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PMC11677492 | core_pubmed_pmc | Pharmacodynamic Model of the Hemodynamic Effects of Propofol and Remifentanil and Their Interaction with Noxious Stimulation † | Pharmacodynamic Model of the Hemodynamic Effects of Propofol and Remifentanil and Their Interaction with Noxious Stimulation † Abstract Abstract Background : Despite the known impact of propofol and remifentanil on hemodynamics and patient outcomes, there is a lack of comprehensive quantitative analysis, particularly i... |
PMC6383944 | core_pubmed_pmc | A non-linear mixed effect model for innate immune response: In vivo kinetics of endotoxin and its induction of the cytokines tumor necrosis factor alpha and interleukin-6 | A non-linear mixed effect model for innate immune response: In vivo kinetics of endotoxin and its induction of the cytokines tumor necrosis factor alpha and interleukin-6 Abstract Endotoxin, a component of the outer membrane of Gram-negative bacteria, has been extensively studied as a stimulator of the innate immune re... |
PMC6809794 | core_pubmed_pmc | Pharmacokinetics and Pharmacodynamics of Conventional-Dose vs Triple-Dose Oseltamivir in Severely Immunocompromised Children With Influenza | Pharmacokinetics and Pharmacodynamics of Conventional-Dose vs Triple-Dose Oseltamivir in Severely Immunocompromised Children With Influenza Abstract Abstract This randomized phase 1b study evaluated the pharmacokinetics/pharmacodynamics of conventional-dose (30–75 mg twice daily [BID]) vs triple-dose (90–225 mg BID; we... |
PMC6958523 | core_pubmed_pmc | Metabolism and Pharmacokinetic Study of the Boron-Containing Prodrug of Belinostat (ZL277), a Pan HDAC Inhibitor with Enhanced Bioavailability | Metabolism and Pharmacokinetic Study of the Boron-Containing Prodrug of Belinostat (ZL277), a Pan HDAC Inhibitor with Enhanced Bioavailability Abstract ZL277 is a prodrug of belinostat with enhanced bioavailability and efficacy as a pan histone deacetylase (HDAC) inhibitor. In this study, we investigated the metabolism... |
PMC6835337 | core_pubmed_pmc | Food–Drug Interaction between the Adlay Bran Oil and Drugs in Rats | Food–Drug Interaction between the Adlay Bran Oil and Drugs in Rats Abstract Abstract Adlay ( Coix lachryma-jobi L. var. ma-yuen Stapf) contains various phytonutrients for treating many diseases in Asia. To investigate whether orally administered adlay bran oil (ABO) can cause drug interactions, the effects of ABO on th... |
PMC9959242 | core_pubmed_pmc | Genetic Variation in CYP2D6 and SLC22A1 Affects Amlodipine Pharmacokinetics and Safety | Genetic Variation in CYP2D6 and SLC22A1 Affects Amlodipine Pharmacokinetics and Safety Abstract Abstract Amlodipine is an antihypertensive drug with unknown pharmacogenetic biomarkers. This research is a candidate gene study that looked for associations between amlodipine pharmacokinetics and safety and pharmacogenes. ... |
PMC7897944 | core_pubmed_pmc | Relmacabtagene autoleucel (relma‐cel) CD19 CAR‐T therapy for adults with heavily pretreated relapsed/refractory large B‐cell lymphoma in China | Relmacabtagene autoleucel (relma‐cel) CD19 CAR‐T therapy for adults with heavily pretreated relapsed/refractory large B‐cell lymphoma in China Abstract Abstract Background Despite numerous chimeric antigen receptor T‐cell (CAR‐T) trials conducted in China, no CAR‐T has been registered in the country. Furthermore, China... |
PMC10773429 | core_pubmed_pmc | Azathioprine metabolite levels and outcomes during pregnancies with rheumatic disease | Azathioprine metabolite levels and outcomes during pregnancies with rheumatic disease Abstract Abstract Objective Despite widespread use of azathioprine (AZA) during pregnancy, no studies evaluated the impact of pregnancy on AZA metabolites 6-thioguanine nucleotide (6-TGN) and 6-methylmercaptopurine nucleotide (6-MMPN)... |
PMC12212626 | core_pubmed_pmc | In Vitro and In Silico Evaluation of Isatin‐Derived Spirooxindoles as Antituberculosis Drug Candidates | In Vitro and In Silico Evaluation of Isatin‐Derived Spirooxindoles as Antituberculosis Drug Candidates Abstract ABSTRACT Tuberculosis (TB) remains a major global health threat, exacerbated by multidrug‐resistant Mycobacterium tuberculosis (MTB) strains. The development of new anti‐TB agents is crucial. In this study, 1... |
PMC3915428 | core_pubmed_pmc | Vancomycin Pharmacokinetic Parameters in Patients Undergoing Hematopoietic Stem Cell Transplantation (HSCT) | Vancomycin Pharmacokinetic Parameters in Patients Undergoing Hematopoietic Stem Cell Transplantation (HSCT) Abstract Abstract Background Vancomycin is used abundantly in patients undergoing HSCT, especially during neutropenic fever. Despite its widespread use little is known about vancomycin pharmacokinetics in HSCT pa... |
PMC9146031 | core_pubmed_pmc | Population Pharmacokinetics and Dosing Regimen Optimization of Latamoxef in Chinese Children | Population Pharmacokinetics and Dosing Regimen Optimization of Latamoxef in Chinese Children Abstract Abstract The present study aimed to establish population pharmacokinetic models of latamoxef, as well as its R- and S-epimers, and generate findings to guide the individualized administration of latamoxef in pediatric ... |
PMC9727182 | core_pubmed_pmc | Identification of pharmacokinetic markers for safflower injection using a combination of system pharmacology, multicomponent pharmacokinetics, and quantitative proteomics study | Identification of pharmacokinetic markers for safflower injection using a combination of system pharmacology, multicomponent pharmacokinetics, and quantitative proteomics study Abstract Safflower injection (SI), a water-extract preparation from safflower ( Carthamus tinctorius L.), has been widely used for the treatmen... |
PMC6659750 | core_pubmed_pmc | Tear Fluid Pharmacokinetics Following Oral Prednisone Administration in Dogs With and Without Conjunctivitis | Tear Fluid Pharmacokinetics Following Oral Prednisone Administration in Dogs With and Without Conjunctivitis Abstract Abstract Purpose: To describe the pharmacokinetics (PK) of prednisone and prednisolone in tear fluid of dogs receiving oral prednisone at anti-inflammatory to immunosuppressive doses and to assess the i... |
PMC10355467 | core_pubmed_pmc | Lumicitabine, an orally administered nucleoside analog, in infants hospitalized with respiratory syncytial virus (RSV) infection: Safety, efficacy, and pharmacokinetic results | Lumicitabine, an orally administered nucleoside analog, in infants hospitalized with respiratory syncytial virus (RSV) infection: Safety, efficacy, and pharmacokinetic results Abstract Abstract Respiratory syncytial virus (RSV) infection is the leading cause of infant hospitalizations and mortality. Lumicitabine, an or... |
PMC5754397 | core_pubmed_pmc | Population pharmacokinetics of nintedanib, an inhibitor of tyrosine kinases, in patients with non-small cell lung cancer or idiopathic pulmonary fibrosis | Population pharmacokinetics of nintedanib, an inhibitor of tyrosine kinases, in patients with non-small cell lung cancer or idiopathic pulmonary fibrosis Abstract Purpose A population pharmacokinetic model was developed for nintedanib in patients with non-small cell lung cancer (NSCLC) or idiopathic pulmonary fibrosis ... |
PMC6680801 | core_pubmed_pmc | Enhanced Intradermal Delivery of Nanosuspensions of Antifilariasis Drugs Using Dissolving Microneedles: A Proof of Concept Study | Enhanced Intradermal Delivery of Nanosuspensions of Antifilariasis Drugs Using Dissolving Microneedles: A Proof of Concept Study Abstract Conventional oral administration of antifilariasis drugs results in nonspecific targeting of the drugs and the intradermal delivery of nanoparticles with sizes of <100 nm could be us... |
PMC9230244 | core_pubmed_pmc | A Prospective Study of Medication Surveillance of a Pediatric Tertiary Care Hospital in Lahore, Pakistan | A Prospective Study of Medication Surveillance of a Pediatric Tertiary Care Hospital in Lahore, Pakistan Abstract Abstract Purpose: Several studies have shown that polypharmacy is the main cause of drug interactions, and the prevalence and the level of the severity varied with the duration of stay in the hospital, sex ... |
PMC6767603 | core_pubmed_pmc | Optimization of Preparation and Preclinical Pharmacokinetics of Celastrol-Encapsulated Silk Fibroin Nanoparticles in the Rat | Optimization of Preparation and Preclinical Pharmacokinetics of Celastrol-Encapsulated Silk Fibroin Nanoparticles in the Rat Abstract Celastrol (CL), a bioactive compound isolated from Tripterygium wilfordii , has demonstrated bioactivities against a variety of diseases including cancer and obesity. However, its poor w... |
PMC7468075 | core_pubmed_pmc | Pharmacokinetics in plasma and alveolar regions of healthy calves subcutaneously administered a single dose of enrofloxacin | Pharmacokinetics in plasma and alveolar regions of healthy calves subcutaneously administered a single dose of enrofloxacin Abstract This study aimed to analyze the pharmacokinetics of enrofloxacin (ERFX) and its metabolite ciprofloxacin (CPFX) in plasma, as well as their migration to, and retention in, the epithelial ... |
PMC10610385 | core_pubmed_pmc | Uptake Transporters at the Blood–Brain Barrier and Their Role in Brain Drug Disposition | Uptake Transporters at the Blood–Brain Barrier and Their Role in Brain Drug Disposition Abstract Abstract Uptake drug transporters play a significant role in the pharmacokinetic of drugs within the brain, facilitating their entry into the central nervous system (CNS). Understanding brain drug disposition is always chal... |
PMC6945951 | core_pubmed_pmc | Nanomedicine for Treatment of Acute Lung Injury and Acute Respiratory Distress Syndrome | Nanomedicine for Treatment of Acute Lung Injury and Acute Respiratory Distress Syndrome Abstract Abstract Acute lung injury and acute respiratory distress syndrome (ARDS) represent a heterogenous group of lung disease in critically ill patients that continues to have high mortality. Despite the increased understanding ... |
PMC8140366 | core_pubmed_pmc | A field trial comparing four oral nonsteroidal anti-inflammatory drugs on controlling cautery dehorning pain and stress in calves | A field trial comparing four oral nonsteroidal anti-inflammatory drugs on controlling cautery dehorning pain and stress in calves Abstract Abstract The purpose of this study was to compare the analgesic effect of four nonsteroidal anti-inflammatory drugs (NSAIDs) administered as a single, standardized, oral dose in dai... |
PMC9772348 | core_pubmed_pmc | Part one: abuse liability of Vuse Solo (G2) electronic nicotine delivery system relative to combustible cigarettes and nicotine gum | Part one: abuse liability of Vuse Solo (G2) electronic nicotine delivery system relative to combustible cigarettes and nicotine gum Abstract Abstract Abuse liability (AL) of electronic nicotine delivery systems (ENDS) is relevant as the category increases in popularity as a potentially less-harmful alternative to cigar... |
PMC8505377 | core_pubmed_pmc | Pharmacokinetics of Lorlatinib After Single and Multiple Dosing in Patients with Anaplastic Lymphoma Kinase ( ALK )-Positive Non-Small Cell Lung Cancer: Results from a Global Phase I/II Study | Pharmacokinetics of Lorlatinib After Single and Multiple Dosing in Patients with Anaplastic Lymphoma Kinase ( ALK )-Positive Non-Small Cell Lung Cancer: Results from a Global Phase I/II Study Abstract Abstract Background Lorlatinib demonstrated efficacy (including intracranial activity) in patients with anaplastic lymp... |
PMC12540523 | core_pubmed_pmc | Clinical Pharmacokinetics, Pharmacodynamics, and Drug Interactions of Remimazolam | Clinical Pharmacokinetics, Pharmacodynamics, and Drug Interactions of Remimazolam Abstract Remimazolam, an ultrashort-acting benzodiazepine, has emerged as a promising sedative agent for procedural sedation and general anesthesia. It combines the favorable properties of traditional benzodiazepines with a rapid onset an... |
PMC9523021 | core_pubmed_pmc | Non-invasive in vivo assessment of 11β-hydroxysteroid dehydrogenase type 1 activity by 19 F-Magnetic Resonance Spectroscopy | Non-invasive in vivo assessment of 11β-hydroxysteroid dehydrogenase type 1 activity by 19 F-Magnetic Resonance Spectroscopy Abstract 11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) amplifies tissue glucocorticoid levels and is a pharmaceutical target in diabetes and cognitive decline. Clinical translation of inhibit... |
PMC6930859 | core_pubmed_pmc | Pharmacokinetics of Capecitabine and Four Metabolites in a Heterogeneous Population of Cancer Patients: A Comprehensive Analysis | Pharmacokinetics of Capecitabine and Four Metabolites in a Heterogeneous Population of Cancer Patients: A Comprehensive Analysis Abstract Capecitabine is an oral prodrug of the anticancer drug 5‐fluorouracil (5‐FU). The primary aim of this study was to develop a pharmacokinetic model for capecitabine and its metabolite... |
PMC9311574 | core_pubmed_pmc | Protein Binding in Translational Antimicrobial Development-Focus on Interspecies Differences | Protein Binding in Translational Antimicrobial Development-Focus on Interspecies Differences Abstract Background/Introduction: Plasma protein binding (PPB) continues to be a key aspect of antibiotic development and clinical use. PPB is essential to understand several properties of drug candidates, including antimicrobi... |
PMC4483248 | core_pubmed_pmc | Pharmacokinetics of rituximab in a pediatric patient with therapy-resistant nephrotic syndrome | Pharmacokinetics of rituximab in a pediatric patient with therapy-resistant nephrotic syndrome Abstract Abstract Background Rituximab (RTX) has recently been introduced as a second-line therapy for nephrotic syndrome in children. Studies show that RTX given during the nephrotic state may be less effective than treatmen... |
PMC10474108 | core_pubmed_pmc | Analysis of clinical failure of anti-tau and anti-synuclein antibodies in neurodegeneration using a quantitative systems pharmacology model | Analysis of clinical failure of anti-tau and anti-synuclein antibodies in neurodegeneration using a quantitative systems pharmacology model Abstract Abstract Misfolded proteins in Alzheimer’s disease and Parkinson’s disease follow a well-defined connectomics-based spatial progression. Several anti-tau and anti-alpha sy... |
PMC11097949 | core_pubmed_pmc | Reversal of Propofol-induced Depression of the Hypoxic Ventilatory Response by BK-channel Blocker ENA-001: A Randomized Controlled Trial | Reversal of Propofol-induced Depression of the Hypoxic Ventilatory Response by BK-channel Blocker ENA-001: A Randomized Controlled Trial Abstract Abstract Background: The use of anesthetics may result in depression of the hypoxic ventilatory response. Since there are no receptor-specific antagonists for most anesthetic... |
PMC12035414 | core_pubmed_pmc | Population Pharmacokinetics of Osimertinib in Patients With Non‐Small Cell Lung Cancer | Population Pharmacokinetics of Osimertinib in Patients With Non‐Small Cell Lung Cancer Abstract ABSTRACT Population pharmacokinetics (popPK) modeling for osimertinib, a third‐generation, irreversible, oral epidermal growth factor receptor (EGFR)‐tyrosine kinase inhibitor (TKI) that potently and selectively inhibits bot... |
PMC8557932 | core_pubmed_pmc | Reproducibility of the Ribosomal RNA Synthesis Ratio in Sputum and Association with Markers of Mycobacterium tuberculosis Burden | Reproducibility of the Ribosomal RNA Synthesis Ratio in Sputum and Association with Markers of Mycobacterium tuberculosis Burden Abstract ABSTRACT There is a critical need for improved pharmacodynamic markers for use in human tuberculosis (TB) drug trials. Pharmacodynamic monitoring in TB has conventionally used cultur... |
PMC10590544 | core_pubmed_pmc | Assessment of risk factors for acute graft- versus -host disease post-hematopoietic stem cell transplantation: a retrospective study based on a proportional odds model using a nonlinear mixed-effects model | Assessment of risk factors for acute graft- versus -host disease post-hematopoietic stem cell transplantation: a retrospective study based on a proportional odds model using a nonlinear mixed-effects model Abstract Abstract Background: Acute graft- versus -host disease (aGVHD) is a major complication following hematopo... |
PMC9311615 | core_pubmed_pmc | Daptomycin Population Pharmacokinetics in Patients Affected by Severe Gram-Positive Infections: An Update | Daptomycin Population Pharmacokinetics in Patients Affected by Severe Gram-Positive Infections: An Update Abstract Abstract Daptomycin pharmacokinetics may not depend on renal function only and it significantly differs between healthy volunteers and severely ill patients. Herein, we propose a population pharmacokinetic... |
PMC9821424 | core_pubmed_pmc | Mathematical models for biomarker calculation of drug-induced liver injury in humans and experimental models based on gadoxetate enhanced magnetic resonance imaging | Mathematical models for biomarker calculation of drug-induced liver injury in humans and experimental models based on gadoxetate enhanced magnetic resonance imaging Abstract Abstract Background Drug induced liver injury (DILI) is a major concern when developing new drugs. A promising biomarker for DILI is the hepatic u... |
PMC7065230 | core_pubmed_pmc | A phase 1, randomized, pharmacokinetic trial of the effect of different meal compositions, whole milk, and alcohol on cannabidiol exposure and safety in healthy subjects | A phase 1, randomized, pharmacokinetic trial of the effect of different meal compositions, whole milk, and alcohol on cannabidiol exposure and safety in healthy subjects Abstract Abstract Objective The pharmacokinetics (PK) and safety of single oral 750‐mg doses of a plant‐derived pharmaceutical formulation of highly p... |
PMC8151315 | core_pubmed_pmc | The Combination of Cell Cultured Technology and In Silico Model to Inform the Drug Development | The Combination of Cell Cultured Technology and In Silico Model to Inform the Drug Development Abstract Human-derived in vitro models can provide high-throughput efficacy and toxicity data without a species gap in drug development. Challenges are still encountered regarding the full utilisation of massive data in clini... |
PMC12617622 | core_pubmed_pmc | Nicotine pouch pharmacokinetics compared to smoked tobacco: A systematic review and meta-analysis | Nicotine pouch pharmacokinetics compared to smoked tobacco: A systematic review and meta-analysis Abstract Nicotine pouches (NP) are novel agents that deliver nicotine through buccal absorption as opposed to combustion. They are proposed as a harm reduction tool compared to smoking tobacco. However, there is limited ev... |
PMC9607610 | core_pubmed_pmc | Performance Verification of CYP2C19 Enzyme Abundance Polymorphism Settings within the Simcyp Simulator v21 | Performance Verification of CYP2C19 Enzyme Abundance Polymorphism Settings within the Simcyp Simulator v21 Abstract Physiologically based pharmacokinetic (PBPK) modeling has a number of applications, including assessing drug–drug interactions (DDIs) in polymorphic populations, and should be iteratively refined as scien... |
PMC4189713 | core_pubmed_pmc | An evidence-based review of ixazomib citrate and its potential in the treatment of newly diagnosed multiple myeloma | An evidence-based review of ixazomib citrate and its potential in the treatment of newly diagnosed multiple myeloma Abstract Abstract Proteasome inhibition represents one of the more important therapeutic targets in the treatment of multiple myeloma (MM), since by suppressing nuclear factor-κB activity, which promotes ... |
PMC6570793 | core_pubmed_pmc | The Prevalence of the Potential Drug-Drug Interactions Involving Anticancer Drugs in China: A Retrospective Study | The Prevalence of the Potential Drug-Drug Interactions Involving Anticancer Drugs in China: A Retrospective Study Abstract Abstract Background: To survey the prevalence of potential drug-drug interactions (DDIs) between anticancer drugs and non-anticancer drugs and evaluate the risk factors associated with these drug-d... |
PMC7934554 | core_pubmed_pmc | An open-label, pilot study of veliparib and lapatinib in patients with metastatic, triple-negative breast cancer | An open-label, pilot study of veliparib and lapatinib in patients with metastatic, triple-negative breast cancer Abstract Background Poly (ADP-ribose)-polymerase inhibitors (PARPi) have been approved for cancer patients with germline BRCA1/2 (g BRCA1/2 ) mutations, and efforts to expand the utility of PARPi beyond BRCA... |
PMC8342319 | core_pubmed_pmc | Predicting blood-to-plasma concentration ratios of drugs from chemical structures and volumes of distribution in humans | Predicting blood-to-plasma concentration ratios of drugs from chemical structures and volumes of distribution in humans Abstract Abstract Despite their importance in determining the dosing regimen of drugs in the clinic, only a few studies have investigated methods for predicting blood-to-plasma concentration ratios (R... |
PMC8136953 | core_pubmed_pmc | Evaluation of absorption and depletion of florfenicol in European seabass Dicentrarchus labrax | Evaluation of absorption and depletion of florfenicol in European seabass Dicentrarchus labrax Abstract Abstract The pharmacokinetic properties and residue elimination of florfenicol (FLO) and its amine were investigated in European seabass Dicentrarchus labrax at 24°C. The trial mainly included analysis of FLO in plas... |
PMC5224788 | core_pubmed_pmc | Population Pharmacokinetic Properties of Piperaquine in Falciparum Malaria: An Individual Participant Data Meta-Analysis | Population Pharmacokinetic Properties of Piperaquine in Falciparum Malaria: An Individual Participant Data Meta-Analysis Abstract Background Artemisinin-based combination therapies (ACTs) are the mainstay of the current treatment of uncomplicated Plasmodium falciparum malaria, but ACT resistance is spreading across Sou... |
PMC10349574 | core_pubmed_pmc | Design, Synthesis and Biological Evaluation of Glycosylated Derivatives of Silibinin as Potential Anti-Tumor Agents | Design, Synthesis and Biological Evaluation of Glycosylated Derivatives of Silibinin as Potential Anti-Tumor Agents Abstract Objective Silibinin, a natural product extracted from the seeds of the Silybum marianum , is versatile with various pharmacological effects. However, its clinical application was strongly hampere... |
PMC9860708 | core_pubmed_pmc | Parent-Metabolite Pharmacokinetic Modeling of Formononetin and Its Active Metabolites in Rats after Oral Administration of Formononetin Formulations | Parent-Metabolite Pharmacokinetic Modeling of Formononetin and Its Active Metabolites in Rats after Oral Administration of Formononetin Formulations Abstract Formononetin is a major isoflavone contained in propolis and is reported to exhibit various pharmacological effects. However, the use of formononetin in pharmaceu... |
PMC10851641 | core_pubmed_pmc | Drug–drug interactions involving classic psychedelics: A systematic review | Drug–drug interactions involving classic psychedelics: A systematic review Abstract Classic psychedelics, including lysergic acid diethylamide (LSD), psilocybin, mescaline, N,N-dimethyltryptamine (DMT) and 5-methoxy-N,N-dimethyltryptamine (5-MeO-DMT), are potent psychoactive substances that have been studied for their ... |
PMC8429954 | core_pubmed_pmc | CYP2C19 Genotyping May Provide a Better Treatment Strategy when Administering Escitalopram in Chinese Population | CYP2C19 Genotyping May Provide a Better Treatment Strategy when Administering Escitalopram in Chinese Population Abstract Depression disorder is one of the most serious mental illnesses in the world. Escitalopram is the essential first-line medication for depression disorder. It is the substrate of hepatic cytochrome P... |
PMC10625992 | core_pubmed_pmc | Bromodomain and extraterminal (BET) proteins: biological functions, diseases and targeted therapy | Bromodomain and extraterminal (BET) proteins: biological functions, diseases and targeted therapy Abstract Abstract BET proteins, which influence gene expression and contribute to the development of cancer, are epigenetic interpreters. Thus, BET inhibitors represent a novel form of epigenetic anticancer treatment. Alth... |
PMC2893758 | core_pubmed_pmc | Investigation of clinical interaction between omeprazole and tacrolimus in CYP3A5 non-expressors, renal transplant recipients | Investigation of clinical interaction between omeprazole and tacrolimus in CYP3A5 non-expressors, renal transplant recipients Abstract Background: As proton pump inhibitors share CYP3A4 enzyme with tacrolimus for their hepatic elimination, they potentially affect its pharmacokinetics, most prominently in patients with ... |
PMC3433319 | core_pubmed_pmc | Rivaroxaban in atrial fibrillation | Rivaroxaban in atrial fibrillation Abstract Abstract Warfarin is the traditional therapeutic option available to manage thromboembolic risk in atrial fibrillation. The hemorrhagic risk with warfarin depends mainly on the international normalized ratio (INR). Data from randomized controlled trials show that patients hav... |
PMC11215690 | core_pubmed_pmc | A phase I randomized study to evaluate safety, pharmacokinetics, and pharmacodynamics of SIR2446M, a selective RIPK1 inhibitor, in healthy participants | A phase I randomized study to evaluate safety, pharmacokinetics, and pharmacodynamics of SIR2446M, a selective RIPK1 inhibitor, in healthy participants Abstract Abstract Activation of receptor‐interacting protein kinase 1 (RIPK1), a broadly expressed serine/threonine protein kinase, by pro‐inflammatory cytokines and pa... |
PMC5640627 | core_pubmed_pmc | Saline is as effective as nitrogen scavengers for treatment of hyperammonemia | Saline is as effective as nitrogen scavengers for treatment of hyperammonemia Abstract Abstract Urea cycle enzyme deficiency (UCED) patients with hyperammonemia are treated with sodium benzoate (SB) and sodium phenylacetate (SPA) to induce alternative pathways of nitrogen excretion. The suggested guidelines supporting ... |
PMC12267601 | core_pubmed_pmc | A pilot study on LC–MS/MS quantification of remifentanil, etomidate, and rocuronium in maternal and fetal serum microsamples | A pilot study on LC–MS/MS quantification of remifentanil, etomidate, and rocuronium in maternal and fetal serum microsamples Abstract Abstract While remifentanil, etomidate, and rocuronium are increasingly used for cesarean section due to their favorable hemodynamic stability and fetal safety profile, their pharmacokin... |
PMC10213340 | core_pubmed_pmc | Therapeutic effect of fenofibrate for non-alcoholic steatohepatitis in mouse models is dependent on regime design | Therapeutic effect of fenofibrate for non-alcoholic steatohepatitis in mouse models is dependent on regime design Abstract Abstract Background: Non-alcoholic fatty liver disease (NAFLD) is the leading cause of chronic liver diseases. In most cases, NAFLD progresses from benign steatosis to steatohepatitis (NASH), and t... |
PMC8586418 | core_pubmed_pmc | Recent Progress in Interferon Therapy for Myeloid Malignancies | Recent Progress in Interferon Therapy for Myeloid Malignancies Abstract Abstract Myeloid malignancies are a heterogeneous group of clonal haematopoietic disorders, caused by abnormalities in haematopoietic stem cells (HSCs) and myeloid progenitor cells that originate in the bone marrow niche. Each of these disorders ar... |
PMC6538812 | core_pubmed_pmc | Leveraging Mathematical Modeling to Quantify Pharmacokinetic and Pharmacodynamic Pathways: Equivalent Dose Metric | Leveraging Mathematical Modeling to Quantify Pharmacokinetic and Pharmacodynamic Pathways: Equivalent Dose Metric Abstract Treatment response assays are often summarized by sigmoidal functions comparing cell survival at a single timepoint to applied drug concentration. This approach has a limited biophysical basis, the... |
PMC8947478 | core_pubmed_pmc | Novel, First-in-Human, Oral PCLX-001 Treatment in a Patient with Relapsed Diffuse Large B-Cell Lymphoma | Novel, First-in-Human, Oral PCLX-001 Treatment in a Patient with Relapsed Diffuse Large B-Cell Lymphoma Abstract Abstract Patients with relapsed or refractory diffuse large B-cell lymphoma (DLBCL) have limited treatment options, particularly if they are transplantation or chimeric antigen receptor (CAR) T-cell ineligib... |
PMC12850558 | core_pubmed_pmc | Prediction of neutrophil nadir and recovery following paediatric haematopoietic cell transplantation with busulfan conditioning | Prediction of neutrophil nadir and recovery following paediatric haematopoietic cell transplantation with busulfan conditioning Abstract Aims In haematopoietic cell transplantation (HCT), neutropenia resulting from myelosuppression is an expected endpoint following busulfan‐based conditioning. However, if prolonged, ne... |
PMC11359469 | core_pubmed_pmc | Unlocking the Potential of Camel Milk-Derived Exosomes as Novel Delivery Systems: Enhanced Bioavailability of ARV-825 PROTAC for Cancer Therapy | Unlocking the Potential of Camel Milk-Derived Exosomes as Novel Delivery Systems: Enhanced Bioavailability of ARV-825 PROTAC for Cancer Therapy Abstract Abstract This study investigates the use of camel milk-derived exosomes (CMEs) as carriers for ARV-825, an anticancer agent targeting bromodomain-containing protein 4 ... |
PMC12420824 | core_pubmed_pmc | Discovery of a selective alpha-kinase 1 inhibitor for the rare genetic disease ROSAH syndrome | Discovery of a selective alpha-kinase 1 inhibitor for the rare genetic disease ROSAH syndrome Abstract Abstract ROSAH (retinal dystrophy, optic nerve edema, splenomegaly, anhidrosis, and headache) syndrome is a rare genetic disease caused by variants in alpha-kinase 1 (ALPK1) resulting in downstream pro-inflammatory si... |
PMC6339964 | core_pubmed_pmc | Pharmacokinetic–pharmacodynamic modelling of platelet response to ticagrelor in stable coronary artery disease and prior myocardial infarction patients | Pharmacokinetic–pharmacodynamic modelling of platelet response to ticagrelor in stable coronary artery disease and prior myocardial infarction patients Abstract Abstract Aims To characterize ticagrelor exposure‐response relationship for platelet inhibition in patients with stable coronary artery disease (CAD) and a his... |
PMC11491386 | core_pubmed_pmc | Prediction of tissue exposures of polymyxin-B, amikacin and sulbactam using physiologically-based pharmacokinetic modeling | Prediction of tissue exposures of polymyxin-B, amikacin and sulbactam using physiologically-based pharmacokinetic modeling Abstract Abstract Background The combination antimicrobial therapy consisting of amikacin, polymyxin-B, and sulbactam demonstrated in vitro synergy against multi-drug resistant Acinetobacter bauman... |
PMC11961502 | core_pubmed_pmc | In Vitro - In Vivo Correlation Of Amorphous Solid Dispersion Enabled Itraconazole Tablets | In Vitro - In Vivo Correlation Of Amorphous Solid Dispersion Enabled Itraconazole Tablets Abstract Abstract Purpose There are scarce reports on in vitro - in vivo correlation (IVIVC) model development of immediate-release (IR) formulations, and few investigations of the impacts of formulation and process of spray-dried... |
PMC9760738 | core_pubmed_pmc | Pharmacokinetics, absorption, distribution, metabolism and excretion of the MEK inhibitor zapnometinib in rats | Pharmacokinetics, absorption, distribution, metabolism and excretion of the MEK inhibitor zapnometinib in rats Abstract Abstract Zapnometinib is a MEK inhibitor currently under clinical development for the treatment of COVID-19 and influenza. Zapnometinib has both antiviral and immunomodulatory effects. Information con... |
PMC12122142 | core_pubmed_pmc | The potential for therapeutic drug monitoring of belatacept and other biologicals in solid organ transplantation | The potential for therapeutic drug monitoring of belatacept and other biologicals in solid organ transplantation Abstract Abstract In solid organ transplantation (SOT), biologicals such as recombinant therapeutic proteins, monoclonal antibodies, fusion proteins and conjugates are increasingly used for immunosuppression... |
PMC10050031 | core_pubmed_pmc | Inhibition of the epigenetically activated miR-483-5p/IGF-2 pathway results in rapid loss of meningioma tumor cell viability | Inhibition of the epigenetically activated miR-483-5p/IGF-2 pathway results in rapid loss of meningioma tumor cell viability Abstract Purpose Meningioma is the most common primary central nervous system tumor often causing serious complications, and presently no medical treatment is available. The goal of this study wa... |
PMC12095307 | core_pubmed_pmc | Developing a generalized nonlinear mixed-effects biomass model at stand-level under different age conditions for Chinese fir based on LiDAR and ground survey data in southern China | Developing a generalized nonlinear mixed-effects biomass model at stand-level under different age conditions for Chinese fir based on LiDAR and ground survey data in southern China Abstract Introduction Chinese fir (Cunninghamia lanceolata) is a crucial afforestation and timber species in southern China. Accurate estim... |
PMC8592513 | core_pubmed_pmc | Exposure–response analysis of efficacy and safety for pexidartinib in patients with tenosynovial giant cell tumor | Exposure–response analysis of efficacy and safety for pexidartinib in patients with tenosynovial giant cell tumor Abstract Abstract This analysis was conducted to assess exposure–response relationships for efficacy and safety of pexidartinib in patients with tenosynovial giant cell tumor. Efficacy was assessed categori... |
PMC7070788 | core_pubmed_pmc | Predicting Cost‐Effectiveness of Generic vs. Brand Dabigatran Using Pharmacometric Estimates Among Patients with Atrial Fibrillation in the United States | Predicting Cost‐Effectiveness of Generic vs. Brand Dabigatran Using Pharmacometric Estimates Among Patients with Atrial Fibrillation in the United States Abstract Generic entry of newer anticoagulants is expected to decrease the costs of atrial fibrillation management. However, when making switches between brand and ge... |
PMC11642635 | core_pubmed_pmc | Effect of Organic Anion Transporting Polypeptide 1B1 on Plasma Concentration Dynamics of Clozapine in Patients with Treatment-Resistant Schizophrenia | Effect of Organic Anion Transporting Polypeptide 1B1 on Plasma Concentration Dynamics of Clozapine in Patients with Treatment-Resistant Schizophrenia Abstract The involvement of drug-metabolizing enzymes and transporters in plasma clozapine (CLZ) dynamics has not been well examined in Japanese patients with treatment-r... |
PMC9214059 | core_pubmed_pmc | Recent advances in the translation of drug metabolism and pharmacokinetics science for drug discovery and development | Recent advances in the translation of drug metabolism and pharmacokinetics science for drug discovery and development Abstract Drug metabolism and pharmacokinetics (DMPK) is an important branch of pharmaceutical sciences. The nature of ADME (absorption, distribution, metabolism, excretion) and PK (pharmacokinetics) inq... |
PMC9881059 | core_pubmed_pmc | Herb-drug Interactions in Neuropsychiatric Pharmacotherapy – A Review of Clinically Relevant Findings | Herb-drug Interactions in Neuropsychiatric Pharmacotherapy – A Review of Clinically Relevant Findings Abstract The management of neuropsychiatric disorders relies heavily on pharmacotherapy. The use of herbal products as complimentary medicine, often concomitantly, is common among patients taking prescription neuropsyc... |
PMC9795956 | core_pubmed_pmc | Effects of Mexiletine and Lacosamide on Nerve Excitability in Healthy Subjects: A Randomized, Double‐Blind, Placebo‐Controlled, Crossover Study | Effects of Mexiletine and Lacosamide on Nerve Excitability in Healthy Subjects: A Randomized, Double‐Blind, Placebo‐Controlled, Crossover Study Abstract Selective voltage‐gated sodium channel blockers are of growing interest as treatment for pain. For drug development of such compounds, it would be critical to have a b... |
PMC4281101 | core_pubmed_pmc | Discovery of a Phosphodiesterase 9A Inhibitor as a Potential Hypoglycemic Agent | Discovery of a Phosphodiesterase 9A Inhibitor as a Potential Hypoglycemic Agent Abstract Abstract Phosphodiesterase 9 (PDE9) inhibitors have been studied as potential therapeutics for treatment of diabetes and Alzheimer’s disease. Here we report a potent PDE9 inhibitor 3r that has an IC 50 of 0.6 nM and >150-fold selec... |
PMC12938331 | core_pubmed_pmc | Immunogenicity in Fabry Disease: Current Issues, Coping Strategies, and Future Directions | Immunogenicity in Fabry Disease: Current Issues, Coping Strategies, and Future Directions Abstract Abstract Fabry disease (FD) is an X-linked systemic lysosomal storage disease caused by mutations in the galactosidase-α ( GLA ) gene, which encodes the α-galactosidase A (α-AGAL) enzyme. FD can lead to serious complicati... |
PMC6225915 | core_pubmed_pmc | Comparative pharmacokinetics of an adalimumab biosimilar SB5 administered via autoinjector or prefilled syringe in healthy subjects | Comparative pharmacokinetics of an adalimumab biosimilar SB5 administered via autoinjector or prefilled syringe in healthy subjects Abstract Purpose The objective of this study was to demonstrate comparable pharmacokinetic (PK), safety, and tolerability parameters of the adalimumab biosimilar SB5 administered via autoi... |
PMC7927811 | core_pubmed_pmc | An Exposure-Response Perspective on the Clinical Dose of Pretomanid | An Exposure-Response Perspective on the Clinical Dose of Pretomanid Abstract Pretomanid was approved by the U.S. FDA, via the limited population pathway for antibacterial and antifungal drugs, as part of a three-drug regimen with bedaquiline and linezolid for the treatment of extensively drug-resistant and treatment-in... |
PMC4967091 | core_pubmed_pmc | Kinetics of Clobetasol-17-Propionate in Psoriatic Lesional and Non-Lesional Skin Assessed by Dermal Open Flow Microperfusion with Time and Space Resolution | Kinetics of Clobetasol-17-Propionate in Psoriatic Lesional and Non-Lesional Skin Assessed by Dermal Open Flow Microperfusion with Time and Space Resolution Abstract Abstract Purpose To evaluate the kinetics of topically applied clobetasol-17-propionate (CP-17) in lesional and non-lesional psoriatic skin when released f... |
PMC4042458 | core_pubmed_pmc | Physiologically Based Pharmacokinetic Modeling Framework for Quantitative Prediction of an Herb–Drug Interaction | Physiologically Based Pharmacokinetic Modeling Framework for Quantitative Prediction of an Herb–Drug Interaction Abstract Abstract Herb–drug interaction predictions remain challenging. Physiologically based pharmacokinetic (PBPK) modeling was used to improve prediction accuracy of potential herb–drug interactions using... |
PMC10223110 | core_pubmed_pmc | An Automated Customizable Live Web Crawler for Curation of Comparative Pharmacokinetic Data: An Intelligent Compilation of Research-Based Comprehensive Article Repository | An Automated Customizable Live Web Crawler for Curation of Comparative Pharmacokinetic Data: An Intelligent Compilation of Research-Based Comprehensive Article Repository Abstract Abstract Data curation has significant research implications irrespective of application areas. As most curated studies rely on databases fo... |
PMC9242541 | core_pubmed_pmc | Importance of Rare DPYD Genetic Polymorphisms for 5-Fluorouracil Therapy in the Japanese Population | Importance of Rare DPYD Genetic Polymorphisms for 5-Fluorouracil Therapy in the Japanese Population Abstract Abstract Dihydropyrimidine dehydrogenase (DPD), encoded by the DPYD gene, is the rate-limiting enzyme in 5-fluorouracil (5-FU) degradation. In Caucasians, four DPYD risk variants are recognized to be responsible... |
PMC11937985 | core_pubmed_pmc | In Vitro Evaluation of CYP‐Mediated Metabolism of Fezolinetant and Pharmacokinetic Interaction Between Fezolinetant and Fluvoxamine in Healthy Postmenopausal Smokers and Nonsmokers | In Vitro Evaluation of CYP‐Mediated Metabolism of Fezolinetant and Pharmacokinetic Interaction Between Fezolinetant and Fluvoxamine in Healthy Postmenopausal Smokers and Nonsmokers Abstract Abstract Fezolinetant is an oral, nonhormonal, neurokinin 3 receptor antagonist treatment option for moderate to severe vasomotor ... |
PMC8589356 | core_pubmed_pmc | A single‐center, open‐label, randomized cross‐over study to evaluate the pharmacokinetics and bioavailability of once‐daily prolonged‐release formulations of tacrolimus in de novo liver transplant recipients | A single‐center, open‐label, randomized cross‐over study to evaluate the pharmacokinetics and bioavailability of once‐daily prolonged‐release formulations of tacrolimus in de novo liver transplant recipients Abstract Abstract Background The narrow therapeutic window of tacrolimus (Tac) requires intense drug monitoring ... |
PMC3666194 | core_pubmed_pmc | Amphetamine, past and present – a pharmacological and clinical perspective | Amphetamine, past and present – a pharmacological and clinical perspective Abstract Abstract Amphetamine was discovered over 100 years ago. Since then, it has transformed from a drug that was freely available without prescription as a panacea for a broad range of disorders into a highly restricted Controlled Drug with ... |
PMC6630509 | core_pubmed_pmc | Intracellular PD Modelling ( PD i ) for the Prediction of Clinical Activity of Increased Rifampicin Dosing | Intracellular PD Modelling ( PD i ) for the Prediction of Clinical Activity of Increased Rifampicin Dosing Abstract Abstract Increasing rifampicin (RIF) dosages could significantly reduce tuberculosis (TB) treatment durations. Understanding the pharmacokinetic-pharmacodynamics (PK–PD) of increasing RIF dosages could in... |
PMC8286666 | core_pubmed_pmc | Pharmacokinetics of Dexamethasone when Administered with Fosaprepitant for Chemotherapy-Induced Nausea and Vomiting and Differences in Dose-Dependent Antiemetic Effects | Pharmacokinetics of Dexamethasone when Administered with Fosaprepitant for Chemotherapy-Induced Nausea and Vomiting and Differences in Dose-Dependent Antiemetic Effects Abstract Background: Fosaprepitant, an NK 1 receptor antagonist, inhibits and induces cytochrome P450 3A4 (CYP3A4) as its substrate. Contrarily dexamet... |
PMC11294697 | core_pubmed_pmc | In vivo pharmacokinetics of Glycyrrhiza uralensis polysaccharides | In vivo pharmacokinetics of Glycyrrhiza uralensis polysaccharides Abstract Glycyrrhiza uralensis polysaccharides (GUPS) are widely applied in biomedicine and functional food due to their multiple pharmacological activities and low toxicity. Despite their widespread use, the in vivo metabolic profile of GUPS remains poo... |
PMC10022862 | core_pubmed_pmc | A First-in-Human Phase I Study of Milademetan, an MDM2 Inhibitor, in Patients With Advanced Liposarcoma, Solid Tumors, or Lymphomas | A First-in-Human Phase I Study of Milademetan, an MDM2 Inhibitor, in Patients With Advanced Liposarcoma, Solid Tumors, or Lymphomas Abstract PURPOSE This study evaluated the safety, pharmacokinetics, pharmacodynamics, and preliminary efficacy of milademetan, a small-molecule murine double minute-2 (MDM2) inhibitor, in ... |
PMC11544453 | core_pubmed_pmc | Effect of concomitant use of yokukansan on steady‐state blood concentrations of donepezil and risperidone in real‐world clinical practice | Effect of concomitant use of yokukansan on steady‐state blood concentrations of donepezil and risperidone in real‐world clinical practice Abstract Abstract Aim Yokukansan is one of the most frequently used herbal medicines that can improve the behavioral and psychological symptoms of dementia. In this exploratory study... |
PMC10638197 | core_pubmed_pmc | An IQ consortium analysis of starting dose selection for oncology small molecule first-in-patient trials suggests an alternative NOAEL-based method can be safe while reducing time to the recommended phase 2 dose | An IQ consortium analysis of starting dose selection for oncology small molecule first-in-patient trials suggests an alternative NOAEL-based method can be safe while reducing time to the recommended phase 2 dose Abstract The first-in-patient (FIP) starting dose for oncology agents should be reasonably safe and provide ... |
PMC7913401 | core_pubmed_pmc | Evaluating a tylosin dosage regimen for treatment of Staphylococcus delphini infection in mink ( Neovison vison ): a pharmacokinetic-pharmacodynamic approach | Evaluating a tylosin dosage regimen for treatment of Staphylococcus delphini infection in mink ( Neovison vison ): a pharmacokinetic-pharmacodynamic approach Abstract Abstract Staphylococcus delphini is one of the most common pathogens isolated from mink infections, especially dermatitis. Tylosin (TYL) is used frequent... |
PMC4198696 | core_pubmed_pmc | A Small-Molecule Inhibitor of PIM Kinases as a Potential Treatment for Urothelial Carcinomas 1 2 | A Small-Molecule Inhibitor of PIM Kinases as a Potential Treatment for Urothelial Carcinomas 1 2 Abstract Abstract The proto-oncogene proviral integration site for moloney murine leukemia virus (PIM) kinases (PIM-1, PIM-2, and PIM-3) are serine/threonine kinases that are involved in a number of signaling pathways impor... |
PMC4736693 | core_pubmed_pmc | Rapid model exploration for complex hierarchical data: application to pharmacokinetics of insulin aspart | Rapid model exploration for complex hierarchical data: application to pharmacokinetics of insulin aspart Abstract We consider situations, which are common in medical statistics, where we have a number of sets of response data, from different individuals, say, potentially under different conditions. A parametric model i... |
PMC7259451 | core_pubmed_pmc | Improvement of Pain Relief of Fentanyl Citrate Drug Encapsulated in Nanostructured Lipid Carrier: Drug Formulation, Parameter Optimization, in vitro and in vivo Studies | Improvement of Pain Relief of Fentanyl Citrate Drug Encapsulated in Nanostructured Lipid Carrier: Drug Formulation, Parameter Optimization, in vitro and in vivo Studies Abstract Abstract Introduction In this study, the encapsulation of fentanyl citrate as an opioid drug with hydrophobic nature in the nanostructured ... |
PMC7178751 | core_pubmed_pmc | Virotheranostics, a double-barreled viral gun pointed toward cancer; ready to shoot? | Virotheranostics, a double-barreled viral gun pointed toward cancer; ready to shoot? Abstract Compared with conventional cancer treatments, the main advantage of oncolytic virotherapy is its tumor-selective replication followed by the destruction of malignant cells without damaging healthy cells. Accordingly, this kind... |
PMC7745062 | core_pubmed_pmc | Discovery of highly selective and orally available benzimidazole-based phosphodiesterase 10 inhibitors with improved solubility and pharmacokinetic properties for treatment of pulmonary arterial hypertension | Discovery of highly selective and orally available benzimidazole-based phosphodiesterase 10 inhibitors with improved solubility and pharmacokinetic properties for treatment of pulmonary arterial hypertension Abstract Abstract Optimization efforts were devoted to discover novel PDE10A inhibitors in order to improve solu... |
PMC4691954 | core_pubmed_pmc | Pharmacodynamic monitoring of (immuno)proteasome inhibition during bortezomib treatment of a critically ill patient with lupus nephritis and myocarditis | Pharmacodynamic monitoring of (immuno)proteasome inhibition during bortezomib treatment of a critically ill patient with lupus nephritis and myocarditis Abstract Abstract Objective To describe the pharmacodynamic monitoring of (immuno)proteasome inhibition following treatment with bortezomib in a therapy-refractory sys... |
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