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PMC8843667 | core_pubmed_pmc | Alpelisib-Induced Diabetes Mellitus: Case Report, Pharmacodynamics and Management Considerations | Alpelisib-Induced Diabetes Mellitus: Case Report, Pharmacodynamics and Management Considerations Abstract Introduction Alpelisib is an orally selective PI3K alpha inhibitor recently available for the treatment of advanced breast cancer. PI3K pathway is an intracellular signaling pathway that plays an important role in ... |
PMC11125931 | core_pubmed_pmc | Impact of LS Mutation on Pharmacokinetics of Preventive HIV Broadly Neutralizing Monoclonal Antibodies: A Cross-Protocol Analysis of 16 Clinical Trials in People without HIV | Impact of LS Mutation on Pharmacokinetics of Preventive HIV Broadly Neutralizing Monoclonal Antibodies: A Cross-Protocol Analysis of 16 Clinical Trials in People without HIV Abstract Abstract Monoclonal antibodies are commonly engineered with an introduction of Met428Leu and Asn434Ser, known as the LS mutation, in the ... |
PMC5437664 | core_pubmed_pmc | Inhibition of O-GlcNAcase leads to elevation of O-GlcNAc tau and reduction of tauopathy and cerebrospinal fluid tau in rTg4510 mice | Inhibition of O-GlcNAcase leads to elevation of O-GlcNAc tau and reduction of tauopathy and cerebrospinal fluid tau in rTg4510 mice Abstract Abstract Background Hyperphosphorylation of microtubule-associated protein tau is a distinct feature of neurofibrillary tangles (NFTs) that are the hallmark of neurodegenerative t... |
PMC11163076 | core_pubmed_pmc | Establishing adherence–concentration–efficacy thresholds of TDF–FTC pre-exposure prophylaxis for HIV prevention in African women: a protocol for the Women TDF–FTC Benchmark Study | Establishing adherence–concentration–efficacy thresholds of TDF–FTC pre-exposure prophylaxis for HIV prevention in African women: a protocol for the Women TDF–FTC Benchmark Study Abstract Background Oral pre-exposure prophylaxis (PrEP) using co-formulated emtricitabine (FTC) and tenofovir disoproxil fumarate (TDF) is a... |
PMC11418394 | core_pubmed_pmc | Chemotherapy for the treatment of alveolar echinococcosis: Where are we? | Chemotherapy for the treatment of alveolar echinococcosis: Where are we? Abstract Abstract Alveolar echinococcosis (AE) is a severe liver disease due to infection with the Echinococcus multilocularis larval stage, called the metacestode. Management of AE is based on benzimidazole chemotherapy (albendazole or mebendazol... |
PMC5971609 | core_pubmed_pmc | Pharmacokinetics and Pharmacodynamics of Fosfomycin and Its Activity against Extended-Spectrum-β-Lactamase-, Plasmid-Mediated AmpC-, and Carbapenemase-Producing Escherichia coli in a Murine Urinary Tract Infection Model | Pharmacokinetics and Pharmacodynamics of Fosfomycin and Its Activity against Extended-Spectrum-β-Lactamase-, Plasmid-Mediated AmpC-, and Carbapenemase-Producing Escherichia coli in a Murine Urinary Tract Infection Model Abstract ABSTRACT Fosfomycin has become an attractive treatment alternative for urinary tract infect... |
PMC10659066 | core_pubmed_pmc | Pharmacokinetic and pharmacodynamic considerations for antifungal therapy optimisation in the treatment of intra-abdominal candidiasis | Pharmacokinetic and pharmacodynamic considerations for antifungal therapy optimisation in the treatment of intra-abdominal candidiasis Abstract Abstract Intra-abdominal candidiasis (IAC) is one of the most common of invasive candidiasis observed in critically ill patients. It is associated with high mortality, with up ... |
PMC9367699 | core_pubmed_pmc | PET imaging to assess fibroblast activation protein inhibitor biodistribution: A training program adapted to pharmacology education | PET imaging to assess fibroblast activation protein inhibitor biodistribution: A training program adapted to pharmacology education Abstract Abstract In the process of pharmacology education, practical teaching is an important complement to theoretical teaching. These activities include the use of experimental animals ... |
PMC12081902 | core_pubmed_pmc | First-in-human phase I study of EMB-02, a bispecific antibody targeting PD-1 and LAG-3 in patients with advanced solid tumors | First-in-human phase I study of EMB-02, a bispecific antibody targeting PD-1 and LAG-3 in patients with advanced solid tumors Abstract Background EMB-02 is a symmetric bispecific antibody targeting programmed cell death protein-1 and lymphocyte-activation gene 3 simultaneously. Here, we present the first-in-human study... |
PMC6899639 | core_pubmed_pmc | Safety, pharmacokinetics, and pharmacodynamic activity of obinutuzumab, a type 2 anti‐ CD 20 monoclonal antibody for the desensitization of candidates for renal transplant | Safety, pharmacokinetics, and pharmacodynamic activity of obinutuzumab, a type 2 anti‐ CD 20 monoclonal antibody for the desensitization of candidates for renal transplant Abstract The limited effectiveness of rituximab plus intravenous immunoglobulin ( IVIG ) in desensitization may be due to incomplete B cell depletio... |
PMC4301837 | core_pubmed_pmc | Aldosterone synthase inhibition: cardiorenal protection in animal disease models and translation of hormonal effects to human subjects | Aldosterone synthase inhibition: cardiorenal protection in animal disease models and translation of hormonal effects to human subjects Abstract Background Aldosterone synthase inhibition provides the potential to attenuate both the mineralocorticoid receptor-dependent and independent actions of aldosterone. In vitro st... |
PMC6989246 | core_pubmed_pmc | PKconverter: R package to convert the pharmacokinetic parameters | PKconverter: R package to convert the pharmacokinetic parameters Abstract Abstract Population pharmacokinetic analysis and modeling procedures typically require estimates of both population and individual pharmacokinetic parameters. However, only some of these parameters are contained in models and only parameters in t... |
PMC7721091 | core_pubmed_pmc | HM30181A, a potent P-glycoprotein inhibitor, potentiates the absorption and in vivo antitumor efficacy of paclitaxel in an orthotopic brain tumor model | HM30181A, a potent P-glycoprotein inhibitor, potentiates the absorption and in vivo antitumor efficacy of paclitaxel in an orthotopic brain tumor model Abstract Abstract Objective: Delivery of chemotherapeutic drugs to the brain has remained a major obstacle in the treatment of glioma, owing to the presence of the bloo... |
PMC4569680 | core_pubmed_pmc | Pharmacokinetics, Pharmacodynamics, and Safety of Canagliflozin in Japanese Patients with Type 2 Diabetes Mellitus | Pharmacokinetics, Pharmacodynamics, and Safety of Canagliflozin in Japanese Patients with Type 2 Diabetes Mellitus Abstract Introduction Canagliflozin is a sodium glucose co-transporter 2 inhibitor approved worldwide for the treatment of patients with type 2 diabetes mellitus (T2DM). The present study evaluated pharmac... |
PMC5681758 | core_pubmed_pmc | Adjunctive use of physostigmine salicylate (Anticholium®) in perioperative sepsis and septic shock: study protocol for a randomized, double-blind, placebo-controlled, monocentric trial (Anticholium® per Se) | Adjunctive use of physostigmine salicylate (Anticholium®) in perioperative sepsis and septic shock: study protocol for a randomized, double-blind, placebo-controlled, monocentric trial (Anticholium® per Se) Abstract Abstract Background Severe sepsis and septic shock remain a major challenge, even in modern intensive ca... |
PMC9314306 | core_pubmed_pmc | Improved Confidence in a Confirmatory Stage by Application of Item-Based Pharmacometrics Model: Illustration with a Phase III Active Comparator-Controlled Trial in COPD Patients | Improved Confidence in a Confirmatory Stage by Application of Item-Based Pharmacometrics Model: Illustration with a Phase III Active Comparator-Controlled Trial in COPD Patients Abstract Abstract Purpose The current study aimed to illustrate how a non-linear mixed effect (NLME) model-based analysis may improve confiden... |
PMC12571850 | core_pubmed_pmc | BYS10, a novel selective RET inhibitor, exhibits potent antitumor activity in preclinical models | BYS10, a novel selective RET inhibitor, exhibits potent antitumor activity in preclinical models Abstract Abstract Background Aberrant alterations in the RET gene serve as oncogenic drivers in multiple cancers, making RET kinase inhibition a promising therapeutic strategy. However, acquired resistance limits the clinic... |
PMC8674005 | core_pubmed_pmc | Population pharmacokinetics of liposomal irinotecan in patients with cancer and exposure–safety analyses in patients with metastatic pancreatic cancer | Population pharmacokinetics of liposomal irinotecan in patients with cancer and exposure–safety analyses in patients with metastatic pancreatic cancer Abstract Abstract Liposomal irinotecan is a liposomal formulation of irinotecan, which prolongs circulation of irinotecan and its active metabolite SN‐38. A population p... |
PMC9992749 | core_pubmed_pmc | Development of thermosensitive hydrogel of Amphotericin-B and Lactoferrin combination-loaded PLGA-PEG-PEI nanoparticles for potential eradication of ocular fungal infections: In-vitro , ex-vivo and in-vivo studies | Development of thermosensitive hydrogel of Amphotericin-B and Lactoferrin combination-loaded PLGA-PEG-PEI nanoparticles for potential eradication of ocular fungal infections: In-vitro , ex-vivo and in-vivo studies Abstract Abstract The most prevalent conditions among ocular surgery and COVID−19 patients are fungal eye ... |
PMC3139194 | core_pubmed_pmc | Molecular Imaging and Pharmacokinetic Analysis of Carbon-11 Labeled Antisense Oligonucleotide LY2181308 in Cancer Patients | Molecular Imaging and Pharmacokinetic Analysis of Carbon-11 Labeled Antisense Oligonucleotide LY2181308 in Cancer Patients Abstract Antisense oligonucleotides (ASOs) have potential as anti-cancer agents by specifically modulating genes involved in tumorigenesis. However, little is known about ASO biodistribution and ti... |
PMC12035594 | core_pubmed_pmc | Killing several birds with one stone: A multi‐indication population pharmacokinetic model and Bayesian estimator for enteric‐coated mycophenolate sodium | Killing several birds with one stone: A multi‐indication population pharmacokinetic model and Bayesian estimator for enteric‐coated mycophenolate sodium Abstract Abstract Aims Mycophenolic acid (MPA), the active component of enteric‐coated mycophenolate sodium (EC‐MPS), exhibits highly variable pharmacokinetics. Only a... |
PMC12065018 | core_pubmed_pmc | ABCB1, SLC22A1, COMT, and OPRM1 genotypes: Study of their influence on plasma methadone levels and clinical response to methadone maintenance treatment in opioid use disorder | ABCB1, SLC22A1, COMT, and OPRM1 genotypes: Study of their influence on plasma methadone levels and clinical response to methadone maintenance treatment in opioid use disorder Abstract Abstract Background Opioid use disorder (OUD) is an emerging and global public health concern, and its management remains inadequate, no... |
PMC2869454 | core_pubmed_pmc | Factors affecting the long-term response to tacrolimus in renal transplant patients: Pharmacokinetic and pharmacogenetic approach | Factors affecting the long-term response to tacrolimus in renal transplant patients: Pharmacokinetic and pharmacogenetic approach Abstract Background: The aim of our study was to determine the impact of CYP3A5*1 and CYP3A5*3 on the kinetics of tacrolimus in renal transplant recipients. Material and methods: Forty kidne... |
PMC11282505 | core_pubmed_pmc | Treatment of a resistant case of schizoaffective disorder with lumateperone: A case report | Treatment of a resistant case of schizoaffective disorder with lumateperone: A case report Abstract To this day, there exists skepticism about the reliability and clinical utility of the diagnostic criteria and classification of schizoaffective disorder. In addition, the treatment of schizoaffective disorder, especiall... |
PMC11725105 | core_pubmed_pmc | Microneedles as transdermal drug delivery system for enhancing skin disease treatment | Microneedles as transdermal drug delivery system for enhancing skin disease treatment Abstract Abstract Microneedles (MNs) serve as a revolutionary paradigm in transdermal drug delivery, heralding a viable resolution to the formidable barriers presented by the cutaneous interface. This review examines MNs as an advance... |
PMC5064724 | core_pubmed_pmc | Evaluation of a Scenario in Which Estimates of Bioequivalence Are Biased and a Proposed Solution: t last (Common) | Evaluation of a Scenario in Which Estimates of Bioequivalence Are Biased and a Proposed Solution: t last (Common) Abstract Abstract In bioequivalence (BE) testing, it is the convention to identify t last separately for each concentration‐vs‐time profile. Within‐subject differences in t last between treatments can arise... |
PMC12047412 | core_pubmed_pmc | Plasma Trough Concentrations of Beta‐Lactam Antibiotics in the Early Phase of Septic Shock | Plasma Trough Concentrations of Beta‐Lactam Antibiotics in the Early Phase of Septic Shock Abstract ABSTRACT Introduction Septic shock necessitates timely antibiotic therapy, often with broad‐spectrum beta‐lactam antibiotics (ß‐LA). To our knowledge, no previous study has examined antibiotic concentrations repeatedly d... |
PMC6541623 | core_pubmed_pmc | Berberine alleviates hyperglycemia by targeting hepatic glucokinase in diabetic db/db mice | Berberine alleviates hyperglycemia by targeting hepatic glucokinase in diabetic db/db mice Abstract Abstract Berberine (BBR) is a widely used anti-diabetic agent, and liver glucokinase (GK) has been reported to be involved. However, the mechanisms of BBR in regulating GK are still unknown. Here, we found that BBR upreg... |
PMC4467258 | core_pubmed_pmc | The Effect of Food and Formulation on the Pharmacokinetics, Safety, and Tolerability of GSK1322322 in Healthy Volunteers | The Effect of Food and Formulation on the Pharmacokinetics, Safety, and Tolerability of GSK1322322 in Healthy Volunteers Abstract GSK1322322 is the first in a new class of antibiotics that inhibit peptide deformylase, necessary for bacterial protein maturation. Previously, low absolute bioavailability was observed for ... |
PMC9952708 | core_pubmed_pmc | Evaluation of Piperacillin/Sulbactam, Piperacillin/Tazobactam and Cefoperazone/Sulbactam Dosages in Gram-Negative Bacterial Bloodstream Infections by Monte Carlo Simulation | Evaluation of Piperacillin/Sulbactam, Piperacillin/Tazobactam and Cefoperazone/Sulbactam Dosages in Gram-Negative Bacterial Bloodstream Infections by Monte Carlo Simulation Abstract The optimal regimens of piperacillin/sulbactam (PIS 2:1), piperacillin/tazobactam (PTZ 8:1), and cefoperazone/sulbactam (CSL 2:1) are not ... |
PMC12830235 | core_pubmed_pmc | First‐in‐Human Study to Evaluate the Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of ASP1617, a Cathepsin‐S Inhibitor, in Healthy Adult Subjects | First‐in‐Human Study to Evaluate the Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of ASP1617, a Cathepsin‐S Inhibitor, in Healthy Adult Subjects Abstract ABSTRACT ASP1617 is a novel, highly selective inhibitor of cathepsin‐S, an important protease for antigen peptide loading onto major histocompatibilit... |
PMC3414087 | core_pubmed_pmc | Preparation and in vivo pharmacokinetics of curcumin-loaded PCL-PEG-PCL triblock copolymeric nanoparticles | Preparation and in vivo pharmacokinetics of curcumin-loaded PCL-PEG-PCL triblock copolymeric nanoparticles Abstract Abstract Background: Curcumin (CUR) has been linked with antioxidant, anti-inflammatory, antimicrobial, anti amyloid, and antitumor effects, but its application is limited because of its low aqueous solub... |
PMC12401397 | core_pubmed_pmc | Optimizing ketamine dosing strategies across diverse clinical applications: a comprehensive review | Optimizing ketamine dosing strategies across diverse clinical applications: a comprehensive review Abstract Abstract Ketamine has emerged as a versatile therapeutic agent with applications spanning anesthesia, pain management, and psychiatric disorders. This review examines ketamine’s clinical utility across diverse ad... |
PMC4968108 | core_pubmed_pmc | Quantitation and pharmacokinetic modeling of therapeutic antibody quality attributes in human studies | Quantitation and pharmacokinetic modeling of therapeutic antibody quality attributes in human studies Abstract ABSTRACT A thorough understanding of drug metabolism and disposition can aid in the assessment of efficacy and safety. However, analytical methods used in pharmacokinetics (PK) studies of protein therapeutics ... |
PMC4716719 | core_pubmed_pmc | Clinical pharmacology study of cariprazine (MP-214) in patients with schizophrenia (12-week treatment) | Clinical pharmacology study of cariprazine (MP-214) in patients with schizophrenia (12-week treatment) Abstract Abstract Purpose Cariprazine is a potent dopamine D 3 -preferring D 3 /D 2 receptor partial agonist in development for the treatment of schizophrenia, bipolar mania, and depression. Pharmacokinetics of caripr... |
PMC8694396 | core_pubmed_pmc | Impact of Maximizing Css/MIC Ratio on Efficacy of Continuous Infusion Meropenem Against Documented Gram-Negative Infections in Critically Ill Patients and Population Pharmacokinetic/Pharmacodynamic Analysis to Support Treatment Optimization | Impact of Maximizing Css/MIC Ratio on Efficacy of Continuous Infusion Meropenem Against Documented Gram-Negative Infections in Critically Ill Patients and Population Pharmacokinetic/Pharmacodynamic Analysis to Support Treatment Optimization Abstract Abstract Introduction: optimal treatment of Gram-negative infections i... |
PMC4230996 | core_pubmed_pmc | Radiosynthesis and Evaluation of an 18 F-Labeled Positron Emission Tomography (PET) Radioligand for Metabotropic Glutamate Receptor Subtype 4 (mGlu 4 ) | Radiosynthesis and Evaluation of an 18 F-Labeled Positron Emission Tomography (PET) Radioligand for Metabotropic Glutamate Receptor Subtype 4 (mGlu 4 ) Abstract Four 4-phthalimide derivatives of N -(3-chlorophenyl)-2-picolinamide were synthesized as potential ligands for the PET imaging of mGlu 4 in the brain. Of these... |
PMC8918679 | core_pubmed_pmc | First experience of a hemophilia monitoring platform: florio HAEMO | First experience of a hemophilia monitoring platform: florio HAEMO Abstract Abstract Background florio HAEMO is a new hemophilia treatment monitoring application consisting of a patient smartphone application (app) and a web‐based dashboard for healthcare professionals, providing several novel features, including activ... |
PMC6058520 | core_pubmed_pmc | Modification of translationally controlled tumor protein-derived protein transduction domain for improved intranasal delivery of insulin | Modification of translationally controlled tumor protein-derived protein transduction domain for improved intranasal delivery of insulin Abstract Abstract Carrier peptides, termed protein transduction domains (PTDs), serve as provide promising vehicles for intranasal delivery of macromolecular drugs. A mutant PTD deriv... |
PMC12699562 | core_pubmed_pmc | Systemic STING agonist therapy drives expression of interferon stimulated genes and downstream production of cytokines in dogs with solid tumors | Systemic STING agonist therapy drives expression of interferon stimulated genes and downstream production of cytokines in dogs with solid tumors Abstract Abstract Background Stimulator of interferon genes (STING) agonist drugs can induce expression of interferon stimulated genes (ISGs) and proinflammatory cytokine prod... |
PMC7322758 | core_pubmed_pmc | Ultra-sensitive bioanalysis of the therapeutic peptide exenatide for accurate pharmacokinetic analyses at effective plasma concentrations utilizing UPLC-MS/MS | Ultra-sensitive bioanalysis of the therapeutic peptide exenatide for accurate pharmacokinetic analyses at effective plasma concentrations utilizing UPLC-MS/MS Abstract Exenatide is the first approved glucagon-like peptide 1 receptor agonist subcutaneously or intramuscularly injected for the treatment of type 2 diabetes... |
PMC6722387 | core_pubmed_pmc | Generation of Human iPSC–Derived Intestinal Epithelial Cell Monolayers by CDX2 Transduction | Generation of Human iPSC–Derived Intestinal Epithelial Cell Monolayers by CDX2 Transduction Abstract Abstract Background & aims To develop an effective and safe orally administered drug, it is important to predict its intestinal absorption rate, intestinal first-pass effect, and drug-drug interactions of orally adminis... |
PMC9966583 | core_pubmed_pmc | The Role of “Physiologically Based Pharmacokinetic Model (PBPK)” New Approach Methodology (NAM) in Pharmaceuticals and Environmental Chemical Risk Assessment | The Role of “Physiologically Based Pharmacokinetic Model (PBPK)” New Approach Methodology (NAM) in Pharmaceuticals and Environmental Chemical Risk Assessment Abstract Physiologically Based Pharmacokinetic (PBPK) models are mechanistic tools generally employed in the pharmaceutical industry and environmental health risk... |
PMC4529213 | core_pubmed_pmc | Oral Migalastat HCl Leads to Greater Systemic Exposure and Tissue Levels of Active α-Galactosidase A in Fabry Patients when Co-Administered with Infused Agalsidase | Oral Migalastat HCl Leads to Greater Systemic Exposure and Tissue Levels of Active α-Galactosidase A in Fabry Patients when Co-Administered with Infused Agalsidase Abstract Abstract Migalastat HCl (AT1001, 1-Deoxygalactonojirimycin) is an investigational pharmacological chaperone for the treatment of α-galactosidase A ... |
PMC6657005 | core_pubmed_pmc | A Comprehensive Framework for Physiologically‐Based Pharmacokinetic Modeling in Matlab | A Comprehensive Framework for Physiologically‐Based Pharmacokinetic Modeling in Matlab Abstract Physiologically‐based pharmacokinetic (PBPK) models are useful tools to predict clinical scenarios for special populations for whom there are high hurdles to conduct clinical trials such as children or the elderly. However, ... |
PMC4712753 | core_pubmed_pmc | Assessing usability, label comprehension, pen robustness and pharmacokinetics of a self-administered prefilled autoinjector pen of methotrexate in patients with rheumatoid arthritis | Assessing usability, label comprehension, pen robustness and pharmacokinetics of a self-administered prefilled autoinjector pen of methotrexate in patients with rheumatoid arthritis Abstract Objective: To assess usability, bioavailability, and safety of subcutaneous self-administration of 0.3 mL of methotrexate 50 mg/m... |
PMC5944578 | core_pubmed_pmc | Assessment of Relative Bioavailability of Moroctocog Alfa and Moroctocog Alfa (AF‐CC) in Subjects With Severe Hemophilia A | Assessment of Relative Bioavailability of Moroctocog Alfa and Moroctocog Alfa (AF‐CC) in Subjects With Severe Hemophilia A Abstract Abstract An open‐label, single‐dose, randomized, two‐period, crossover study comparing the pharmacokinetics of factor VIII activity in plasma (FVIII:C) after administration of an albumin‐f... |
PMC10539503 | core_pubmed_pmc | Reproducibility in pharmacometrics applied in a phase III trial of BCG-vaccination for COVID-19 | Reproducibility in pharmacometrics applied in a phase III trial of BCG-vaccination for COVID-19 Abstract Large clinical trials often generate complex and large datasets which need to be presented frequently throughout the trial for interim analysis or to inform a data safety monitory board (DSMB). In addition, reliable... |
PMC6114027 | core_pubmed_pmc | A Controlled Release System for Long-Acting Intravitreal Delivery of Small Molecules | A Controlled Release System for Long-Acting Intravitreal Delivery of Small Molecules Abstract Purpose The short half lives of small molecules in the vitreous requires frequent repeated intravitreal injections that are impractical for treatment of chronic eye diseases. We sought to develop a method for increasing the in... |
PMC12061369 | core_pubmed_pmc | Mechanism-Based Pharmacokinetic/Pharmacodynamic Model of Voriconazole for Predicting the Clinical Outcomes of Adult Patients With Invasive Aspergillosis | Mechanism-Based Pharmacokinetic/Pharmacodynamic Model of Voriconazole for Predicting the Clinical Outcomes of Adult Patients With Invasive Aspergillosis Abstract Supplemental Digital Content is Available in the Text. Background: Voriconazole is the first-line therapy for invasive aspergillosis (IA). To determine the mi... |
PMC2945360 | core_pubmed_pmc | Early clinical development of artemether-lumefantrine dispersible tablet: palatability of three flavours and bioavailability in healthy subjects | Early clinical development of artemether-lumefantrine dispersible tablet: palatability of three flavours and bioavailability in healthy subjects Abstract Background Efforts to ease administration and enhance acceptability of the oral anti-malarial artemether-lumefantrine (A-L) crushed tablet to infants and children tri... |
PMC8707067 | core_pubmed_pmc | Predictors of Efavirenz Plasma Exposure, Auto-Induction Profile, and Effect of Pharmacogenetic Variations among HIV-Infected Children in Ethiopia: A Prospective Cohort Study | Predictors of Efavirenz Plasma Exposure, Auto-Induction Profile, and Effect of Pharmacogenetic Variations among HIV-Infected Children in Ethiopia: A Prospective Cohort Study Abstract Abstract (1) Background: Efavirenz plasma concentration displays wide between-patient variability partly due to pharmacogenetic variation... |
PMC7153006 | core_pubmed_pmc | Kaji-Ichigoside F1 and Rosamultin Protect Vascular Endothelial Cells against Hypoxia-Induced Apoptosis via the PI3K/AKT or ERK1/2 Signaling Pathway | Kaji-Ichigoside F1 and Rosamultin Protect Vascular Endothelial Cells against Hypoxia-Induced Apoptosis via the PI3K/AKT or ERK1/2 Signaling Pathway Abstract Abstract As a pair of differential isomers, Kaji-ichigoside F1 and Rosamultin are both pentacyclic triterpenoids isolated from the subterranean root of Potentilla ... |
PMC11749192 | core_pubmed_pmc | Clinical predictors of 3-month isoniazid rifapentine (3HP)-related adverse drug reactions (ADR) during tuberculosis preventive therapy (PAnDoRA-3HP study): an observational study protocol | Clinical predictors of 3-month isoniazid rifapentine (3HP)-related adverse drug reactions (ADR) during tuberculosis preventive therapy (PAnDoRA-3HP study): an observational study protocol Abstract Abstract Abstract Introduction Tuberculosis (TB) is the leading infectious cause of death globally. Despite WHO recommendat... |
PMC12641639 | core_pubmed_pmc | Virtual Biomarkers and Simplified Metrics in the Modeling of Breast Cancer Neoadjuvant Therapy: A Proof-of-Concept Case Study Based on Diagnostic Imaging | Virtual Biomarkers and Simplified Metrics in the Modeling of Breast Cancer Neoadjuvant Therapy: A Proof-of-Concept Case Study Based on Diagnostic Imaging Abstract Abstract Background: Neoadjuvant chemotherapy (NAC) is a standard preoperative intervention for early-stage breast cancer (BC). Dynamic contrast-enhanced mag... |
PMC9463470 | core_pubmed_pmc | Enzyme-linked immunosorbent assays for quantification of MMAE-conjugated ADCs and total antibodies in cynomolgus monkey sera | Enzyme-linked immunosorbent assays for quantification of MMAE-conjugated ADCs and total antibodies in cynomolgus monkey sera Abstract Abstract Antibody-drug conjugates (ADCs) are commonly heterogeneous and require extensive assessment of exposure-efficacy and exposure-safety relationships in preclinical and clinical st... |
PMC11273741 | core_pubmed_pmc | Development and ELISA Characterization of Antibodies against the Colistin, Vancomycin, Daptomycin, and Meropenem: A Therapeutic Drug Monitoring Approach | Development and ELISA Characterization of Antibodies against the Colistin, Vancomycin, Daptomycin, and Meropenem: A Therapeutic Drug Monitoring Approach Abstract More than 70% of bacteria are resistant to all or nearly all known antimicrobials, creating the need for the development of new types of antimicrobials or the... |
PMC7926796 | core_pubmed_pmc | Utilisation of Chick Embryo Chorioallantoic Membrane as a Model Platform for Imaging-Navigated Biomedical Research | Utilisation of Chick Embryo Chorioallantoic Membrane as a Model Platform for Imaging-Navigated Biomedical Research Abstract Abstract The fertilised chick egg and particularly its chorioallantoic membrane (CAM) have drawn continuing interest in biomedicine and bioengineering fields, especially for research on vascular s... |
PMC4406960 | core_pubmed_pmc | Mixed Effects Modeling Using Stochastic Differential Equations: Illustrated by Pharmacokinetic Data of Nicotinic Acid in Obese Zucker Rats | Mixed Effects Modeling Using Stochastic Differential Equations: Illustrated by Pharmacokinetic Data of Nicotinic Acid in Obese Zucker Rats Abstract Abstract Inclusion of stochastic differential equations in mixed effects models provides means to quantify and distinguish three sources of variability in data. In addition... |
PMC6485087 | core_pubmed_pmc | Association between vancomycin pharmacokinetic/pharmacodynamic parameters, patient characteristics, and mortality in patients with bacteremia caused by vancomycin-susceptible Enterococcus faecium : a single-center retrospective study | Association between vancomycin pharmacokinetic/pharmacodynamic parameters, patient characteristics, and mortality in patients with bacteremia caused by vancomycin-susceptible Enterococcus faecium : a single-center retrospective study Abstract Abstract Background Vancomycin is commonly used to treat Enterococcus faecium... |
PMC9483622 | core_pubmed_pmc | Citrus aurantium ‘Changshan-huyou’—An ethnopharmacological and phytochemical review | Citrus aurantium ‘Changshan-huyou’—An ethnopharmacological and phytochemical review Abstract Abstract Citrus fruits are composed of oil cells layer, white membrane layer, pulp and seeds. The cultivar Citrus aurantium ‘Changshan-huyou’ (CACH) is a hybridization of Citrus grandis Osbeck and C. sinensis Osbeck. It is a ru... |
PMC12941221 | core_pubmed_pmc | Association of PFAS, Metals, Phthalate and Organophosphate Metabolites with Depression Among U.S. Adults | Association of PFAS, Metals, Phthalate and Organophosphate Metabolites with Depression Among U.S. Adults Abstract Highlights Public health relevance—How does this work relate to a public health issue? Depression is a major public health concern, and this study evaluates whether exposure to common environmental chemical... |
PMC6220789 | core_pubmed_pmc | Duvelisib, an oral dual PI3K‐δ, γ inhibitor, shows clinical activity in indolent non‐Hodgkin lymphoma in a phase 1 study | Duvelisib, an oral dual PI3K‐δ, γ inhibitor, shows clinical activity in indolent non‐Hodgkin lymphoma in a phase 1 study Abstract Abstract Duvelisib (IPI‐145) is an oral dual inhibitor of phosphoinositide‐3‐kinase (PI3K)‐δ and ‐γ in clinical development for the treatment of hematologic malignancies, including indolent ... |
PMC9606564 | core_pubmed_pmc | Can Faster Aspart Be Used to Optimize Glycemic Control With Insulin Pump Therapy? From Expectations to Lessons Learned After a Year of Use in the United States | Can Faster Aspart Be Used to Optimize Glycemic Control With Insulin Pump Therapy? From Expectations to Lessons Learned After a Year of Use in the United States Abstract Fast-acting insulin aspart (faster aspart) is an ultra-rapid-acting formulation of insulin aspart developed to more closely match the prandial endogeno... |
PMC9968170 | core_pubmed_pmc | Interplay of Breast Cancer Resistance Protein (Bcrp/Abcg2), Sex, and Fed State in Oral Pharmacokinetic Variability of Furosemide in Rats | Interplay of Breast Cancer Resistance Protein (Bcrp/Abcg2), Sex, and Fed State in Oral Pharmacokinetic Variability of Furosemide in Rats Abstract Poor and variable oral bioavailability of furosemide (FUR) presents critical challenges in pharmacotherapy. We investigated the interplay of breast cancer resistance protein ... |
PMC9878197 | core_pubmed_pmc | Population pharmacokinetics of nadroparin for thromboprophylaxis in COVID‐19 intensive care unit patients | Population pharmacokinetics of nadroparin for thromboprophylaxis in COVID‐19 intensive care unit patients Abstract Aims Nadroparin is administered to COVID‐19 intensive care unit (ICU) patients as thromboprophylaxis. Despite existing population pharmacokinetic (PK) models for nadroparin in literature, the population PK... |
PMC11357215 | core_pubmed_pmc | Impact of Probiotics on the Glycemic Control of Pediatric and Adolescent Individuals with Type 1 Diabetes: A Systematic Review and Meta-Analysis | Impact of Probiotics on the Glycemic Control of Pediatric and Adolescent Individuals with Type 1 Diabetes: A Systematic Review and Meta-Analysis Abstract Abstract Aims: Human recombinant insulin is currently the only therapy for children and adolescents with type 1 diabetes (T1D), although not always efficient for the ... |
PMC12858804 | core_pubmed_pmc | Rational design of cisplatin and carboplatin complexes for enhanced anticancer efficacy based on DFT QTAIM and docking analyses | Rational design of cisplatin and carboplatin complexes for enhanced anticancer efficacy based on DFT QTAIM and docking analyses Abstract Abstract Cisplatin (CP) and carboplatin (CBP), two key platinum‑based anticancer drugs, face clinical limitations that prompt the search for new strategies to enhance efficacy and red... |
PMC8212712 | core_pubmed_pmc | Early Clinical Experience With AZD4831, A Novel Myeloperoxidase Inhibitor, Developed for Patients With Heart Failure With Preserved Ejection Fraction | Early Clinical Experience With AZD4831, A Novel Myeloperoxidase Inhibitor, Developed for Patients With Heart Failure With Preserved Ejection Fraction Abstract Abstract We evaluated safety, tolerability, pharmacokinetics (PKs), and pharmacodynamics of AZD4831, a novel oral myeloperoxidase (MPO) inhibitor, in a randomize... |
PMC6017899 | core_pubmed_pmc | Quantitative Analysis of Four Catechins from Green Tea Extract in Human Plasma Using Ultra-Performance Liquid Chromatography-Tandem Mass Spectrometry for Pharmacokinetic Studies | Quantitative Analysis of Four Catechins from Green Tea Extract in Human Plasma Using Ultra-Performance Liquid Chromatography-Tandem Mass Spectrometry for Pharmacokinetic Studies Abstract Green tea is consumed as a beverage worldwide and has beneficial effects, such as a lower risk of cardiovascular disease and cancer. ... |
PMC3790178 | core_pubmed_pmc | The interaction between prognostic and pharmacodynamic biomarkers | The interaction between prognostic and pharmacodynamic biomarkers Abstract Abstract Background: Interactions between prognostic and pharmacodynamic (PD) biomarkers have received little attention. Methods: Prognostic and PD utilities were assessed with linear mixed-effects models using published data on repeated measure... |
PMC10027063 | core_pubmed_pmc | PhysiPKPD: A pharmacokinetics and pharmacodynamics module for PhysiCell | PhysiPKPD: A pharmacokinetics and pharmacodynamics module for PhysiCell Abstract Abstract Pharmacokinetics and pharmacodynamics (PKPD) are key considerations in any study of molecular therapies. It is thus imperative to factor their effects into any in silico model of biological tissue involving such therapies. Further... |
PMC12633374 | core_pubmed_pmc | In Silico Post-screening of Anti-polymerization Agents to Treat Sickle Cell Disease | In Silico Post-screening of Anti-polymerization Agents to Treat Sickle Cell Disease Abstract Sickle cell disease (SCD) is a genetic disorder that affects approximately 100,000 individuals in the United States and millions globally. Although curative therapies, such as stem cell transplant and gene therapy, are availabl... |
PMC11304681 | core_pubmed_pmc | Thorough QT/QTc study to evaluate the effect of a single supratherapeutic dose of islatravir on QTc interval prolongation in healthy adults | Thorough QT/QTc study to evaluate the effect of a single supratherapeutic dose of islatravir on QTc interval prolongation in healthy adults Abstract ABSTRACT Islatravir is a deoxynucleoside analog being developed for the treatment of HIV-1 infection. Clinical studies are being conducted to evaluate islatravir, administ... |
PMC8648050 | core_pubmed_pmc | Synthesis and structure-activity relationship study of new biaryl amide derivatives and their inhibitory effects against hepatitis C virus | Synthesis and structure-activity relationship study of new biaryl amide derivatives and their inhibitory effects against hepatitis C virus Abstract Abstract A series of novel biaryl amide derivatives were synthesized and evaluated for anti-HCV virus activity. Some significant SARs were uncovered. The intensive structur... |
PMC11311774 | core_pubmed_pmc | An Injury-like Signature of the Extracellular Glioma Metabolome | An Injury-like Signature of the Extracellular Glioma Metabolome Abstract Simple Summary In this study, we performed microdialysis in patient-derived xenografts of glioma, intending to evaluate the extracellular metabolic impacts of temozolomide, a component of standard-of-care treatment. Unexpectedly, the most striking... |
PMC10406176 | core_pubmed_pmc | A Phase I Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of Novel Intravenous Formulation of Meloxicam (QP001) in Healthy Chinese Subjects | A Phase I Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of Novel Intravenous Formulation of Meloxicam (QP001) in Healthy Chinese Subjects Abstract Background Meloxicam is a selective cyclooxygenase-2 inhibitor used for pain relief, but its poor solubility limits its clinical applications. QP001 is a ... |
PMC7754455 | core_pubmed_pmc | An Adaptive Physiologically Based Pharmacokinetic–Driven Design to Investigate the Effect of Itraconazole and Rifampicin on the Pharmacokinetics of Molibresib (GSK525762) in Healthy Female Volunteers | An Adaptive Physiologically Based Pharmacokinetic–Driven Design to Investigate the Effect of Itraconazole and Rifampicin on the Pharmacokinetics of Molibresib (GSK525762) in Healthy Female Volunteers Abstract Abstract Molibresib (GSK525762), an orally bioavailable small molecule with 2 major equipotent active metabolit... |
PMC5890728 | core_pubmed_pmc | Improved power for TB Phase IIa trials using a model-based pharmacokinetic–pharmacodynamic approach compared with commonly used analysis methods | Improved power for TB Phase IIa trials using a model-based pharmacokinetic–pharmacodynamic approach compared with commonly used analysis methods Abstract Abstract Background: The demand for new anti-TB drugs is high, but development programmes are long and costly. Consequently there is a need for new strategies capable... |
PMC9426762 | core_pubmed_pmc | Tralesinidase Alfa Enzyme Replacement Therapy Prevents Disease Manifestations in a Canine Model of Mucopolysaccharidosis Type IIIB | Tralesinidase Alfa Enzyme Replacement Therapy Prevents Disease Manifestations in a Canine Model of Mucopolysaccharidosis Type IIIB Abstract Mucopolysaccharidosis type IIIB (MPS IIIB; Sanfilippo syndrome B; OMIM #252920) is a lethal, pediatric, neuropathic, autosomal recessive, and lysosomal storage disease with no appr... |
PMC12146532 | core_pubmed_pmc | First-in-human study of FAZ053, an anti-programmed death-ligand 1 (anti-PD-L1) monoclonal antibody, alone and in combination with spartalizumab, in patients with advanced malignancies | First-in-human study of FAZ053, an anti-programmed death-ligand 1 (anti-PD-L1) monoclonal antibody, alone and in combination with spartalizumab, in patients with advanced malignancies Abstract Abstract Background FAZ053 triggers an antitumor response by targeting programmed death-ligand 1 (PD-L1), thereby activating ef... |
PMC9563210 | core_pubmed_pmc | Subcutaneous injection of trastuzumab into the thigh versus abdominal wall in patients with HER2-positive early breast cancer: Pharmacokinetic, safety and patients' preference - Substudy of the randomised phase III GAIN-2 study | Subcutaneous injection of trastuzumab into the thigh versus abdominal wall in patients with HER2-positive early breast cancer: Pharmacokinetic, safety and patients' preference - Substudy of the randomised phase III GAIN-2 study Abstract Background Trastuzumab given intravenously in combination with chemotherapy is stan... |
PMC8664889 | core_pubmed_pmc | Dopamine dysfunction in stimulant-use disorders: Mechanistic comparisons and implications for treatment | Dopamine dysfunction in stimulant-use disorders: Mechanistic comparisons and implications for treatment Abstract Dopamine system deficiencies and associated behavioral phenotypes may be a critical barrier to success in treating stimulant use disorders. Similarities in dopamine dysfunction between cocaine and methamphet... |
PMC6194777 | core_pubmed_pmc | Rhenium-188 Hydroxyethane 1,1-Diphosphonic Acid (HEDP) for Bone Pain Palliation Using BARC-HEDP Kits versus Pars-HEDP Kits: A Comparison on Preparation and Performance Aspects at Hospital Radiopharmacy | Rhenium-188 Hydroxyethane 1,1-Diphosphonic Acid (HEDP) for Bone Pain Palliation Using BARC-HEDP Kits versus Pars-HEDP Kits: A Comparison on Preparation and Performance Aspects at Hospital Radiopharmacy Abstract Purpose of the Study: Rhenium-188 hydroxyethane 1,1-diphosphonic acid (HEDP) is a clinically established radi... |
PMC12888459 | core_pubmed_pmc | Interpretation of the efficacy-oriented components of decoction pieces in compounds based on the spectrum-effect relationship: Huangqin Qingfei decoction as an example | Interpretation of the efficacy-oriented components of decoction pieces in compounds based on the spectrum-effect relationship: Huangqin Qingfei decoction as an example Abstract Abstract Background Acute lung injury (ALI) is a severe respiratory inflammatory disorder with high morbidity and mortality. Huangqin Qingfei D... |
PMC10811527 | core_pubmed_pmc | PEGylated porcine–human recombinant uricase: A novel fusion protein with improved efficacy and safety for the treatment of hyperuricemia and renal complications | PEGylated porcine–human recombinant uricase: A novel fusion protein with improved efficacy and safety for the treatment of hyperuricemia and renal complications Abstract Abstract The growing prevalence of hyperuricemia necessitates the urgent development of more potent treatments. This study aimed to develop, optimize,... |
PMC5494186 | core_pubmed_pmc | Oral contraceptives cause evolutionarily novel increases in hormone exposure | Oral contraceptives cause evolutionarily novel increases in hormone exposure Abstract Abstract Background and objectives In the evolutionary past, women spent most of their reproductive lives either pregnant or in lactational amenorrhea, and rarely menstruated. The current pattern of frequent menses, and the associated... |
PMC6875516 | core_pubmed_pmc | Totality of Scientific Evidence in the Development of ABP 980, a Biosimilar to Trastuzumab | Totality of Scientific Evidence in the Development of ABP 980, a Biosimilar to Trastuzumab Abstract Abstract ABP 980 was developed as a biosimilar to trastuzumab, a monoclonal antibody targeting human epidermal growth factor receptor 2 (HER2), that is indicated for the treatment of HER2-positive metastatic breast cance... |
PMC12807933 | core_pubmed_pmc | A network meta-analysis of first-line treatment options for patients with Child-Pugh class B functional hepatocellular carcinoma: comparison of efficacy and safety | A network meta-analysis of first-line treatment options for patients with Child-Pugh class B functional hepatocellular carcinoma: comparison of efficacy and safety Abstract Introduction Management of patients with advanced hepatocellular carcinoma (HCC) and Child-Pugh class B liver function is challenging owing to comp... |
PMC5069304 | core_pubmed_pmc | Liraglutide 3.0 mg for Weight Management: A Population Pharmacokinetic Analysis | Liraglutide 3.0 mg for Weight Management: A Population Pharmacokinetic Analysis Abstract Abstract Background and Objectives This analysis used a population pharmacokinetic approach to identify covariates that influence plasma exposure of liraglutide 3.0 mg, a glucagon-like peptide-1 (GLP-1) receptor agonist approved fo... |
PMC10972361 | core_pubmed_pmc | Metaphedrone (3-Methylmethcathinone): Pharmacological, Clinical, and Toxicological Profile | Metaphedrone (3-Methylmethcathinone): Pharmacological, Clinical, and Toxicological Profile Abstract Abstract Introduction: Synthetic cathinones are a group of novel psychoactive substances used as an alternative to classical recreational drugs. As a result of legal prohibitions on older generations of these compounds, ... |
PMC11888825 | core_pubmed_pmc | Dosing, Toxicity and Drug Concentrations for Ganciclovir/Valganciclovir in Preterm and Low Birthweight Infants Treated for Cytomegalovirus | Dosing, Toxicity and Drug Concentrations for Ganciclovir/Valganciclovir in Preterm and Low Birthweight Infants Treated for Cytomegalovirus Abstract Background: There is a lack of data regarding suitable dosage when administering intravenous ganciclovir (GCV) or oral valganciclovir (valGCV) to preterm and low birthweigh... |
PMC9283351 | core_pubmed_pmc | Applying pharmacokinetic/pharmacodynamic measurements for linezolid in critically ill patients: optimizing efficacy and reducing resistance occurrence | Applying pharmacokinetic/pharmacodynamic measurements for linezolid in critically ill patients: optimizing efficacy and reducing resistance occurrence Abstract Purpose Linezolid (LZD) levels are frequently insufficient in intensive care unit (ICU) patients receiving standard dose, which is predictive of a poor prognosi... |
PMC6890583 | core_pubmed_pmc | A Bottom-Up Whole-Body Physiologically Based Pharmacokinetic Model to Mechanistically Predict Tissue Distribution and the Rate of Subcutaneous Absorption of Therapeutic Proteins | A Bottom-Up Whole-Body Physiologically Based Pharmacokinetic Model to Mechanistically Predict Tissue Distribution and the Rate of Subcutaneous Absorption of Therapeutic Proteins Abstract The ability to predict subcutaneous (SC) absorption rate and tissue distribution of therapeutic proteins (TPs) using a bottom-up appr... |
PMC3895279 | core_pubmed_pmc | Chemoembolization of Hepatocellular Carcinoma with Hepasphere 30–60 μm. Safety and Efficacy Study | Chemoembolization of Hepatocellular Carcinoma with Hepasphere 30–60 μm. Safety and Efficacy Study Abstract Abstract Background This study examined the safety, pharmacokinetics, and efficacy of transarterial chemoembolization of hepatocellular carcinoma (HCC) using a newly developed size of a superabsorbent polymer drug... |
PMC6071545 | core_pubmed_pmc | Optimal Regimens and Cutoff Evaluation of Tildipirosin Against Pasteurella multocida | Optimal Regimens and Cutoff Evaluation of Tildipirosin Against Pasteurella multocida Abstract Abstract Pasteurella multocida (PM) can invade the upper respiratory tract of the body and cause death and high morbidity. Tildipirosin, a new 16-membered-ring macrolide antimicrobial, has been recommended for the treatment of... |
PMC9320266 | core_pubmed_pmc | Systematic Comparison of Hospital-Wide Standard and Model-Based Therapeutic Drug Monitoring of Vancomycin in Adults | Systematic Comparison of Hospital-Wide Standard and Model-Based Therapeutic Drug Monitoring of Vancomycin in Adults Abstract Abstract We aimed to evaluate the predictive performance and predicted doses of a single-model approach or several multi-model approaches compared with the standard therapeutic drug monitoring (T... |
PMC3171673 | core_pubmed_pmc | Phase II study of sunitinib as second-line treatment for advanced gastric cancer | Phase II study of sunitinib as second-line treatment for advanced gastric cancer Abstract Summary Purpose. This phase II, open-label, multicenter study assessed the oral, multitargeted, tyrosine kinase inhibitor sunitinib in patients with advanced gastric or gastroesophageal junction adenocarcinoma who had received pri... |
PMC11649425 | core_pubmed_pmc | Global research trends in therapeutic drug monitoring of antimicrobials from 2000 to 2023: a bibliometric analysis | Global research trends in therapeutic drug monitoring of antimicrobials from 2000 to 2023: a bibliometric analysis Abstract Abstract Objective The practice of therapeutic drug monitoring (TDM) is widely used for maximizing the clinical efficacy of antimicrobials. However, a systematic bibliometric analysis providing an... |
PMC11768776 | core_pubmed_pmc | The Clinical Pharmacokinetics and Pharmacodynamics of Glimepiride—A Systematic Review and Meta-Analysis | The Clinical Pharmacokinetics and Pharmacodynamics of Glimepiride—A Systematic Review and Meta-Analysis Abstract Background/Objectives: Glimepiride (GLM), a commonly used sulphonylurea drug for the management of type 2 diabetes mellitus (T2DM), has been the subject of numerous studies exploring its kinetic behaviors. H... |
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