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PMC5833910 | core_pubmed_pmc | Comparison of the Pharmacokinetics of Droxidopa After Dosing in the Fed Versus Fasted State and with 3-Times-Daily Dosing in Healthy Elderly Subjects | Comparison of the Pharmacokinetics of Droxidopa After Dosing in the Fed Versus Fasted State and with 3-Times-Daily Dosing in Healthy Elderly Subjects Abstract Abstract Background Droxidopa is an oral prodrug of norepinephrine approved for the treatment of symptomatic neurogenic orthostatic hypotension. This two-part, r... |
PMC6815754 | core_pubmed_pmc | Single-Use Autoinjector Functionality And Reliability For At-Home Administration Of Benralizumab For Patients With Severe Asthma: GRECO Trial Results | Single-Use Autoinjector Functionality And Reliability For At-Home Administration Of Benralizumab For Patients With Severe Asthma: GRECO Trial Results Abstract Abstract Purpose Accessorized prefilled syringes (APFS) have demonstrated functionality and reliability for subcutaneous (SC) delivery, including self-administra... |
PMC11393952 | core_pubmed_pmc | Pharmacokinetic Pattern of Menbutone in Calves after Single Intravenous and Intramuscular Administration | Pharmacokinetic Pattern of Menbutone in Calves after Single Intravenous and Intramuscular Administration Abstract Abstract Simple Summary Menbutone is a drug that increases hepato-digestive secretions and has been used for more than 50 years in Europe to treat a wide number of digestive disorders in livestock and dogs.... |
PMC9411795 | core_pubmed_pmc | A multidimensional metabolomics workflow to image biodistribution and evaluate pharmacodynamics in adult zebrafish | A multidimensional metabolomics workflow to image biodistribution and evaluate pharmacodynamics in adult zebrafish Abstract ABSTRACT An integrated evaluation of the tissue distribution and pharmacodynamic properties of a therapeutic is essential for successful translation to the clinic. To date, however, cost-effective... |
PMC6572242 | core_pubmed_pmc | Ocular Biodistribution Studies Using Molecular Imaging | Ocular Biodistribution Studies Using Molecular Imaging Abstract Abstract Classical methodologies used in ocular pharmacokinetics studies have difficulties to obtain information about topical and intraocular distribution and clearance of drugs and formulations. This is associated with multiple factors related to ophthal... |
PMC3415310 | core_pubmed_pmc | Posiphen as a candidate drug to lower CSF amyloid precursor protein, amyloid-β peptide and τ levels: target engagement, tolerability and pharmacokinetics in humans | Posiphen as a candidate drug to lower CSF amyloid precursor protein, amyloid-β peptide and τ levels: target engagement, tolerability and pharmacokinetics in humans Abstract Abstract Aim A first in human study to evaluate tolerability and pharmacokinetics followed by an early proof of mechanism (POM) study to determine ... |
PMC12719615 | core_pubmed_pmc | Screening the Active Phytochemicals From Eclipta prostrata and Unraveling Their Molecular Insight Into Human Malignancies | Screening the Active Phytochemicals From Eclipta prostrata and Unraveling Their Molecular Insight Into Human Malignancies Abstract ABSTRACT Current drugs against multiple human malignancies are limited, and developing new treatment strategies is improbable within a short time. So, considering the current situation, phy... |
PMC3052269 | core_pubmed_pmc | Methods Development for Blood Borne Macrophage Carriage of Nanoformulated Antiretroviral Drugs | Methods Development for Blood Borne Macrophage Carriage of Nanoformulated Antiretroviral Drugs Abstract Abstract Nanoformulated drugs can improve pharmacodynamics and bioavailability while serving also to reduce drug toxicities for antiretroviral (ART) medicines. To this end, our laboratory has applied the principles o... |
PMC12619193 | core_pubmed_pmc | Severe myocardium suppression in two congenital heart disease patients after remdesivir use – a case report | Severe myocardium suppression in two congenital heart disease patients after remdesivir use – a case report Abstract Abstract Background Remdesivir, the first FDA-approved antiviral for SARS-CoV-2, has shown clinical benefits in early COVID-19 but is associated with cardiac adverse events. Experimental studies indicate... |
PMC5955975 | core_pubmed_pmc | Discovery of a novel IL-15 based protein with improved developability and efficacy for cancer immunotherapy | Discovery of a novel IL-15 based protein with improved developability and efficacy for cancer immunotherapy Abstract Interleukin-15 (IL-15) can promote both innate and adaptive immune reactions by stimulating CD8 + /CD4 + T cells and natural killer cells (NK) while showing no effect in activating T-regulatory (Treg) ce... |
PMC12158826 | core_pubmed_pmc | Regulatory and Industry Perspective on the Model Master File Framework for Locally Acting Drug Products | Regulatory and Industry Perspective on the Model Master File Framework for Locally Acting Drug Products Abstract Graphical Abstract Modeling EMA Experience with Qualification of Modelling and Simulation Methods Flora Musuamba, PhD University of Namur; Belgian FAMHP To provide global context on the proposed use of MMFs,... |
PMC5004159 | core_pubmed_pmc | Circulating intestine-derived exosomal miR-328 in plasma, a possible biomarker for estimating BCRP function in the human intestines | Circulating intestine-derived exosomal miR-328 in plasma, a possible biomarker for estimating BCRP function in the human intestines Abstract Abstract A variant in the breast cancer resistance protein (BCRP) gene, 421C> A is a useful biomarker for describing large inter-individual differences in the pharmacokinetics of ... |
PMC12202197 | core_pubmed_pmc | Examining the Impact of Diet‐and‐Exercise‐Induced Weight Loss on Drug Metabolism and Gastric Emptying in Patients with Obesity | Examining the Impact of Diet‐and‐Exercise‐Induced Weight Loss on Drug Metabolism and Gastric Emptying in Patients with Obesity Abstract Abstract Obesity significantly influences drug pharmacokinetics (PK), which challenges optimal dosing. This study examines the effects of diet‐and‐exercise‐induced weight loss on key d... |
PMC4499424 | core_pubmed_pmc | A Simple and Sensitive HPLC Method for Fluorescence Quantitation of Doxorubicin in Micro-volume Plasma: Applications to Pharmacokinetic Studies in Rats | A Simple and Sensitive HPLC Method for Fluorescence Quantitation of Doxorubicin in Micro-volume Plasma: Applications to Pharmacokinetic Studies in Rats Abstract Abstract A validated HPLC method was developed to determine the doxorubicin concentration in a small volume of rat plasma (60 µL) with convenient fluorescence ... |
PMC6402191 | core_pubmed_pmc | Prediction of Transporter‐Mediated Drug‐Drug Interactions for Baricitinib | Prediction of Transporter‐Mediated Drug‐Drug Interactions for Baricitinib Abstract Abstract Baricitinib, an oral selective Janus kinase 1 and 2 inhibitor, undergoes active renal tubular secretion. Baricitinib was not predicted to inhibit hepatic and renal uptake and efflux drug transporters, based on the ratio of the u... |
PMC10684372 | core_pubmed_pmc | Plasma-derived C1 esterase inhibitor pharmacokinetics and safety in patients with hereditary angioedema | Plasma-derived C1 esterase inhibitor pharmacokinetics and safety in patients with hereditary angioedema Abstract Background Over 40 years of use demonstrates that complement 1 esterase inhibitor (C1-INH) concentrate is effective and well tolerated for acute edema attacks and prophylaxis in patients with hereditary angi... |
PMC9464066 | core_pubmed_pmc | Tenofovir Alafenamide Plasma Concentrations Are Reduced in Pregnant Women Living With Human Immunodeficiency Virus (HIV): Data From the PANNA Network | Tenofovir Alafenamide Plasma Concentrations Are Reduced in Pregnant Women Living With Human Immunodeficiency Virus (HIV): Data From the PANNA Network Abstract Abstract Background Tenofovir alafenamide (TAF), a prodrug of tenofovir (TFV), is included in the majority of the recommended first-line antiretroviral regimens ... |
PMC8371347 | core_pubmed_pmc | Subcutaneous engineered factor VIIa marzeptacog alfa (activated) in hemophilia with inhibitors: Phase 2 trial of pharmacokinetics, pharmacodynamics, efficacy, and safety | Subcutaneous engineered factor VIIa marzeptacog alfa (activated) in hemophilia with inhibitors: Phase 2 trial of pharmacokinetics, pharmacodynamics, efficacy, and safety Abstract Abstract Background Marzeptacog alfa (activated) (MarzAA), a novel recombinant activated human factor VII (FVIIa) variant, was developed to p... |
PMC8004065 | core_pubmed_pmc | Determination of Pharmacokinetic and Pharmacokinetic-Pharmacodynamic Parameters of Doxycycline against Edwardsiella ictaluri in Yellow Catfish ( Pelteobagrus fulvidraco ) | Determination of Pharmacokinetic and Pharmacokinetic-Pharmacodynamic Parameters of Doxycycline against Edwardsiella ictaluri in Yellow Catfish ( Pelteobagrus fulvidraco ) Abstract Abstract This study aimed to examine the pharmacokinetics of doxycycline (DC) in yellow catfish ( Pelteobagrus fulvidraco ) and to calculate... |
PMC7656302 | core_pubmed_pmc | SFCE-RAPIRI Phase I Study of Rapamycin Plus Irinotecan: A New Way to Target Intra-Tumor Hypoxia in Pediatric Refractory Cancers | SFCE-RAPIRI Phase I Study of Rapamycin Plus Irinotecan: A New Way to Target Intra-Tumor Hypoxia in Pediatric Refractory Cancers Abstract Abstract Simple Summary More and more relapsing or refractory pediatric cancers are described to present hypoxic features linked to a worse outcome. Therefore, the aim of our phase I ... |
PMC5484509 | core_pubmed_pmc | Intranasal agomelatine solid lipid nanoparticles to enhance brain delivery: formulation, optimization and in vivo pharmacokinetics | Intranasal agomelatine solid lipid nanoparticles to enhance brain delivery: formulation, optimization and in vivo pharmacokinetics Abstract Purpose Agomelatine is a novel antidepressant drug suffering from an extensive first-pass metabolism leading to a diminished absolute bioavailability. The aim of the study is: firs... |
PMC8728392 | core_pubmed_pmc | Synthesis, Anticancer Assessment, and Molecular Docking of Novel Chalcone-Thienopyrimidine Derivatives in HepG2 and MCF-7 Cell Lines | Synthesis, Anticancer Assessment, and Molecular Docking of Novel Chalcone-Thienopyrimidine Derivatives in HepG2 and MCF-7 Cell Lines Abstract Abstract Heterocycles containing thienopyrimidine moieties have attracted attention due to their interesting biological and pharmacological activities. In this research article, ... |
PMC11002075 | core_pubmed_pmc | Adaptative Strategy of Immunosuppressive Drugs Dosage Adjustments When Combined With Nirmatrelvir/Ritonavir in Solid Organ Transplant Recipients With COVID-19 | Adaptative Strategy of Immunosuppressive Drugs Dosage Adjustments When Combined With Nirmatrelvir/Ritonavir in Solid Organ Transplant Recipients With COVID-19 Abstract Abstract Nirmatrelvir/ritonavir is a promising option for preventing severe COVID-19 in solid organ transplant recipients with SARS-CoV-2 infection. How... |
PMC10024496 | core_pubmed_pmc | Personalized Dose of Adjuvant Imatinib in Patients with Gastrointestinal Stromal Tumors: Results from a Population Pharmacokinetic Analysis | Personalized Dose of Adjuvant Imatinib in Patients with Gastrointestinal Stromal Tumors: Results from a Population Pharmacokinetic Analysis Abstract Abstract Purpose Imatinib is the first-line treatment for patients with gastrointestinal stromal tumors (GIST) after surgery. However, its pharmacokinetic profile varies r... |
PMC7006881 | core_pubmed_pmc | Exposure–Response Relationships for Efficacy and Safety of Risankizumab in Phase II and III Trials in Psoriasis Patients | Exposure–Response Relationships for Efficacy and Safety of Risankizumab in Phase II and III Trials in Psoriasis Patients Abstract Abstract Risankizumab has demonstrated efficacy in phase III trials in patients with moderate‐to‐severe plaque psoriasis. The exposure–response relationships for risankizumab efficacy (Psori... |
PMC3167660 | core_pubmed_pmc | Risks associated with melamine and related triazine contamination of food | Risks associated with melamine and related triazine contamination of food Abstract Recent adulteration of milk products with melamine (ME) in several countries caused adverse health effects and even deaths in infants. Earlier, in 2007, contamination of pet food with ME and its related contaminants was associated with m... |
PMC5868852 | core_pubmed_pmc | Comparative pharmacokinetics and safety assessment of transdermal berberine and dihydroberberine | Comparative pharmacokinetics and safety assessment of transdermal berberine and dihydroberberine Abstract The natural alkaloid berberine has been ascribed numerous health benefits including lipid and cholesterol reduction and improved insulin sensitivity in diabetics. However, oral (PO) administration of berberine is h... |
PMC9739780 | core_pubmed_pmc | Pharmacokinetic Comparison of Eight Major Compounds of Lonicerae japonicae flos after Oral Administration in Normal Rats and Rats with Liver Injury | Pharmacokinetic Comparison of Eight Major Compounds of Lonicerae japonicae flos after Oral Administration in Normal Rats and Rats with Liver Injury Abstract Traditional Chinese medicine considers Lonicerae japonicae flos to have antibacterial detoxification, liver protection, and gallbladder protection. At present, stu... |
PMC4023753 | core_pubmed_pmc | Population Pharmacokinetic Assessment of the Effect of Food on Piperaquine Bioavailability in Patients with Uncomplicated Malaria | Population Pharmacokinetic Assessment of the Effect of Food on Piperaquine Bioavailability in Patients with Uncomplicated Malaria Abstract Previously published literature reports various impacts of food on the oral bioavailability of piperaquine. The aim of this study was to use a population modeling approach to invest... |
PMC8347723 | core_pubmed_pmc | The Course of AαVal541 as a Proteinase 3 Specific Neo-Epitope after Alpha-1-Antitrypsin Augmentation in Severe Deficient Patients | The Course of AαVal541 as a Proteinase 3 Specific Neo-Epitope after Alpha-1-Antitrypsin Augmentation in Severe Deficient Patients Abstract In alpha-1-antitrypsin deficiency (AATD), neutrophil serine proteases such as elastase and proteinase 3 (PR3) are insufficiently inhibited. A previous study in AATD patients showed ... |
PMC12678841 | core_pubmed_pmc | Safety, Tolerability, and Pharmacokinetics of a Novel Nitroimidazooxazole Antitubercular Agent in Healthy Adults: A Phase I Trial | Safety, Tolerability, and Pharmacokinetics of a Novel Nitroimidazooxazole Antitubercular Agent in Healthy Adults: A Phase I Trial Abstract ABSTRACT This study evaluated the safety, tolerability, and pharmacokinetics of JBD0131, a novel nitroimidazooxazole antitubercular agent, in healthy adults. We previously reported ... |
PMC6189379 | core_pubmed_pmc | Population pharmacokinetics of extended‐release levetiracetam in epileptic dogs when administered alone, with phenobarbital or zonisamide | Population pharmacokinetics of extended‐release levetiracetam in epileptic dogs when administered alone, with phenobarbital or zonisamide Abstract Abstract Background Extended‐release levetiracetam (LEV‐XR) has gained acceptance as an antiepileptic drug in dogs. No studies have evaluated its disposition in dogs with ep... |
PMC4590802 | core_pubmed_pmc | The Population Pharmacokinetic Models of Tacrolimus in Chinese Adult Liver Transplantation Patients | The Population Pharmacokinetic Models of Tacrolimus in Chinese Adult Liver Transplantation Patients Abstract Aim . The aim of this study was to establish population pharmacokinetic models of tacrolimus in Chinese adult liver transplantation patients. Methods . Tacrolimus dose and concentration data ( n = 435) were obta... |
PMC11001683 | core_pubmed_pmc | ACD856, a novel positive allosteric modulator of Trk receptors, single ascending doses in healthy subjects: Safety and pharmacokinetics | ACD856, a novel positive allosteric modulator of Trk receptors, single ascending doses in healthy subjects: Safety and pharmacokinetics Abstract Abstract Purpose AlzeCure Pharma AB is developing novel positive allosteric modulators of Trk-receptors for treatment of Alzheimer’s disease, depression, other psychiatric con... |
PMC7611291 | core_pubmed_pmc | Plasma Pharmacokinetics of High-Dose Oral versus Intravenous Rifampicin in Patients with Tuberculous Meningitis: a Randomized Controlled Trial | Plasma Pharmacokinetics of High-Dose Oral versus Intravenous Rifampicin in Patients with Tuberculous Meningitis: a Randomized Controlled Trial Abstract ABSTRACT Higher doses of intravenous rifampicin may improve outcomes in tuberculous meningitis but are impractical in high-burden settings. We hypothesized that plasma ... |
PMC10812395 | core_pubmed_pmc | New Antibiotics for the Treatment of Nosocomial Central Nervous System Infections | New Antibiotics for the Treatment of Nosocomial Central Nervous System Infections Abstract Nosocomial central nervous system (CNS) infections with carbapenem- and colistin-resistant Gram-negative and vancomycin-resistant Gram-positive bacteria are an increasing therapeutic challenge. Here, we review pharmacokinetic and... |
PMC5394527 | core_pubmed_pmc | Discovery of 4-((3′ R ,4′ S ,5′ R )-6″-Chloro-4′-(3-chloro-2-fluorophenyl)-1′-ethyl-2″-oxodispiro[cyclohexane-1,2′-pyrrolidine-3′,3″-indoline]-5′-carboxamido)bicyclo[2.2.2]octane-1-carboxylic Acid (AA-115/APG-115): A Potent and Orally Active Murine Double Minute 2 (MDM2) Inhibitor in Clinical Development | Discovery of 4-((3′ R ,4′ S ,5′ R )-6″-Chloro-4′-(3-chloro-2-fluorophenyl)-1′-ethyl-2″-oxodispiro[cyclohexane-1,2′-pyrrolidine-3′,3″-indoline]-5′-carboxamido)bicyclo[2.2.2]octane-1-carboxylic Acid (AA-115/APG-115): A Potent and Orally Active Murine Double Minute 2 (MDM2) Inhibitor in Clinical Development Abstract We pr... |
PMC4143598 | core_pubmed_pmc | Effect of Rifampicin on the Pharmacokinetics of Lenvatinib in Healthy Adults | Effect of Rifampicin on the Pharmacokinetics of Lenvatinib in Healthy Adults Abstract Background and Objectives Lenvatinib is an oral, multitargeted tyrosine kinase inhibitor under clinical investigation in solid tumours. This study evaluated the influence of P-glycoprotein (P-gp) inhibition (single-dose rifampicin) an... |
PMC4768392 | core_pubmed_pmc | Dose modifications in Asian cancer patients with hepatic dysfunction receiving weekly docetaxel: A prospective pharmacokinetic and safety study | Dose modifications in Asian cancer patients with hepatic dysfunction receiving weekly docetaxel: A prospective pharmacokinetic and safety study Abstract Abstract Hepatic dysfunction may modify the safety profile and pharmacokinetics of docetaxel in cancer patients, but no validated guideline exists to guide dose modifi... |
PMC7547940 | core_pubmed_pmc | Understanding the Clinical Profile of Insulin Degludec, the Latest Basal Insulin Approved for Use in Canada: a Narrative Review | Understanding the Clinical Profile of Insulin Degludec, the Latest Basal Insulin Approved for Use in Canada: a Narrative Review Abstract Abstract In recent years, the development of basal insulin therapies has focused on insulin analogues that have longer durations of action and more predictable pharmacokinetic/pharmac... |
PMC12620829 | core_pubmed_pmc | Towards new approach methodologies for biological therapeutics: a novel model-informed metric to assess immunogenicity risk | Towards new approach methodologies for biological therapeutics: a novel model-informed metric to assess immunogenicity risk Abstract Abstract Immunogenicity poses a significant challenge in biotherapeutics development due to the formation of anti-drug antibodies (ADA), which can alter drug pharmacokinetics (PK) and red... |
PMC7592742 | core_pubmed_pmc | Preclinical evaluation of a next-generation, subcutaneously administered, coagulation factor IX variant, dalcinonacog alfa | Preclinical evaluation of a next-generation, subcutaneously administered, coagulation factor IX variant, dalcinonacog alfa Abstract Abstract Introduction The rapid clearance of factor IX necessitates frequent intravenous administrations to achieve effective prophylaxis for patients with hemophilia B. Subcutaneous admin... |
PMC6963779 | core_pubmed_pmc | Understanding Inter-Individual Variability in Monoclonal Antibody Disposition | Understanding Inter-Individual Variability in Monoclonal Antibody Disposition Abstract Abstract Monoclonal antibodies (mAbs) are currently the largest and most dominant class of therapeutic proteins. Inter-individual variability has been observed for several mAbs; however, an understanding of the underlying mechanisms ... |
PMC11520665 | core_pubmed_pmc | Rezafungin versus caspofungin for patients with candidaemia or invasive candidiasis in the intensive care unit: pooled analyses of the ReSTORE and STRIVE randomised trials | Rezafungin versus caspofungin for patients with candidaemia or invasive candidiasis in the intensive care unit: pooled analyses of the ReSTORE and STRIVE randomised trials Abstract Background Rezafungin is an echinocandin approved in the US and EU to treat candidaemia and/or invasive candidiasis. This post-hoc, pooled ... |
PMC5888114 | core_pubmed_pmc | A Population Pharmacokinetic Model Incorporating Saturable Pharmacokinetics and Autoinduction for High Rifampicin Doses | A Population Pharmacokinetic Model Incorporating Saturable Pharmacokinetics and Autoinduction for High Rifampicin Doses Abstract Accumulating evidence suggests that increasing doses of rifampicin may shorten tuberculosis treatment. The PanACEA HIGHRIF1 trial assessed safety, pharmacokinetics, and antimycobacterial acti... |
PMC4427505 | core_pubmed_pmc | Extraction of Pharmacokinetic Evidence of Drug–Drug Interactions from the Literature | Extraction of Pharmacokinetic Evidence of Drug–Drug Interactions from the Literature Abstract Drug-drug interaction (DDI) is a major cause of morbidity and mortality and a subject of intense scientific interest. Biomedical literature mining can aid DDI research by extracting evidence for large numbers of potential inte... |
PMC8146233 | core_pubmed_pmc | Decorating sdAbs with Chelators: Effect of Conjugation on Biodistribution and Functionality | Decorating sdAbs with Chelators: Effect of Conjugation on Biodistribution and Functionality Abstract Abstract Single domain antibodies (sdAbs) have proven to be valuable probes for molecular imaging. In order to produce such probes, one strategy is the functionalization of the reactive amine side chain of lysines with ... |
PMC9201062 | core_pubmed_pmc | Interactions Between Natural Products and Tamoxifen in Breast Cancer: A Comprehensive Literature Review | Interactions Between Natural Products and Tamoxifen in Breast Cancer: A Comprehensive Literature Review Abstract Abstract Introduction: Tamoxifen (TAM) is the most commonly used hormone therapeutic drug for the treatment of estrogen receptor-positive (ER+) breast cancer. 30%–70% of clinical breast cancer patients use n... |
PMC9439988 | core_pubmed_pmc | Allopregnanolone Concentrations in Breast Milk and Plasma from Healthy Volunteers Receiving Brexanolone Injection, With Population Pharmacokinetic Modeling of Potential Relative Infant Dose | Allopregnanolone Concentrations in Breast Milk and Plasma from Healthy Volunteers Receiving Brexanolone Injection, With Population Pharmacokinetic Modeling of Potential Relative Infant Dose Abstract Abstract Background and Objective Women with postpartum depression (PPD) may expose their infants to antidepressants via ... |
PMC8516195 | core_pubmed_pmc | Evaluation of ceftazidime/avibactam alone and in combination with amikacin, colistin and tigecycline against Klebsiella pneumoniae carbapenemase-producing K . pneumoniae by in vitro time-kill experiment | Evaluation of ceftazidime/avibactam alone and in combination with amikacin, colistin and tigecycline against Klebsiella pneumoniae carbapenemase-producing K . pneumoniae by in vitro time-kill experiment Abstract Abstract Klebsiella pneumoniae carbapenemase-producing K . pneumoniae (KPC-Kp) poses a major threat to human... |
PMC11561648 | core_pubmed_pmc | Preclinical development and characterisation of PP353 , a formulation of linezolid for intradiscal administration | Preclinical development and characterisation of PP353 , a formulation of linezolid for intradiscal administration Abstract Abstract Introduction Bacterial infection of the intervertebral disc can lead to vertebral endplate edema known as Modic changes, with associated chronic low back pain. Oral antimicrobial therapy h... |
PMC12469605 | core_pubmed_pmc | The Impact of Genetic Polymorphisms on the Clinical Efficacy of Azole Antifungals | The Impact of Genetic Polymorphisms on the Clinical Efficacy of Azole Antifungals Abstract Azoles are the primary agents for antifungal activity in clinical medicine due to their broad-spectrum efficacy and favorable safety profiles compared to older agents. Triazoles, including fluconazole, itraconazole, voriconazole,... |
PMC11423908 | core_pubmed_pmc | Plasma and Milk Pharmacokinetics and Estimated Milk Withdrawal Time of Tolfenamic Acid in Lactating Sheep | Plasma and Milk Pharmacokinetics and Estimated Milk Withdrawal Time of Tolfenamic Acid in Lactating Sheep Abstract ABSTRACT Objective This study aimed to investigate the plasma and milk pharmacokinetics, as well as the withdrawal time (WT) from milk of tolfenamic acid (2 and 4 mg/kg) following intravenous (IV) administ... |
PMC8412106 | core_pubmed_pmc | Bedaquiline for multidrug-resistant TB in paediatric patients | Bedaquiline for multidrug-resistant TB in paediatric patients Abstract SUMMARY BACKGROUND: TMC207-C211 ( NCT02354014 ) is a Phase 2, open-label, multicentre, single-arm study to evaluate pharmacokinetics, safety/tolerability, antimycobacterial activity and dose selection of bedaquiline (BDQ) in children (birth to <18 y... |
PMC11359797 | core_pubmed_pmc | Advances in Modeling Approaches for Oral Drug Delivery: Artificial Intelligence, Physiologically-Based Pharmacokinetics, and First-Principles Models | Advances in Modeling Approaches for Oral Drug Delivery: Artificial Intelligence, Physiologically-Based Pharmacokinetics, and First-Principles Models Abstract Oral drug absorption is the primary route for drug administration. However, this process hinges on multiple factors, including the drug’s physicochemical properti... |
PMC7912990 | core_pubmed_pmc | Combination Regimens of Favipiravir Plus Interferon Alpha Inhibit Chikungunya Virus Replication in Clinically Relevant Human Cell Lines | Combination Regimens of Favipiravir Plus Interferon Alpha Inhibit Chikungunya Virus Replication in Clinically Relevant Human Cell Lines Abstract Abstract Chikungunya virus (CHIKV) is an alphavirus associated with a broad tissue tropism for which no antivirals or vaccines are approved. This study evaluated the antiviral... |
PMC12671527 | core_pubmed_pmc | Development of a novel ultrashort antimicrobial peptide-levofloxacin conjugate with enhanced synergistic activity against multidrug and levofloxacin-resistant bacterial isolates | Development of a novel ultrashort antimicrobial peptide-levofloxacin conjugate with enhanced synergistic activity against multidrug and levofloxacin-resistant bacterial isolates Abstract Background and purpose: Antimicrobial resistance poses a significant global health threat. A previously developed penta-amino acid ul... |
PMC10651641 | core_pubmed_pmc | Pharmacokinetics, safety, and tolerability of inhaled remdesivir in healthy participants | Pharmacokinetics, safety, and tolerability of inhaled remdesivir in healthy participants Abstract Abstract Intravenous remdesivir (RDV) is US Food and Drug Administration–approved for hospitalized and nonhospitalized individuals with coronavirus disease 2019. RDV undergoes intracellular metabolic activation to form the... |
PMC4727771 | core_pubmed_pmc | Improved Pharmacokinetics of Aceclofenac Immediate Release Tablets Incorporating its Inclusion Complex with Hydroxypropyl-β-Cyclodextrin | Improved Pharmacokinetics of Aceclofenac Immediate Release Tablets Incorporating its Inclusion Complex with Hydroxypropyl-β-Cyclodextrin Abstract The present investigation reports the various pharmacokinetic parameters of immediate release aceclofenac tablets incorporating its inclusion complex with hydroxypropyl-β-cyc... |
PMC11452715 | core_pubmed_pmc | Pharmacokinetic and pharmacodynamic evaluation of various vasopressin doses and routes of administration in a neonatal piglet model | Pharmacokinetic and pharmacodynamic evaluation of various vasopressin doses and routes of administration in a neonatal piglet model Abstract Abstract Epinephrine is the only recommended vasopressor during neonatal cardiopulmonary resuscitation. However, there are concerns about the potential adverse effects of epinephr... |
PMC11025498 | core_pubmed_pmc | First-in-human Phase I Trial of TPST-1120, an Inhibitor of PPARα, as Monotherapy or in Combination with Nivolumab, in Patients with Advanced Solid Tumors | First-in-human Phase I Trial of TPST-1120, an Inhibitor of PPARα, as Monotherapy or in Combination with Nivolumab, in Patients with Advanced Solid Tumors Abstract Abstract Purpose: TPST-1120 is a first-in-class oral inhibitor of peroxisome proliferator-activated receptor α (PPARα), a fatty acid ligand-activated transcr... |
PMC8184216 | core_pubmed_pmc | Multi-step vs. single-step resistance evolution under different drugs, pharmacokinetics, and treatment regimens | Multi-step vs. single-step resistance evolution under different drugs, pharmacokinetics, and treatment regimens Abstract The success of antimicrobial treatment is threatened by the evolution of drug resistance. Population genetic models are an important tool in mitigating that threat. However, most such models consider... |
PMC6174986 | core_pubmed_pmc | Population Pharmacokinetic Analysis for Daclatasvir and Asunaprevir in Japanese Subjects With Chronic Hepatitis C Virus Infection | Population Pharmacokinetic Analysis for Daclatasvir and Asunaprevir in Japanese Subjects With Chronic Hepatitis C Virus Infection Abstract Abstract Daclatasvir is a nonstructural protein 5A replication complex inhibitor, and asunaprevir is a nonstructural protein 3 protease inhibitor for hepatitis C virus (HCV). In 201... |
PMC12609569 | core_pubmed_pmc | When Nature Meets Oncology: Unraveling Herb–Drug Interactions in Cancer Therapy | When Nature Meets Oncology: Unraveling Herb–Drug Interactions in Cancer Therapy Abstract Natural product (NP) use by patients alongside their conventional cancer therapies is ubiquitous. This common, yet often hidden, practice can potentially contribute to significant patient harm, given the narrow therapeutic window o... |
PMC6901045 | core_pubmed_pmc | In vivo Studies on Pharmacokinetics, Toxicity and Immunogenicity of Polyelectrolyte Nanocapsules Functionalized with Two Different Polymers: Poly-L-Glutamic Acid or PEG | In vivo Studies on Pharmacokinetics, Toxicity and Immunogenicity of Polyelectrolyte Nanocapsules Functionalized with Two Different Polymers: Poly-L-Glutamic Acid or PEG Abstract Background The functionalization of a nanoparticle surface with PEG (polyethylene glycol) is an approach most often used for extending nanomat... |
PMC12775080 | core_pubmed_pmc | Risks encountered when not adjusting for diurnal variation and food effect in QTcF analysis based on phase I data | Risks encountered when not adjusting for diurnal variation and food effect in QTcF analysis based on phase I data Abstract Abstract Phase I single and multiple ascending dose studies are more and more often used to evaluate QT liability of new drugs. However, these studies are not primarily tailored to concentration-QT... |
PMC12802960 | core_pubmed_pmc | β-Lactam dosing in critically ill children: predictors for target non-attainment | β-Lactam dosing in critically ill children: predictors for target non-attainment Abstract Abstract Introduction β-Lactam antibiotics are among the most frequently prescribed antibiotics on the paediatric ICU (PICU). For β-lactam antibiotics, unbound plasma concentrations above at least one to four times the MIC for 100... |
PMC8442631 | core_pubmed_pmc | Radiolabeling and PET–MRI microdosing of the experimental cancer therapeutic, MN-anti-miR10b, demonstrates delivery to metastatic lesions in a murine model of metastatic breast cancer | Radiolabeling and PET–MRI microdosing of the experimental cancer therapeutic, MN-anti-miR10b, demonstrates delivery to metastatic lesions in a murine model of metastatic breast cancer Abstract Background In our earlier work, we identified microRNA-10b (miR10b) as a master regulator of the viability of metastatic tumor ... |
PMC3080921 | core_pubmed_pmc | Similarity of Bisphenol A Pharmacokinetics in Rhesus Monkeys and Mice: Relevance for Human Exposure | Similarity of Bisphenol A Pharmacokinetics in Rhesus Monkeys and Mice: Relevance for Human Exposure Abstract Objective Daily adult human exposure to bisphenol A (BPA) has been estimated at < 1 μg/kg, with virtually complete first-pass conjugation in the liver in primates but not in mice. We measured unconjugated and co... |
PMC11764841 | core_pubmed_pmc | Comparative Pharmacokinetic Analysis of Aflibercept and Brolucizumab in Human Aqueous Humor Using Nano-Surface and Molecular-Orientation Limited Proteolysis | Comparative Pharmacokinetic Analysis of Aflibercept and Brolucizumab in Human Aqueous Humor Using Nano-Surface and Molecular-Orientation Limited Proteolysis Abstract Aflibercept and brolucizumab, two anti-VEGF agents used as intravitreal injections in ophthalmology, differ significantly in molecular weight (aflibercept... |
PMC6454300 | core_pubmed_pmc | Emergency treatment of adrenal crisis with prednisone suppositories: a bioequivalence study in female patients with Addison’s disease | Emergency treatment of adrenal crisis with prednisone suppositories: a bioequivalence study in female patients with Addison’s disease Abstract Abstract Objective Patients with adrenal insufficiency (AI) need to adapt their glucocorticoid replacement under stressful conditions to prevent adrenal crisis (AC). Prednisone ... |
PMC7179444 | core_pubmed_pmc | Liquid Chromatography–Tandem Mass Spectrometry for the Simultaneous Determination of Doxorubicin and its Metabolites Doxorubicinol, Doxorubicinone, Doxorubicinolone, and 7-Deoxydoxorubicinone in Mouse Plasma | Liquid Chromatography–Tandem Mass Spectrometry for the Simultaneous Determination of Doxorubicin and its Metabolites Doxorubicinol, Doxorubicinone, Doxorubicinolone, and 7-Deoxydoxorubicinone in Mouse Plasma Abstract Doxorubicin, an anthracycline antitumor antibiotic, acts as a cancer treatment by interfering with the ... |
PMC12706395 | core_pubmed_pmc | Application of Physiologically‐Based Pharmacokinetic Modeling to Support Drug Labeling: Prediction of CYP3A4 ‐Mediated Pirtobrutinib‐Drug Interactions | Application of Physiologically‐Based Pharmacokinetic Modeling to Support Drug Labeling: Prediction of CYP3A4 ‐Mediated Pirtobrutinib‐Drug Interactions Abstract ABSTRACT Pirtobrutinib is a reversible Bruton tyrosine kinase (BTK) inhibitor. In vitro, pirtobrutinib is metabolized by cytochrome P450 (CYP) 3A4 and uridine 5... |
PMC6377041 | core_pubmed_pmc | Effective vancomycin concentrations in children: a cross-sectional study | Effective vancomycin concentrations in children: a cross-sectional study Abstract ABSTRACT Objective Analyze the microbiological effectiveness, based on the pharmacokinetics/pharmacodynamics correlation of vancomycin in pediatric patients, and to propose dose adjustment. Methods This is an observational, cross-sectiona... |
PMC3671798 | core_pubmed_pmc | Pharmacokinetic drug interaction profile of omeprazole with adverse consequences and clinical risk management | Pharmacokinetic drug interaction profile of omeprazole with adverse consequences and clinical risk management Abstract Background Omeprazole, a proton pump inhibitor (PPI), is widely used for the treatment of dyspepsia, peptic ulcer, gastroesophageal reflux disease, and functional dyspepsia. Polypharmacy is common in p... |
PMC6862422 | core_pubmed_pmc | Transdermal delivery of 4-aminopyridine accelerates motor functional recovery and improves nerve morphology following sciatic nerve crush injury in mice | Transdermal delivery of 4-aminopyridine accelerates motor functional recovery and improves nerve morphology following sciatic nerve crush injury in mice Abstract Abstract Oral 4-aminopyridine (4-AP) is clinically used for symptomatic relief in multiple sclerosis and we recently demonstrated that systemic 4-AP had previ... |
PMC10651648 | core_pubmed_pmc | Model‐informed precision dosing of vancomycin for rapid achievement of target area under the concentration‐time curve: A simulation study | Model‐informed precision dosing of vancomycin for rapid achievement of target area under the concentration‐time curve: A simulation study Abstract Abstract In this study, we aimed to evaluate limited sampling strategies for achieving the therapeutic ranges of the area under the concentration‐time curve (AUC) of vancomy... |
PMC12114986 | core_pubmed_pmc | Use of Computational Intelligence in Customizing Drug Release from 3D-Printed Products: A Comprehensive Review | Use of Computational Intelligence in Customizing Drug Release from 3D-Printed Products: A Comprehensive Review Abstract Computational intelligence (CI) mimics human intelligence by expanding the capabilities of machines in data analysis, pattern recognition, and making informed decisions. CI has shown promising contrib... |
PMC12114635 | core_pubmed_pmc | Pharmacokinetics of Different Tacrolimus Formulations in the Early Post-Liver Transplant Period: A Scoping Review | Pharmacokinetics of Different Tacrolimus Formulations in the Early Post-Liver Transplant Period: A Scoping Review Abstract Abstract Background: Tacrolimus (TAC) is the cornerstone of immunosuppression after liver transplantation (LT). TAC has a narrow therapeutic index and high inter- and intra-individual pharmacokinet... |
PMC11493102 | core_pubmed_pmc | Pharmacokinetics, pharmacodynamics, and safety of izuforant, an H4R inhibitor, in healthy subjects: A phase I single and multiple ascending dose study | Pharmacokinetics, pharmacodynamics, and safety of izuforant, an H4R inhibitor, in healthy subjects: A phase I single and multiple ascending dose study Abstract Abstract Izuforant is a selective, and potent histamine H4 receptor (H4R) antagonist developed to treat atopic dermatitis (AD). There is an unmet medical need f... |
PMC7407764 | core_pubmed_pmc | mTHPC-Loaded Extracellular Vesicles Significantly Improve mTHPC Diffusion and Photodynamic Activity in Preclinical Models | mTHPC-Loaded Extracellular Vesicles Significantly Improve mTHPC Diffusion and Photodynamic Activity in Preclinical Models Abstract Extracellular vesicles (EVs), derived from the cell, display a phospholipid bilayer membrane that protects the cargo molecules from degradation and contributes to increasing their stability... |
PMC11742576 | core_pubmed_pmc | Recombinant Erwinia asparaginase (JZP458) in ALL/LBL: complete follow-up of the Children’s Oncology Group AALL1931 study | Recombinant Erwinia asparaginase (JZP458) in ALL/LBL: complete follow-up of the Children’s Oncology Group AALL1931 study Abstract Key Points • Recombinant Erwinia asparaginase JZP458 maintains therapeutic serum asparaginase activity levels via multiple IM and IV dosing schedules. • The safety profile of JZP458 is consi... |
PMC4980036 | core_pubmed_pmc | Extended Evaluation of Virological, Immunological and Pharmacokinetic Endpoints of CELADEN: A Randomized, Placebo-Controlled Trial of Celgosivir in Dengue Fever Patients | Extended Evaluation of Virological, Immunological and Pharmacokinetic Endpoints of CELADEN: A Randomized, Placebo-Controlled Trial of Celgosivir in Dengue Fever Patients Abstract Abstract CELADEN was a randomized placebo-controlled trial of 50 patients with confirmed dengue fever to evaluate the efficacy and safety of ... |
PMC7598599 | core_pubmed_pmc | Utility of Three-Dimensional Cultures of Primary Human Hepatocytes (Spheroids) as Pharmacokinetic Models | Utility of Three-Dimensional Cultures of Primary Human Hepatocytes (Spheroids) as Pharmacokinetic Models Abstract Abstract This paper reviews the usefulness, current status, and potential of primary human hepatocytes (PHHs) in three-dimensional (3D) cultures, also known as spheroids, in the field of pharmacokinetics (P... |
PMC7341317 | core_pubmed_pmc | Effects of Single and Repeated Doses on Disposition and Kinetics of Doxycycline Hyclate in Goats | Effects of Single and Repeated Doses on Disposition and Kinetics of Doxycycline Hyclate in Goats Abstract Abstract Simple Summary Doxycycline is used to treat bacterial infections such as pneumonia, skin and soft tissue infections, urinary tract infections, salmonellosis, and colibacillosis in goats. In goats, the sing... |
PMC8505369 | core_pubmed_pmc | Estimation of Clearance and Bioavailability of Therapeutic Monoclonal Antibodies from Only Subcutaneous Injection Data in Humans Based on Comprehensive Analysis of Clinical Data | Estimation of Clearance and Bioavailability of Therapeutic Monoclonal Antibodies from Only Subcutaneous Injection Data in Humans Based on Comprehensive Analysis of Clinical Data Abstract Abstract Introduction Theoretically, the separate estimation of clearance (CL) and bioavailability (F) requires both intravenous and ... |
PMC3669611 | core_pubmed_pmc | Comparison of bioavailability between the most available generic tablet formulation containing artemether and lumefantrine on the Tanzanian market and the innovator’s product | Comparison of bioavailability between the most available generic tablet formulation containing artemether and lumefantrine on the Tanzanian market and the innovator’s product Abstract Abstract Background Existence of anti-malarial generic drugs with low bioavailability marketed on sub-Saharan Africa raises a concern on... |
PMC8278799 | core_pubmed_pmc | Hyponatremia Following Antipsychotic Treatment: In Silico Pharmacodynamics Analysis of Spontaneous Reports From the US Food and Drug Administration Adverse Event Reporting System Database and an Updated Systematic Review | Hyponatremia Following Antipsychotic Treatment: In Silico Pharmacodynamics Analysis of Spontaneous Reports From the US Food and Drug Administration Adverse Event Reporting System Database and an Updated Systematic Review Abstract Abstract Background Hyponatremia associated with antipsychotic drugs is a rare but potenti... |
PMC7057061 | core_pubmed_pmc | Pharmacodynamics of natalizumab extended interval dosing in MS | Pharmacodynamics of natalizumab extended interval dosing in MS Abstract Objective To determine if the concentration and saturation of natalizumab (NTZ) administration at extended interval dosing (EID; every 5–8 weeks) over 18 months is able to be maintained in the range considered adequate to sustain the clinical effic... |
PMC12139688 | core_pubmed_pmc | CD20×CD3 Bispecific Antibodies in B‐NHL: A Review of Translational Science, Pharmacokinetics, Pharmacodynamics, and Dose Strategy in Clinical Research | CD20×CD3 Bispecific Antibodies in B‐NHL: A Review of Translational Science, Pharmacokinetics, Pharmacodynamics, and Dose Strategy in Clinical Research Abstract ABSTRACT Despite advancements in treatment for B‐cell non‐Hodgkin lymphoma (B‐NHL) in recent decades, many patients still relapse or are refractory to treatment... |
PMC12363326 | core_pubmed_pmc | Nanotechnological innovations in paediatric tuberculosis management: current trends and future prospects | Nanotechnological innovations in paediatric tuberculosis management: current trends and future prospects Abstract Paediatric Tuberculosis (TB) continues to be a major global cause of morbidity and mortality. Children are more prone to contracting TB, which can spread quickly to extrapulmonary infection sites. Although ... |
PMC11271895 | core_pubmed_pmc | In silico exploration of deep-sea fungal metabolites as inhibitor of Ebola and Marburg VP35 and VP40 | In silico exploration of deep-sea fungal metabolites as inhibitor of Ebola and Marburg VP35 and VP40 Abstract VP30 and VP40 proteins of Ebola and Marburg viruses have been recognized as potential targets for antiviral drug development due to their essential roles in the viral lifecycle. Targeting these proteins could d... |
PMC5124576 | core_pubmed_pmc | San-Huang-Xie-Xin-Tang Constituents Exert Drug-Drug Interaction of Mutual Reinforcement at Both Pharmacodynamics and Pharmacokinetic Level: A Review | San-Huang-Xie-Xin-Tang Constituents Exert Drug-Drug Interaction of Mutual Reinforcement at Both Pharmacodynamics and Pharmacokinetic Level: A Review Abstract Inflammatory disorders underlie varieties of human diseases. San-Huang-Xie-xin-Tang (SHXXT), composed with Rhizoma Rhei ( Rheum palmatum L.), Rhizoma Coptidis ( C... |
PMC10946406 | core_pubmed_pmc | Model-Informed Precision Dosing of Isoniazid: Parametric Population Pharmacokinetics Model Repository | Model-Informed Precision Dosing of Isoniazid: Parametric Population Pharmacokinetics Model Repository Abstract Abstract Introduction Isoniazid (INH) is a crucial first-line anti tuberculosis (TB) drug used in adults and children. However, various factors can alter its pharmacokinetics (PK). This article aims to establi... |
PMC3627014 | core_pubmed_pmc | Effect of Prucalopride on the Pharmacokinetics of Oral Contraceptives in Healthy Women | Effect of Prucalopride on the Pharmacokinetics of Oral Contraceptives in Healthy Women Abstract Background Prucalopride is a selective, high-affinity, 5-hydroxytryptamine 4 (5-HT 4 ) receptor agonist, which is approved for the symptomatic treatment of chronic constipation in women in whom laxatives fail to provide adeq... |
PMC12571837 | core_pubmed_pmc | A bibliometric analysis and systematic review of drug repurposing against drug-resistant ESKAPE pathogens: a particular focus on Pseudomonas aeruginosa | A bibliometric analysis and systematic review of drug repurposing against drug-resistant ESKAPE pathogens: a particular focus on Pseudomonas aeruginosa Abstract Abstract Purpose Drug-resistant ESKAPE pathogens represent a major global health challenge. This study included a comprehensive bibliometric analysis and syste... |
PMC9328435 | core_pubmed_pmc | The effects of vilaprisan on the pharmacodynamics and pharmacokinetics of a combined oral contraceptive—A randomized controlled trial | The effects of vilaprisan on the pharmacodynamics and pharmacokinetics of a combined oral contraceptive—A randomized controlled trial Abstract Abstract Aims The primary objective was to explore whether the suppression of ovarian activity induced by a combined oral contraceptive (COC) is influenced by the simultaneous i... |
PMC10339693 | core_pubmed_pmc | A single ascending dose study of single‐stranded oligodeoxyribonucleotide RO7062931 in Chinese healthy volunteers | A single ascending dose study of single‐stranded oligodeoxyribonucleotide RO7062931 in Chinese healthy volunteers Abstract Abstract RO7062931 is an N‐acetylgalactosamine (GalNAc)‐conjugated single‐stranded oligodeoxyribonucleotide complementary to hepatitis B virus RNA. GalNAc conjugation targets the liver through the ... |
PMC12835379 | core_pubmed_pmc | A rapid method to reduce drug interferences for antibody measurements in pegunigalsidase alfa-treated patients with Fabry disease | A rapid method to reduce drug interferences for antibody measurements in pegunigalsidase alfa-treated patients with Fabry disease Abstract Aim Neutralizing anti-drug antibodies (ADA) limit therapy efficacies significantly. Pegunigalsidase alfa is a newly approved drug for the treatment of Fabry disease. The increased p... |
PMC12454471 | core_pubmed_pmc | Belantamab Mafodotin with Pomalidomide and Dexamethasone in Relapsed/Refractory Multiple Myeloma: A Comprehensive Exposure-Response Analysis of the DREAMM-8 Study | Belantamab Mafodotin with Pomalidomide and Dexamethasone in Relapsed/Refractory Multiple Myeloma: A Comprehensive Exposure-Response Analysis of the DREAMM-8 Study Abstract Abstract Background In the phase 3 DREAMM-8 study ( NCT04484623 ), belantamab mafodotin (anti-B-cell maturation antigen [BCMA] antibody-drug conjuga... |
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