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PMC12001260 | core_pubmed_pmc | Covariate Model Selection Approaches for Population Pharmacokinetics: A Systematic Review of Existing Methods, From SCM to AI | Covariate Model Selection Approaches for Population Pharmacokinetics: A Systematic Review of Existing Methods, From SCM to AI Abstract ABSTRACT A growing number of covariate modeling methods have been proposed in the field of popPK modeling, but limited information exists on how they all compare. The objective of this ... |
PMC12158833 | core_pubmed_pmc | A Systematic Review and Classification of the Effects of P-glycoprotein Inhibitors and Inducers in Humans, Using Digoxin, Fexofenadine, and Dabigatran as Probe Drugs | A Systematic Review and Classification of the Effects of P-glycoprotein Inhibitors and Inducers in Humans, Using Digoxin, Fexofenadine, and Dabigatran as Probe Drugs Abstract Abstract P-glycoprotein is a critical efflux transporter that may significantly affect the pharmacokinetics of various drugs by influencing their... |
PMC11754507 | core_pubmed_pmc | Population Pharmacokinetics of Pegcetacoplan in Patients with Geographic Atrophy or Neovascular Age-related Macular Degeneration | Population Pharmacokinetics of Pegcetacoplan in Patients with Geographic Atrophy or Neovascular Age-related Macular Degeneration Abstract Abstract Objective To develop a population pharmacokinetic (PK) model to characterize serum pegcetacoplan concentration-time data after intravitreal administration in patients with g... |
PMC11808975 | core_pubmed_pmc | Virtual Screening, Toxicity Evaluation and Pharmacokinetics of Erythrina Alkaloids as Acetylcholinesterase Inhibitor Candidates from Natural Products | Virtual Screening, Toxicity Evaluation and Pharmacokinetics of Erythrina Alkaloids as Acetylcholinesterase Inhibitor Candidates from Natural Products Abstract Purpose Alzheimer’s disease (AD) is a progressive neurodegenerative disorder with limited treatment options, necessitating the development of safer and more effe... |
PMC5351336 | core_pubmed_pmc | A Novel Method for Studying the Pharmacokinetics of [ 14 C]Umeclidinium After Application to the Axilla or Palm of Healthy Male Subjects | A Novel Method for Studying the Pharmacokinetics of [ 14 C]Umeclidinium After Application to the Axilla or Palm of Healthy Male Subjects Abstract Abstract Umeclidinium (UMEC), a long‐acting muscarinic antagonist approved for chronic obstructive pulmonary disease (COPD), was investigated for primary hyperhidrosis as top... |
PMC11296087 | core_pubmed_pmc | Development of a novel dosing paradigm to model diazepam rescue therapy in preclinical seizure and epilepsy models | Development of a novel dosing paradigm to model diazepam rescue therapy in preclinical seizure and epilepsy models Abstract Abstract Diazepam is a cornerstone immediate‐use antiseizure rescue therapy that may extend the duration between seizure clusters in people living with epilepsy. However, our mechanistic understan... |
PMC11573852 | core_pubmed_pmc | Understanding Voriconazole Metabolism: A Middle-Out Physiologically-Based Pharmacokinetic Modelling Framework Integrating In Vitro and Clinical Insights | Understanding Voriconazole Metabolism: A Middle-Out Physiologically-Based Pharmacokinetic Modelling Framework Integrating In Vitro and Clinical Insights Abstract Background and Objective Voriconazole (VRC), a broad-spectrum antifungal drug, exhibits nonlinear pharmacokinetics (PK) due to saturable metabolic processes, ... |
PMC7470061 | core_pubmed_pmc | Enhanced oral bioavailability of magnolol via mixed micelles and nanosuspensions based on Soluplus ® -Poloxamer 188 | Enhanced oral bioavailability of magnolol via mixed micelles and nanosuspensions based on Soluplus ® -Poloxamer 188 Abstract Abstract Magnolol, known to have extensive biological activities, is the major bioactive ingredient isolated from the root and stem bark of Magnolia officinalis . However, the clinical applicatio... |
PMC8157843 | core_pubmed_pmc | Synthetic Biology towards Improved Flavonoid Pharmacokinetics | Synthetic Biology towards Improved Flavonoid Pharmacokinetics Abstract Abstract Flavonoids are a structurally diverse class of natural products that have been found to have a range of beneficial activities in humans. However, the clinical utilisation of these molecules has been limited due to their low solubility, chem... |
PMC6882900 | core_pubmed_pmc | Pharmacokinetics of Micafungin in Critically Ill Patients | Pharmacokinetics of Micafungin in Critically Ill Patients Abstract Abstract We investigated covariates of pharmacokinetics of micafungin in critically ill patients. After application of micafungin, plasma samples were collected. Non-linear mixed effects modelling (NONMEM 7.3) was used to develop the pharmacokinetic mod... |
PMC6203112 | core_pubmed_pmc | Safety, tolerability, and pharmacokinetics of single and repeat ascending doses of CHF6001, a novel inhaled phosphodiesterase-4 inhibitor: two randomized trials in healthy volunteers | Safety, tolerability, and pharmacokinetics of single and repeat ascending doses of CHF6001, a novel inhaled phosphodiesterase-4 inhibitor: two randomized trials in healthy volunteers Abstract Purpose The purpose of this study was to evaluate safety, tolerability, and pharmacokinetics (PK) of CHF6001, an inhaled phospho... |
PMC6881382 | core_pubmed_pmc | Radio-Telemetric Assessment of Cardiac Variables and Locomotion With Experimentally Induced Hypermagnesemia in Horses Using Chronically Implanted Catheters | Radio-Telemetric Assessment of Cardiac Variables and Locomotion With Experimentally Induced Hypermagnesemia in Horses Using Chronically Implanted Catheters Abstract Abstract The objective of this study was to characterize the pharmacokinetics and pharmacodynamics of intravenous administration of magnesium sulfate to ho... |
PMC6046597 | core_pubmed_pmc | Focusing in on use of pharmacokinetic profiles in routine hemophilia care | Focusing in on use of pharmacokinetic profiles in routine hemophilia care Abstract Abstract Background Emergence of population pharmacokinetic models for prediction of individual pharmacokinetic ( PK ) profiles facilitates individualization of prescribed prophylactic therapy for patients with hemophilia A and B and may... |
PMC10366539 | core_pubmed_pmc | Preparation of a Sunitinib loaded microemulsion for ocular delivery and evaluation for the treatment of corneal neovascularization in vitro and in vivo | Preparation of a Sunitinib loaded microemulsion for ocular delivery and evaluation for the treatment of corneal neovascularization in vitro and in vivo Abstract Background: Corneal neovascularization (CNV) is a pathological condition that can disrupt corneal transparency, thus harming visual acuity. However, there is n... |
PMC4453660 | core_pubmed_pmc | Exposure-response analysis of rilotumumab in gastric cancer: the role of tumour MET expression | Exposure-response analysis of rilotumumab in gastric cancer: the role of tumour MET expression Abstract Background: Rilotumumab, an investigational, monoclonal antibody, inhibits MET-mediated signalling. In a randomized phase 2 trial of rilotumumab±epirubicin/cisplatin/capecitabine in gastric or oesophagogastric juncti... |
PMC9543103 | core_pubmed_pmc | Boosting the anti MERS-CoV activity and oral bioavailability of resveratrol via PEG-stabilized emulsomal nano-carrier: Factorial design, in-vitro and in-vivo assessments | Boosting the anti MERS-CoV activity and oral bioavailability of resveratrol via PEG-stabilized emulsomal nano-carrier: Factorial design, in-vitro and in-vivo assessments Abstract Abstract Resveratrol (RSV) is a phytoceutical polyphenolic compound exhibiting a well evidenced wide range of therapeutic activities. Unfortu... |
PMC8594444 | core_pubmed_pmc | Eculizumab Pharmacokinetics and Pharmacodynamics in Patients With Generalized Myasthenia Gravis | Eculizumab Pharmacokinetics and Pharmacodynamics in Patients With Generalized Myasthenia Gravis Abstract Objective: To investigate the pharmacokinetics, pharmacodynamics, and exposure–response of the approved 900/1,200 mg dosing regimen for the terminal complement component 5 (C5) inhibitor eculizumab in patients with ... |
PMC5736858 | core_pubmed_pmc | En Route towards European Clinical Breakpoints for Veterinary Antimicrobial Susceptibility Testing: A Position Paper Explaining the VetCAST Approach | En Route towards European Clinical Breakpoints for Veterinary Antimicrobial Susceptibility Testing: A Position Paper Explaining the VetCAST Approach Abstract Abstract VetCAST is the EUCAST sub-committee for Veterinary Antimicrobial Susceptibility Testing. Its remit is to define clinical breakpoints (CBPs) for antimicro... |
PMC12353974 | core_pubmed_pmc | Population Pharmacokinetic/Toxicodynamic Model for Polymyxin B in Critically Ill Patients to Identify the Risk of Nephrotoxicity | Population Pharmacokinetic/Toxicodynamic Model for Polymyxin B in Critically Ill Patients to Identify the Risk of Nephrotoxicity Abstract Abstract Polymyxins are used against highly resistant Gram‐negative pathogens, and nephrotoxicity (acute kidney injury, AKI) is the major dose‐limiting adverse effect. We aimed to de... |
PMC9752101 | core_pubmed_pmc | β-lactam precision dosing in critically ill children: Current state and knowledge gaps | β-lactam precision dosing in critically ill children: Current state and knowledge gaps Abstract There has been emerging interest in implementing therapeutic drug monitoring and model-informed precision dosing of β-lactam antibiotics in critically ill patients, including children. Despite a position paper endorsed by mu... |
PMC5709251 | core_pubmed_pmc | Pharmacokinetic Analysis of Four Bioactive Iridoid and Secoiridoid Glycoside Components of Radix Gentianae Macrophyllae and Their Synergistic Excretion by HPLC-DAD Combined with Second-Order Calibration | Pharmacokinetic Analysis of Four Bioactive Iridoid and Secoiridoid Glycoside Components of Radix Gentianae Macrophyllae and Their Synergistic Excretion by HPLC-DAD Combined with Second-Order Calibration Abstract Abstract Abstract An HPLC-DAD method combined with second-order calibration based on the alternating triline... |
PMC8251251 | core_pubmed_pmc | In vitro activity of cefiderocol and comparators against isolates of Gram-negative pathogens from a range of infection sources: SIDERO-WT-2014–2018 studies in France | In vitro activity of cefiderocol and comparators against isolates of Gram-negative pathogens from a range of infection sources: SIDERO-WT-2014–2018 studies in France Abstract Abstract Objectives Over recent years, France has experienced an increase of infections caused by carbapenem-resistant Gram-negative (GN) pathoge... |
PMC6418056 | core_pubmed_pmc | The Influence of Diabetes Mellitus on Glucuronidation and Sulphation of Paracetamol in Patients with Febrile Neutropenia | The Influence of Diabetes Mellitus on Glucuronidation and Sulphation of Paracetamol in Patients with Febrile Neutropenia Abstract Abstract Background and Objectives Numerous studies have confirmed the influence of diabetes mellitus on the pharmacokinetics of drugs. Paracetamol (APAP) is an antipyretic that is commonly ... |
PMC4833154 | core_pubmed_pmc | The effect of mild and moderate renal impairment on the pharmacokinetics of pridopidine, a new drug for Huntington's disease | The effect of mild and moderate renal impairment on the pharmacokinetics of pridopidine, a new drug for Huntington's disease Abstract Abstract Aim Pridopidine, a new oral drug for treatment of patients with motor symptoms associated with Huntington's Disease (HD) is currently under development. In steady‐state conditio... |
PMC9652434 | core_pubmed_pmc | Safety, tolerability, pharmacokinetic, and pharmacodynamic characteristics of vutiglabridin: A first‐in‐class, first‐in‐human study | Safety, tolerability, pharmacokinetic, and pharmacodynamic characteristics of vutiglabridin: A first‐in‐class, first‐in‐human study Abstract Abstract This study aimed to evaluate the safety, tolerability, pharmacokinetics, and pharmacodynamics of vutiglabridin, a potential anti‐obesity treatment under development, for ... |
PMC4334601 | core_pubmed_pmc | Pharmacokinetic and pharmacodynamic evaluation of rivaroxaban: considerations for the treatment of venous thromboembolism | Pharmacokinetic and pharmacodynamic evaluation of rivaroxaban: considerations for the treatment of venous thromboembolism Abstract Patients with deep vein thrombosis or pulmonary embolism are recommended to receive anticoagulation for acute treatment and secondary prevention of venous thromboembolism (VTE). Fast-acting... |
PMC8572679 | core_pubmed_pmc | Transformation of berberine to its demethylated metabolites by the CYP51 enzyme in the gut microbiota | Transformation of berberine to its demethylated metabolites by the CYP51 enzyme in the gut microbiota Abstract Berberine (BBR) is an isoquinoline alkaloid extracted from Coptis chinensis that improves diabetes, hyperlipidemia and inflammation. Due to the low oral bioavailability of BBR, its mechanism of action is close... |
PMC6635675 | core_pubmed_pmc | Interpersonal Factors in the Pharmacokinetics and Pharmacodynamics of Voriconazole: Are CYP2C19 Genotypes Enough for Us to Make a Clinical Decision? | Interpersonal Factors in the Pharmacokinetics and Pharmacodynamics of Voriconazole: Are CYP2C19 Genotypes Enough for Us to Make a Clinical Decision? Abstract Background: Invasive mycoses are serious infections with high mortality and increasing inci-dence. Voriconazole, an important drug to treat invasive mycosis, is m... |
PMC12295952 | core_pubmed_pmc | Evaluation of Ropivacaine and 3-OH-Ropivacaine Pharmacokinetics Following Interpectoral Nerve Block via LC-MS/MS—A Pilot Study | Evaluation of Ropivacaine and 3-OH-Ropivacaine Pharmacokinetics Following Interpectoral Nerve Block via LC-MS/MS—A Pilot Study Abstract Regional anesthesia techniques such as the ultrasound-guided PECS II (pectoral nerve block) block are increasingly employed to optimize perioperative analgesia while minimizing systemi... |
PMC7070800 | core_pubmed_pmc | Translational Model‐Informed Dose Selection for a Human Positron Emission Tomography Imaging Study of JNJ‐54175446, a P2X7 Receptor Antagonist | Translational Model‐Informed Dose Selection for a Human Positron Emission Tomography Imaging Study of JNJ‐54175446, a P2X7 Receptor Antagonist Abstract Abstract Positron emission tomography (PET) provides useful information in target engagement or receptor occupancy in the brain for central nervous system (CNS) drug de... |
PMC4767718 | core_pubmed_pmc | Effect of Food on the Pharmacokinetics of the Investigational Aurora A Kinase Inhibitor Alisertib (MLN8237) in Patients with Advanced Solid Tumors | Effect of Food on the Pharmacokinetics of the Investigational Aurora A Kinase Inhibitor Alisertib (MLN8237) in Patients with Advanced Solid Tumors Abstract Objective This study was conducted to characterize the effects of food on single-dose pharmacokinetics (PK) of the investigational Aurora A kinase inhibitor alisert... |
PMC6496076 | core_pubmed_pmc | Cycloserine Population Pharmacokinetics and Pharmacodynamics in Patients with Tuberculosis | Cycloserine Population Pharmacokinetics and Pharmacodynamics in Patients with Tuberculosis Abstract Limited pharmacokinetic/pharmacodynamic (PK/PD) data exist on cycloserine in tuberculosis (TB) patients. We pooled several studies into a large PK data set to estimate the population PK parameters for cycloserine in TB p... |
PMC3546862 | core_pubmed_pmc | Assessing the utility of an anti-malarial pharmacokinetic-pharmacodynamic model for aiding drug clinical development | Assessing the utility of an anti-malarial pharmacokinetic-pharmacodynamic model for aiding drug clinical development Abstract Abstract Background Mechanistic within-host models relating blood anti-malarial drug concentrations with the parasite-time profile help in assessing dosing schedules and partner drugs for new an... |
PMC8056737 | core_pubmed_pmc | Dose prediction for repurposing nitazoxanide in SARS‐CoV‐2 treatment or chemoprophylaxis | Dose prediction for repurposing nitazoxanide in SARS‐CoV‐2 treatment or chemoprophylaxis Abstract Background Severe acute respiratory syndrome coronavirus 2 (SARS‐CoV‐2) has been declared a global pandemic and urgent treatment and prevention strategies are needed. Nitazoxanide, an anthelmintic drug, has been shown to e... |
PMC9398121 | core_pubmed_pmc | Preclinical and Early Clinical Development of PTC596, a Novel Small-Molecule Tubulin-Binding Agent | Preclinical and Early Clinical Development of PTC596, a Novel Small-Molecule Tubulin-Binding Agent Abstract Abstract PTC596 is an investigational small-molecule tubulin-binding agent. Unlike other tubulin-binding agents, PTC596 is orally bioavailable and is not a P-glycoprotein substrate. So as to characterize PTC596 t... |
PMC9161154 | core_pubmed_pmc | Identification of Candidate Therapeutic Genes for More Precise Treatment of Esophageal Squamous Cell Carcinoma and Adenocarcinoma | Identification of Candidate Therapeutic Genes for More Precise Treatment of Esophageal Squamous Cell Carcinoma and Adenocarcinoma Abstract Abstract The standard therapy administered to patients with advanced esophageal cancer remains uniform, despite its two main histological subtypes, namely esophageal squamous cell c... |
PMC8048619 | core_pubmed_pmc | Exposure‐Response and Population Pharmacokinetic Analyses of a Novel Subcutaneous Formulation of Daratumumab Administered to Multiple Myeloma Patients | Exposure‐Response and Population Pharmacokinetic Analyses of a Novel Subcutaneous Formulation of Daratumumab Administered to Multiple Myeloma Patients Abstract Abstract We report the population pharmacokinetic (PK) and exposure‐response analyses of a novel subcutaneous formulation of daratumumab (DARA) using data from ... |
PMC8362215 | core_pubmed_pmc | Evaluation of the pharmacokinetics of prednisolone in paediatric patients with acute lymphoblastic leukaemia treated according to Dutch Childhood Oncology Group protocols and its relation to treatment response | Evaluation of the pharmacokinetics of prednisolone in paediatric patients with acute lymphoblastic leukaemia treated according to Dutch Childhood Oncology Group protocols and its relation to treatment response Abstract Summary Glucocorticoids form the backbone of paediatric acute lymphoblastic leukaemia (ALL) treatment... |
PMC11598835 | core_pubmed_pmc | Benzocarbazoledinones as SARS-CoV-2 Replication Inhibitors: Synthesis, Cell-Based Studies, Enzyme Inhibition, Molecular Modeling, and Pharmacokinetics Insights | Benzocarbazoledinones as SARS-CoV-2 Replication Inhibitors: Synthesis, Cell-Based Studies, Enzyme Inhibition, Molecular Modeling, and Pharmacokinetics Insights Abstract Abstract Endemic and pandemic viruses represent significant public health challenges, leading to substantial morbidity and mortality over time. The COV... |
PMC10673748 | core_pubmed_pmc | Clinical implications of augmented renal clearance after unrelated single cord blood transplantation in adults | Clinical implications of augmented renal clearance after unrelated single cord blood transplantation in adults Abstract Augmented renal clearance (ARC) is a phenomenon characterized by increased renal functionality, which can impact the pharmacokinetics and pharmacodynamics of antimicrobial drugs eliminated by the kidn... |
PMC6784242 | core_pubmed_pmc | Pharmacokinetic/Pharmacodynamic (PK/PD) Simulation for Dosage Optimization of Colistin Against Carbapenem-Resistant Klebsiella pneumoniae and Carbapenem-Resistant Escherichia coli | Pharmacokinetic/Pharmacodynamic (PK/PD) Simulation for Dosage Optimization of Colistin Against Carbapenem-Resistant Klebsiella pneumoniae and Carbapenem-Resistant Escherichia coli Abstract Abstract The purpose was to explore the optimal dosage regimen of colistin using Monte Carlo simulations, for the treatment of carb... |
PMC12619576 | core_pubmed_pmc | Human Adipose Tissue 11β‐Hydroxysteroid Dehydrogenase Type 1 Inhibition Without Tachyphylaxis by Clofutriben, a Pseudo‐Irreversible Enzyme Inhibitor | Human Adipose Tissue 11β‐Hydroxysteroid Dehydrogenase Type 1 Inhibition Without Tachyphylaxis by Clofutriben, a Pseudo‐Irreversible Enzyme Inhibitor Abstract ABSTRACT Inhibitors of 11β‐hydroxysteroid dehydrogenase type 1 (HSD‐1), the pre‐receptor regulator of intracellular active glucocorticoid levels, have promise to ... |
PMC12283411 | core_pubmed_pmc | TERN-501 monotherapy and combination therapy with TERN-101 in metabolic dysfunction-associated steatohepatitis: the randomized phase 2a DUET trial | TERN-501 monotherapy and combination therapy with TERN-101 in metabolic dysfunction-associated steatohepatitis: the randomized phase 2a DUET trial Abstract Thyroid hormone receptor-β (THRβ) agonism is a validated mechanism for treating metabolic dysfunction-associated steatohepatitis (MASH). DUET was a 12-week, randomi... |
PMC12578057 | core_pubmed_pmc | A comparative observational study on the effect of two different doses of fentanyl on the effect site concentration of propofol during induction of anesthesia using clinical assessment score and bispectral index | A comparative observational study on the effect of two different doses of fentanyl on the effect site concentration of propofol during induction of anesthesia using clinical assessment score and bispectral index Abstract Abstract Background and Aims: Opioids are known to reduce the propofol dose required to blunt movem... |
PMC5575539 | core_pubmed_pmc | Dose Finding of Lenvatinib in Subjects With Advanced Hepatocellular Carcinoma Based on Population Pharmacokinetic and Exposure–Response Analyses | Dose Finding of Lenvatinib in Subjects With Advanced Hepatocellular Carcinoma Based on Population Pharmacokinetic and Exposure–Response Analyses Abstract Abstract Hepatocellular carcinoma (HCC) accounts for up to 90% of primary liver cancer occurrences worldwide. Lenvatinib, a multikinase inhibitor, was approved in rad... |
PMC9286715 | core_pubmed_pmc | Prediction of CYP‐mediated DDIs involving inhibition: Approaches to address the requirements for system qualification of the Simcyp Simulator | Prediction of CYP‐mediated DDIs involving inhibition: Approaches to address the requirements for system qualification of the Simcyp Simulator Abstract Abstract Physiologically‐based pharmacokinetic (PBPK) modeling is being increasingly used in drug development to avoid unnecessary clinical drug–drug interaction (DDI) s... |
PMC12577036 | core_pubmed_pmc | Comparative analysis of the uptake of the H + /OC antiporter substrate oxycodone across and into brain endothelial and parenchymal cells with in vitro–in vivo extrapolation | Comparative analysis of the uptake of the H + /OC antiporter substrate oxycodone across and into brain endothelial and parenchymal cells with in vitro–in vivo extrapolation Abstract Background In vitro evaluation of substances utilizing the putative proton‑coupled organic cation (H + /OC) antiporter for active uptake a... |
PMC10496502 | core_pubmed_pmc | Radioimmunotherapy Targeting B7-H3 in situ glioma models enhanced antitumor efficacy by Reconstructing the tumor microenvironment | Radioimmunotherapy Targeting B7-H3 in situ glioma models enhanced antitumor efficacy by Reconstructing the tumor microenvironment Abstract Abstract Radionuclide drug conjugates (RDCs) with antibodies serve as a novel approach for the treatment of malignant tumors including glioblastoma. However, RDCs require optimal an... |
PMC8846632 | core_pubmed_pmc | Physiologically‐based pharmacokinetic modeling to predict CYP3A4‐mediated drug‐drug interactions of finerenone | Physiologically‐based pharmacokinetic modeling to predict CYP3A4‐mediated drug‐drug interactions of finerenone Abstract Abstract Finerenone is a nonsteroidal, selective mineralocorticoid receptor antagonist that recently demonstrated its efficacy to delay chronic kidney disease (CKD) progression and reduce cardiovascul... |
PMC11943305 | core_pubmed_pmc | 4-Hydroxycoumarin Exhibits Antinociceptive and Anti-Inflammatory Effects Through Cytokine Modulation: An Integrated In Silico and In Vivo Study | 4-Hydroxycoumarin Exhibits Antinociceptive and Anti-Inflammatory Effects Through Cytokine Modulation: An Integrated In Silico and In Vivo Study Abstract Chronic pain significantly impacts quality of life and is often accompanied by inflammation, a natural bodily response that can become harmful when excessive. The orof... |
PMC4029330 | core_pubmed_pmc | Dose response of umeclidinium administered once or twice daily in patients with COPD: a randomised cross-over study | Dose response of umeclidinium administered once or twice daily in patients with COPD: a randomised cross-over study Abstract Abstract Background Umeclidinium bromide (UMEC) is an inhaled long-acting muscarinic antagonist in development for chronic obstructive pulmonary disease (COPD). Methods This was a multicentre, ra... |
PMC4242982 | core_pubmed_pmc | Drug–drug interactions between sucroferric oxyhydroxide and losartan, furosemide, omeprazole, digoxin and warfarin in healthy subjects | Drug–drug interactions between sucroferric oxyhydroxide and losartan, furosemide, omeprazole, digoxin and warfarin in healthy subjects Abstract Background The novel iron-based phosphate binder sucroferric oxyhydroxide is being investigated for the treatment of hyperphosphatemia. Patients with chronic kidney disease oft... |
PMC9490083 | core_pubmed_pmc | Optimal dose of cefotaxime in neonates with early-onset sepsis: A developmental pharmacokinetic model-based evaluation | Optimal dose of cefotaxime in neonates with early-onset sepsis: A developmental pharmacokinetic model-based evaluation Abstract Abstract Objective: The perspective of real-world study is especially relevant to newborns, enabling dosage regimen optimization and regulatory approval of medications for use in newborns. The... |
PMC11925553 | core_pubmed_pmc | Development of an LC–MS/MS Method for Quantifying Occidiofungin in Rabbit Plasma | Development of an LC–MS/MS Method for Quantifying Occidiofungin in Rabbit Plasma Abstract ABSTRACT Fungal infections are caused by opportunistic pathogens that can be life threatening and have been growing in prevalence. Many clinically relevant pathogens have resistance to or are developing resistance to the commonly ... |
PMC4338259 | core_pubmed_pmc | Estimation of the binding modes with important human cytochrome P450 enzymes, drug interaction potential, pharmacokinetics, and hepatotoxicity of ginger components using molecular docking, computational, and pharmacokinetic modeling studies | Estimation of the binding modes with important human cytochrome P450 enzymes, drug interaction potential, pharmacokinetics, and hepatotoxicity of ginger components using molecular docking, computational, and pharmacokinetic modeling studies Abstract Abstract Ginger is one of the most commonly used herbal medicines for ... |
PMC6527208 | core_pubmed_pmc | Vaginal microbiota and mucosal pharmacokinetics of tenofovir in healthy women using tenofovir and tenofovir/levonorgestrel vaginal rings | Vaginal microbiota and mucosal pharmacokinetics of tenofovir in healthy women using tenofovir and tenofovir/levonorgestrel vaginal rings Abstract Abstract Recent data support that the vaginal microbiota may alter mucosal pharmacokinetics (PK) of topically delivered microbicides. Our team developed an intravaginal ring ... |
PMC7746746 | core_pubmed_pmc | Identification of hnRNP-A1 as a pharmacodynamic biomarker of type I PRMT inhibition in blood and tumor tissues | Identification of hnRNP-A1 as a pharmacodynamic biomarker of type I PRMT inhibition in blood and tumor tissues Abstract Arginine methylation has been recognized as a post-translational modification with pleiotropic effects that span from regulation of transcription to metabolic processes that contribute to aberrant cel... |
PMC10980656 | core_pubmed_pmc | SAFE-ROCK: A Phase I Trial of an Oral Application of the ROCK Inhibitor Fasudil to Assess Bioavailability, Safety, and Tolerability in Healthy Participants | SAFE-ROCK: A Phase I Trial of an Oral Application of the ROCK Inhibitor Fasudil to Assess Bioavailability, Safety, and Tolerability in Healthy Participants Abstract Background The intravenous (IV) formulation of Rho-kinase (ROCK) inhibitor fasudil has been approved for the treatment of subarachnoid haemorrhage since 19... |
PMC9779550 | core_pubmed_pmc | Arylcyclohexylamine Derivatives: Pharmacokinetic, Pharmacodynamic, Clinical and Forensic Aspects | Arylcyclohexylamine Derivatives: Pharmacokinetic, Pharmacodynamic, Clinical and Forensic Aspects Abstract Abstract Since the 2000s, an increasing number of new psychoactive substances (NPS) have appeared on the drug market. Arylcyclohexylamine (ACH) compounds such as ketamine, phencyclidine and eticyclidine derivatives... |
PMC7981967 | core_pubmed_pmc | Systematic review: the bioavailability of orally administered antibiotics during the initial phase of a systemic infection in non-ICU patients | Systematic review: the bioavailability of orally administered antibiotics during the initial phase of a systemic infection in non-ICU patients Abstract Background The systemic response to an infection might influence the pharmacokinetics of antibiotics. To evaluate the desired possibility of an earlier (< 24 h) IV-to-o... |
PMC5881137 | core_pubmed_pmc | Clozapine Use During Pregnancy and Lactation: A Case-Series Report | Clozapine Use During Pregnancy and Lactation: A Case-Series Report Abstract Abstract The current prescription of clozapine in psychotic women of reproductive age makes it crucial to understand its pharmacokinetics during pregnancy and lactation as well as its risk profile for neonatal outcome. The aim of this case seri... |
PMC5655850 | core_pubmed_pmc | Exploratory Population PK Analysis of Dupilumab, a Fully Human Monoclonal Antibody Against IL‐4Rα, in Atopic Dermatitis Patients and Normal Volunteers | Exploratory Population PK Analysis of Dupilumab, a Fully Human Monoclonal Antibody Against IL‐4Rα, in Atopic Dermatitis Patients and Normal Volunteers Abstract An exploratory population pharmacokinetic model for functional dupilumab was developed. Data from healthy volunteers and patients with atopic dermatitis (AD) re... |
PMC9553116 | core_pubmed_pmc | Mitochondrial Dysfunction and Pharmacodynamics of Mitofusin Activation in Murine Charcot-Marie-Tooth Disease Type 2A | Mitochondrial Dysfunction and Pharmacodynamics of Mitofusin Activation in Murine Charcot-Marie-Tooth Disease Type 2A Abstract Abstract Mitofusin (MFN) 1 and MFN2 are dynamin GTPase family mitochondrial proteins that mediate mitochondrial fusion requiring MFN conformational shifts, formation of macromolecular complexes ... |
PMC12916490 | core_pubmed_pmc | The 4-alkyl chain length of 2,5-dimethoxyamphetamines differentially affects in vitro serotonin receptor actions versus in vivo psychedelic-like effects | The 4-alkyl chain length of 2,5-dimethoxyamphetamines differentially affects in vitro serotonin receptor actions versus in vivo psychedelic-like effects Abstract Various ring-substituted α-methylphenethylamines (i.e., amphetamines) produce psychedelic-like effects that are primarily mediated by activity at 5-hydroxytry... |
PMC11255087 | core_pubmed_pmc | On inductive biases for the robust and interpretable prediction of drug concentrations using deep compartment models | On inductive biases for the robust and interpretable prediction of drug concentrations using deep compartment models Abstract Abstract Conventional pharmacokinetic (PK) models contain several useful inductive biases guiding model convergence to more realistic predictions of drug concentrations. Implementing similar bia... |
PMC9727977 | core_pubmed_pmc | Pharmacokinetics and pharmacodynamics of bioactive compounds in Penyanqing preparation in THP-1 inflammatory cells induced by Lipopolysaccharide | Pharmacokinetics and pharmacodynamics of bioactive compounds in Penyanqing preparation in THP-1 inflammatory cells induced by Lipopolysaccharide Abstract Abstract Background Penyanqing (PYQ), a traditional Chinese medicine (TCM), has a good clinical efficacy for the treatment of pelvic inflammatory disease (PID). Previ... |
PMC10879011 | core_pubmed_pmc | Optimized Ribociclib nanostructured lipid carrier for the amelioration of skin cancer: Inferences from ex-vivo skin permeation and dermatokinetic studies | Optimized Ribociclib nanostructured lipid carrier for the amelioration of skin cancer: Inferences from ex-vivo skin permeation and dermatokinetic studies Abstract Abstract Current research focuses on explicitly developing and evaluating nanostructured lipidic carriers (NLCs) for the chemotherapeutic drug Ribociclib (RC... |
PMC12796778 | core_pubmed_pmc | Comparing Pharmacokinetics of Meloxicam When Administered With a Needle‐Free Injection Device Versus Needle‐And‐Syringe in Piglets | Comparing Pharmacokinetics of Meloxicam When Administered With a Needle‐Free Injection Device Versus Needle‐And‐Syringe in Piglets Abstract ABSTRACT Meloxicam is a common analgesic for castration in pigs. While needle‐free technology is effective for swine vaccination, its implementation for administering meloxicam has... |
PMC7691416 | core_pubmed_pmc | Comparisons of Four Protein-Binding Models Characterizing the Pharmacokinetics of Unbound Phenytoin in Adult Patients Using Non-Linear Mixed-Effects Modeling | Comparisons of Four Protein-Binding Models Characterizing the Pharmacokinetics of Unbound Phenytoin in Adult Patients Using Non-Linear Mixed-Effects Modeling Abstract Abstract Background and objective Phenytoin is extensively protein bound with a narrow therapeutic range. The unbound phenytoin is pharmacologically acti... |
PMC11783651 | core_pubmed_pmc | The influence of haemorrhagic shock on the pharmacokinetic and pharmacodynamic effects of remimazolam in a swine model | The influence of haemorrhagic shock on the pharmacokinetic and pharmacodynamic effects of remimazolam in a swine model Abstract Abstract BACKGROUND Haemorrhagic shock enhances the potency of several intravenous anaesthetics. OBJECTIVE To assess the influence of haemorrhagic shock on the pharmacokinetic and pharmacodyna... |
PMC8760971 | core_pubmed_pmc | Model-Informed Precision Dosing of Antibiotics in Osteoarticular Infections | Model-Informed Precision Dosing of Antibiotics in Osteoarticular Infections Abstract Abstract As a heterogeneous and wide inflammation, osteoarticular infection (OAI) shows an increasing incidence in recent years. Staphylococcus aureus is the most important pathogen causing OAI. The antibiotic treatment will affect the... |
PMC10269146 | core_pubmed_pmc | Population Pharmacokinetic Analyses for Tebipenem after Oral Administration of Pro-Drug Tebipenem Pivoxil Hydrobromide | Population Pharmacokinetic Analyses for Tebipenem after Oral Administration of Pro-Drug Tebipenem Pivoxil Hydrobromide Abstract ABSTRACT Tebipenem pivoxil hydrobromide (TBP-PI-HBr) is an oral (PO) carbapenem pro-drug that is converted to the active moiety tebipenem in the enterocytes. Tebipenem has activity against mul... |
PMC11052100 | core_pubmed_pmc | The Increased Dissolution and Oral Absorption of Itraconazole by Nanocrystals with an Endogenous Small-Molecule Surfactant as a Stabilizer | The Increased Dissolution and Oral Absorption of Itraconazole by Nanocrystals with an Endogenous Small-Molecule Surfactant as a Stabilizer Abstract Abstract The aim of this study was to develop cholic-acid-stabilized itraconazole nanosuspensions (ITZ-Nanos) with the objective of enhancing drug dissolution and oral abso... |
PMC12054080 | core_pubmed_pmc | Machine learning and population pharmacokinetics: a hybrid approach for optimizing vancomycin therapy in sepsis patients | Machine learning and population pharmacokinetics: a hybrid approach for optimizing vancomycin therapy in sepsis patients Abstract ABSTRACT Predicting vancomycin exposure is essential for optimizing dosing regimens in sepsis patients. While population pharmacokinetic (PPK) models are commonly used, their performance is ... |
PMC5769417 | core_pubmed_pmc | Single- and Multiple-Dose Trials to Determine the Pharmacokinetics, Safety, Tolerability, and Sex Effect of Oral Ginsenoside Compound K in Healthy Chinese Volunteers | Single- and Multiple-Dose Trials to Determine the Pharmacokinetics, Safety, Tolerability, and Sex Effect of Oral Ginsenoside Compound K in Healthy Chinese Volunteers Abstract Background and objectives: Ginsenoside compound K (CK) is a candidate drug for rheumatoid arthritis therapy. The objective of this study was to i... |
PMC7218117 | core_pubmed_pmc | Gender Differences in Cardiovascular Pharmacotherapy—the Example of Hypertension: A Mini Review | Gender Differences in Cardiovascular Pharmacotherapy—the Example of Hypertension: A Mini Review Abstract Abstract Cardiovascular disease (CVD) is the leading cause of mortality worldwide in both sexes. Despite considerable progress in better understanding the patterns of disease in women, they are still often undertrea... |
PMC7515216 | core_pubmed_pmc | The Use of Direct Oral Anticoagulants in the Management of Venous Thromboembolism in Patients With Obesity | The Use of Direct Oral Anticoagulants in the Management of Venous Thromboembolism in Patients With Obesity Abstract Introduction The use of direct oral anticoagulants (DOACs) has gained significant traction given the lack of therapeutic monitoring and the need for anticoagulant bridging. There is a paucity of data on t... |
PMC7989285 | core_pubmed_pmc | Caffeine modulates pharmacokinetic and pharmacodynamic profiles of pioglitazone in diabetic rats | Caffeine modulates pharmacokinetic and pharmacodynamic profiles of pioglitazone in diabetic rats Abstract Objectives: To determine the influence of caffeine on pharmacokinetics and pharmacodynamics of pioglitazone (PIO) in diabetic rats. Methods: This was a preclinical study conducted in the College of Pharmacy, Najran... |
PMC12816431 | core_pubmed_pmc | Longitudinal Analysis of Manually and Automatically Classified Circulating Tumor Biomarkers and their Prediction of Survival in Metastatic Colorectal Cancer | Longitudinal Analysis of Manually and Automatically Classified Circulating Tumor Biomarkers and their Prediction of Survival in Metastatic Colorectal Cancer Abstract Circulating tumor cells (CTCs) and tumor‐derived extracellular vesicles (tdEVs) are promising biomarkers for predicting survival and informing treatment d... |
PMC10953624 | core_pubmed_pmc | Pharmacokinetics, safety, and efficacy of 20% subcutaneous immunoglobulin (Ig20Gly) administered weekly or every 2 weeks in Japanese patients with primary immunodeficiency diseases: a phase 3, open-label study | Pharmacokinetics, safety, and efficacy of 20% subcutaneous immunoglobulin (Ig20Gly) administered weekly or every 2 weeks in Japanese patients with primary immunodeficiency diseases: a phase 3, open-label study Abstract Abstract This phase 3, open-label, multidose study ( NCT04346108 ) evaluated the pharmacokinetics, sa... |
PMC4968835 | core_pubmed_pmc | A Three-Pulse Release Tablet for Amoxicillin: Preparation, Pharmacokinetic Study and Physiologically Based Pharmacokinetic Modeling | A Three-Pulse Release Tablet for Amoxicillin: Preparation, Pharmacokinetic Study and Physiologically Based Pharmacokinetic Modeling Abstract Abstract Background Amoxicillin is a commonly used antibiotic which has a short half-life in human. The frequent administration of amoxicillin is often required to keep the plasma... |
PMC10041991 | core_pubmed_pmc | Pharmacokinetics of Antituberculosis Drugs in Plasma and Cerebrospinal Fluid in a Patient with Pre-Extensive Drug Resistant Tuberculosis Meningitis | Pharmacokinetics of Antituberculosis Drugs in Plasma and Cerebrospinal Fluid in a Patient with Pre-Extensive Drug Resistant Tuberculosis Meningitis Abstract Abstract Drug-resistant tuberculous meningitis (TBM) is the most devastating and critical form of extrapulmonary tuberculosis. Here, we present a case of a 45-year... |
PMC3878000 | core_pubmed_pmc | Development and Validation of a Liquid Chromatography-Tandem Mass Spectrometry Method for the Determination of ε-Acetamidocaproic Acid in Rat Plasma | Development and Validation of a Liquid Chromatography-Tandem Mass Spectrometry Method for the Determination of ε-Acetamidocaproic Acid in Rat Plasma Abstract Abstract A simple and rapid liquid chromatography-tandem mass spectrometry (LC-MS/MS) method was developed and validated for the quantification of ε-acetamidocapr... |
PMC9663450 | core_pubmed_pmc | Improved pharmacodynamics of epidermal growth factor via microneedles-based self-powered transcutaneous electrical stimulation | Improved pharmacodynamics of epidermal growth factor via microneedles-based self-powered transcutaneous electrical stimulation Abstract Abstract Epidermal growth factor is an excellent drug for promoting wound healing; however, its conventional administration strategies are associated with pharmacodynamic challenges, s... |
PMC11624482 | core_pubmed_pmc | A systematic review of dexmedetomidine pharmacology in pediatric patients | A systematic review of dexmedetomidine pharmacology in pediatric patients Abstract Abstract Dexmedetomidine is a centrally acting alpha‐2 agonist used for initiation and maintenance of procedural sedation and mechanical ventilation in adult and pediatric settings. It is commonly used in both pediatric and neonatal inte... |
PMC5907632 | core_pubmed_pmc | Integrated population pharmacokinetics of etirinotecan pegol and its four metabolites in cancer patients with solid tumors | Integrated population pharmacokinetics of etirinotecan pegol and its four metabolites in cancer patients with solid tumors Abstract Abstract Purpose Etirinotecan pegol (EP), a long-acting topoisomerase-1 inhibitor, is a polyethylene glycol conjugate of irinotecan, with an intended indication for treatment of breast can... |
PMC6590375 | core_pubmed_pmc | Characterization of the Effect of Renal Impairment on Upadacitinib Pharmacokinetics | Characterization of the Effect of Renal Impairment on Upadacitinib Pharmacokinetics Abstract Abstract Upadacitinib is a novel selective Janus kinase 1 inhibitor developed for treatment of rheumatoid arthritis and other autoimmune diseases. The objective of this study was to assess the pharmacokinetics and safety of a s... |
PMC6886437 | core_pubmed_pmc | Olaptesed pegol (NOX-A12) with bendamustine and rituximab: a phase IIa study in patients with relapsed/refractory chronic lymphocytic leukemia | Olaptesed pegol (NOX-A12) with bendamustine and rituximab: a phase IIa study in patients with relapsed/refractory chronic lymphocytic leukemia Abstract Abstract Olaptesed pegol (NOX-A12) is a pegylated structured L-oligoribonucleotide that binds and neutralizes CXCL12, a chemokine tightly regulating the life cycle of c... |
PMC4429576 | core_pubmed_pmc | Application of Physiologically Based Pharmacokinetic (PBPK) Modeling to Support Dose Selection: Report of an FDA Public Workshop on PBPK | Application of Physiologically Based Pharmacokinetic (PBPK) Modeling to Support Dose Selection: Report of an FDA Public Workshop on PBPK Abstract Abstract The US Food and Drug Administration (FDA) public workshop, entitled “Application of Physiologically-based Pharmacokinetic (PBPK) Modeling to Support Dose Selection f... |
PMC10538094 | core_pubmed_pmc | Development of a Liquid Chromatography–Tandem Mass Spectrometry (LC–MS/MS) Method for Characterizing Linalool Oral Pharmacokinetics in Humans | Development of a Liquid Chromatography–Tandem Mass Spectrometry (LC–MS/MS) Method for Characterizing Linalool Oral Pharmacokinetics in Humans Abstract Lavender ( Lavandula angustifolia Miller or Lavandula officinalis Chaix) is an ethnopharmacological plant commonly known as English lavender. Linalool and linalyl acetat... |
PMC11040352 | core_pubmed_pmc | CD38‐Specific Gallium‐68 Labeled Peptide Radiotracer Enables Pharmacodynamic Monitoring in Multiple Myeloma with PET | CD38‐Specific Gallium‐68 Labeled Peptide Radiotracer Enables Pharmacodynamic Monitoring in Multiple Myeloma with PET Abstract Abstract The limited availability of molecularly targeted low‐molecular‐weight imaging agents for monitoring multiple myeloma (MM)‐targeted therapies has been a significant challenge in the fiel... |
PMC9306736 | core_pubmed_pmc | Efruxifermin, a long‐acting Fc‐fusion FGF21 analogue, reduces body weight gain but does not increase sympathetic tone or urine volume in Sprague Dawley rats | Efruxifermin, a long‐acting Fc‐fusion FGF21 analogue, reduces body weight gain but does not increase sympathetic tone or urine volume in Sprague Dawley rats Abstract Abstract Background and Purpose Analogues of fibroblast growth factor 21 (FGF21) demonstrate diverse metabolic benefits in preclinical models of type 2 di... |
PMC12832527 | core_pubmed_pmc | Food contaminants: mechanisms of toxicity, computational assessment, and mitigation | Food contaminants: mechanisms of toxicity, computational assessment, and mitigation Abstract Abstract Understanding the toxicological mechanisms of food contaminants is critical for assessing risks to human health. This review comprehensively examines their adverse effects, tracing the pathway from molecular initiation... |
PMC12706418 | core_pubmed_pmc | A Step‐by‐Step Workflow for Performing In Silico Clinical Trials With Nonlinear Mixed Effects Models | A Step‐by‐Step Workflow for Performing In Silico Clinical Trials With Nonlinear Mixed Effects Models Abstract ABSTRACT In silico clinical trials (ISCT) are computational frameworks that employ mathematical models to generate virtual patients and simulate their responses to new treatments, treatment regimens, or medical... |
PMC7971233 | core_pubmed_pmc | Functional GLP-1R antibodies identified from a synthetic GPCR-focused library demonstrate potent blood glucose control | Functional GLP-1R antibodies identified from a synthetic GPCR-focused library demonstrate potent blood glucose control Abstract ABSTRACT G protein-coupled receptors (GPCRs) are a group of seven-transmembrane receptor proteins that have proven to be successful drug targets. Antibodies are becoming an increasingly promis... |
PMC12589532 | core_pubmed_pmc | Computational and molecular docking analysis of a novel azo compound and its nanocomposite biopolymer synthesized via a single-pot method | Computational and molecular docking analysis of a novel azo compound and its nanocomposite biopolymer synthesized via a single-pot method Abstract Abstract The synthesis of an azo molecule from phenol and dapsone was investigated using density functional theory (DFT) and infrared spectroscopy. The electronic structure ... |
PMC6473695 | core_pubmed_pmc | Effects of Cross-Training on Medical Teams’ Teamwork and Collaboration: Use of Simulation | Effects of Cross-Training on Medical Teams’ Teamwork and Collaboration: Use of Simulation Abstract Abstract Previous research in the US Navy demonstrated that cross-training enhances teamwork and interpersonal collaboration. Limited data exists on cross-training effectiveness in medical education. This research aimed t... |
PMC6647215 | core_pubmed_pmc | Phase I study of ipatasertib as a single agent and in combination with abiraterone plus prednisolone in Japanese patients with advanced solid tumors | Phase I study of ipatasertib as a single agent and in combination with abiraterone plus prednisolone in Japanese patients with advanced solid tumors Abstract Abstract Purpose Ipatasertib is a selective inhibitor of Akt, a frequently activated protein kinase in human cancers. The current study assessed the safety, toler... |
PMC9712475 | core_pubmed_pmc | Efficacy and safety of adjunctive padsevonil in adults with drug‐resistant focal epilepsy: Results from two double‐blind, randomized, placebo‐controlled trials | Efficacy and safety of adjunctive padsevonil in adults with drug‐resistant focal epilepsy: Results from two double‐blind, randomized, placebo‐controlled trials Abstract Abstract Objective To characterize efficacy, safety/tolerability, and pharmacokinetics of padsevonil (PSL) administered concomitantly with ≤3 antiseizu... |
PMC4697230 | core_pubmed_pmc | A comparative evaluation of 4% articaine and 2% lidocaine in mandibular buccal infiltration anesthesia: A clinical study | A comparative evaluation of 4% articaine and 2% lidocaine in mandibular buccal infiltration anesthesia: A clinical study Abstract Background: To compare 4% articaine and 2% lidocaine local anesthetics in achieving pulpal anesthesia of the lower first permanent molar teeth objectively, and to assess and compare lip and ... |
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