Bile Salts on Drug Absorption Using PBPK Modeling: Case Studies With Efavirenz, Cinnarizine, and Posaconazole | Evaluating the Impact of Intestinal Bile Salts on Drug Absorption Using PBPK Modeling: Case Studies With Efavirenz, Cinnarizine, and Posaconazole Abstract ABSTRACT A high number of poorly soluble compounds are being developed; thus, understanding the factors that influence their absorption is critical. Intestinal bile ... |
PMC4410963 | core_pubmed_pmc | Medical Marijuana in the Workplace | Medical Marijuana in the Workplace Abstract Abstract Although possession and use of marijuana is prohibited by federal law, legalization in four states (Alaska, Colorado, Oregon, and Washington) and allowance for palliation and therapy in 19 others may reposition the drug away from the fringes of society. This evolving... |
PMC9571628 | core_pubmed_pmc | Development of UPLC-MS/MS Method to Study the Pharmacokinetic Interaction between Sorafenib and Dapagliflozin in Rats | Development of UPLC-MS/MS Method to Study the Pharmacokinetic Interaction between Sorafenib and Dapagliflozin in Rats Abstract Abstract Sorafenib (SOR), an inhibitor of multiple kinases, is a classic targeted drug for advanced hepatocellular carcinoma (HCC) which often coexists with type 2 diabetes mellitus (T2DM). Dap... |
PMC9952017 | core_pubmed_pmc | Therapeutic Drug Monitoring of Amikacin in Neutropenic Oncology Patients | Therapeutic Drug Monitoring of Amikacin in Neutropenic Oncology Patients Abstract Abstract Amikacin is the antibiotic of choice for the treatment of Gram-negative infections, namely, those in neutropenic oncology patients. No populational pharmacokinetic studies are currently available reporting amikacin pharmacokineti... |
PMC7304851 | core_pubmed_pmc | First-in-human phase I study of immunomodulatory E7046, an antagonist of PGE 2 -receptor E-type 4 (EP4), in patients with advanced cancers | First-in-human phase I study of immunomodulatory E7046, an antagonist of PGE 2 -receptor E-type 4 (EP4), in patients with advanced cancers Abstract Background E7046 is a highly selective, small-molecule antagonist of the E-type prostanoid receptor 4 (EP4) for prostaglandin E2, an immunosuppressive mediator of the tumor... |
PMC9455594 | core_pubmed_pmc | SimRFlow: An R-based workflow for automated high-throughput PBPK simulation with the Simcyp ® simulator | SimRFlow: An R-based workflow for automated high-throughput PBPK simulation with the Simcyp ® simulator Abstract Abstract SimRFlow is a high-throughput physiologically based pharmacokinetic (PBPK) modelling tool which uses Certara’s Simcyp® simulator. The workflow is comprised of three main modules: 1) a Data Collectio... |
PMC12106615 | core_pubmed_pmc | Population pharmacokinetics of colistin sulfate in critically ill patients based on NONMEM | Population pharmacokinetics of colistin sulfate in critically ill patients based on NONMEM Abstract Abstract As the last defense against multidrug-resistant gram-negative bacteria, colistin sulfate’s clinical use, which is often empirical, risks resistance and adverse reactions. This study aimed to develop a population... |
PMC12859863 | core_pubmed_pmc | Pharmacokinetic interactions and clinical implications of PPIs and CDKIs in breast cancer: a systematic review and meta-analysis | Pharmacokinetic interactions and clinical implications of PPIs and CDKIs in breast cancer: a systematic review and meta-analysis Abstract Background Breast cancer is the fourth leading cause of cancer mortality worldwide. New drugs, such as cyclin-dependent kinase 4/6 inhibitors (CDKIs), increase the life expectancy of... |
PMC7937819 | core_pubmed_pmc | Pharmacokinetics, safety, and immunogenicity of HLX03, an adalimumab biosimilar, compared with reference biologic in healthy Chinese male volunteers: Results of a randomized, double‐blind, parallel‐controlled, phase 1 study | Pharmacokinetics, safety, and immunogenicity of HLX03, an adalimumab biosimilar, compared with reference biologic in healthy Chinese male volunteers: Results of a randomized, double‐blind, parallel‐controlled, phase 1 study Abstract Abstract The primary objective of this randomized, double‐blind, parallel‐controlled st... |
PMC10278458 | core_pubmed_pmc | Effect of c o‐medications and potential risk factors of high‐dose methotrexate‐mediated acute hepatotoxicity in patients with osteosarcoma | Effect of c o‐medications and potential risk factors of high‐dose methotrexate‐mediated acute hepatotoxicity in patients with osteosarcoma Abstract Abstract Background Taiwanese patients frequently experience severe hepatotoxicity associated with high‐dose methotrexate (HD‐MTX) treatment, which interferes with subseque... |
PMC8298373 | core_pubmed_pmc | Population Pharmacokinetic Analysis of Indacaterol/Glycopyrronium/Mometasone Furoate After Administration of Combination Therapies Using the Breezhaler ® Device in Patients with Asthma | Population Pharmacokinetic Analysis of Indacaterol/Glycopyrronium/Mometasone Furoate After Administration of Combination Therapies Using the Breezhaler ® Device in Patients with Asthma Abstract Background and Objective Clinical evidence suggests no clinically relevant pharmacokinetic interactions between indacaterol (I... |
PMC9306620 | core_pubmed_pmc | Relative Bioavailability and Food Effect of GSK3640254 Tablet and Capsule Formulations in Healthy Participants | Relative Bioavailability and Food Effect of GSK3640254 Tablet and Capsule Formulations in Healthy Participants Abstract Abstract GSK3640254 is a next‐generation maturation inhibitor with demonstrated potency across HIV‐1 subtypes and a high barrier to emergent resistance. This phase I, 2‐part, randomized, open‐label st... |
PMC7310276 | core_pubmed_pmc | Effect of age on pharmacokinetics, efficacy, and safety of galcanezumab treatment in adult patients with migraine: results from six phase 2 and phase 3 randomized clinical trials | Effect of age on pharmacokinetics, efficacy, and safety of galcanezumab treatment in adult patients with migraine: results from six phase 2 and phase 3 randomized clinical trials Abstract Abstract Background Migraine clinical profile may change with age, making it necessary to verify that migraine treatments are equall... |
PMC9144259 | core_pubmed_pmc | Poloxamer 407/188 Binary Thermosensitive Gel as a Moxidectin Delivery System: In Vitro Release and In Vivo Evaluation | Poloxamer 407/188 Binary Thermosensitive Gel as a Moxidectin Delivery System: In Vitro Release and In Vivo Evaluation Abstract Moxidectin (MXD) is an antiparasitic drug used extensively in veterinary clinics. In this study, to develop a new formulation of MXD, a thermosensitive gel of MXD (MXD-TG) was prepared based on... |
PMC7216797 | core_pubmed_pmc | Effects of cytochrome P450 oxidoreductase genotypes on the pharmacokinetics of amlodipine in healthy Korean subjects | Effects of cytochrome P450 oxidoreductase genotypes on the pharmacokinetics of amlodipine in healthy Korean subjects Abstract Abstract Background The aim of this study was to investigate the effects of P450 oxidoreductase ( POR ) genetic polymorphisms on the pharmacokinetic parameters of amlodipine. Methods After a sin... |
PMC7231776 | core_pubmed_pmc | Pharmacokinetics and Metabolism Research of Shenkang Injection in Rats Based on UHPLC-MS/MS and UHPLC-Q-Orbitrap HRMS | Pharmacokinetics and Metabolism Research of Shenkang Injection in Rats Based on UHPLC-MS/MS and UHPLC-Q-Orbitrap HRMS Abstract Abstract Purpose Shenkang injection, a traditional Chinese herbal prescription, had been widely used in renal disease due to its perfect curative effect. In this research, a novel, sensitive, a... |
PMC6631943 | core_pubmed_pmc | Physiologically Relevant In Vitro-In Vivo Correlation (IVIVC) Approach for Sildenafil with Site-Dependent Dissolution | Physiologically Relevant In Vitro-In Vivo Correlation (IVIVC) Approach for Sildenafil with Site-Dependent Dissolution Abstract Abstract This study aimed to establish a physiologically relevant in vitro-in vivo correlation (IVIVC) model reflecting site-dependent dissolution kinetics for sildenafil based on population-ph... |
PMC9819597 | core_pubmed_pmc | What Is Known about Midazolam? A Bibliometric Approach of the Literature | What Is Known about Midazolam? A Bibliometric Approach of the Literature Abstract Midazolam is a drug with actions towards the central nervous system producing sedative and anticonvulsants effects, used for sedation and seizures treatments. A better understanding about its effects in the different scenarios presented i... |
PMC10905536 | core_pubmed_pmc | Design and use of an ex vivo peripheral simulating bioreactor system for pharmacokinetic analysis of a drug coated stent | Design and use of an ex vivo peripheral simulating bioreactor system for pharmacokinetic analysis of a drug coated stent Abstract Abstract Currently, there are no ex vivo systems that can model the motion of peripheral arteries and allow for the evaluation of pharmacokinetics (PK) of endovascular devices. The objective... |
PMC7779838 | core_pubmed_pmc | Quantifying ADC bystander payload penetration with cellular resolution using pharmacodynamic mapping | Quantifying ADC bystander payload penetration with cellular resolution using pharmacodynamic mapping Abstract With the recent approval of 3 new antibody drug conjugates (ADCs) for solid tumors, this class of drugs is gaining momentum for the targeted treatment of cancer. Despite significant investment, there are still ... |
PMC12669667 | core_pubmed_pmc | A nanoMIP sensor for real-time in vivo monitoring of levodopa pharmacokinetics in precision Parkinson’s therapy | A nanoMIP sensor for real-time in vivo monitoring of levodopa pharmacokinetics in precision Parkinson’s therapy Abstract Real-time in vivo monitoring of levodopa pharmacokinetics is essential to address its narrow therapeutic window in Parkinson’s disease (PD) therapy. However, current methods require excessive sample ... |
PMC12455320 | core_pubmed_pmc | Pharmacokinetics and Pharmacodynamics of Fosravuconazole, Itraconazole, and Hydroxyitraconazole in Sudanese Patients With Eumycetoma | Pharmacokinetics and Pharmacodynamics of Fosravuconazole, Itraconazole, and Hydroxyitraconazole in Sudanese Patients With Eumycetoma Abstract Abstract Background The first clinical trial on eumycetoma was recently conducted in Sudan, comparing oral fosravuconazole, prodrug of active ravuconazole, with the standard-of-c... |
PMC11494923 | core_pubmed_pmc | Population pharmacokinetics of total and unbound valemetostat and platelet dynamics in healthy volunteers and patients with non‐Hodgkin lymphoma | Population pharmacokinetics of total and unbound valemetostat and platelet dynamics in healthy volunteers and patients with non‐Hodgkin lymphoma Abstract Abstract Valemetostat is an EZH2/1 inhibitor that has been approved in Japan for the treatment of patients with relapsed/refractory adult T‐cell leukemia/lymphoma, ba... |
PMC8927936 | core_pubmed_pmc | Pharmacokinetic Parameters and Estimating Extra-Label Tissue Withdrawal Intervals Using Three Approaches and Various Matrices for Domestic Laying Chickens Following Meloxicam Administration | Pharmacokinetic Parameters and Estimating Extra-Label Tissue Withdrawal Intervals Using Three Approaches and Various Matrices for Domestic Laying Chickens Following Meloxicam Administration Abstract Meloxicam is commonly prescribed for treating chickens in backyard or small commercial operations despite a paucity of sc... |
PMC4998580 | core_pubmed_pmc | Chemical Structure and Concentration of Intratumor Catabolites Determine Efficacy of Antibody Drug Conjugates | Chemical Structure and Concentration of Intratumor Catabolites Determine Efficacy of Antibody Drug Conjugates Abstract Abstract Despite recent technological advances in quantifying antibody drug conjugate (ADC) species, such as total antibody, conjugated antibody, conjugated drug, and payload drug in circulation, the c... |
PMC9279905 | core_pubmed_pmc | Clinical Application Value of Pharmacokinetic Parameters of Vancomycin in Children Treated in the Pediatric Intensive Care Unit | Clinical Application Value of Pharmacokinetic Parameters of Vancomycin in Children Treated in the Pediatric Intensive Care Unit Abstract Abstract Objective To explore the efficacy and safety of vancomycin as measured by pharmacokinetic/pharmacodynamic parameters in children with severe infection in the Pediatric Intens... |
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