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PMC12598914 | core_pubmed_pmc | Concurrent Use of Tasipimidine Oral Solution and Clomipramine in Dogs | Concurrent Use of Tasipimidine Oral Solution and Clomipramine in Dogs Abstract ABSTRACT The study evaluated pharmacokinetics, effects on functional alertness, and cardiovascular parameters of tasipimidine oral solution (Tessie, Orion Corporation) alone and in combination with oral clomipramine in six healthy laboratory... |
PMC10233844 | core_pubmed_pmc | New Natural Eugenol Derivatives as Antiproliferative Agents: Synthesis, Biological Evaluation, and Computational Studies | New Natural Eugenol Derivatives as Antiproliferative Agents: Synthesis, Biological Evaluation, and Computational Studies Abstract Semisynthetic modifications of natural products have bestowed us with many anticancer drugs. In the present work, a natural product, eugenol, has been modified synthetically to generate new ... |
PMC5075013 | core_pubmed_pmc | Effects of Renal Impairment on Steady-State Plasma Concentrations of Rivastigmine: A Population Pharmacokinetic Analysis of Capsule and Patch Formulations in Patients with Alzheimer’s Disease | Effects of Renal Impairment on Steady-State Plasma Concentrations of Rivastigmine: A Population Pharmacokinetic Analysis of Capsule and Patch Formulations in Patients with Alzheimer’s Disease Abstract Introduction The glomerular filtration rate (GFR), a measure of renal function, decreases by approximately 10 mL/min ev... |
PMC8495120 | core_pubmed_pmc | Evaluation of Placental Transfer and Tissue Distribution of cis - and Trans -Permethrin in Pregnant Rats and Fetuses Using a Physiological-Based Pharmacokinetic Model | Evaluation of Placental Transfer and Tissue Distribution of cis - and Trans -Permethrin in Pregnant Rats and Fetuses Using a Physiological-Based Pharmacokinetic Model Abstract Abstract Biomonitoring studies have highlighted the exposure of pregnant women to pyrethroids based on the measurement of their metabolites in u... |
PMC12706416 | core_pubmed_pmc | Toward a Quantitative Understanding of Aficamten Clinical Pharmacology: Population Pharmacokinetic Modeling | Toward a Quantitative Understanding of Aficamten Clinical Pharmacology: Population Pharmacokinetic Modeling Abstract ABSTRACT Aficamten is a next‐in‐class, cardiac myosin inhibitor in development as a potential chronic oral treatment for patients with hypertrophic cardiomyopathy (HCM). A population pharmacokinetic (PK)... |
PMC7525767 | core_pubmed_pmc | On the Role of the Objective in the Optimization of Compartmental Models for Biomedical Therapies | On the Role of the Objective in the Optimization of Compartmental Models for Biomedical Therapies Abstract We review and discuss results obtained through an application of tools of nonlinear optimal control to biomedical problems. We discuss various aspects of the modeling of the dynamics (such as growth and interactio... |
PMC4257570 | core_pubmed_pmc | Population Pharmacokinetic Meta-Analysis of Vortioxetine in Healthy Individuals | Population Pharmacokinetic Meta-Analysis of Vortioxetine in Healthy Individuals Abstract The objective was to describe the pharmacokinetics of vortioxetine and evaluate the effect of intrinsic and extrinsic factors in the healthy population. Data from 26 clinical pharmacology studies were pooled. A total of 21,758 vort... |
PMC8765308 | core_pubmed_pmc | Pharmacokinetics and Pharmacodynamics of Clofazimine for Treatment of Cryptosporidiosis | Pharmacokinetics and Pharmacodynamics of Clofazimine for Treatment of Cryptosporidiosis Abstract ABSTRACT Infection with Cryptosporidium spp. can cause severe diarrhea, leading to long-term adverse impacts and even death in malnourished children and immunocompromised patients. The only FDA-approved drug for treating cr... |
PMC8917038 | core_pubmed_pmc | Impact of Antibodies Against Polyethylene Glycol on the Pharmacokinetics of PEGylated Asparaginase in Children with Acute Lymphoblastic Leukaemia: A Population Pharmacokinetic Approach | Impact of Antibodies Against Polyethylene Glycol on the Pharmacokinetics of PEGylated Asparaginase in Children with Acute Lymphoblastic Leukaemia: A Population Pharmacokinetic Approach Abstract Abstract Background and Objectives Besides allergic reactions, antibodies against polyethylene glycol (PEG) have been associat... |
PMC5760908 | core_pubmed_pmc | Quantification of sibutramine and its two metabolites in human plasma by LC–ESI-MS/MS and its application in a bioequivalence study | Quantification of sibutramine and its two metabolites in human plasma by LC–ESI-MS/MS and its application in a bioequivalence study Abstract Obesity can be considered as a chronic illness of epidemic proportion and its incidents have increased exponentially in recent years. The use of anti-obesity drugs such as sibutra... |
PMC4348513 | core_pubmed_pmc | Effect of the excipient concentration on the pharmacokinetics of PM181104, a novel antimicrobial thiazolyl cyclic peptide antibiotic, following intravenous administration to mice | Effect of the excipient concentration on the pharmacokinetics of PM181104, a novel antimicrobial thiazolyl cyclic peptide antibiotic, following intravenous administration to mice Abstract Abstract Thiazolyl cyclic peptide antibiotics are known for their poor aqueous solubility and unfavorable pharmacokinetics (PK) and ... |
PMC6738068 | core_pubmed_pmc | Safety and tolerability of CFI-400945, a first-in-class, selective PLK4 inhibitor in advanced solid tumours: a phase 1 dose-escalation trial | Safety and tolerability of CFI-400945, a first-in-class, selective PLK4 inhibitor in advanced solid tumours: a phase 1 dose-escalation trial Abstract Abstract Background CFI-400945 is a first-in-class oral inhibitor of polo-like kinase 4 (PLK4) that regulates centriole duplication. Primary objectives of this first-in-h... |
PMC6783587 | core_pubmed_pmc | Dose‐linearity of the pharmacokinetics of an intravenous [ 14 C]midazolam microdose in children | Dose‐linearity of the pharmacokinetics of an intravenous [ 14 C]midazolam microdose in children Abstract Aims Drug disposition in children may vary from adults due to age‐related variation in drug metabolism. Microdose studies present an innovation to study pharmacokinetics (PK) in paediatrics; however, they should be ... |
PMC5772927 | core_pubmed_pmc | A phase I clinical trial of dTCApFs, a derivative of a novel human hormone peptide, for the treatment of advanced/metastatic solid tumors | A phase I clinical trial of dTCApFs, a derivative of a novel human hormone peptide, for the treatment of advanced/metastatic solid tumors Abstract Abstract The aim of the present phase I first-in-human study was to investigate the safety/efficacy of dTCApFs (a novel hormone peptide that enters cells through the T1/ST2 ... |
PMC7935845 | core_pubmed_pmc | Therapeutic drug monitoring of oral targeted antineoplastic drugs | Therapeutic drug monitoring of oral targeted antineoplastic drugs Abstract Abstract Purpose This review provides an overview of the current challenges in oral targeted antineoplastic drug (OAD) dosing and outlines the unexploited value of therapeutic drug monitoring (TDM). Factors influencing the pharmacokinetic exposu... |
PMC7698174 | core_pubmed_pmc | Vancomycin Serum Concentration after 48 h of Administration: A 3-Years Survey in an Intensive Care Unit | Vancomycin Serum Concentration after 48 h of Administration: A 3-Years Survey in an Intensive Care Unit Abstract Abstract The present study assessed the proportion of intensive care unit (ICU) patients who had a vancomycin serum concentration between 20 and 25 mg/L after 24–48 h of intravenous vancomycin administration... |
PMC12046122 | core_pubmed_pmc | Population Pharmacokinetics‐Pharmacodynamics and Exposure‐Response of Ropeginterferon Alfa‐2b in Chinese and Japanese Patients With Polycythemia Vera | Population Pharmacokinetics‐Pharmacodynamics and Exposure‐Response of Ropeginterferon Alfa‐2b in Chinese and Japanese Patients With Polycythemia Vera Abstract ABSTRACT Ropeginterferon alfa‐2b (ropeg) represents a new‐generation interferon‐based therapy approved for polycythaemia vera (PV) treatment. This study aimed to... |
PMC10982092 | core_pubmed_pmc | Go beyond the limits of genetic algorithm in daily covariate selection practice | Go beyond the limits of genetic algorithm in daily covariate selection practice Abstract Covariate identification is an important step in the development of a population pharmacokinetic/pharmacodynamic model. Among the different available approaches, the stepwise covariate model (SCM) is the most used. However, SCM is ... |
PMC12485072 | core_pubmed_pmc | Psilocybin during the postpartum period induces long-lasting adverse effects in both mothers and offspring | Psilocybin during the postpartum period induces long-lasting adverse effects in both mothers and offspring Abstract Abstract Psilocybin increases social connectedness and has strong clinical transdiagnostic efficacy for mental illness, making it a candidate treatment to reduce maternal disconnect, anxiety, and blunted ... |
PMC5602457 | core_pubmed_pmc | Reversing factor Xa inhibitors – clinical utility of andexanet alfa | Reversing factor Xa inhibitors – clinical utility of andexanet alfa Abstract Abstract Approximately half of patients started on an oral anticoagulant in the USA now receive one of the newer direct oral anticoagulants (DOACs). Although there is an approved reversal agent for the direct thrombin inhibitor dabigatran, a s... |
PMC8909191 | core_pubmed_pmc | Extracorporeal Removal of Thermosensitive Liposomal Doxorubicin from Systemic Circulation after Tumor Delivery to Reduce Toxicities | Extracorporeal Removal of Thermosensitive Liposomal Doxorubicin from Systemic Circulation after Tumor Delivery to Reduce Toxicities Abstract Simple Summary Thermosensitive liposomes (TSL) are lipid-based nanoparticles that release the encapsulated drug in response to heat. TSL are administered systemically, e.g., by in... |
PMC12204373 | core_pubmed_pmc | Longitudinal pharmacokinetic and safety studies for dose optimization of a brain- penetrating erythropoietin for Alzheimer’s disease | Longitudinal pharmacokinetic and safety studies for dose optimization of a brain- penetrating erythropoietin for Alzheimer’s disease Abstract Abstract Background: Erythropoietin (EPO) is a potential therapeutic for Alzheimer’s disease (AD), but has limited brain penetration, requiring high systemic doses that lead to h... |
PMC8376131 | core_pubmed_pmc | Population pharmacokinetic analysis of dupilumab in adult and adolescent patients with asthma | Population pharmacokinetic analysis of dupilumab in adult and adolescent patients with asthma Abstract Abstract A population pharmacokinetic model was developed using data from healthy subjects and patients with moderate‐to‐severe asthma receiving intravenous or subcutaneous dupilumab doses. A total of nine phase I to ... |
PMC11622681 | core_pubmed_pmc | Population Pharmacokinetics and Dosing Regimen Analysis of Nirmatrelvir in Chinese Patients with COVID-19 Infection | Population Pharmacokinetics and Dosing Regimen Analysis of Nirmatrelvir in Chinese Patients with COVID-19 Infection Abstract Purpose Nirmatrelvir/ritonavir (N/R) is the first drug to receive emergency authorization for the treatment of COVID-19 infection. We aimed to develop a population pharmacokinetic (PopPK) model t... |
PMC9264615 | core_pubmed_pmc | Development of a multi-route physiologically based pharmacokinetic (PBPK) model for nanomaterials: a comparison between a traditional versus a new route-specific approach using gold nanoparticles in rats | Development of a multi-route physiologically based pharmacokinetic (PBPK) model for nanomaterials: a comparison between a traditional versus a new route-specific approach using gold nanoparticles in rats Abstract Abstract Background Physiologically based pharmacokinetic (PBPK) modeling is an important tool in predictin... |
PMC6484095 | core_pubmed_pmc | Association of anti-tuberculosis drug concentrations in hair and treatment outcomes in MDR- and XDR-TB | Association of anti-tuberculosis drug concentrations in hair and treatment outcomes in MDR- and XDR-TB Abstract Anti-tuberculosis drug concentrations in hair, a non-biohazardous and noninvasively collected biomatrix, predict extensively drug-resistant-TB clinical outcomes in a high-burden setting. http://ow.ly/80xi30o8... |
PMC11576823 | core_pubmed_pmc | An industry perspective on current QSP trends in drug development | An industry perspective on current QSP trends in drug development Abstract 2023 marks the 10th anniversary of Natpara’s submission to the US FDA, which led to the first recorded regulatory interaction where a decision was supported by Quantitative and Systems Pharmacology (QSP) simulations. It had taken about 5 years f... |
PMC8437420 | core_pubmed_pmc | An Evidence-Based Review of OLZ/SAM for Treatment of Adults with Schizophrenia or Bipolar I Disorder | An Evidence-Based Review of OLZ/SAM for Treatment of Adults with Schizophrenia or Bipolar I Disorder Abstract Abstract Olanzapine effectively treats schizophrenia and bipolar I disorder (BD-I); however, its use is limited by the risk of significant weight gain and metabolic effects. OLZ/SAM, a combination of olanzapine... |
PMC6370119 | core_pubmed_pmc | Population pharmacokinetics and individualized lobaplatin regimen for the treatment of Chinese small cell lung cancer in the elderly | Population pharmacokinetics and individualized lobaplatin regimen for the treatment of Chinese small cell lung cancer in the elderly Abstract Abstract Background: Lobaplatin (LBP) is a third-generation platinum compound. Material and methods: This prospective study was performed in 7 institutions in 2014–2016. Elderly ... |
PMC10610237 | core_pubmed_pmc | Development of Osthole-Loaded Microemulsions as a Prospective Ocular Delivery System for the Treatment of Corneal Neovascularization: In Vitro and In Vivo Assessments | Development of Osthole-Loaded Microemulsions as a Prospective Ocular Delivery System for the Treatment of Corneal Neovascularization: In Vitro and In Vivo Assessments Abstract Abstract Osthole (OST), a natural coumarin compound, has shown a significant inhibitory effect on corneal neovascularization (CNV). But, its eff... |
PMC8080744 | core_pubmed_pmc | Vancomycin-related convulsion in a pediatric patient with neuroblastoma: A case report and review of the literature | Vancomycin-related convulsion in a pediatric patient with neuroblastoma: A case report and review of the literature Abstract Abstract BACKGROUND Vancomycin is often used as an anti-infective drug in patients receiving anti-tumor chemotherapy. There are concerns about its adverse drug reactions during treatment, such as... |
PMC7491553 | core_pubmed_pmc | Ledipasvir plus sofosbuvir in pregnant women with hepatitis C virus infection: a phase 1 pharmacokinetic study | Ledipasvir plus sofosbuvir in pregnant women with hepatitis C virus infection: a phase 1 pharmacokinetic study Abstract Summary Background Hepatitis C virus (HCV) infection is increasing among pregnant women because of the opioid epidemic, yet there are no interventions to reduce perinatal HCV transmission or to treat ... |
PMC3817377 | core_pubmed_pmc | Cardiovascular Disease: The Other Face of Diabetes | Cardiovascular Disease: The Other Face of Diabetes Abstract Abstract Despite glycemic control, evidence suggests that mortality and morbidity remain high in diabetes. Regulatory agencies deem, therefore, additional safety trials necessary for the approval of new antidiabetic drugs. Nevertheless, markers of cardiovascul... |
PMC10681519 | core_pubmed_pmc | Model‐based prediction of effective target exposure for MEN1611 in combination with trastuzumab in HER2 ‐positive advanced or metastatic breast cancer patients | Model‐based prediction of effective target exposure for MEN1611 in combination with trastuzumab in HER2 ‐positive advanced or metastatic breast cancer patients Abstract Abstract MEN1611 is a novel orally bioavailable PI3K inhibitor currently in clinical development for patients with HER2‐positive (HER2+) PI3KCA mutated... |
PMC12641123 | core_pubmed_pmc | Results from the Survey of Antibiotic Resistance (SOAR) 2018–21 in Ukraine: data based on CLSI, EUCAST (dose-specific) and pharmacokinetic/pharmacodynamic (PK/PD) breakpoints | Results from the Survey of Antibiotic Resistance (SOAR) 2018–21 in Ukraine: data based on CLSI, EUCAST (dose-specific) and pharmacokinetic/pharmacodynamic (PK/PD) breakpoints Abstract Abstract Objectives To determine the antibiotic susceptibility of Streptococcus pneumoniae and Haemophilus influenzae from community-acq... |
PMC9986545 | core_pubmed_pmc | A novel oral formulation of the melanocortin-1 receptor agonist PL8177 resolves inflammation in preclinical studies of inflammatory bowel disease and is gut restricted in rats, dogs, and humans | A novel oral formulation of the melanocortin-1 receptor agonist PL8177 resolves inflammation in preclinical studies of inflammatory bowel disease and is gut restricted in rats, dogs, and humans Abstract Introduction PL8177 is a potent and selective agonist of the melanocortin 1 receptor (MC1R). PL8177 has shown efficac... |
PMC8388891 | core_pubmed_pmc | Non- β -Lactam Allosteric Inhibitors Target Methicillin-Resistant Staphylococcus aureus : An In Silico Drug Discovery Study | Non- β -Lactam Allosteric Inhibitors Target Methicillin-Resistant Staphylococcus aureus : An In Silico Drug Discovery Study Abstract Abstract Penicillin-binding proteins (PBPs) catalyze the final stages for peptidoglycan cell-wall bio-synthesis. Mutations in the PBP2a subunit can attenuate β -lactam antibiotic activity... |
PMC12167913 | core_pubmed_pmc | Mechanistic Physiologically Based Pharmacokinetic Modeling of Dry Powder and Nebulized Formulations of Orally Inhaled TMEM16A Potentiator GDC ‐6988 | Mechanistic Physiologically Based Pharmacokinetic Modeling of Dry Powder and Nebulized Formulations of Orally Inhaled TMEM16A Potentiator GDC ‐6988 Abstract ABSTRACT The orally inhaled route of administration for respiratory indications can maximize drug exposure to the site of action (lung) to increase efficacy while ... |
PMC6271300 | core_pubmed_pmc | The pharmacokinetics of gabapentin in cats | The pharmacokinetics of gabapentin in cats Abstract Abstract Background Gabapentin is the most commonly prescribed medication for the treatment of chronic musculoskeletal pain in cats. Despite this common and chronic usage, clinically relevant pharmacokinetic data is lacking. Objectives To evaluate the pharmacokinetics... |
PMC9143883 | core_pubmed_pmc | Pharmacokinetics and Pharmacodynamics of Butorphanol and Dexmedetomidine after Intranasal Administration in Broiler Chickens ( Gallus gallus domesticus ) | Pharmacokinetics and Pharmacodynamics of Butorphanol and Dexmedetomidine after Intranasal Administration in Broiler Chickens ( Gallus gallus domesticus ) Abstract Abstract Butorphanol and dexmedetomidine (DXM) can produce analgesia in birds. Intranasal (IN) route of drug administration is easier, and free of risks such... |
PMC6260283 | core_pubmed_pmc | A quick and simple method for the determination of ivermectin in dog plasma by LC–MS/MS | A quick and simple method for the determination of ivermectin in dog plasma by LC–MS/MS Abstract Abstract Ivermectin is an endectocide belonging to the macrocyclic lactone class, commonly used in dogs as a heartworm preventative and for the treatment of several external and internal parasite infections. Among the analy... |
PMC7079947 | core_pubmed_pmc | PEGylated human catalase elicits potent therapeutic effects on H1N1 influenza-induced pneumonia in mice | PEGylated human catalase elicits potent therapeutic effects on H1N1 influenza-induced pneumonia in mice Abstract Abstract Therapeutic recombinant human catalase (rhCAT) can quench infection-induced reactive oxygen species (ROS), thereby alleviating the associated tissue damage. Although the intranasal route is efficien... |
PMC5485013 | core_pubmed_pmc | Insulin degludec: Lower day‐to‐day and within‐day variability in pharmacodynamic response compared with insulin glargine 300 U/mL in type 1 diabetes | Insulin degludec: Lower day‐to‐day and within‐day variability in pharmacodynamic response compared with insulin glargine 300 U/mL in type 1 diabetes Abstract Abstract Aim To compare day‐to‐day and within‐day variability in glucose‐lowering effect between insulin degludec (IDeg) and insulin glargine 300 U/mL (IGlar‐U300... |
PMC4625865 | core_pubmed_pmc | Development of a Multicompartment Permeability-Limited Lung PBPK Model and Its Application in Predicting Pulmonary Pharmacokinetics of Antituberculosis Drugs | Development of a Multicompartment Permeability-Limited Lung PBPK Model and Its Application in Predicting Pulmonary Pharmacokinetics of Antituberculosis Drugs Abstract Achieving sufficient concentrations of antituberculosis (TB) drugs in pulmonary tissue at the optimum time is still a challenge in developing therapeutic... |
PMC4623309 | core_pubmed_pmc | Albumin-deficient mouse models for studying metabolism of human albumin and pharmacokinetics of albumin-based drugs | Albumin-deficient mouse models for studying metabolism of human albumin and pharmacokinetics of albumin-based drugs Abstract Serum albumin is the major determinant of blood colloidal osmotic pressure acting as a depot and distributor of compounds including drugs. In humans, serum albumin exhibits an unusually long half... |
PMC3271541 | core_pubmed_pmc | Dose escalation pharmacokinetics and lipid lowering activity of a novel farnesoid X receptor modulator: 16-Dehydropregnenolone | Dose escalation pharmacokinetics and lipid lowering activity of a novel farnesoid X receptor modulator: 16-Dehydropregnenolone Abstract Objectives: To study the dose escalation pharmacokinetics and lipid lowering activity of a novel FXR modulator, 16-Dehydropregnenolone (DHP). Materials and Methods: The disposition of ... |
PMC12298447 | core_pubmed_pmc | Effect of Hepatic Impairment on the Pharmacokinetics of Baicalin in Rats: Critical Roles of Gut Microbiota and Hepatic Transporters | Effect of Hepatic Impairment on the Pharmacokinetics of Baicalin in Rats: Critical Roles of Gut Microbiota and Hepatic Transporters Abstract Abstract Background : Baicalin (BG) has been used in the treatment of many diseases. However, the effect of hepatic insufficiency on its pharmacokinetics has not been reported, an... |
PMC6440574 | core_pubmed_pmc | Pharmacokinetic and Pharmacodynamic Considerations in the Design of Therapeutic Antibodies | Pharmacokinetic and Pharmacodynamic Considerations in the Design of Therapeutic Antibodies Abstract The design and development of therapeutic monoclonal antibodies (mAbs) through optimizing their pharmacokinetic ( PK ) and pharmacodynamic ( PD ) properties is crucial to improve efficacy while minimizing adverse events.... |
PMC8817607 | core_pubmed_pmc | Comparative pharmacokinetics and tissue distribution of primaquine enantiomers in mice | Comparative pharmacokinetics and tissue distribution of primaquine enantiomers in mice Abstract Background Primaquine (PQ) has been used for the radical cure of relapsing Plasmodium vivax malaria for more than 60 years. PQ is also recommended for prophylaxis and prevention of transmission of Plasmodium falciparum . How... |
PMC4885546 | core_pubmed_pmc | A Comparison of Differences Between the Systemic Pharmacokinetics of Levobupivacaine and Ropivacaine During Continuous Epidural Infusion: A Prospective, Randomized, Multicenter, Double-Blind Controlled Trial | A Comparison of Differences Between the Systemic Pharmacokinetics of Levobupivacaine and Ropivacaine During Continuous Epidural Infusion: A Prospective, Randomized, Multicenter, Double-Blind Controlled Trial Abstract Abstract BACKGROUND: Epidural infusion of levobupivacaine and ropivacaine provides adequate postoperati... |
PMC3612473 | core_pubmed_pmc | Towards Polypharmacokinetics: Pharmacokinetics of Multicomponent Drugs and Herbal Medicines Using a Metabolomics Approach | Towards Polypharmacokinetics: Pharmacokinetics of Multicomponent Drugs and Herbal Medicines Using a Metabolomics Approach Abstract Abstract Determination of pharmacokinetics (PKs) of multicomponent pharmaceuticals and/or nutraceuticals (polypharmacokinetics, poly-PKs) is difficult due to the vast number of compounds pr... |
PMC8742646 | core_pubmed_pmc | Propsective evaluation of high‐dose methotrexate pharmacokinetics in adult patients with lymphoma using novel determinants of kidney function | Propsective evaluation of high‐dose methotrexate pharmacokinetics in adult patients with lymphoma using novel determinants of kidney function Abstract Abstract High‐dose methotrexate (HDMTX) pharmacokinetics (PKs), including the best estimated glomerular filtration rate (eGFR) equation that reflects methotrexate (MTX) ... |
PMC8139892 | core_pubmed_pmc | Fosfomycin in continuous or prolonged infusion for systemic bacterial infections: a systematic review of its dosing regimen proposal from in vitro, in vivo and clinical studies | Fosfomycin in continuous or prolonged infusion for systemic bacterial infections: a systematic review of its dosing regimen proposal from in vitro, in vivo and clinical studies Abstract Abstract Fosfomycin (FOS) administered intravenously has been recently rediscovered for the treatment of systemic infections due to mu... |
PMC9260690 | core_pubmed_pmc | Optimizing Antimicrobial Therapy by Integrating Multi-Omics With Pharmacokinetic/Pharmacodynamic Models and Precision Dosing | Optimizing Antimicrobial Therapy by Integrating Multi-Omics With Pharmacokinetic/Pharmacodynamic Models and Precision Dosing Abstract Abstract In the era of “ Bad Bugs, No Drugs ,” optimizing antibiotic therapy against multi-drug resistant (MDR) pathogens is crucial. Mathematical modelling has been employed to further ... |
PMC12521061 | core_pubmed_pmc | Development and Verification of Virtual Population Models for Predicting Drug Pharmacokinetics in Ethnic North American Populations | Development and Verification of Virtual Population Models for Predicting Drug Pharmacokinetics in Ethnic North American Populations Abstract ABSTRACT Ethnic variabilities can affect the outcome of drug pharmacokinetics (PK) and drug–drug interactions (DDI). This work aimed to develop four North American (NA) sub‐popula... |
PMC3173598 | core_pubmed_pmc | Evaluation of the effect of dapagliflozin on cardiac repolarization: a thorough QT/QTc study | Evaluation of the effect of dapagliflozin on cardiac repolarization: a thorough QT/QTc study Abstract Abstract Introduction Dapagliflozin is a first-in-class sodium-glucose transporter 2 (SGLT2) inhibitor under investigation for the treatment of type 2 diabetes mellitus. A thorough QTc study was conducted, according to... |
PMC6342244 | core_pubmed_pmc | Effects of Common CYP 1A2 Genotypes and Other Key Factors on Intraindividual Variation in the Caffeine Metabolic Ratio: An Exploratory Analysis | Effects of Common CYP 1A2 Genotypes and Other Key Factors on Intraindividual Variation in the Caffeine Metabolic Ratio: An Exploratory Analysis Abstract The caffeine metabolic ratio is an established marker for cytochrome P450 ( CYP ) 1A2 activity. Optimal sample size calculation for clinical pharmacokinetic xenobiotic... |
PMC6611615 | core_pubmed_pmc | Ambrosin, a potent NF-κβ inhibitor, ameliorates lipopolysaccharide induced memory impairment, comparison to curcumin | Ambrosin, a potent NF-κβ inhibitor, ameliorates lipopolysaccharide induced memory impairment, comparison to curcumin Abstract Abstract Despite its poor bioavailability, curcumin is a promising natural polyphenol targeting NF-κβ. NF-κβ is a target for new therapeutics because it plays a pivotal role in the pathophysiolo... |
PMC3910016 | core_pubmed_pmc | A General Network Pharmacodynamic Model–Based Design Pipeline for Customized Cancer Therapy Applied to the VEGFR Pathway | A General Network Pharmacodynamic Model–Based Design Pipeline for Customized Cancer Therapy Applied to the VEGFR Pathway Abstract Abstract A unified approach to optimize multidrug chemotherapy using a pharmacokinetic (PK)/enhanced pharmacodynamic model was developed using the vascular endothelial growth factor receptor... |
PMC9748077 | core_pubmed_pmc | Pharmacokinetics, tissue distribution, and plasma protein binding rate of curcumol in rats using liquid chromatography tandem mass spectrometry | Pharmacokinetics, tissue distribution, and plasma protein binding rate of curcumol in rats using liquid chromatography tandem mass spectrometry Abstract Abstract Objective: Curcumol is one of the major active ingredients isolated from the traditional Chinese medicine Curcumae Rhizoma and is reported to exhibit various ... |
PMC6255772 | core_pubmed_pmc | Enhanced anti-metastatic bioactivity of an IGF-TRAP re-engineered to improve physicochemical properties | Enhanced anti-metastatic bioactivity of an IGF-TRAP re-engineered to improve physicochemical properties Abstract Abstract The insulin-like growth factor (IGF) axis has been implicated in the progression of malignant disease and identified as a clinically important therapeutic target. Several IGF-1 receptor (IGF-1R) tar... |
PMC12937382 | core_pubmed_pmc | Pharmacokinetic Characteristics of Florfenicol in Freshwater Crocodiles ( Crocodylus siamensis ) After Intramuscular Administration | Pharmacokinetic Characteristics of Florfenicol in Freshwater Crocodiles ( Crocodylus siamensis ) After Intramuscular Administration Abstract Simple Summary Pharmacokinetic information on antimicrobial use in reptiles is extremely limited. Often, drug dosages and approaches are extrapolated from other animal species, wh... |
PMC12287611 | core_pubmed_pmc | Pharmacokinetics and tissue distribution analysis of ginsenoside Rh 3 in rats using a novel LC-MS/MS quantification strategy | Pharmacokinetics and tissue distribution analysis of ginsenoside Rh 3 in rats using a novel LC-MS/MS quantification strategy Abstract Introduction: Ginsenoside Rh3 (GRh 3 ), a rare ginsenoside, demonstrates diverse pharmacological activities in vitro ; however, the lack of pharmacokinetic and tissue distribution data h... |
PMC3722550 | core_pubmed_pmc | Influence of the Duration of Intravenous Drug Administration on Tumor Uptake | Influence of the Duration of Intravenous Drug Administration on Tumor Uptake Abstract Abstract Enhancing tumor uptake of anticancer drugs is an important therapeutic goal, because insufficient drug accumulation is now considered to be an important reason for unresponsiveness or resistance to antitumor therapy. Based on... |
PMC12280840 | core_pubmed_pmc | Development and Validation of a Rapid LC–MS/MS Method for Plasma Analysis of Ketamine, Norketamine, Dehydronorketamine, and Hydroxynorketamine | Development and Validation of a Rapid LC–MS/MS Method for Plasma Analysis of Ketamine, Norketamine, Dehydronorketamine, and Hydroxynorketamine Abstract ABSTRACT Ketamine, a well‐established dissociative anesthetic, has recently gained significant attention for its rapid‐acting antidepressant effects, particularly in tr... |
PMC8655230 | core_pubmed_pmc | Data-Driven Discovery of Mathematical and Physical Relations in Oncology Data Using Human-Understandable Machine Learning | Data-Driven Discovery of Mathematical and Physical Relations in Oncology Data Using Human-Understandable Machine Learning Abstract For decades, researchers have used the concepts of rate of change and differential equations to model and forecast neoplastic processes. This expressive mathematical apparatus brought signi... |
PMC3816049 | core_pubmed_pmc | Opposite Effects of Single-Dose and Multidose Administration of the Ethanol Extract of Danshen on CYP3A in Healthy Volunteers | Opposite Effects of Single-Dose and Multidose Administration of the Ethanol Extract of Danshen on CYP3A in Healthy Volunteers Abstract Abstract The aim of this study was to investigate the effect of single- and multidose administration of the ethanol extract of danshen on in vivo CYP3A activity in healthy volunteers. A... |
PMC12960285 | core_pubmed_pmc | Beyond the Needle: Reimagining Insulin Delivery and the Evolution of Inhaled Insulins | Beyond the Needle: Reimagining Insulin Delivery and the Evolution of Inhaled Insulins Abstract Abstract Insulin has been around for a century since its discovery and has seen multiple innovations to improve its pharmacokinetic profile, thus impacting its efficacy, safety, and patient compliance. Despite its powerful gl... |
PMC11011490 | core_pubmed_pmc | Virus-Induced Epilepsy vs. Epilepsy Patients Acquiring Viral Infection: Unravelling the Complex Relationship for Precision Treatment | Virus-Induced Epilepsy vs. Epilepsy Patients Acquiring Viral Infection: Unravelling the Complex Relationship for Precision Treatment Abstract The intricate relationship between viruses and epilepsy involves a bidirectional interaction. Certain viruses can induce epilepsy by infecting the brain, leading to inflammation,... |
PMC11792624 | core_pubmed_pmc | Iron(III)–Quercetin Complex: In Vivo Acute Toxicity and Biodistribution of Novel MRI Agent | Iron(III)–Quercetin Complex: In Vivo Acute Toxicity and Biodistribution of Novel MRI Agent Abstract Background The iron(III)–quercetin complex, known as “IronQ”, is an innovative MRI contrast agent composed of one Fe(III) ion and two quercetin molecules. IronQ is efficiently internalized by cells, enabling T1-weighted ... |
PMC8424645 | core_pubmed_pmc | [ 18 F]Atorvastatin Pharmacokinetics and Biodistribution in Healthy Female and Male Rats | [ 18 F]Atorvastatin Pharmacokinetics and Biodistribution in Healthy Female and Male Rats Abstract Abstract Statins are 3-hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors that are widely used to prevent cardiovascular diseases. However, a series of pleiotropic mechanisms have been associated with statins, partic... |
PMC9182147 | core_pubmed_pmc | Preclinical Pharmacokinetics and Bioavailability of Oxypeucedanin in Rats after Single Intravenous and Oral Administration | Preclinical Pharmacokinetics and Bioavailability of Oxypeucedanin in Rats after Single Intravenous and Oral Administration Abstract Abstract Oxypeucedanin, a furanocoumarin extracted from many traditional Chinese herbal medicines, has a variety of pharmacological effects. However, the independent pharmacokinetic charac... |
PMC12738524 | core_pubmed_pmc | Waste valorization utilizing green nanotechnology: a sustainable approach for pomegranate peel agro wastes in skincare formulations | Waste valorization utilizing green nanotechnology: a sustainable approach for pomegranate peel agro wastes in skincare formulations Abstract Abstract Pomegranate peels, a valuable waste byproduct, aligned with the Sustainable Development Goals by United Nations offering a possibility for use as a raw material in herbal... |
PMC7671486 | core_pubmed_pmc | Development of an Orally Bioavailable Isoliquiritigenin Self-Nanoemulsifying Drug Delivery System to Effectively Treat Ovalbumin-Induced Asthma | Development of an Orally Bioavailable Isoliquiritigenin Self-Nanoemulsifying Drug Delivery System to Effectively Treat Ovalbumin-Induced Asthma Abstract Abstract Purpose Isoliquiritigenin (ILQ), an important component of Anti-Asthma Herbal Medicine Intervention (ASHMI), had shown potent anti-asthma effect in vitro in o... |
PMC11695911 | core_pubmed_pmc | The distinctive pharmacokinetic profile of rezafungin, a long-acting echinocandin developed in the era of modern pharmacometrics | The distinctive pharmacokinetic profile of rezafungin, a long-acting echinocandin developed in the era of modern pharmacometrics Abstract Abstract Echinocandin drugs are the current first-line therapy for fungal infections caused by Candida spp. Most patients require once-daily intravenous (IV) administration in a hosp... |
PMC12042295 | core_pubmed_pmc | Factor XI and Atrial Fibrillation: A Mismatched Pairing? | Factor XI and Atrial Fibrillation: A Mismatched Pairing? Abstract Abstract Factor XI (FXI) is a liver-produced coagulation zymogen that evolutionarily originated from duplication of the gene encoding for prekallikrein. It circulates in complex with high-molecular-weight kininogen, and consists of two identical subunits... |
PMC7211202 | core_pubmed_pmc | Phase 1 study of the MDM2 inhibitor AMG 232 in patients with advanced P53 wild-type solid tumors or multiple myeloma | Phase 1 study of the MDM2 inhibitor AMG 232 in patients with advanced P53 wild-type solid tumors or multiple myeloma Abstract Summary Background This open-label, first-in-human, phase 1 study evaluated AMG 232, an oral selective MDM2 inhibitor in patients with TP53 wild-type (P53WT), advanced solid tumors or multiple m... |
PMC7059485 | core_pubmed_pmc | Severity of coeliac disease and clinical management study when using a CYP3A4 metabolised medication: a phase I pharmacokinetic study | Severity of coeliac disease and clinical management study when using a CYP3A4 metabolised medication: a phase I pharmacokinetic study Abstract Abstract Objective Severity of coeliac disease depends in part on the extent of small intestinal mucosa injury. Patients with the most abnormal pathology have loss of duodenal v... |
PMC8379255 | core_pubmed_pmc | Excessive unbound cefazolin concentrations in critically ill patients receiving veno-arterial extracorporeal membrane oxygenation (vaECMO): an observational study | Excessive unbound cefazolin concentrations in critically ill patients receiving veno-arterial extracorporeal membrane oxygenation (vaECMO): an observational study Abstract Abstract The scope of extracorporeal membrane oxygenation (ECMO) is expanding, nevertheless, pharmacokinetics in patients receiving cardiorespirator... |
PMC6875707 | core_pubmed_pmc | Linking Tumor Growth Dynamics to Survival in Ipilimumab‐Treated Patients With Advanced Melanoma Using Mixture Tumor Growth Dynamic Modeling | Linking Tumor Growth Dynamics to Survival in Ipilimumab‐Treated Patients With Advanced Melanoma Using Mixture Tumor Growth Dynamic Modeling Abstract Early tumor assessments have been widely used to predict overall survival ( OS ), with potential application to dose selection and early go/no‐go decisions. Most published... |
PMC10776547 | core_pubmed_pmc | Efficacy and Safety of Biosimilar QL1207 vs. the Reference Aflibercept for Patients with Neovascular Age-Related Macular Degeneration: A Randomized Phase 3 Trial | Efficacy and Safety of Biosimilar QL1207 vs. the Reference Aflibercept for Patients with Neovascular Age-Related Macular Degeneration: A Randomized Phase 3 Trial Abstract Abstract Introduction This trial aimed to compare the efficacy and safety between biosimilar QL1207 and the reference aflibercept for the treatment o... |
PMC10064817 | core_pubmed_pmc | Absolute oral bioavailability and possible metabolic pathway of panduratin A from Boesenbergia rotunda extract in beagle dogs | Absolute oral bioavailability and possible metabolic pathway of panduratin A from Boesenbergia rotunda extract in beagle dogs Abstract Abstract Context Attempts are ongoing to develop medications to fight against the COVID-19 pandemic. Our previous study revealed the in vitro anti-SARS-CoV-2 activity of fingerroot [ Bo... |
PMC8301588 | core_pubmed_pmc | Evaluating risk factors for acute graft versus host disease in pediatric hematopoietic stem cell transplant patients receiving tacrolimus | Evaluating risk factors for acute graft versus host disease in pediatric hematopoietic stem cell transplant patients receiving tacrolimus Abstract Abstract To identify the clinical and pharmacological risk factors associated with tacrolimus pharmacodynamics for acute graft‐versus‐host disease (aGVHD) in pediatric patie... |
PMC5559372 | core_pubmed_pmc | Pharmacokinetics of ceftiofur in healthy and lipopolysaccharide-induced endotoxemic newborn calves treated with single and combined therapy | Pharmacokinetics of ceftiofur in healthy and lipopolysaccharide-induced endotoxemic newborn calves treated with single and combined therapy Abstract The aim of this research was to compare plasma pharmacokinetics of ceftiofur sodium (CS) in healthy calves, and in calves with experimentally induced endotoxemia. Six calv... |
PMC4368841 | core_pubmed_pmc | Dose-Exposure Proportionality of a Novel Recombinant Follicle-Stimulating Hormone (rFSH), FE 999049, Derived from a Human Cell Line, with Comparison Between Caucasian and Japanese Women After Subcutaneous Administration | Dose-Exposure Proportionality of a Novel Recombinant Follicle-Stimulating Hormone (rFSH), FE 999049, Derived from a Human Cell Line, with Comparison Between Caucasian and Japanese Women After Subcutaneous Administration Abstract Abstract Background and Objectives FE 999049 is a novel recombinant follicle-stimulating ho... |
PMC6218676 | core_pubmed_pmc | Randomized, Double‐Blind, Placebo‐Controlled, Single Ascending Dose Trial of Synthetic Preimplantation Factor in Autoimmune Hepatitis | Randomized, Double‐Blind, Placebo‐Controlled, Single Ascending Dose Trial of Synthetic Preimplantation Factor in Autoimmune Hepatitis Abstract Preimplantation factor (PIF) is an evolutionary conserved peptide secreted by viable embryos which promotes maternal tolerance without immune suppression. Synthetic PIF (sPIF) r... |
PMC5651322 | core_pubmed_pmc | The effects of advanced age and serum α 1 ‐acid glycoprotein on docetaxel unbound exposure and dose‐limiting toxicity in cancer patients | The effects of advanced age and serum α 1 ‐acid glycoprotein on docetaxel unbound exposure and dose‐limiting toxicity in cancer patients Abstract Aim α 1 ‐Acid glycoprotein (AAG), which is a major binding protein of docetaxel, is considered to be a determinant for docetaxel pharmacokinetics. However, there are no repor... |
PMC9540484 | core_pubmed_pmc | Pharmacometric and Electrocardiographic Evaluation of Chloroquine and Azithromycin in Healthy Volunteers | Pharmacometric and Electrocardiographic Evaluation of Chloroquine and Azithromycin in Healthy Volunteers Abstract Chloroquine and azithromycin were developed in combination for the preventive treatment of malaria in pregnancy, and more recently were proposed as coronavirus disease 2019 (COVID‐19) treatment options. Bil... |
PMC5721397 | core_pubmed_pmc | Pharmacokinetics and pharmacodynamics modeling of lonafarnib in patients with chronic hepatitis delta virus infection | Pharmacokinetics and pharmacodynamics modeling of lonafarnib in patients with chronic hepatitis delta virus infection Abstract Abstract The prenylation inhibitor lonafarnib (LNF) is a potent antiviral agent providing a breakthrough for the treatment of hepatitis delta virus (HDV). The current study used a maximum likel... |
PMC10785662 | core_pubmed_pmc | Improved Targeting and Safety of Doxorubicin through a Novel Albumin Binding Prodrug Approach | Improved Targeting and Safety of Doxorubicin through a Novel Albumin Binding Prodrug Approach Abstract Human serum albumin (HSA) improves the pharmacokinetic profile of drugs attached to it, making it an attractive carrier with proven clinical success. In our previous studies, we have shown that Caveolin-1 (Cav-1) and ... |
PMC8322774 | core_pubmed_pmc | Persistency of Mesenchymal Stromal/Stem Cells in Lungs | Persistency of Mesenchymal Stromal/Stem Cells in Lungs Abstract Abstract Mesenchymal stromal/stem cells (MSCs) are a fibroblast-like cell population with high regenerative potential that can be isolated from many different tissues. Several data suggest MSCs as a therapeutic tool capable of migrating to a site of injury... |
PMC8714938 | core_pubmed_pmc | Pharmacodynamic effects of direct AMP kinase activation in humans with insulin resistance and non-alcoholic fatty liver disease: A phase 1b study | Pharmacodynamic effects of direct AMP kinase activation in humans with insulin resistance and non-alcoholic fatty liver disease: A phase 1b study Abstract Summary AMPK is an energy sensor modulating metabolism, inflammation, and a target for metabolic disorders. Metabolic dysfunction results in lower AMPK activity. PXL... |
PMC9648981 | core_pubmed_pmc | Pharmacokinetic Model Based on Stochastic Simulation and Estimation for Therapeutic Drug Monitoring of Tacrolimus in Korean Adult Transplant Recipients | Pharmacokinetic Model Based on Stochastic Simulation and Estimation for Therapeutic Drug Monitoring of Tacrolimus in Korean Adult Transplant Recipients Abstract Background: Tacrolimus shows high variability in inter- and intraindividual pharmacokinetics (PK); therefore, it is important to develop an appropriate model f... |
PMC7589268 | core_pubmed_pmc | PK/PD Mediated Dose Optimization of Emactuzumab, a CSF1R Inhibitor, in Patients With Advanced Solid Tumors and Diffuse‐Type Tenosynovial Giant Cell Tumor | PK/PD Mediated Dose Optimization of Emactuzumab, a CSF1R Inhibitor, in Patients With Advanced Solid Tumors and Diffuse‐Type Tenosynovial Giant Cell Tumor Abstract Targeted biological therapies may achieve maximal therapeutic efficacy at doses below the maximum tolerated dose (MTD); therefore, the search for the MTD in ... |
PMC6961218 | core_pubmed_pmc | Study of gender-related pharmacokinetics of ezogabine in Egyptian volunteers by a validated LC-MS/MS bioanalytical method | Study of gender-related pharmacokinetics of ezogabine in Egyptian volunteers by a validated LC-MS/MS bioanalytical method Abstract Abstract Gender-based pharmacokinetics and/or pharmacodynamics differences can result in differences in treatment which can accordingly affect the drug safety and/or efficacy. A new validat... |
PMC5403841 | core_pubmed_pmc | A randomized, single-blind, single-dose study evaluating the pharmacokinetic equivalence of proposed biosimilar ABP 980 and trastuzumab in healthy male subjects | A randomized, single-blind, single-dose study evaluating the pharmacokinetic equivalence of proposed biosimilar ABP 980 and trastuzumab in healthy male subjects Abstract Abstract Purpose This study compared the pharmacokinetic (PK) profiles of the proposed biosimilar ABP 980 and trastuzumab in healthy males. Methods In... |
PMC9167373 | core_pubmed_pmc | Pharmacokinetics and Safety of Ferric Pyrophosphate Citrate in Chinese Subjects with and without Hemodialysis-Dependent Stage 5 Chronic Kidney Disease | Pharmacokinetics and Safety of Ferric Pyrophosphate Citrate in Chinese Subjects with and without Hemodialysis-Dependent Stage 5 Chronic Kidney Disease Abstract Abstract Background and Objective Anemia caused by iron depletion is common in patients with hemodialysis-dependent stage 5 chronic kidney disease (CKD-5HD) pat... |
PMC12534026 | core_pubmed_pmc | Exposure Matching Using Population Pharmacokinetic Modeling and Simulation to Support Rimegepant Dose Selection for Pediatric Patients With Migraine | Exposure Matching Using Population Pharmacokinetic Modeling and Simulation to Support Rimegepant Dose Selection for Pediatric Patients With Migraine Abstract ABSTRACT Rimegepant is a small molecule calcitonin gene‐related peptide receptor antagonist approved as a 75 mg orally disintegrating tablet for the acute treatme... |
PMC4475328 | core_pubmed_pmc | The pharmacokinetics and pharmacodynamics of danirixin (GSK1325756) − a selective CXCR2 antagonist − in healthy adult subjects | The pharmacokinetics and pharmacodynamics of danirixin (GSK1325756) − a selective CXCR2 antagonist − in healthy adult subjects Abstract Background Excessive neutrophil presence and activation is important in a number of acute and chronic inflammatory diseases. The CXCR2 chemokine receptor is important in controlling th... |
PMC12821657 | core_pubmed_pmc | Irisin as a Neuroprotective Agent in Parkinson’s Disease: The Role of Physical Exercise in Modulating Dopaminergic Neurons | Irisin as a Neuroprotective Agent in Parkinson’s Disease: The Role of Physical Exercise in Modulating Dopaminergic Neurons Abstract Abstract Exercise-induced myokines have emerged as crucial mediators of the beneficial effects of physical activity on neurodegenerative diseases through complex molecular mechanisms invol... |
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