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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... |
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