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PMC9662173
core_pubmed_pmc
Beta-Lactam Antibiotic Therapeutic Drug Monitoring in Critically Ill Patients: A Systematic Review and Meta-Analysis
Beta-Lactam Antibiotic Therapeutic Drug Monitoring in Critically Ill Patients: A Systematic Review and Meta-Analysis Abstract Abstract Therapeutic drug monitoring (TDM) of beta-lactam antibiotics is recommended to address the variability in exposure observed in critical illness. However, the impact of TDM-guided dosing...
PMC6363065
core_pubmed_pmc
Children Are Not Small Adults, but Can We Treat Them As Such?
Children Are Not Small Adults, but Can We Treat Them As Such? Abstract Although children cannot be considered small adults due to nonlinear processes underlying the pharmacokinetics of drugs, pediatric doses are typically still expressed per kilogram. We use a physiologically based pharmacokinetic (PBPK) workflow to as...
PMC4812395
core_pubmed_pmc
Visualizing spatial distribution of alectinib in murine brain using quantitative mass spectrometry imaging
Visualizing spatial distribution of alectinib in murine brain using quantitative mass spectrometry imaging Abstract In the development of anticancer drugs, drug concentration measurements in the target tissue have been thought to be crucial for predicting drug efficacy and safety. Liquid chromatography-tandem mass spec...
PMC9075780
core_pubmed_pmc
Minocycline Susceptibility and tetB Gene in Carbapenem-Resistant Acinetobacter baumannii in Taiwan
Minocycline Susceptibility and tetB Gene in Carbapenem-Resistant Acinetobacter baumannii in Taiwan Abstract Abstract Purpose In this study, we evaluated the minocycline susceptibility rate in carbapenem-resistant Acinetobacter baumannii (CRAB) clinical strains, and the association between tetB carriage and minocycline ...
PMC10203776
core_pubmed_pmc
The antidiabetic effect of methanolic extract of Holarrhena pubescens seeds is mediated through multiple mechanisms of action
The antidiabetic effect of methanolic extract of Holarrhena pubescens seeds is mediated through multiple mechanisms of action Abstract Abstract Holarrhena pubescens is widely used in Indian and Chinese medicine in the treatment of diabetes. The current work determined the oral hypoglycemic and antidiabetic effects of s...
PMC7984432
core_pubmed_pmc
Proteomics‐Informed Prediction of Rosuvastatin Plasma Profiles in Patients With a Wide Range of Body Weight
Proteomics‐Informed Prediction of Rosuvastatin Plasma Profiles in Patients With a Wide Range of Body Weight Abstract Rosuvastatin is a frequently used probe to study transporter‐mediated hepatic uptake. Pharmacokinetic models have therefore been developed to predict transporter impact on rosuvastatin disposition in viv...
PMC6688513
core_pubmed_pmc
Polysaccharide Chain Length of Lipopolysaccharides From Salmonella Minnesota Is a Determinant of Aggregate Stability, Plasma Residence Time and Proinflammatory Propensity in vivo
Polysaccharide Chain Length of Lipopolysaccharides From Salmonella Minnesota Is a Determinant of Aggregate Stability, Plasma Residence Time and Proinflammatory Propensity in vivo Abstract Abstract Lipopolysaccharides (LPS) originate from the outer membrane of Gram-negative bacteria and trigger an inflammatory response ...
PMC9253459
core_pubmed_pmc
Effects of Huangqi Liuyi Decoction in the Treatment of Diabetic Nephropathy and Tissue Distribution Difference of its Six Active Constituents Between Normal and Diabetic Nephropathy Mouse Models
Effects of Huangqi Liuyi Decoction in the Treatment of Diabetic Nephropathy and Tissue Distribution Difference of its Six Active Constituents Between Normal and Diabetic Nephropathy Mouse Models Abstract The purpose of this study was to investigate the effects of Huangqi Liuyi decoction extract (HQD) on diabetic nephro...
PMC4186441
core_pubmed_pmc
Gene expression analysis of membrane transporters and drug-metabolizing enzymes in the lung of healthy and COPD subjects
Gene expression analysis of membrane transporters and drug-metabolizing enzymes in the lung of healthy and COPD subjects Abstract This study describes for the first time the expression levels of genes encoding membrane transporters and drug-metabolizing enzymes in the lungs of ex-smoking patients with chronic obstructi...
PMC6182462
core_pubmed_pmc
Pharmacokinetics, Pharmacodynamics, and Safety of the Novel Calcimimetic Agent Evocalcet in Healthy Japanese Subjects: First-in-Human Phase I Study
Pharmacokinetics, Pharmacodynamics, and Safety of the Novel Calcimimetic Agent Evocalcet in Healthy Japanese Subjects: First-in-Human Phase I Study Abstract Background and Objectives Evocalcet is a novel calcimimetic agent with potential to improve the treatment of secondary hyperparathyroidism in patients with chronic...
PMC12918599
core_pubmed_pmc
OCTN2-targeted and ROS-responsive hybrid polymeric micelles for oral delivery of docetaxel
OCTN2-targeted and ROS-responsive hybrid polymeric micelles for oral delivery of docetaxel Abstract Our previous research identified that an oral mPEG- b -PCL polymeric micelle (PM) maintained satisfactory integrity but exhibited limited transcytosis efficiency. To enhance transcytosis and enable ROS-responsive release...
PMC5652462
core_pubmed_pmc
Drugs and life-threatening ventricular arrhythmia risk: results from the DARE study cohort
Drugs and life-threatening ventricular arrhythmia risk: results from the DARE study cohort Abstract Objectives To establish a unique sample of proarrhythmia cases, determine the characteristics of cases and estimate the contribution of individual drugs to the incidence of proarrhythmia within these cases. Setting Suspe...
PMC6323151
core_pubmed_pmc
In vitro dissolution and bioavailability study of furosemide nanosuspension prepared using design of experiment (DoE)
In vitro dissolution and bioavailability study of furosemide nanosuspension prepared using design of experiment (DoE) Abstract Abstract Background Nanotechnology can offer the advantages of increasing solubility and bioavailability of delivering drugs like Furosemide. The aim of the current study is to investigate the ...
PMC11806196
core_pubmed_pmc
Inhibition of Tacrolimus Metabolism by Cannabidiol and Its Metabolites In Vitro
Inhibition of Tacrolimus Metabolism by Cannabidiol and Its Metabolites In Vitro Abstract ABSTRACT Drug interactions are major causes of interindividual variability in tacrolimus exposure and effect. Tacrolimus, a widely used drug in transplant patients, is metabolized by CYP3A4 and CYP3A5. Cannabidiol (CBD) use after t...
PMC8604241
core_pubmed_pmc
Applying an equity lens to pharmacogenetic research and translation to under‐represented populations
Applying an equity lens to pharmacogenetic research and translation to under‐represented populations Abstract Abstract Since the publication of the Human Genome Project, genetic information has been used as an accepted, evidence‐based biomarker to optimize patient care through the delivery of precision health. Pharmaco...
PMC6996317
core_pubmed_pmc
The challenge of HIV treatment in an era of polypharmacy
The challenge of HIV treatment in an era of polypharmacy Abstract Abstract Introduction The availability of potent antiretroviral therapy has transformed HIV infection into a chronic disease such that people living with HIV (PLWH) have a near normal life expectancy. However, there are continuing challenges in managing ...
PMC4501059
core_pubmed_pmc
Responding to the challenge of untreatable gonorrhea: ETX0914, a first-in-class agent with a distinct mechanism-of-action against bacterial Type II topoisomerases
Responding to the challenge of untreatable gonorrhea: ETX0914, a first-in-class agent with a distinct mechanism-of-action against bacterial Type II topoisomerases Abstract Abstract With the diminishing effectiveness of current antibacterial therapies, it is critically important to discover agents that operate by a mech...
PMC2805874
core_pubmed_pmc
The effects of sitaxentan on sildenafil pharmacokinetics and pharmacodynamics in healthy subjects
The effects of sitaxentan on sildenafil pharmacokinetics and pharmacodynamics in healthy subjects Abstract Abstract AIMS This study evaluated the effects of sitaxentan on the pharmacodynamic [systemic blood pressure (BP)] and pharmacokinetic (PK) parameters of sildenafil in healthy volunteers. METHODS Healthy subjects ...
PMC5731976
core_pubmed_pmc
Magnetic resonance imaging of RRx-001 pharmacodynamics in preclinical tumors
Magnetic resonance imaging of RRx-001 pharmacodynamics in preclinical tumors Abstract RRx-001 is an anticancer agent that subjects cancer cells to reactive oxygen/nitrogen species (ROS/RNS) and acts as an epigenetic modifier. We have used a thiol-bearing MRI contrast agent, Gd-LC7-SH, to investigate the pharmacodynamic...
PMC6015619
core_pubmed_pmc
Assessment of the abuse liability of three menthol Vuse Solo electronic cigarettes relative to combustible cigarettes and nicotine gum
Assessment of the abuse liability of three menthol Vuse Solo electronic cigarettes relative to combustible cigarettes and nicotine gum Abstract Abstract Rationale We previously reported that following a short-term product use period, use of non-menthol Vuse Solo electronic cigarettes (ECs) resulted in product effect-re...
PMC10681497
core_pubmed_pmc
Population pharmacokinetic and exposure‐response analyses of pemigatinib in patients with advanced solid tumors including cholangiocarcinoma
Population pharmacokinetic and exposure‐response analyses of pemigatinib in patients with advanced solid tumors including cholangiocarcinoma Abstract Abstract Pemigatinib is a selective, potent, oral inhibitor of fibroblast growth factor receptor (FGFR)1–3 with efficacy in patients with previously treated, advanced/met...
PMC10517026
core_pubmed_pmc
Model-based optimization of controlled release formulation of levodopa for Parkinson’s disease
Model-based optimization of controlled release formulation of levodopa for Parkinson’s disease Abstract Abstract Levodopa is currently the standard of care treatment for Parkinson’s disease, but chronic therapy has been linked to motor complications. Designing a controlled release formulation (CRF) that maintains susta...
PMC6209214
core_pubmed_pmc
Variability in pharmacologically-induced coma for treatment of refractory status epilepticus
Variability in pharmacologically-induced coma for treatment of refractory status epilepticus Abstract Objective To characterize the amount of EEG suppression achieved in refractory status epilepticus (RSE) patients treated with pharmacologically-induced coma (PIC). Methods We analyzed EEG recordings from 35 RSE patient...
PMC5400404
core_pubmed_pmc
Aripiprazole Lauroxil
Aripiprazole Lauroxil Abstract Abstract Background Aripiprazole lauroxil is an extended-release prodrug of aripiprazole for intramuscular injection, approved for schizophrenia treatment. We developed a population pharmacokinetic (PopPK) model to characterize aripiprazole lauroxil PK and evaluate dosing scenarios likely...
PMC6786704
core_pubmed_pmc
Status Epilepticus and Beyond: A Clinical Review of Status Epilepticus and an Update on Current Management Strategies in Super-refractory Status Epilepticus
Status Epilepticus and Beyond: A Clinical Review of Status Epilepticus and an Update on Current Management Strategies in Super-refractory Status Epilepticus Abstract Abstract Status epilepticus and refractory status epilepticus represent some of the most complex conditions encountered in the neurological intensive care...
PMC11337541
core_pubmed_pmc
Extracellular vesicles as the next‐generation modulators of pharmacokinetics and pharmacodynamics of medications and their potential as adjuvant therapeutics
Extracellular vesicles as the next‐generation modulators of pharmacokinetics and pharmacodynamics of medications and their potential as adjuvant therapeutics Abstract Abstract Background and main body Pharmacokinetics (PK) and pharmacodynamics (PD) are central concepts to guide the dosage and administration of drug the...
PMC7728665
core_pubmed_pmc
Tissue Residues and Pharmacokinetic/Pharmacodynamic Modeling of Tiamulin Against Mycoplasma anatis in Ducks
Tissue Residues and Pharmacokinetic/Pharmacodynamic Modeling of Tiamulin Against Mycoplasma anatis in Ducks Abstract Abstract The pharmacokinetics of tiamulin were studied in 2 groups of ducks ( n = 6) after its oral administration at 2 different doses (30 and 60 mg/kg, respectively). Plasma concentrations of tiamulin ...
PMC6662325
core_pubmed_pmc
Current Scientific Considerations to Verify Physiologically‐Based Pharmacokinetic Models and Their Implications for Locally Acting Products
Current Scientific Considerations to Verify Physiologically‐Based Pharmacokinetic Models and Their Implications for Locally Acting Products Modeling Current Considerations to Verify PBPK Models In both drug development and regulatory settings, PBPK modeling has become a key methodology that integrates up‐to‐date knowle...
PMC9787161
core_pubmed_pmc
Current knowledge, challenges and innovations in developmental pharmacology: A combined conect4children Expert Group and European Society for Developmental, Perinatal and Paediatric Pharmacology White Paper
Current knowledge, challenges and innovations in developmental pharmacology: A combined conect4children Expert Group and European Society for Developmental, Perinatal and Paediatric Pharmacology White Paper Abstract Developmental pharmacology describes the impact of maturation on drug disposition (pharmacokinetics, PK)...
PMC10182956
core_pubmed_pmc
In vitro to in vivo extrapolation and high-content imaging for simultaneous characterization of chemically induced liver steatosis and markers of hepatotoxicity
In vitro to in vivo extrapolation and high-content imaging for simultaneous characterization of chemically induced liver steatosis and markers of hepatotoxicity Abstract Chemically induced steatosis is characterized by lipid accumulation associated with mitochondrial dysfunction, oxidative stress and nucleus distortion...
PMC9311793
core_pubmed_pmc
Pharmacokinetics of orally administered single‐dose ponazuril in cats
Pharmacokinetics of orally administered single‐dose ponazuril in cats Abstract Abstract Cats and kittens in animal shelters and catteries regularly suffer from severe gastrointestinal coccidiosis, which can be fatal, and there are no drugs labeled for feline coccidiosis in the United States. Ponazuril, a triazine‐class...
PMC7814034
core_pubmed_pmc
Analysis of insulin glulisine at the molecular level by X-ray crystallography and biophysical techniques
Analysis of insulin glulisine at the molecular level by X-ray crystallography and biophysical techniques Abstract Abstract This study concerns glulisine, a rapid-acting insulin analogue that plays a fundamental role in diabetes management. We have applied a combination of methods namely X-ray crystallography, and bioph...
PMC4166769
core_pubmed_pmc
Virtual screening of phytochemicals to novel targets in Haemophilus ducreyi towards the treatment of Chancroid
Virtual screening of phytochemicals to novel targets in Haemophilus ducreyi towards the treatment of Chancroid Abstract Abstract Conventionally, drugs are discovered by testing chemically synthesized compounds against a battery of in vivo biological screens. Information technology and Omic science enabled us for high t...
PMC12838218
core_pubmed_pmc
Analysis of Pharmacokinetic and Pharmacodynamic Interactions Between Chlorpromazine and Risperidone via Simultaneous Measurement of Multiple Receptor Occupancy in the Rat Brain
Analysis of Pharmacokinetic and Pharmacodynamic Interactions Between Chlorpromazine and Risperidone via Simultaneous Measurement of Multiple Receptor Occupancy in the Rat Brain Abstract Background/Objectives: Combination therapy for schizophrenia may exacerbate side effects mediated by multiple brain receptors. This st...
PMC4659844
core_pubmed_pmc
Pharmacokinetics, Safety, and Tolerability of a Single 500-mg or 1000-mg Intravenous Dose of Dalbavancin in Healthy Japanese Subjects
Pharmacokinetics, Safety, and Tolerability of a Single 500-mg or 1000-mg Intravenous Dose of Dalbavancin in Healthy Japanese Subjects Abstract Abstract Background and Objectives Dalbavancin is a novel, once-weekly glycopeptide antibiotic approved for treatment of acute bacterial skin infections. Given the importance of...
PMC9026613
core_pubmed_pmc
Dasiglucagon Effects on QTc in Healthy Volunteers: A Randomized, Placebo-Controlled, Dose-Escalation, Double-Blind Study
Dasiglucagon Effects on QTc in Healthy Volunteers: A Randomized, Placebo-Controlled, Dose-Escalation, Double-Blind Study Abstract Abstract Background Dasiglucagon is a novel glucagon analog that is stable in aqueous formulation and approved for use in severe hypoglycemia. Concentration QTc analyses are critical for ass...
PMC7335747
core_pubmed_pmc
A New Pharmacokinetic Model Describing the Biodistribution of Intravenously and Intratumorally Administered Superparamagnetic Iron Oxide Nanoparticles (SPIONs) in a GL261 Xenograft Glioblastoma Model
A New Pharmacokinetic Model Describing the Biodistribution of Intravenously and Intratumorally Administered Superparamagnetic Iron Oxide Nanoparticles (SPIONs) in a GL261 Xenograft Glioblastoma Model Abstract Abstract Background Superparamagnetic iron oxide nanoparticles (SPIONs) have displayed multifunctional applicat...
PMC11705865
core_pubmed_pmc
Nutrient conditions affect antimicrobial pharmacodynamics in Pseudomonas aeruginosa
Nutrient conditions affect antimicrobial pharmacodynamics in Pseudomonas aeruginosa Abstract ABSTRACT The infectious microenvironment in chronic respiratory tract infections is characterized by substantial variability in nutrient conditions, which may impact colonization and treatment response of pathogens. Metabolic a...
PMC12257257
core_pubmed_pmc
Single‐Dose, Intravenous, and Oral Pharmacokinetics of Isavuconazole in Dogs
Single‐Dose, Intravenous, and Oral Pharmacokinetics of Isavuconazole in Dogs Abstract ABSTRACT Isavuconazole, a triazole antifungal used in humans for invasive fungal infections, may be effective for treating canine fungal infections, although data on its use in dogs is limited. This study aimed to determine the pharma...
PMC10086964
core_pubmed_pmc
Evaluation of Deutetrabenazine's Potential to Delay Cardiac Repolarization Using Concentration‐QTc Analysis
Evaluation of Deutetrabenazine's Potential to Delay Cardiac Repolarization Using Concentration‐QTc Analysis Abstract Abstract Deutetrabenazine (Austedo) is indicated in adults for chorea associated with Huntington disease and tardive dyskinesia. Escalating deutetrabenazine doses were administered to healthy volunteers ...
PMC12128054
core_pubmed_pmc
Pharmacokinetics and Safety of Clofazimine in Children With Rifampicin-Resistant Tuberculosis
Pharmacokinetics and Safety of Clofazimine in Children With Rifampicin-Resistant Tuberculosis Abstract Abstract Background We described the pharmacokinetics and safety of clofazimine in children treated for multidrug/rifampicin-resistant tuberculosis (MDR/RR-TB). Methods Children aged <18 years were eligible. Clofazimi...
PMC8762261
core_pubmed_pmc
Clinical and Immunological Factors Associated with Recommended Trough Levels of Adalimumab and Infliximab in Patients with Crohn’s Disease
Clinical and Immunological Factors Associated with Recommended Trough Levels of Adalimumab and Infliximab in Patients with Crohn’s Disease Abstract Abstract Introduction: Up to 40% of patients with Crohn’s disease do not respond to treatment with anti-TNF or lose response after the initial benefit. Low drug concentrati...
PMC11564001
core_pubmed_pmc
NaCTR: Natural product-derived compound-based drug discovery pipeline from traditional oriental medicine by search space reduction
NaCTR: Natural product-derived compound-based drug discovery pipeline from traditional oriental medicine by search space reduction Abstract The drug discovery pipelines require enormous time and cost, albeit their infamously high risk of failures. Reducing such risk has therefore been the utmost goal in the process. Re...
PMC10967030
core_pubmed_pmc
Non-invasive single cell aptasensing in live cells and animals †
Non-invasive single cell aptasensing in live cells and animals † Abstract Abstract We report a genetically encoded aptamer biosensor platform for non-invasive measurement of drug distribution in cells and animals. We combined the high specificity of aptamer molecular recognition with the easy-to-detect properties of fl...
PMC6033295
core_pubmed_pmc
The Effects of the Honey-Roasting Process on the Pharmacokinetics of the Six Active Compounds of Licorice
The Effects of the Honey-Roasting Process on the Pharmacokinetics of the Six Active Compounds of Licorice Abstract A convenient UPLC-MS/MS method was established to determine the contents of six bioactive compounds, namely, liquiritin apioside, liquiritin, isoliquiritin, liquiritigenin, isoliquiritigenin, and glycyrrhe...
PMC7391357
core_pubmed_pmc
Mathematical model of blood glucose dynamics by emulating the pathophysiology of glucose metabolism in type 2 diabetes mellitus
Mathematical model of blood glucose dynamics by emulating the pathophysiology of glucose metabolism in type 2 diabetes mellitus Abstract Abstract Mathematical modelling has established itself as a theoretical tool to understand fundamental aspects of a variety of medical-biological phenomena. The predictive power of ma...
PMC10108264
core_pubmed_pmc
Single‐dose Pharmacokinetics of Eluxadoline in Healthy Participants With Normal Renal Function and Participants With Renal Impairment
Single‐dose Pharmacokinetics of Eluxadoline in Healthy Participants With Normal Renal Function and Participants With Renal Impairment Abstract Abstract Eluxadoline is approved for the treatment of diarrhea‐predominant irritable bowel syndrome in the United States. The impact of renal impairment on the pharmacokinetic (...
PMC9835129
core_pubmed_pmc
Population pharmacokinetic modeling of daridorexant, a novel dual orexin receptor antagonist
Population pharmacokinetic modeling of daridorexant, a novel dual orexin receptor antagonist Abstract Abstract The analysis aimed at identifying subject‐specific characteristics (covariates) influencing exposure to daridorexant and quantification of covariate effects to determine clinical relevance. Data from 13 phase ...
PMC7329758
core_pubmed_pmc
Population Pharmacokinetics of Imipenem in Critically Ill Patients: A Parametric and Nonparametric Model Converge on CKD-EPI Estimated Glomerular Filtration Rate as an Impactful Covariate
Population Pharmacokinetics of Imipenem in Critically Ill Patients: A Parametric and Nonparametric Model Converge on CKD-EPI Estimated Glomerular Filtration Rate as an Impactful Covariate Abstract Abstract Background Population pharmacokinetic (popPK) models for antibiotics are used to improve dosing strategies and ind...
PMC7032234
core_pubmed_pmc
Succinylated whey protein isolate as a sustained-release excipient of puerarin derivative oral tablets: Preparation, optimization and pharmacokinetics
Succinylated whey protein isolate as a sustained-release excipient of puerarin derivative oral tablets: Preparation, optimization and pharmacokinetics Abstract Abstract This work was done to investigate succinylated commercial whey protein isolate (S-WPI) as an oral sustained-release delivery carrier for puerarin 5 (PR...
PMC4203513
core_pubmed_pmc
A phase I/II trial of hydroxychloroquine in conjunction with radiation therapy and concurrent and adjuvant temozolomide in patients with newly diagnosed glioblastoma multiforme
A phase I/II trial of hydroxychloroquine in conjunction with radiation therapy and concurrent and adjuvant temozolomide in patients with newly diagnosed glioblastoma multiforme Abstract Abstract Preclinical studies indicate autophagy inhibition with hydroxychloroquine (HCQ) can augment the efficacy of DNA-damaging ther...
PMC8464329
core_pubmed_pmc
Farnesylthiosalicylic Acid-Loaded Albumin Nanoparticle Alleviates Renal Fibrosis by Inhibiting Ras/Raf1/p38 Signaling Pathway
Farnesylthiosalicylic Acid-Loaded Albumin Nanoparticle Alleviates Renal Fibrosis by Inhibiting Ras/Raf1/p38 Signaling Pathway Abstract Background Renal fibrosis is the common pathway in chronic kidney diseases progression to end-stage renal disease, but to date, no clinical drug for its treatment is approved. It has be...
PMC11922982
core_pubmed_pmc
Clinical pharmacology—how it shapes the drug development journey
Clinical pharmacology—how it shapes the drug development journey Abstract Abstract Every drug development is a complex and long journey. Clinical pharmacology is an essential discipline in modern drug development. With its applications, computational modelling, and simulation techniques, it can significantly contribute...
PMC3531954
core_pubmed_pmc
Pharmacokinetic/Pharmacodynamic Analysis of a Hemodialyzed Patient Treated with 25 mg of Sunitinib
Pharmacokinetic/Pharmacodynamic Analysis of a Hemodialyzed Patient Treated with 25 mg of Sunitinib Abstract Sunitinib has been approved for the treatment of advanced and/or metastatic renal cell carcinoma (RCC). Information on the dosage adjustment of sunitinib for patients undergoing hemodialysis is limited. Especiall...
PMC12846905
core_pubmed_pmc
Identifying and Resolving Drug-Related Problems in Geriatric Patients
Identifying and Resolving Drug-Related Problems in Geriatric Patients Abstract As individuals age, age-related biologic and physiologic changes, alterations to pharmacokinetic and pharmacodynamic variables, and multimorbidity place geriatric patients at high risk for drug-related problems. Drug therapy problems in thes...
PMC9497180
core_pubmed_pmc
Association between ABCB1 rs2235048 Polymorphism and THC Pharmacokinetics and Subjective Effects following Smoked Cannabis in Young Adults
Association between ABCB1 rs2235048 Polymorphism and THC Pharmacokinetics and Subjective Effects following Smoked Cannabis in Young Adults Abstract Genetic influences on acute responses to psychoactive drugs may contribute to individual variability in addiction risk. ABCB1 is a human gene that encodes P-glycoprotein, a...
PMC6321172
core_pubmed_pmc
Analysis of Vipadenant and Its In Vitro and In Vivo Metabolites via Liquid Chromatography-Quadrupole-Time-of-Flight Mass Spectrometry
Analysis of Vipadenant and Its In Vitro and In Vivo Metabolites via Liquid Chromatography-Quadrupole-Time-of-Flight Mass Spectrometry Abstract A simple and sensitive liquid chromatography–quadrupole-time-of-flight–mass spectrometric (LC-QTOF-MS) assay has been developed for the evaluation of drug metabolism and pharmac...
PMC9305443
core_pubmed_pmc
Effect of Phosphate Binders and a Dietary Iron Supplement on the Pharmacokinetics of a Single Dose of Vadadustat in Healthy Adults
Effect of Phosphate Binders and a Dietary Iron Supplement on the Pharmacokinetics of a Single Dose of Vadadustat in Healthy Adults Abstract Abstract Vadadustat is a hypoxia‐inducible factor prolyl‐hydroxylase inhibitor being developed for the treatment of anemia in patients with chronic kidney disease. Sequelae of chro...
PMC9964161
core_pubmed_pmc
Complex Mixtures: Array PBPK Modeling of Jet Fuel Components
Complex Mixtures: Array PBPK Modeling of Jet Fuel Components Abstract Abstract An array physiologically-based pharmacokinetic (PBPK) model represents a streamlined method to simultaneously quantify dosimetry of multiple compounds. To predict internal dosimetry of jet fuel components simultaneously, an array PBPK model ...
PMC10666248
core_pubmed_pmc
Nanoliposomes for Controlled Release of Cannabinodiol at Relevant Gastrointestinal Conditions
Nanoliposomes for Controlled Release of Cannabinodiol at Relevant Gastrointestinal Conditions Abstract Cannabidiol (CBD) has significant therapeutic potential; nevertheless, its advance as an effective drug by the pharmaceutical business is hindered by its inherent characteristics, such as low bioavailability, low wate...
PMC6964958
core_pubmed_pmc
Impact of High Body Weight on Mortality in Critically Ill Patients Receiving Meropenem for Pneumonia
Impact of High Body Weight on Mortality in Critically Ill Patients Receiving Meropenem for Pneumonia Abstract Introduction: Body size has a significant impact on pharmacokinetics of antibiotics, and leaving body size out of consideration may increase the probability of therapeutic failure. The objective of this study i...
PMC11505481
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Deciphering the Intricate Interplay in the Framework of Antibiotic-Drug Interactions: A Narrative Review
Deciphering the Intricate Interplay in the Framework of Antibiotic-Drug Interactions: A Narrative Review Abstract Abstract Drug interactions are a significant and integral part of the concept of medication-related adverse events, whether referring to potential interactions or those currently observed in real-world cond...
PMC4621059
core_pubmed_pmc
Pharmacokinetics of Isoniazid, Pyrazinamide, and Ethambutol in Newly Diagnosed Pulmonary TB Patients in Tanzania
Pharmacokinetics of Isoniazid, Pyrazinamide, and Ethambutol in Newly Diagnosed Pulmonary TB Patients in Tanzania Abstract Abstract Exposure to lower-than-therapeutic levels of anti-tuberculosis drugs is likely to cause selection of resistant strains of Mycobacterium tuberculosis and treatment failure. The first-line an...
PMC10245392
core_pubmed_pmc
Fed- and Fasted-State Performance of Pretomanid Amorphous Solid Dispersions Formulated with an Enteric Polymer
Fed- and Fasted-State Performance of Pretomanid Amorphous Solid Dispersions Formulated with an Enteric Polymer Abstract Abstract Weakly acid polymers with pH-responsive solubility are being used with increasing frequency in amorphous solid dispersion (ASD) formulations of drugs with low aqueous solubility. However, dru...
PMC6125471
core_pubmed_pmc
Pharmacodynamic analysis of eribulin safety in breast cancer patients using real‐world postmarketing surveillance data
Pharmacodynamic analysis of eribulin safety in breast cancer patients using real‐world postmarketing surveillance data Abstract Postmarketing surveillance is useful to collect safety data in real‐world clinical settings. In this study, we applied postmarketing real‐world data on a mechanistic model analysis for neutrop...
PMC9545691
core_pubmed_pmc
Relationship Between Anifrolumab Pharmacokinetics, Pharmacodynamics, and Efficacy in Patients With Moderate to Severe Systemic Lupus Erythematosus
Relationship Between Anifrolumab Pharmacokinetics, Pharmacodynamics, and Efficacy in Patients With Moderate to Severe Systemic Lupus Erythematosus Abstract Abstract This study aimed to elucidate the pharmacokinetic/pharmacodynamic and pharmacodynamic/efficacy relationships of anifrolumab, a type I interferon receptor a...
PMC3927056
core_pubmed_pmc
Towards Quantitation of the Effects of Renal Impairment and Probenecid Inhibition on Kidney Uptake and Efflux Transporters, Using Physiologically Based Pharmacokinetic Modelling and Simulations
Towards Quantitation of the Effects of Renal Impairment and Probenecid Inhibition on Kidney Uptake and Efflux Transporters, Using Physiologically Based Pharmacokinetic Modelling and Simulations Abstract Background and Objectives The kidney is a major drug-eliminating organ. Renal impairment or concomitant use of transp...
PMC12907769
core_pubmed_pmc
Evaluation of Ginsenosides and Their Derivatives From Panax ginseng as Aromatase Inhibitors for Breast Cancer Treatment—An in silico study
Evaluation of Ginsenosides and Their Derivatives From Panax ginseng as Aromatase Inhibitors for Breast Cancer Treatment—An in silico study Abstract Abstract Breast cancer, particularly estrogen receptor‐positive subtypes, is a leading cause of cancer‐related mortality worldwide. Aromatase inhibitors, which target estro...
PMC4746878
core_pubmed_pmc
A pharmacogenetic pilot study reveals MTHFR , DRD3 , and MDR1 polymorphisms as biomarker candidates for slow atorvastatin metabolizers
A pharmacogenetic pilot study reveals MTHFR , DRD3 , and MDR1 polymorphisms as biomarker candidates for slow atorvastatin metabolizers Abstract Background The genetic variation underlying atorvastatin (ATV) pharmacokinetics was evaluated in a Mexican population. Aims of this study were: 1) to reveal the frequency of 87...
PMC11067710
core_pubmed_pmc
Acute pharmacodynamic responses to sitagliptin: Drug‐induced increase in early insulin secretion in oral glucose tolerance test
Acute pharmacodynamic responses to sitagliptin: Drug‐induced increase in early insulin secretion in oral glucose tolerance test Abstract Abstract DPP4 inhibitors are widely prescribed as treatments for type 2 diabetes. Because drug responses vary among individuals, we initiated investigations to identify genetic varian...
PMC8482224
core_pubmed_pmc
Silica Xerogel Doped with Iron(III) as Sensor Material for Salicylhydroxamic Acid Determination in Urine
Silica Xerogel Doped with Iron(III) as Sensor Material for Salicylhydroxamic Acid Determination in Urine Abstract Abstract Salicylhydroxamic acid (SHA) is used as antimicrobic medicine and its concentration has to be monitored in urine. For the first time, silica xerogels doped with iron(III) have been proposed as sens...
PMC12819659
core_pubmed_pmc
Refined target-mediated drug disposition modeling of the anti-tissue factor pathway inhibitor antibody MG1113 in cynomolgus monkeys and rabbits
Refined target-mediated drug disposition modeling of the anti-tissue factor pathway inhibitor antibody MG1113 in cynomolgus monkeys and rabbits Abstract Introduction MG1113 is a humanized immunoglobulin G4 antibody targeting the Kunitz-type protease inhibitor 2 domain of tissue factor pathway inhibitor (TFPI) and is un...
PMC5615911
core_pubmed_pmc
Toxicological evaluation of a novel umami flavour compound: 2-(((3-(2,3-Dimethoxyphenyl)-1 H -1,2,4-triazol-5-yl)thio)methyl)pyridine
Toxicological evaluation of a novel umami flavour compound: 2-(((3-(2,3-Dimethoxyphenyl)-1 H -1,2,4-triazol-5-yl)thio)methyl)pyridine Abstract Abstract A toxicological evaluation of a umami flavour compound, 2-(((3-(2,3-dimethoxyphenyl)-1 H -1,2,4-triazol-5-yl)thio)methyl)pyridine (S3643; CAS 902136-79-2), was complete...
PMC11767451
core_pubmed_pmc
Novel Approaches to Monitor Pharmacokinetics and Metabolism of Gemcitabine-Ibandronate Conjugate in Mice and Dogs
Novel Approaches to Monitor Pharmacokinetics and Metabolism of Gemcitabine-Ibandronate Conjugate in Mice and Dogs Abstract Abstract Background. The use of the bone-seeking properties of bisphosphonates (BPs) to target the delivery of therapeutic drugs is a promising approach for the treatment of bone metastases. Curren...
PMC9026172
core_pubmed_pmc
Pharmacodynamics, Network Pharmacology, and Pharmacokinetics of Chinese Medicine Formula 9002A in the Treatment of Alzheimer’s Disease
Pharmacodynamics, Network Pharmacology, and Pharmacokinetics of Chinese Medicine Formula 9002A in the Treatment of Alzheimer’s Disease Abstract Alzheimer’s disease (AD) is a common and serious neurodegenerative disease in the elderly; however, the treatment of AD is still lacking of rational drugs. In this paper, the a...
PMC6882435
core_pubmed_pmc
Preparation and study of two kinds of ophthalmic nano-preparations of everolimus
Preparation and study of two kinds of ophthalmic nano-preparations of everolimus Abstract Abstract Objective: To prepare everolimus nanoformulations and increase their solubility to suit their application in the eye. Methods: The everolimus micelles was prepared by thin film dispersion method using Tween-80 (P80) and p...
PMC10433679
core_pubmed_pmc
Core protocol development for phase 2/3 clinical trials in the leukodystrophy vanishing white matter: a consensus statement by the VWM consortium and patient advocates
Core protocol development for phase 2/3 clinical trials in the leukodystrophy vanishing white matter: a consensus statement by the VWM consortium and patient advocates Abstract Abstract Background The leukodystrophy “Vanishing White Matter” (VWM) is an orphan disease with neurological decline and high mortality. Curren...
PMC5830590
core_pubmed_pmc
Phase I dose-escalation study of copanlisib in combination with gemcitabine or cisplatin plus gemcitabine in patients with advanced cancer
Phase I dose-escalation study of copanlisib in combination with gemcitabine or cisplatin plus gemcitabine in patients with advanced cancer Abstract Background: Copanlisib is a pan-class I phosphatidylinositol 3-kinase (PI3K) inhibitor with predominant PI3K- α / δ activity that has demonstrated clinical activity and man...
PMC11993144
core_pubmed_pmc
Review of acamprosate pharmacokinetics and dosing strategies
Review of acamprosate pharmacokinetics and dosing strategies Abstract Abstract Introduction Alcohol use disorder (AUD) is associated with significant morbidity and mortality, contributing to 5% of annual deaths. Although some literature suggests that acamprosate is an effective treatment for AUD, its traditional dosing...
PMC12594887
core_pubmed_pmc
Epimedii Folium flavonoids: A double-edged sword effect on the liver, a dual exploration of efficacy and toxicity
Epimedii Folium flavonoids: A double-edged sword effect on the liver, a dual exploration of efficacy and toxicity Abstract Flavonoids, the key active compounds in Epimedii Folium , have both protective and toxic effects on the liver. Their hepatoprotective effects are associated with reducing lipid accumulation and oxi...
PMC12159028
core_pubmed_pmc
Case Report: Adverse reaction to butorphanol in a Collie homozygous for the ABCB1-1∆ ( MDR1 ) mutation
Case Report: Adverse reaction to butorphanol in a Collie homozygous for the ABCB1-1∆ ( MDR1 ) mutation Abstract Abstract Certain dog breeds, particularly herding breeds like Collies, are predisposed to drug sensitivity due to the ABCB1-1∆ (previously known as MDR1 ) mutation, which disrupts P-glycoprotein (P-gp) functi...
PMC6231011
core_pubmed_pmc
Clinical pharmacology of alemtuzumab, an anti‐CD52 immunomodulator, in multiple sclerosis
Clinical pharmacology of alemtuzumab, an anti‐CD52 immunomodulator, in multiple sclerosis Abstract Summary Alemtuzumab, a humanized anti‐CD52 monoclonal antibody, is approved for treatment of relapsing multiple sclerosis (MS). In the Phase II/III trials, patients received 12 or 24 mg/day of alemtuzumab in two treatment...
PMC10610465
core_pubmed_pmc
An Examination of the Complex Pharmacological Properties of the Non-Selective Opioid Modulator Buprenorphine
An Examination of the Complex Pharmacological Properties of the Non-Selective Opioid Modulator Buprenorphine Abstract The goal of this review is to provide a recent examination of the pharmacodynamics as well as pharmacokinetics, misuse potential, toxicology, and prenatal consequences of buprenorphine. Buprenorphine is...
PMC7879788
core_pubmed_pmc
Pharmacokinetics of piperine after oral administration of Sahastara remedy capsules in healthy volunteers
Pharmacokinetics of piperine after oral administration of Sahastara remedy capsules in healthy volunteers Abstract Abstract Background and purpose: To investigate the pharmacokinetics of piperine after single oral doses of capsules containing Sahastara (SHT) remedy dried ethanolic extracts in healthy Thai volunteers. E...
PMC7689791
core_pubmed_pmc
Population Pharmacokinetics and Exposure‐Response Analyses for the Most Frequent Adverse Events Following Treatment With Lemborexant, an Orexin Receptor Antagonist, in Subjects With Insomnia Disorder
Population Pharmacokinetics and Exposure‐Response Analyses for the Most Frequent Adverse Events Following Treatment With Lemborexant, an Orexin Receptor Antagonist, in Subjects With Insomnia Disorder Abstract Abstract Lemborexant is a novel orexin receptor antagonist approved in the United States and Japan for the trea...
PMC11758838
core_pubmed_pmc
Elritercept, a modified activin receptor IIA ligand trap, increased erythropoiesis and thrombopoiesis in a phase 1 trial
Elritercept, a modified activin receptor IIA ligand trap, increased erythropoiesis and thrombopoiesis in a phase 1 trial Abstract Key Points • Elritercept was generally well tolerated at all dose levels, with no dose-limiting toxicities observed after single or multiple doses. • Onset and duration of changes in RBC par...
PMC7252427
core_pubmed_pmc
Cohort study to evaluate efficacy, safety and acceptability of a two-rod contraceptive implant during third, fourth and fifth year of product use in China
Cohort study to evaluate efficacy, safety and acceptability of a two-rod contraceptive implant during third, fourth and fifth year of product use in China Abstract Objective Sino-implant (II) is a contraceptive implant approved for 4 years of use in China. We evaluated the contraceptive efficacy during the third, fourt...
PMC4504437
core_pubmed_pmc
An Overview of Current Regulatory Requirements for Approval of Biosimilar Insulins
An Overview of Current Regulatory Requirements for Approval of Biosimilar Insulins Abstract Abstract Insulin analog patent expiry is likely to mean that, increasingly, copies of original biopharmaceutical products will be submitted for authorization. Experience with biosimilars in other therapeutic areas suggests that ...
PMC7689974
core_pubmed_pmc
Antibiotic therapeutic drug monitoring in intensive care patients treated with different modalities of extracorporeal membrane oxygenation (ECMO) and renal replacement therapy: a prospective, observational single-center study
Antibiotic therapeutic drug monitoring in intensive care patients treated with different modalities of extracorporeal membrane oxygenation (ECMO) and renal replacement therapy: a prospective, observational single-center study Abstract Abstract Background Effective antimicrobial treatment is key to reduce mortality asso...
PMC12477600
core_pubmed_pmc
Translational and clinical development of therapeutic siRNA and ASOs: current industry practices, perspectives, and recommendations
Translational and clinical development of therapeutic siRNA and ASOs: current industry practices, perspectives, and recommendations Abstract Abstract RNA-based therapies, particularly small interfering RNA (siRNA) and antisense oligonucleotides (ASOs), represent a promising modality class with the potential to target p...
PMC12272323
core_pubmed_pmc
Model‐Informed Drug Development‐Based Bridging from Subcutaneous to Intravenous Secukinumab Dosing: Approval in Psoriatic Arthritis and Axial Spondyloarthritis
Model‐Informed Drug Development‐Based Bridging from Subcutaneous to Intravenous Secukinumab Dosing: Approval in Psoriatic Arthritis and Axial Spondyloarthritis Abstract Abstract The objective of this modeling and simulation analysis was to determine an intravenous (IV) secukinumab dosing regimen with steady‐state expos...
PMC12862099
core_pubmed_pmc
Estimation of the Orexin Receptor Occupancy From Human Plasma Pharmacokinetics of Vornorexant, a Novel Dual Orexin 1/2 Receptor Antagonist for the Treatment of Insomnia
Estimation of the Orexin Receptor Occupancy From Human Plasma Pharmacokinetics of Vornorexant, a Novel Dual Orexin 1/2 Receptor Antagonist for the Treatment of Insomnia Abstract ABSTRACT Vornorexant is a novel dual orexin receptor antagonist (DORA) for the treatment of insomnia with a short elimination half‐life. Estim...
PMC10635340
core_pubmed_pmc
Effects of Sleeve Gastrectomy and Roux-en-Y Gastric Bypass on Escitalopram Pharmacokinetics: A Cohort Study
Effects of Sleeve Gastrectomy and Roux-en-Y Gastric Bypass on Escitalopram Pharmacokinetics: A Cohort Study Abstract Supplemental Digital Content is Available in the Text. Background: Changes in the gastrointestinal physiology after bariatric surgery may affect the pharmacokinetics of medications. Data on the impact of...
PMC5685716
core_pubmed_pmc
Oral 4-( N )-stearoyl gemcitabine nanoparticles inhibit tumor growth in mouse models
Oral 4-( N )-stearoyl gemcitabine nanoparticles inhibit tumor growth in mouse models Abstract Abstract In spite of recent advances in targeted tumor therapy, systemic chemotherapy with cytotoxic agents remains a vital cancer treatment modality. Gemcitabine is a nucleoside analog commonly used in the treatment of variou...
PMC4800446
core_pubmed_pmc
Minocycline as a re-purposed anti- Wolbachia macrofilaricide: superiority compared with doxycycline regimens in a murine infection model of human lymphatic filariasis
Minocycline as a re-purposed anti- Wolbachia macrofilaricide: superiority compared with doxycycline regimens in a murine infection model of human lymphatic filariasis Abstract Abstract Lymphatic filariasis and onchocerciasis are parasitic helminth diseases, which cause severe morbidities such as elephantiasis, skin dis...
PMC6843717
core_pubmed_pmc
Pharmacokinetics of the Rac/Cdc42 Inhibitor MBQ-167 in Mice by Supercritical Fluid Chromatography–Tandem Mass Spectrometry
Pharmacokinetics of the Rac/Cdc42 Inhibitor MBQ-167 in Mice by Supercritical Fluid Chromatography–Tandem Mass Spectrometry Abstract The Rho GTPases Rac and Cdc42 are potential targets against metastatic diseases. We characterized the small molecule MBQ-167 as an effective dual Rac/Cdc42 inhibitor that reduces HER2-type...
PMC12162372
core_pubmed_pmc
Imaging Cell Surface Plectin in PDAC Patients – A First-In-Human Phase 0 Study Report
Imaging Cell Surface Plectin in PDAC Patients – A First-In-Human Phase 0 Study Report Abstract Purpose Plectin is traditionally an intracellular cytoskeletal protein that maintains cell structure and stability. However, we and others have identified its surface-localized form in cancer (CSP), where it influences cell a...
PMC6904673
core_pubmed_pmc
Customisation and validation of a low-volume plasma renin activity immunoassay: Enabling of regulatory compliant determination in paediatric trials
Customisation and validation of a low-volume plasma renin activity immunoassay: Enabling of regulatory compliant determination in paediatric trials Abstract Abstract Objectives Investigations of plasma renin activity (PRA) in children are urgently required. Small-volume, regulatory guideline compliant, bioanalytical as...
PMC10288581
core_pubmed_pmc
Pharmacokinetic interaction of voriconazole and clarithromycin in Pakistani healthy male volunteers: a single dose, randomized, crossover, open-label study
Pharmacokinetic interaction of voriconazole and clarithromycin in Pakistani healthy male volunteers: a single dose, randomized, crossover, open-label study Abstract Background: Voriconazole an antifungal drug, has a potential for drug-drug interactions (DDIs) with administered drugs. Clarithromycin is a Cytochromes P45...
PMC7438806
core_pubmed_pmc
Mini‐Review: Comprehensive Drug Disposition Knowledge Generated in the Modern Human Radiolabeled ADME Study
Mini‐Review: Comprehensive Drug Disposition Knowledge Generated in the Modern Human Radiolabeled ADME Study Abstract Abstract The human radiolabeled absorption, distribution, metabolism, and excretion (ADME) study offers a quantitative and comprehensive overall picture of the disposition of a drug, including excretion ...