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PMC6934468
core_pubmed_pmc
The effect of ligand amount, affinity and internalization on PSMA-targeted imaging and therapy: A simulation study using a PBPK model
The effect of ligand amount, affinity and internalization on PSMA-targeted imaging and therapy: A simulation study using a PBPK model Abstract The aim of this work was to investigate the effect of ligand amount, affinity and internalization of prostate-specific membrane antigen (PSMA)-specific ligands on the activity c...
PMC12389012
core_pubmed_pmc
Once-Daily Versus Four-Times-Daily Intravenous Busulfan with Therapeutic Drug Monitoring as Conditioning for Hematopoietic Cell Transplantation in Children
Once-Daily Versus Four-Times-Daily Intravenous Busulfan with Therapeutic Drug Monitoring as Conditioning for Hematopoietic Cell Transplantation in Children Abstract Background/Objectives: Busulfan is a key component of myeloablative conditioning regimens in hematopoietic stem cell transplantation (HSCT) for pediatric p...
PMC10203027
core_pubmed_pmc
Bcl-2 pathway inhibition in solid tumors: a review of clinical trials
Bcl-2 pathway inhibition in solid tumors: a review of clinical trials Abstract Abstract Due to their key role in the pathogenesis of cancer through the regulation of apoptosis, the B-cell leukemia/lymphoma-2 (BCL-2) family proteins have been an attractive target for cancer therapy for the past decades. Throughout the y...
PMC4972157
core_pubmed_pmc
Pharmacokinetic/pharmacodynamic modelling of the antimalarial effect of Actelion‐451840 in an induced blood stage malaria study in healthy subjects
Pharmacokinetic/pharmacodynamic modelling of the antimalarial effect of Actelion‐451840 in an induced blood stage malaria study in healthy subjects Abstract Aims The aim of this study was to use data from an experimental induced blood stage malaria clinical trial to characterize the antimalarial activity of the new com...
PMC6523420
core_pubmed_pmc
Role of Intestinal Microbiota in Metabolism of Gastrodin In Vitro and In Vivo
Role of Intestinal Microbiota in Metabolism of Gastrodin In Vitro and In Vivo Abstract Abstract Alteration in the number and composition of intestinal microbiota affects the metabolism of several xenobiotics. Gastrodin, isolated from Gastrodia elata, is prone to be hydrolyzed by intestinal microbiota. In the present st...
PMC11858930
core_pubmed_pmc
Exploring the Therapeutic Potential of Mitragynine and Corynoxeine: Kratom-Derived Indole and Oxindole Alkaloids for Pain Management
Exploring the Therapeutic Potential of Mitragynine and Corynoxeine: Kratom-Derived Indole and Oxindole Alkaloids for Pain Management Abstract The search for effective pain management solutions remains a critical challenge, especially amidst growing concerns over the use of conventional opioids. In the US, opioid-relate...
PMC6255988
core_pubmed_pmc
The impact of CYP2D6 mediated drug–drug interaction: a systematic review on a combination of metoprolol and paroxetine/fluoxetine
The impact of CYP2D6 mediated drug–drug interaction: a systematic review on a combination of metoprolol and paroxetine/fluoxetine Abstract Abstract Aim Metoprolol (a CYP2D6 substrate) is often co‐prescribed with paroxetine/fluoxetine (a CYP2D6 inhibitor) because the clinical relevance of this drug–drug interaction (DDI...
PMC8066277
core_pubmed_pmc
Repurposing Avermectins and Milbemycins against Mycobacteroides abscessus and Other Nontuberculous Mycobacteria
Repurposing Avermectins and Milbemycins against Mycobacteroides abscessus and Other Nontuberculous Mycobacteria Abstract Infections caused by nontuberculous mycobacteria (NTM) are increasing worldwide, resulting in a new global health concern. NTM treatment is complex and requires combinations of several drugs for leng...
PMC4666160
core_pubmed_pmc
In vitro Dynamic Pharmacokinetic/Pharamcodynamic (PK/PD) study and CO PD of Marbofloxacin against Haemophilus parasuis
In vitro Dynamic Pharmacokinetic/Pharamcodynamic (PK/PD) study and CO PD of Marbofloxacin against Haemophilus parasuis Abstract Background Haemophilus parasuis ( H. parasuis ) can invade the body and cause systemic infection under stress conditions. Marbofloxacin has been recommended for the treatment of swine infectio...
PMC12005403
core_pubmed_pmc
Metagenomic source tracking after microbiota transplant therapy
Metagenomic source tracking after microbiota transplant therapy Abstract ABSTRACT Reliable engraftment assessment of donor microbial communities and individual strains is an essential component of characterizing the pharmacokinetics of microbiota transplant therapies (MTTs). Recent methods for measuring donor engraftme...
PMC12326967
core_pubmed_pmc
Externally validated population pharmacokinetics of amikacin and evaluation of dosage regimen based on achieved serum concentrations in neonates
Externally validated population pharmacokinetics of amikacin and evaluation of dosage regimen based on achieved serum concentrations in neonates Abstract ABSTRACT Combination antibiotics consisting of beta-lactam and aminoglycoside are commonly utilized in the treatment of neonatal septicaemia. The aims of this study w...
PMC7203552
core_pubmed_pmc
A Study on Acetylglutamine Pharmacokinetics in Rat Blood and Brain Based on Liquid Chromatography-Tandem Mass Spectrometry and Microdialysis Technique
A Study on Acetylglutamine Pharmacokinetics in Rat Blood and Brain Based on Liquid Chromatography-Tandem Mass Spectrometry and Microdialysis Technique Abstract Acetylglutamine (NAG) is the derivative of glutamine, which is the richest free amino acid in the human body. In this work, a novel reliable method of the combi...
PMC7272065
core_pubmed_pmc
Evaluation of the pharmacokinetic-pharmacodynamic integration of marbofloxacin in combination with methyl gallate against Salmonella Typhimurium in rats
Evaluation of the pharmacokinetic-pharmacodynamic integration of marbofloxacin in combination with methyl gallate against Salmonella Typhimurium in rats Abstract Abstract Fluoroquinolone resistance in Salmonella Typhimurium is becoming a major concern. Hence, an intervention to limit the growth in resistance is inevita...
PMC11945278
core_pubmed_pmc
Evaluation of Different Polysaccharide–Iron Complex Preparations In Vitro and In Vivo
Evaluation of Different Polysaccharide–Iron Complex Preparations In Vitro and In Vivo Abstract Abstract Objectives : Iron-deficiency anemia is one of the most common nutritional deficiencies worldwide. Polysaccharide–iron complexes (PICs), as novel organic iron supplements, have garnered increasing attention due to the...
PMC4623385
core_pubmed_pmc
First human study of a chimeric anti-methamphetamine monoclonal antibody in healthy volunteers
First human study of a chimeric anti-methamphetamine monoclonal antibody in healthy volunteers Abstract This first-in-human study examined the safety and pharmacokinetics of ch-mAb7F9, an anti-methamphetamine monoclonal antibody, in healthy volunteers. Single, escalating doses of ch-mAb7F9 over the range of 0.2 to 20 m...
PMC7182238
core_pubmed_pmc
Simulated Comparison of a Bayesian Clinical Decision Support System Versus Standard of Care For Achieving Gentamicin Pharmacokinetic Targets in Neonates
Simulated Comparison of a Bayesian Clinical Decision Support System Versus Standard of Care For Achieving Gentamicin Pharmacokinetic Targets in Neonates Abstract Background: Gentamicin therapy in neonates is optimized through achieving specific peak and trough concentrations. The objective of this study was to compare ...
PMC6202474
core_pubmed_pmc
PBPK Models for CYP3A4 and P‐gp DDI Prediction: A Modeling Network of Rifampicin, Itraconazole, Clarithromycin, Midazolam, Alfentanil, and Digoxin
PBPK Models for CYP3A4 and P‐gp DDI Prediction: A Modeling Network of Rifampicin, Itraconazole, Clarithromycin, Midazolam, Alfentanil, and Digoxin Abstract Abstract According to current US Food and Drug Administration (FDA) and European Medicines Agency (EMA) guidance documents, physiologically based pharmacokinetic (P...
PMC12757353
core_pubmed_pmc
Predicting individual tree diameter at breast height for genetically diverse Catalpa bungei using nonlinear mixed-effects models and UAV LiDAR data
Predicting individual tree diameter at breast height for genetically diverse Catalpa bungei using nonlinear mixed-effects models and UAV LiDAR data Abstract Introduction Diameter at breast height (DBH) is a key parameter for assessing tree growth, carbon storage, and ecological functions. Traditional ground surveys are...
PMC7915939
core_pubmed_pmc
The Glomerular Filtration Rate Estimators in the Pharmacokinetic Modelling in Acute Kidney Injury: An Observational Study
The Glomerular Filtration Rate Estimators in the Pharmacokinetic Modelling in Acute Kidney Injury: An Observational Study Abstract Abstract The glomerular filtration rate (GFR), according to which the drug dose for patients with chronic kidney disease (CKD) is adjusted, is computed with estimators (eGFR) that are devel...
PMC12122129
core_pubmed_pmc
The feasibility of pharmacokinetic‐based dosing of hydroxyurea for children with sickle cell anaemia in Uganda: Baseline results of the alternative dosing and prevention of transfusions trial
The feasibility of pharmacokinetic‐based dosing of hydroxyurea for children with sickle cell anaemia in Uganda: Baseline results of the alternative dosing and prevention of transfusions trial Abstract Abstract Pharmacokinetic (PK)‐guided dosing of hydroxyurea for children with sickle cell anaemia (SCA) could optimize d...
PMC10704330
core_pubmed_pmc
Efficacy and safety of MP1032 plus standard-of-care compared to standard-of-care in hospitalised patients with COVID-19: a multicentre, randomised double-blind, placebo-controlled phase 2a trial
Efficacy and safety of MP1032 plus standard-of-care compared to standard-of-care in hospitalised patients with COVID-19: a multicentre, randomised double-blind, placebo-controlled phase 2a trial Abstract Summary Background SARS-CoV-2 infections still have a significant impact on the global population. The existing vacc...
PMC12315851
core_pubmed_pmc
Pharmacokinetics of Bocidelpar, ASP0367 , in Renal and Hepatic Impairment: Results From Two Phase 1 Studies
Pharmacokinetics of Bocidelpar, ASP0367 , in Renal and Hepatic Impairment: Results From Two Phase 1 Studies Abstract ABSTRACT Bocidelpar is a peroxisome proliferator‐activated receptor δ modulator designed to address mitochondrial impairment. Two open‐label, single‐dose phase 1 studies ( NCT05117294 / NCT04942964 ) inv...
PMC9326876
core_pubmed_pmc
Effects of processing adjuvants on traditional Chinese herbs
Effects of processing adjuvants on traditional Chinese herbs Abstract Abstract Processing of Chinese medicines is a pharmaceutical technique that transforms medicinal raw materials into decoction pieces for use in different therapies. Various adjuvants, such as vinegar, wine, honey, and brine, are used in the processin...
PMC11936910
core_pubmed_pmc
Population pharmacokinetics of polymyxin B in critically ill patients with carbapenem-resistant organisms infections: insights from steady-state trough and peak plasma concentration
Population pharmacokinetics of polymyxin B in critically ill patients with carbapenem-resistant organisms infections: insights from steady-state trough and peak plasma concentration Abstract Abstract Aims To establish a population pharmacokinetic (PopPK) model of polymyxin B (PMB) in critically ill patients based on st...
PMC12326986
core_pubmed_pmc
Cethromycin pharmacokinetics and pharmacodynamics for single dose cure of Plasmodium berghei liver stages
Cethromycin pharmacokinetics and pharmacodynamics for single dose cure of Plasmodium berghei liver stages Abstract ABSTRACT Cethromycin combines a quinoline nucleus and a macrolide for broad-spectrum antibacterial and antiprotozoan activity. Here, we characterized the murine pharmacokinetics and Plasmodium berghei life...
PMC6775499
core_pubmed_pmc
Formulation and evaluation of multilamellar vesicles ropivacaine in pain management
Formulation and evaluation of multilamellar vesicles ropivacaine in pain management Abstract Abstract Purpose The improvement of postoperative pain control plays an important role in recovery outcomes and patient satisfaction. Multilamellar vesicles ropivacaine, MVR, is being developed to sustain the release of ropivac...
PMC5766731
core_pubmed_pmc
Phase I Clinical Study of ZYAN1, A Novel Prolyl-Hydroxylase (PHD) Inhibitor to Evaluate the Safety, Tolerability, and Pharmacokinetics Following Oral Administration in Healthy Volunteers
Phase I Clinical Study of ZYAN1, A Novel Prolyl-Hydroxylase (PHD) Inhibitor to Evaluate the Safety, Tolerability, and Pharmacokinetics Following Oral Administration in Healthy Volunteers Abstract Objective This phase I study of ZYAN1 was conducted to evaluate the safety, tolerability, and pharmacokinetics following ora...
PMC12414069
core_pubmed_pmc
Revisiting Acyclovir Dosing for Adult Viral Encephalitis Using a Full Bayesian LeiCNS PBPK Modeling Approach
Revisiting Acyclovir Dosing for Adult Viral Encephalitis Using a Full Bayesian LeiCNS PBPK Modeling Approach Abstract Abstract Background and Objective Acyclovir is a primary treatment for central nervous system (CNS) infections caused by herpes simplex virus (HSV) and varicella-zoster virus (VZV). However, patient out...
PMC9780528
core_pubmed_pmc
Applications of the hollow-fibre infection model (HFIM) in viral infection studies
Applications of the hollow-fibre infection model (HFIM) in viral infection studies Abstract Abstract Conventional cell culture systems involve growing cells in stationary cultures in the presence of growth medium containing various types of supplements. At confluency, the cells are divided and further expanded in new c...
PMC6460377
core_pubmed_pmc
Development of a hybrid CFD-PBPK model to predict the transport of xenon gas around a human respiratory system to systemic regions
Development of a hybrid CFD-PBPK model to predict the transport of xenon gas around a human respiratory system to systemic regions Abstract Administering incorrect doses of conventional anesthetic agents through the pulmonary route can cause potential health risks such as blood coagulation, platelet dysfunction, and de...
PMC11239005
core_pubmed_pmc
Preclinical studies of RA475, a guanidine-substituted spirocyclic candidate RPN13/ADRM1 inhibitor for treatment of ovarian cancer
Preclinical studies of RA475, a guanidine-substituted spirocyclic candidate RPN13/ADRM1 inhibitor for treatment of ovarian cancer Abstract There is an urgent unmet need for more targeted and effective treatments for advanced epithelial ovarian cancer (EOC). The emergence of drug resistance is a particular challenge, bu...
PMC9056296
core_pubmed_pmc
Development of long-circulating lapachol nanoparticles: formation, characterization, pharmacokinetics, distribution and cytotoxicity
Development of long-circulating lapachol nanoparticles: formation, characterization, pharmacokinetics, distribution and cytotoxicity Abstract Abstract Lapachol is an active compound for the treatment of malignant brain glioma. However, its physicochemical properties limit its clinical application. The purpose of this s...
PMC10772472
core_pubmed_pmc
Developing a mechanistic translational PK/PD model for a trifunctional NK cell engager to predict the first‐in‐human dose for acute myeloid leukemia
Developing a mechanistic translational PK/PD model for a trifunctional NK cell engager to predict the first‐in‐human dose for acute myeloid leukemia Abstract Abstract Natural killer cell engagers (NKCEs), a treatment that stimulates innate immunity, have lately gained attention owing to their favorable safety profile, ...
PMC9414027
core_pubmed_pmc
Association between the Co-administration of Histamine H 2 Receptor Antagonists and the Effectiveness of Capecitabine in Patients with Colorectal Cancer: Propensity Score Analysis
Association between the Co-administration of Histamine H 2 Receptor Antagonists and the Effectiveness of Capecitabine in Patients with Colorectal Cancer: Propensity Score Analysis Abstract Abstract Background: The association between the effectiveness of capecitabine and the concomitant administration of gastric acid s...
PMC8120342
core_pubmed_pmc
Levofloxacin pharmacokinetics in saliva as measured by a mobile microvolume UV spectrophotometer among people treated for rifampicin-resistant TB in Tanzania
Levofloxacin pharmacokinetics in saliva as measured by a mobile microvolume UV spectrophotometer among people treated for rifampicin-resistant TB in Tanzania Abstract Abstract Background Early detection and correction of low fluoroquinolone exposure may improve treatment of MDR-TB. Objectives To explore a recently deve...
PMC4112793
core_pubmed_pmc
Implementation of pharmacokinetic and pharmacodynamic strategies in early research phases of drug discovery and development at Novartis Institute of Biomedical Research
Implementation of pharmacokinetic and pharmacodynamic strategies in early research phases of drug discovery and development at Novartis Institute of Biomedical Research Abstract Characterizing the relationship between the pharmacokinetics (PK, concentration vs. time) and pharmacodynamics (PD, effect vs. time) is an imp...
PMC4468955
core_pubmed_pmc
Dose proportionality and pharmacokinetics of carvedilol sustained-release formulation: a single dose-ascending 10-sequence incomplete block study
Dose proportionality and pharmacokinetics of carvedilol sustained-release formulation: a single dose-ascending 10-sequence incomplete block study Abstract Abstract Background Carvedilol is a third-generation β-blocker indicated for congestive heart failure and high blood pressure. The aim of this study was to investiga...
PMC12272313
core_pubmed_pmc
Inhibition of OATP1B1 /3 Rather Than UGT1A1 May Be the Major Cause of the Bilirubin Elevation After Atazanavir Administration
Inhibition of OATP1B1 /3 Rather Than UGT1A1 May Be the Major Cause of the Bilirubin Elevation After Atazanavir Administration Abstract Atazanavir has been reported to increase total serum bilirubin level up to ninefold. It is widely believed that the observed total bilirubin elevation is primarily due to UGT1A1 inhibit...
PMC10789040
core_pubmed_pmc
Clinical antiviral efficacy of favipiravir in early COVID-19 (PLATCOV): an open-label, randomised, controlled, adaptive platform trial
Clinical antiviral efficacy of favipiravir in early COVID-19 (PLATCOV): an open-label, randomised, controlled, adaptive platform trial Abstract Abstract Brief summary In early symptomatic COVID-19 treatment, high dose oral favipiravir did not accelerate viral clearance. Background Favipiravir, an anti-influenza drug, h...
PMC12202195
core_pubmed_pmc
Mathematical Albumin Function for Neonates Undergoing Therapeutic Hypothermia in Comparison with Control Neonates
Mathematical Albumin Function for Neonates Undergoing Therapeutic Hypothermia in Comparison with Control Neonates Abstract Abstract Hypoxic‐ischemic encephalopathy (HIE) resulting from perinatal asphyxia presents a substantial risk of mortality and long‐term sequelae in neonates. Therapeutic hypothermia (TH) improves b...
PMC8249295
core_pubmed_pmc
A Model-Informed Method for the Purpose of Precision Dosing of Isoniazid in Pulmonary Tuberculosis
A Model-Informed Method for the Purpose of Precision Dosing of Isoniazid in Pulmonary Tuberculosis Abstract Abstract Background and Objective This study aimed to develop and evaluate a population pharmacokinetic model and limited sampling strategy for isoniazid to be used in model-based therapeutic drug monitoring. Met...
PMC10073089
core_pubmed_pmc
Synthesis, cytotoxicity, and pharmacokinetic evaluations of niclosamide analogs for anti-SARS-CoV-2
Synthesis, cytotoxicity, and pharmacokinetic evaluations of niclosamide analogs for anti-SARS-CoV-2 Abstract Abstract Niclosamide, an oral anthelmintic drug, could inhibit SARS-CoV-2 virus replication through autophagy induction, but high cytotoxicity and poor oral bioavailability limited its application. Twenty-three ...
PMC3487914
core_pubmed_pmc
Repeated intranasal TLR7 stimulation reduces allergen responsiveness in allergic rhinitis
Repeated intranasal TLR7 stimulation reduces allergen responsiveness in allergic rhinitis Abstract Background Interactions between Th1 and Th2 immune responses are of importance to the onset and development of allergic disorders. A Toll-like receptor 7 agonist such as AZD8848 may have potential as a treatment for aller...
PMC9536290
core_pubmed_pmc
Phase IIa Proof-of-Concept Evaluation of the Antiviral Efficacy, Safety, Tolerability, and Pharmacokinetics of the Next-Generation Maturation Inhibitor GSK3640254
Phase IIa Proof-of-Concept Evaluation of the Antiviral Efficacy, Safety, Tolerability, and Pharmacokinetics of the Next-Generation Maturation Inhibitor GSK3640254 Abstract Abstract Background GSK3640254 (GSK’254) is a next-generation human immunodeficiency virus type 1 (HIV-1) maturation inhibitor with pharmacokinetics...
PMC11661806
core_pubmed_pmc
Pharmacokinetics/pharmacodynamics of glucocorticoids: modeling the glucocorticoid receptor dynamics and dose/response of commonly prescribed glucocorticoids
Pharmacokinetics/pharmacodynamics of glucocorticoids: modeling the glucocorticoid receptor dynamics and dose/response of commonly prescribed glucocorticoids Abstract Abstract Background and purpose The main features of the dynamics of the glucocorticoid receptor (GR) have been known for 50 years: 1) in the absence of g...
PMC7356968
core_pubmed_pmc
Key-Protease Inhibition Regimens Promote Tumor Targeting of Neurotensin Radioligands
Key-Protease Inhibition Regimens Promote Tumor Targeting of Neurotensin Radioligands Abstract Abstract Neurotensin subtype 1 receptors (NTS1R) represent attractive molecular targets for directing radiolabeled neurotensin (NT) analogs to tumor lesions for diagnostic and therapeutic purposes. This approach has been large...
PMC9286711
core_pubmed_pmc
Guide to development of compound files for PBPK modeling in the Simcyp population‐based simulator
Guide to development of compound files for PBPK modeling in the Simcyp population‐based simulator Abstract Abstract The Simcyp Simulator is a software platform for population physiologically‐based pharmacokinetic (PBPK) modeling and simulation. It links in vitro data to in vivo absorption, distribution, metabolism, exc...
PMC5884906
core_pubmed_pmc
Single Administration of HBK-15—a Triple 5-HT 1A , 5-HT 7 , and 5-HT 3 Receptor Antagonist—Reverses Depressive-Like Behaviors in Mouse Model of Depression Induced by Corticosterone
Single Administration of HBK-15—a Triple 5-HT 1A , 5-HT 7 , and 5-HT 3 Receptor Antagonist—Reverses Depressive-Like Behaviors in Mouse Model of Depression Induced by Corticosterone Abstract Abstract Studies suggest that the blockade of 5-HT 1A , 5-HT 7 , and 5-HT 3 receptor may increase the speed of antidepressant resp...
PMC5222999
core_pubmed_pmc
Severe Rhabdomyolysis as Complication of Interaction between Atorvastatin and Fusidic Acid in a Patient in Lifelong Antibiotic Prophylaxis: A Dangerous Combination
Severe Rhabdomyolysis as Complication of Interaction between Atorvastatin and Fusidic Acid in a Patient in Lifelong Antibiotic Prophylaxis: A Dangerous Combination Abstract Atorvastatin and HMG-CoA reductase inhibitors are the most frequently used medication in the world due to very few adverse toxic side effects. One ...
PMC3388253
core_pubmed_pmc
Phase I and pharmacokinetic study of capecitabine and the oral mTOR inhibitor everolimus in patients with advanced solid malignancies
Phase I and pharmacokinetic study of capecitabine and the oral mTOR inhibitor everolimus in patients with advanced solid malignancies Abstract Summary Background Everolimus is an oral mTOR-inhibitor. Preclinical data show synergistic effects of mTOR inhibition in combination with 5-fluorouracil-based anticancer therapy...
PMC12110726
core_pubmed_pmc
Physiologically Based Pharmacokinetic Modeling and Simulation to Support a Change in the FDA‐Labeled Dosing Frequency of RHB‐105 Low‐Dose Rifabutin Triple Therapy for Helicobacter pylori Eradication
Physiologically Based Pharmacokinetic Modeling and Simulation to Support a Change in the FDA‐Labeled Dosing Frequency of RHB‐105 Low‐Dose Rifabutin Triple Therapy for Helicobacter pylori Eradication Abstract Abstract Patient adherence is vital for Helicobacter pylori eradication. Simplifying therapy dosing schedules ma...
PMC10634207
core_pubmed_pmc
Pharmacokinetic–pharmacodynamic cutoff values for benzylpenicillin in horses to support the establishment of clinical breakpoints for benzylpenicillin antimicrobial susceptibility testing in horses
Pharmacokinetic–pharmacodynamic cutoff values for benzylpenicillin in horses to support the establishment of clinical breakpoints for benzylpenicillin antimicrobial susceptibility testing in horses Abstract Abstract Introduction The aim of this international project was to establish a species-specific Clinical Breakpoi...
PMC7154752
core_pubmed_pmc
A new paradigm for personalized prophylaxis for patients with severe haemophilia A
A new paradigm for personalized prophylaxis for patients with severe haemophilia A Abstract Abstract Aim For patients with severe haemophilia A, guidelines recommend prophylactic treatment with FVIII, with dose calculations targeting a predetermined FVIII trough level. However, this pharmacokinetic (PK) approach is sub...
PMC11914757
core_pubmed_pmc
Computational modelling of CAR T-cell therapy: from cellular kinetics to patient-level predictions
Computational modelling of CAR T-cell therapy: from cellular kinetics to patient-level predictions Abstract Summary Chimeric Antigen Receptor (CAR) T-cell therapy is characterised by the heterogeneous cellular kinetic profile seen across patients. Unlike traditional chemotherapy, which displays predictable dose-exposur...
PMC9605309
core_pubmed_pmc
Therapeutic Drug Monitoring of Subcutaneous Infliximab in Inflammatory Bowel Disease—Understanding Pharmacokinetics and Exposure Response Relationships in a New Era of Subcutaneous Biologics
Therapeutic Drug Monitoring of Subcutaneous Infliximab in Inflammatory Bowel Disease—Understanding Pharmacokinetics and Exposure Response Relationships in a New Era of Subcutaneous Biologics Abstract CT-P13 is the first subcutaneous infliximab molecule approved for the management of inflammatory bowel disease (IBD). Co...
PMC11124388
core_pubmed_pmc
Effects of CYP3A5 Genotype on Tacrolimus Pharmacokinetics and Graft-versus-Host Disease Incidence in Allogeneic Hematopoietic Stem Cell Transplantation
Effects of CYP3A5 Genotype on Tacrolimus Pharmacokinetics and Graft-versus-Host Disease Incidence in Allogeneic Hematopoietic Stem Cell Transplantation Abstract Tacrolimus (Tac) is pivotal in preventing acute graft-versus-host disease (GVHD) after allogeneic hematopoietic stem cell transplantation (alloHSCT). It has be...
PMC10182164
core_pubmed_pmc
Clinical Pharmacokinetics, Pharmacodynamics, and Immunogenicity of Anifrolumab
Clinical Pharmacokinetics, Pharmacodynamics, and Immunogenicity of Anifrolumab Abstract Abstract The type I interferon (IFN) signaling pathway is implicated in the pathogenesis of systemic lupus erythematosus (SLE). Anifrolumab is a monoclonal antibody that targets the type I IFN receptor subunit 1. Anifrolumab is appr...
PMC3502432
core_pubmed_pmc
High creatinine clearance in critically ill patients with community-acquired acute infectious meningitis
High creatinine clearance in critically ill patients with community-acquired acute infectious meningitis Abstract Background A high dose of anti-infective agents is recommended when treating infectious meningitis. High creatinine clearance (CrCl) may affect the pharmacokinetic / pharmacodynamic relationships of anti-in...
PMC12896384
core_pubmed_pmc
Preclinical Modeling and Simulation to Explore the Tissue/Plasma Exposure and Pharmacodynamic Effect of Vildagliptin in Diabetes Treatment
Preclinical Modeling and Simulation to Explore the Tissue/Plasma Exposure and Pharmacodynamic Effect of Vildagliptin in Diabetes Treatment Abstract ABSTRACT Vildagliptin (VDG) is a dipeptidyl‐peptidase‐4 (DPP‐4) inhibitor used for type 2 diabetes (T2DM) treatment. Viewing to improve VDG treatment, a population pharmaco...
PMC9029035
core_pubmed_pmc
Daunorubicin and Its Active Metabolite Pharmacokinetic Profiles in Acute Myeloid Leukaemia Patients: A Pharmacokinetic Ancillary Study of the BIG-1 Trial
Daunorubicin and Its Active Metabolite Pharmacokinetic Profiles in Acute Myeloid Leukaemia Patients: A Pharmacokinetic Ancillary Study of the BIG-1 Trial Abstract Daunorubicin pharmacokinetics (PK) are characterised by an important inter-individual variability, which raises questions about the optimal dose regimen in p...
PMC5961100
core_pubmed_pmc
Pharmacology of Corticosteroids for Diabetic Macular Edema
Pharmacology of Corticosteroids for Diabetic Macular Edema Abstract Abstract Purpose Corticosteroids remain the mainstay of treatment for inflammatory diseases almost 80 years after their first clinical use. Topical ophthalmic formulations of corticosteroids have been available to treat disease of the anterior segment ...
PMC3581698
core_pubmed_pmc
Linagliptin: A thorough Characterization beyond Its Clinical Efficacy
Linagliptin: A thorough Characterization beyond Its Clinical Efficacy Abstract Linagliptin, one of the five dipeptidyl peptidase-4 inhibitors available, has recently entered the market both in the US and in most European countries for treatment of type 2 diabetes mellitus. It presents a xanthine-based structure, and is...
PMC12567141
core_pubmed_pmc
Design, Synthesis and Biological Evaluation of Pyrazolopyrimidine Derivatives as Aryl Hydrocarbon Receptor Antagonists for Colorectal Cancer Immunotherapy
Design, Synthesis and Biological Evaluation of Pyrazolopyrimidine Derivatives as Aryl Hydrocarbon Receptor Antagonists for Colorectal Cancer Immunotherapy Abstract Background: Aryl hydrocarbon receptor (AhR) is a transcription factor that is involved in the regulation of immunity. AhR inhibits T cell activation in tumo...
PMC5288240
core_pubmed_pmc
DMET™ (Drug Metabolism Enzymes and Transporters): a pharmacogenomic platform for precision medicine
DMET™ (Drug Metabolism Enzymes and Transporters): a pharmacogenomic platform for precision medicine Abstract In the era of personalized medicine, high-throughput technologies have allowed the investigation of genetic variations underlying the inter-individual variability in drug pharmacokinetics/pharmacodynamics. Sever...
PMC12073391
core_pubmed_pmc
Novel Molecular Weight Gradient Hyaluronate Dissolving Microneedles for Sustained Intralesional Delivery and Photodynamic Activation of Hematoporphyrin in Port-Wine Stain Therapy
Novel Molecular Weight Gradient Hyaluronate Dissolving Microneedles for Sustained Intralesional Delivery and Photodynamic Activation of Hematoporphyrin in Port-Wine Stain Therapy Abstract Abstract Port-wine stain (PWS), a progressive congenital vascular malformation characterized by ectatic dermal capillaries, demonstr...
PMC6542327
core_pubmed_pmc
Effects of teriparatide in Chinese and Caucasian women with osteoporosis: bridging study on efficacy
Effects of teriparatide in Chinese and Caucasian women with osteoporosis: bridging study on efficacy Abstract Objective To bridge the efficacy and compare the safety of the 24-week teriparatide treatment in a Chinese osteoporosis study ( NCT00414973 ) to a large international trial (FPT, NCT00670501 ) to determine whet...
PMC12550937
core_pubmed_pmc
Managing Infections in Burn Patients: Strategies and Considerations for Antimicrobial Dosing
Managing Infections in Burn Patients: Strategies and Considerations for Antimicrobial Dosing Abstract Burn injuries are a major cause of morbidity and mortality, largely due to complications such as infection. Impairment of the immune system following burns increases susceptibility to both internal and external infecti...
PMC12333675
core_pubmed_pmc
Identifying a next-generation antimalarial trioxolane in a landscape of artemisinin partial resistance
Identifying a next-generation antimalarial trioxolane in a landscape of artemisinin partial resistance Abstract For over two decades, artemisinin-based combination therapy (ACT) has been the standard of care for the treatment of uncomplicated falciparum malaria. However, artemisinin partial resistance (ART-R) is now pr...
PMC3483207
core_pubmed_pmc
Review of pyronaridine anti-malarial properties and product characteristics
Review of pyronaridine anti-malarial properties and product characteristics Abstract Pyronaridine was synthesized in 1970 at the Institute of Chinese Parasitic Disease and has been used in China for over 30 years for the treatment of malaria. Pyronaridine has high potency against Plasmodium falciparum , including chlor...
PMC12072104
core_pubmed_pmc
High-Performance Liquid Chromatographic Separation of Stereoisomers of ß -Methyl-Substituted Unusual Amino Acids Utilizing Ion Exchangers Based on Cinchona Alkaloids
High-Performance Liquid Chromatographic Separation of Stereoisomers of ß -Methyl-Substituted Unusual Amino Acids Utilizing Ion Exchangers Based on Cinchona Alkaloids Abstract Abstract Novel peptides based on common amino acid building blocks may serve as possible drug candidates; however, their flexible structures may ...
PMC9863705
core_pubmed_pmc
Formulation Development of Fast Dissolving Microneedles Loaded with Cubosomes of Febuxostat: In Vitro and In Vivo Evaluation
Formulation Development of Fast Dissolving Microneedles Loaded with Cubosomes of Febuxostat: In Vitro and In Vivo Evaluation Abstract Febuxostat is a widely prescribed drug for the treatment of gout, which is a highly prevalent disease worldwide and is a major cause of disability in mankind. Febuxostat suffers from sev...
PMC7731208
core_pubmed_pmc
In Silico Food-Drug Interaction: A Case Study of Eluxadoline and Fatty Meal
In Silico Food-Drug Interaction: A Case Study of Eluxadoline and Fatty Meal Abstract Abstract Food-drug interaction is an infrequently considered aspect in clinical practice. Usually, drugs are taken together with meals and what follows may adversely affect pharmacokinetic and pharmacodynamic properties, and hence, the...
PMC12428288
core_pubmed_pmc
Cell-Based Drug Delivery Systems: Innovative Drug Transporters for Targeted Therapy
Cell-Based Drug Delivery Systems: Innovative Drug Transporters for Targeted Therapy Abstract Significant progress has been made in developing cell-based drug delivery systems that utilize the intrinsic biological properties of various cell types—erythrocytes, leukocytes, platelets, stem cells, and even spermatozoa—to i...
PMC9502277
core_pubmed_pmc
Oligonucleotide-Based Therapies for Chronic HBV Infection: A Primer on Biochemistry, Mechanisms and Antiviral Effects
Oligonucleotide-Based Therapies for Chronic HBV Infection: A Primer on Biochemistry, Mechanisms and Antiviral Effects Abstract Abstract Three types of oligonucleotide-based medicines are under clinical development for the treatment of chronic HBV infection. Antisense oligonucleotides (ASOs) and synthetic interfering RN...
PMC12920268
core_pubmed_pmc
Unraveling Network Pharmacology‐Based Therapeutics of Anthranilate Sulfonamides via Sirtuins/ FOXO3a Cascade in Alzheimer's Disease
Unraveling Network Pharmacology‐Based Therapeutics of Anthranilate Sulfonamides via Sirtuins/ FOXO3a Cascade in Alzheimer's Disease Abstract ABSTRACT Sulfonamide‐based compounds have been a clinically attractive scaffold for drug development and proven as antioxidant and antimicrobial agents, but their pharmacological ...
PMC7778726
core_pubmed_pmc
Population pharmacokinetic modeling of intramuscular and oral dexamethasone and betamethasone in Indian women
Population pharmacokinetic modeling of intramuscular and oral dexamethasone and betamethasone in Indian women Abstract Abstract Population analysis of pharmacokinetic data for five differing dosage forms and routes for dexamethasone and betamethasone in 48 healthy nonpregnant Indian women was performed that accounted f...
PMC12778405
core_pubmed_pmc
Analysis of Current Industry Practices for Informing Dosing Recommendation for Patients With Renal Impairment
Analysis of Current Industry Practices for Informing Dosing Recommendation for Patients With Renal Impairment Abstract ABSTRACT Recent updates in clinical guidelines and health authority guidance documents have aimed to standardize best practices for assessing renal function; however, it remains unclear whether the pha...
PMC9239932
core_pubmed_pmc
A Computational Platform Integrating a Mechanistic Model of Crohn’s Disease for Predicting Temporal Progression of Mucosal Damage and Healing
A Computational Platform Integrating a Mechanistic Model of Crohn’s Disease for Predicting Temporal Progression of Mucosal Damage and Healing Abstract Introduction Physicians are often required to make treatment decisions for patients with Crohn’s disease on the basis of limited objective information about the state of...
PMC9109297
core_pubmed_pmc
Dalbavancin as an option for treatment of S. aureus bacteremia (DOTS): study protocol for a phase 2b, multicenter, randomized, open-label clinical trial
Dalbavancin as an option for treatment of S. aureus bacteremia (DOTS): study protocol for a phase 2b, multicenter, randomized, open-label clinical trial Abstract Abstract Background Staphylococcus aureus bacteremia is a life-threatening infection and leading cause of infective endocarditis, with mortality rates of 15–5...
PMC8756278
core_pubmed_pmc
Immuno-oncology trends: preclinical models, biomarkers, and clinical development
Immuno-oncology trends: preclinical models, biomarkers, and clinical development Abstract Abstract The landscape in immuno-oncology (I-O) has undergone profound changes since its early beginnings up through the rapid advances happening today. The current drug development pipeline consists of thousands of potential I-O ...
PMC4565647
core_pubmed_pmc
Effects of Menthol on Nicotine Pharmacokinetic, Pharmacology and Dependence in Mice
Effects of Menthol on Nicotine Pharmacokinetic, Pharmacology and Dependence in Mice Abstract Although menthol, a common flavoring additive to cigarettes, has been found to impact the addictive properties of nicotine cigarettes in smokers little is known about its pharmacological and molecular actions in the brain. Stud...
PMC4475799
core_pubmed_pmc
Bioanalytical Method for Carbocisteine in Human Plasma by Using LC-MS/MS: A Pharmacokinetic Application
Bioanalytical Method for Carbocisteine in Human Plasma by Using LC-MS/MS: A Pharmacokinetic Application Abstract Abstract A simple, sensitive, and selective LC-MS/MS method was developed and validated for the quantification of carbocisteine in human plasma. Rosiglitazone was used as the internal standard and heparin wa...
PMC12856051
core_pubmed_pmc
Some Common Dose–Exposure–Response Estimands and Conditions for Their Causal Identifiability
Some Common Dose–Exposure–Response Estimands and Conditions for Their Causal Identifiability Abstract ABSTRACT Exposure–response analyses are central to dose selection in drug development. The estimand framework, formalized in ICH E9(R1) regulatory guidance, provides a structured approach to define scientific objective...
PMC10604709
core_pubmed_pmc
Population Pharmacokinetic Model of Adalimumab Based on Prior Information Using Real World Data
Population Pharmacokinetic Model of Adalimumab Based on Prior Information Using Real World Data Abstract Adalimumab is a fully human monoclonal antibody used for the treatment of inflammatory bowel disease (IBD). Due to its considerably variable pharmacokinetics and the risk of developing antibodies against adalimumab,...
PMC10952588
core_pubmed_pmc
Adaptation of a population pharmacokinetic model to inform tacrolimus therapy in heart transplant recipients
Adaptation of a population pharmacokinetic model to inform tacrolimus therapy in heart transplant recipients Abstract Aim Existing tacrolimus population pharmacokinetic models are unsuitable for guiding tacrolimus dosing in heart transplant recipients. This study aimed to develop and evaluate a population pharmacokinet...
PMC12295124
core_pubmed_pmc
Quercetin, Catechin, and Diosmin as Modulators of Haloperidol–HSA Interactions: A Biophysical and Computational Study
Quercetin, Catechin, and Diosmin as Modulators of Haloperidol–HSA Interactions: A Biophysical and Computational Study Abstract Potential interactions of haloperidol with food ingredients such as flavonoids may be of great importance both for understanding the pharmacokinetic interactions of xenobiotics with human serum...
PMC7854405
core_pubmed_pmc
Pharmacokinetics and Safety of Single and Multiple Doses of Oral N -Acetylcysteine in Healthy Chinese and Caucasian Volunteers: An Open-Label, Phase I Clinical Study
Pharmacokinetics and Safety of Single and Multiple Doses of Oral N -Acetylcysteine in Healthy Chinese and Caucasian Volunteers: An Open-Label, Phase I Clinical Study Abstract Abstract Introduction Few studies have evaluated whether the pharmacokinetics of N -acetyl-cysteine (NAC) are different in Chinese and Caucasian ...
PMC8589991
core_pubmed_pmc
Impact of ceftolozane/tazobactam concentrations in continuous infusion against extensively drug-resistant Pseudomonas aeruginosa isolates in a hollow-fiber infection model
Impact of ceftolozane/tazobactam concentrations in continuous infusion against extensively drug-resistant Pseudomonas aeruginosa isolates in a hollow-fiber infection model Abstract Abstract Ceftolozane/tazobactam (C/T) has emerged as a potential agent for the treatment of extensively drug-resistant (XDR) Pseudomonas ae...
PMC9958172
core_pubmed_pmc
Concentrations of escitalopram in blood of patients treated in a naturalistic setting: focus on patients with alcohol and benzodiazepine use disorder
Concentrations of escitalopram in blood of patients treated in a naturalistic setting: focus on patients with alcohol and benzodiazepine use disorder Abstract Abstract The selective serotonin reuptake inhibitor escitalopram (ESC) is indicated for the treatment of major depressive disorder (MDD) and of generalized anxie...
PMC11913679
core_pubmed_pmc
Model-informed drug development of novel ROCK2 inhibitor TDI01: population pharmacokinetic study and simulation
Model-informed drug development of novel ROCK2 inhibitor TDI01: population pharmacokinetic study and simulation Abstract Abstract Introduction TDI01 is a novel and highly selective ROCK2 inhibitor, which provides a potential valuable candidate for the treatment of ALI/ARDS due to COVID-19. Methods The objective of this...
PMC3975950
core_pubmed_pmc
Pharmacological considerations in the design of anti-malarial drug combination therapies – is matching half-lives enough?
Pharmacological considerations in the design of anti-malarial drug combination therapies – is matching half-lives enough? Abstract Anti-malarial drugs are now mainly deployed as combination therapy (CT), primarily as a mechanism to prevent or slow the spread of resistance. This strategy is justified by mathematical arg...
PMC9845776
core_pubmed_pmc
Therapeutic effect and rebound evaluation of dapagliflozin on glycated hemoglobin (HbA1c) in type 1 diabetes mellitus patients
Therapeutic effect and rebound evaluation of dapagliflozin on glycated hemoglobin (HbA1c) in type 1 diabetes mellitus patients Abstract Dapagliflozin has been used to treat patients with type 1 diabetes mellitus; however, the actual drug efficacy of dapagliflozin on glycated hemoglobin (HbA1c) and whether there is a re...
PMC3015066
core_pubmed_pmc
The Dose Proportionality of Telcagepant after Administration of Single Oral and Intravenous Doses in Healthy Adult Subjects
The Dose Proportionality of Telcagepant after Administration of Single Oral and Intravenous Doses in Healthy Adult Subjects Abstract Abstract Introduction Telcagepant (MK-0974) is a novel, orally active and selective CGRP receptor antagonist being investigated for acute treatment of migraine. Early clinical data sugges...
PMC8144895
core_pubmed_pmc
Synergistic integration of metal nanoclusters and biomolecules as hybrid systems for therapeutic applications
Synergistic integration of metal nanoclusters and biomolecules as hybrid systems for therapeutic applications Abstract Abstract Therapeutic nanoparticles are designed to enhance efficacy, real-time monitoring, targeting accuracy, biocompatibility, biodegradability, safety, and the synergy of diagnosis and treatment of ...
PMC10243242
core_pubmed_pmc
A clinical pharmacokinetic drug-drug interaction study between dextromethorphan and emvododstat, a potent anti-SARS-CoV-2 dihydroorotate dehydrogenase inhibitor
A clinical pharmacokinetic drug-drug interaction study between dextromethorphan and emvododstat, a potent anti-SARS-CoV-2 dihydroorotate dehydrogenase inhibitor Abstract Abstract Purpose A therapeutic agent that targets both viral replication and the hyper-reactive immune response would offer a highly desirable treatme...
PMC10893614
core_pubmed_pmc
Multienzymatic biotransformation of flavokawain B by entomopathogenic filamentous fungi: structural modifications and pharmacological predictions
Multienzymatic biotransformation of flavokawain B by entomopathogenic filamentous fungi: structural modifications and pharmacological predictions Abstract Background Flavokawain B is one of the naturally occurring chalcones in the kava plant ( Piper methysticum ). It exhibits anticancer, anti-inflammatory and antimalar...
PMC10726354
core_pubmed_pmc
Design, Synthesis, and Biological Evaluation of Small-Molecule-Based Radioligands with Improved Pharmacokinetic Properties for Imaging of Programmed Death Ligand 1
Design, Synthesis, and Biological Evaluation of Small-Molecule-Based Radioligands with Improved Pharmacokinetic Properties for Imaging of Programmed Death Ligand 1 Abstract Small molecules offer some advantages for developing positron emission tomography (PET) tracers and are therefore a promising approach for imaging ...
PMC7968666
core_pubmed_pmc
The pharmacokinetics and drug-drug interactions of ivermectin in Aedes aegypti mosquitoes
The pharmacokinetics and drug-drug interactions of ivermectin in Aedes aegypti mosquitoes Abstract Abstract Mosquitoes are vectors of major diseases such as dengue fever and malaria. Mass drug administration of endectocides to humans and livestock is a promising complementary approach to current insecticide-based vecto...
PMC4944867
core_pubmed_pmc
Phase II evaluation of sunitinib in the treatment of recurrent or refractory high‐grade glioma or ependymoma in children: a children's Oncology Group Study ACNS1021
Phase II evaluation of sunitinib in the treatment of recurrent or refractory high‐grade glioma or ependymoma in children: a children's Oncology Group Study ACNS1021 Abstract Abstract Sunitinib malate is a small multi‐targeted tyrosine kinase inhibitor that inhibits vascular endothelial growth factor receptor (VEGFR), p...
PMC7321193
core_pubmed_pmc
Liquid Chromatography-Tandem Mass Spectrometry (LC-MS/MS)-Based Proteomics of Drug-Metabolizing Enzymes and Transporters
Liquid Chromatography-Tandem Mass Spectrometry (LC-MS/MS)-Based Proteomics of Drug-Metabolizing Enzymes and Transporters Abstract Liquid chromatography-tandem mass spectrometry (LC-MS/MS)-based proteomics is a powerful tool for identifying and quantifying proteins in biological samples, outperforming conventional antib...