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PMC4356664 | core_pubmed_pmc | Development of an oral push–pull osmotic pump of fenofibrate-loaded mesoporous silica nanoparticles | Development of an oral push–pull osmotic pump of fenofibrate-loaded mesoporous silica nanoparticles Abstract In this study, mesoporous silica nanoparticles (MSNs) were used to prepare an oral push–pull osmotic pump. Fenofibrate, the selected model drug, was firstly loaded into the MSNs, followed by a suspending agent c... |
PMC7179606 | core_pubmed_pmc | Abacavir Exposure in Children Cotreated for Tuberculosis with Rifampin and Superboosted Lopinavir-Ritonavir | Abacavir Exposure in Children Cotreated for Tuberculosis with Rifampin and Superboosted Lopinavir-Ritonavir Abstract In children requiring lopinavir coformulated with ritonavir in a 4:1 ratio (lopinavir-ritonavir-4:1) and rifampin, adding ritonavir to achieve a 4:4 ratio with lopinavir (LPV/r-4:4) overcomes the drug-dr... |
PMC12955343 | core_pubmed_pmc | Population Pharmacokinetic Modeling Practice of Time‐Varying Clearance: Insights from a First‐in‐Human Study Case | Population Pharmacokinetic Modeling Practice of Time‐Varying Clearance: Insights from a First‐in‐Human Study Case Abstract Abstract Accurate characterization of time‐varying clearance (CL) is critical during early drug development, as it informs clinical study design and dosing strategies for future trials. However, de... |
PMC7704527 | core_pubmed_pmc | QSAR, molecular docking, design, and pharmacokinetic analysis of 2-(4-fluorophenyl) imidazol-5-ones as anti-breast cancer drug compounds against MCF-7 cell line | QSAR, molecular docking, design, and pharmacokinetic analysis of 2-(4-fluorophenyl) imidazol-5-ones as anti-breast cancer drug compounds against MCF-7 cell line Abstract The anti-proliferative activities of Novel series of 2-(4-fluorophenyl) imidazol-5-ones against MCF-7 breast cancer cell line were explored via in-sli... |
PMC6324689 | core_pubmed_pmc | A comparative pharmacokinetic study of PARP inhibitors demonstrates favorable properties for niraparib efficacy in preclinical tumor models | A comparative pharmacokinetic study of PARP inhibitors demonstrates favorable properties for niraparib efficacy in preclinical tumor models Abstract Abstract Niraparib is an orally bioavailable and selective poly (ADP-ribose) polymerase (PARP)-1/-2 inhibitor approved for maintenance treatment of both BRCA mutant (mut) ... |
PMC5889769 | core_pubmed_pmc | A Double-Blind, Placebo-Controlled, Phase II Study to Determine the Efficacy, Safety, Tolerability and Pharmacokinetics of a Controlled Release (CR) Formulation of Mazindol in Adults with DSM-5 Attention-Deficit/Hyperactivity Disorder (ADHD) | A Double-Blind, Placebo-Controlled, Phase II Study to Determine the Efficacy, Safety, Tolerability and Pharmacokinetics of a Controlled Release (CR) Formulation of Mazindol in Adults with DSM-5 Attention-Deficit/Hyperactivity Disorder (ADHD) Abstract Background Mazindol is under investigation for the treatment of atten... |
PMC8082156 | core_pubmed_pmc | Population Pharmacokinetics of Lithium in Young Pediatric Patients With Intellectual Disability | Population Pharmacokinetics of Lithium in Young Pediatric Patients With Intellectual Disability Abstract Abstract Background: Lithium is a well-established treatment for bipolar disorders and has been shown to be neuroprotective, and thus low doses might be useful for the treatment of childhood brain injury and neurolo... |
PMC12568798 | core_pubmed_pmc | Toward Regulatory Convergence and Streamlined Biosimilar Development: Recommendations from an International Qualitative Study | Toward Regulatory Convergence and Streamlined Biosimilar Development: Recommendations from an International Qualitative Study Abstract Abstract Objectives This study aims to assess perspectives of stakeholders on scientific and regulatory challenges associated with biosimilarity demonstration and to formulate consensus... |
PMC11244631 | core_pubmed_pmc | Adequacy of the Dosing and Infusion Time of Ceftazidime/Avibactam for the Treatment of Gram-Negative Bacterial Infections: A PK/PD Simulation Study | Adequacy of the Dosing and Infusion Time of Ceftazidime/Avibactam for the Treatment of Gram-Negative Bacterial Infections: A PK/PD Simulation Study Abstract Abstract Introduction Recent studies suggested the potential benefits of extended infusion times to optimize the treatment efficacy of ceftazidime/avibactam, which... |
PMC5468495 | core_pubmed_pmc | Large-scale pharmacogenomic study of sulfonylureas and the QT, JT, and QRS intervals: CHARGE Pharmacogenomics Working Group | Large-scale pharmacogenomic study of sulfonylureas and the QT, JT, and QRS intervals: CHARGE Pharmacogenomics Working Group Abstract Sulfonylureas, a commonly-used class of medication used to treat type 2 diabetes, have been associated with an increased risk of cardiovascular disease. Their effects on QT interval durat... |
PMC12033145 | core_pubmed_pmc | Safety of bronchial artery infusion immunotherapy: from comparative analysis in beagle canines to clinical validation | Safety of bronchial artery infusion immunotherapy: from comparative analysis in beagle canines to clinical validation Abstract Background Despite advancements in systemic chemotherapy and immune checkpoint inhibitors (ICIs), advanced non-small cell lung cancer (NSCLC) continues to exhibit poor prognosis, underscoring a... |
PMC3135080 | core_pubmed_pmc | Age-Related Changes in the Hepatic Pharmacology and Toxicology of Paracetamol | Age-Related Changes in the Hepatic Pharmacology and Toxicology of Paracetamol Abstract Abstract Optimal pharmacotherapy is determined when the pharmacokinetics and pharmacodynamics of the drug are understood. However, the age-related changes in pharmacokinetics and pharmacodynamics, as well as the increased interindivi... |
PMC3968086 | core_pubmed_pmc | Review of extended-release formulations of Tramadol for the management of chronic non-cancer pain: focus on marketed formulations | Review of extended-release formulations of Tramadol for the management of chronic non-cancer pain: focus on marketed formulations Abstract Abstract Patients with chronic non-malignant pain report impairments of physical, social, and psychological well-being. The goal of pain management should include reducing pain and ... |
PMC11945186 | core_pubmed_pmc | Physiologically Based Pharmacokinetic Modeling of Tofacitinib: Predicting Drug Exposure and Optimizing Dosage in Special Populations and Drug–Drug Interaction Scenarios | Physiologically Based Pharmacokinetic Modeling of Tofacitinib: Predicting Drug Exposure and Optimizing Dosage in Special Populations and Drug–Drug Interaction Scenarios Abstract Background: Tofacitinib is mainly used in the adult population for immune-mediated inflammatory diseases. There is little information availabl... |
PMC6437426 | core_pubmed_pmc | Differences between intravenous iron products: focus on treatment of iron deficiency in chronic heart failure patients | Differences between intravenous iron products: focus on treatment of iron deficiency in chronic heart failure patients Abstract Abstract Iron deficiency is the leading cause of anaemia and is highly prevalent in patients with chronic heart failure (CHF). Iron deficiency, with or without anaemia, can be corrected with i... |
PMC11102454 | core_pubmed_pmc | Enhancing in vivo cell and tissue targeting by modulation of polymer nanoparticles and macrophage decoys | Enhancing in vivo cell and tissue targeting by modulation of polymer nanoparticles and macrophage decoys Abstract Abstract The in vivo efficacy of polymeric nanoparticles (NPs) is dependent on their pharmacokinetics, including time in circulation and tissue tropism. Here we explore the structure-function relationships ... |
PMC9971821 | core_pubmed_pmc | Refinement and calibration of a human PBPK model for the plasticiser, Di-(2-propylheptyl) phthalate (DPHP) using in silico , in vitro and human biomonitoring data | Refinement and calibration of a human PBPK model for the plasticiser, Di-(2-propylheptyl) phthalate (DPHP) using in silico , in vitro and human biomonitoring data Abstract An existing physiologically based pharmacokinetic model for Di-(2-propylheptyl) phthalate (DPHP) was refined to improve the simulations of the venou... |
PMC10675618 | core_pubmed_pmc | A Critical Analysis of the FDA’s Omics-Driven Pharmacodynamic Biomarkers to Establish Biosimilarity | A Critical Analysis of the FDA’s Omics-Driven Pharmacodynamic Biomarkers to Establish Biosimilarity Abstract Demonstrating biosimilarity entails comprehensive analytical assessment, clinical pharmacology profiling, and efficacy testing in patients for at least one medical indication, as required by the U.S. Biologics P... |
PMC8435708 | core_pubmed_pmc | A Review of CYP3A Drug-Drug Interaction Studies: Practical Guidelines for Patients Using Targeted Oral Anticancer Drugs | A Review of CYP3A Drug-Drug Interaction Studies: Practical Guidelines for Patients Using Targeted Oral Anticancer Drugs Abstract Many oral anticancer drugs are metabolized by CYP3A. Clinical drug-drug interaction (DDI) studies often only examine the effect of strong CYP3A inhibitors and inducers. The effect of moderate... |
PMC12679040 | core_pubmed_pmc | Clinical trial on the pharmacokinetics, pharmacodynamics and safety of tolvaptan in healthy Chinese males: an open-label, single and multiple dosage, parallel group study | Clinical trial on the pharmacokinetics, pharmacodynamics and safety of tolvaptan in healthy Chinese males: an open-label, single and multiple dosage, parallel group study Abstract Abstract Background To determine the pharmacokinetics (PK), pharmacodynamics (PD) and safety of tolvaptan in healthy Chinese males. Methods ... |
PMC12108255 | core_pubmed_pmc | Pharmacokinetic Characteristics of a Single Cannabidiol Dose in Oil and Treat Forms and Health Impacts After 30 Days of Administration in Dogs | Pharmacokinetic Characteristics of a Single Cannabidiol Dose in Oil and Treat Forms and Health Impacts After 30 Days of Administration in Dogs Abstract Simple Summary This study evaluated the comparative plasma pharmacokinetics of two oral CBD formulations—oil-based (5 mg/kg) and treat-mixed (50 mg)—in dogs following a... |
PMC12184483 | core_pubmed_pmc | A comparative study of intramuscular versus epidural administration of follicle-stimulating hormone for embryo production in Wagyu Cattle | A comparative study of intramuscular versus epidural administration of follicle-stimulating hormone for embryo production in Wagyu Cattle Abstract Abstract Background: The increasing demand for high-quality livestock products necessitates the optimization of reproductive technologies, particularly superovulation and em... |
PMC8449650 | core_pubmed_pmc | TPGS-Modified Long-Circulating Liposomes Loading Ziyuglycoside I for Enhanced Therapy of Myelosuppression | TPGS-Modified Long-Circulating Liposomes Loading Ziyuglycoside I for Enhanced Therapy of Myelosuppression Abstract Background Ziyuglycoside I (ZgI), an active ingredient isolated from traditional Chinese medicine Sanguisorba officinalis L, has been demonstrated to increase the leucocytes and protect hematopoietic stem ... |
PMC10044130 | core_pubmed_pmc | Hypoalbuminemia and Pharmacokinetics: When the Misunderstanding of a Fundamental Concept Leads to Repeated Errors over Decades | Hypoalbuminemia and Pharmacokinetics: When the Misunderstanding of a Fundamental Concept Leads to Repeated Errors over Decades Abstract Surprisingly, misinterpretation of the influence of hypoalbuminemia on pharmacokinetics and the clinical effects of drugs seems to be a current problem, even though hypoalbuminemia has... |
PMC4359184 | core_pubmed_pmc | Pharmacokinetics of Cefozopran by Single and Multiple Intravenous Infusions in Healthy Chinese Volunteers | Pharmacokinetics of Cefozopran by Single and Multiple Intravenous Infusions in Healthy Chinese Volunteers Abstract Background and Objectives Cefozopran is a parenteral cephalosporin with a broad spectrum of activity against Gram-positive and Gram-negative bacteria. The objective of this study was to evaluate the pharma... |
PMC5001226 | core_pubmed_pmc | An Overview of Concentrated Insulin Products | An Overview of Concentrated Insulin Products Abstract IN BRIEF This article provides a summary of the use of available concentrated insulins in the outpatient treatment of patients with diabetes. Concentrated insulins work through the same mechanisms as other insulin products. They vary from each other in concentration... |
PMC7099657 | core_pubmed_pmc | Network Pharmacology-Based Dissection of the Anti-diabetic Mechanism of Lobelia chinensis | Network Pharmacology-Based Dissection of the Anti-diabetic Mechanism of Lobelia chinensis Abstract Diabetes mellitus (DM) is a chronic inflammatory disease, and the rapidly increasing DM is becoming a major problem of global public health. Traditional Chinese medicine (TCM) has a long history of treating diabetes. It h... |
PMC5355968 | core_pubmed_pmc | A Study on CYP2C19 and CYP2D6 Polymorphic Effects on Pharmacokinetics and Pharmacodynamics of Amitriptyline in Healthy Koreans | A Study on CYP2C19 and CYP2D6 Polymorphic Effects on Pharmacokinetics and Pharmacodynamics of Amitriptyline in Healthy Koreans Abstract Abstract We performed a double‐blinded, genotype‐based stratification study to explore the pharmacokinetics and pharmacodynamics of amitriptyline according to CYP2C19 and CYP2D6 genoty... |
PMC12034907 | core_pubmed_pmc | Drug–Drug Interaction Potential of Mavacamten with Midazolam: Combined Results from Clinical and Model‐Based Studies | Drug–Drug Interaction Potential of Mavacamten with Midazolam: Combined Results from Clinical and Model‐Based Studies Abstract Abstract Mavacamten is a potential inducer of cytochrome P450 (CYP) 3A4 and could reduce the effectiveness of concomitant drugs that are metabolized by CYP3A4, such as midazolam. This study aime... |
PMC7383779 | core_pubmed_pmc | Pharmacokinetics and safety of VALTOCO (NRL‐1; diazepam nasal spray) in patients with epilepsy during seizure (ictal/peri‐ictal) and nonseizure (interictal) conditions: A phase 1, open‐label study | Pharmacokinetics and safety of VALTOCO (NRL‐1; diazepam nasal spray) in patients with epilepsy during seizure (ictal/peri‐ictal) and nonseizure (interictal) conditions: A phase 1, open‐label study Abstract Abstract Objective To assess pharmacokinetics and safety of diazepam nasal spray (NRL‐1; VALTOCO®) in pediatric an... |
PMC8817205 | core_pubmed_pmc | A Novel Approach for Quantifying the Pharmacological Activity of T-Cell Engagers Utilizing In Vitro Time Course Experiments and Streamlined Data Analysis | A Novel Approach for Quantifying the Pharmacological Activity of T-Cell Engagers Utilizing In Vitro Time Course Experiments and Streamlined Data Analysis Abstract CD3-bispecific antibodies are a new class of immunotherapeutic drugs against cancer. The pharmacological activity of CD3-bispecifics is typically assessed th... |
PMC10303160 | core_pubmed_pmc | Pharmacokinetics of Venetoclax Co-Administered with Posaconazole in Patients with Acute Myeloid Leukemia | Pharmacokinetics of Venetoclax Co-Administered with Posaconazole in Patients with Acute Myeloid Leukemia Abstract Abstract The Food and Drug Administration currently approves the combination of hypomethylating agents (HMA), azacytidine or decitabine with venetoclax (VEN) for acute myeloid leukemia (AML) patients aged m... |
PMC4464358 | core_pubmed_pmc | Clinical pharmacology of atypical antipsychotics: an update | Clinical pharmacology of atypical antipsychotics: an update Abstract Abstract This review will concentrate on the clinical pharmacology, in particular pharmacodynamic data, related to atypical antipsychotics, clozapine, risperidone, paliperidone, olanzapine, que¬tiapine, amisulpride, ziprasidone, aripiprazole, asenapin... |
PMC5036423 | core_pubmed_pmc | Population Pharmacokinetics and Pharmacodynamics of the Calcimimetic Etelcalcetide in Chronic Kidney Disease and Secondary Hyperparathyroidism Receiving Hemodialysis | Population Pharmacokinetics and Pharmacodynamics of the Calcimimetic Etelcalcetide in Chronic Kidney Disease and Secondary Hyperparathyroidism Receiving Hemodialysis Abstract Etelcalcetide is a novel calcimimetic in development for the treatment of secondary hyperparathyroidism (SHPT). A population pharmacokinetic/phar... |
PMC7924840 | core_pubmed_pmc | In Silico Simulation of the Systemic Drug Exposure Following the Topical Application of Opioid Analgesics in Patients with Cutaneous Lesions | In Silico Simulation of the Systemic Drug Exposure Following the Topical Application of Opioid Analgesics in Patients with Cutaneous Lesions Abstract The use of opioid analgesics in treating severe pain is frequently associated with putative adverse effects in humans. Topical agents that are shown to have high efficacy... |
PMC7722354 | core_pubmed_pmc | 7-Substituted 2-Nitro-5,6-dihydroimidazo[2,1- b ][1,3]oxazines: Novel Antitubercular Agents Lead to a New Preclinical Candidate for Visceral Leishmaniasis | 7-Substituted 2-Nitro-5,6-dihydroimidazo[2,1- b ][1,3]oxazines: Novel Antitubercular Agents Lead to a New Preclinical Candidate for Visceral Leishmaniasis Abstract Within a backup program for the clinical investigational agent pretomanid (PA-824), scaffold hopping from delamanid inspired the discovery of a novel class ... |
PMC11940597 | core_pubmed_pmc | Effects of sleeve gastrectomy and Roux-en-Y gastric bypass on the pharmacokinetics of gabapentin and pregabalin: A cohort study | Effects of sleeve gastrectomy and Roux-en-Y gastric bypass on the pharmacokinetics of gabapentin and pregabalin: A cohort study Abstract Background Bariatric surgery may affect the pharmacokinetics of medications by altering the gastrointestinal physiology. Pharmacokinetic changes of first-line neuropathic pain medicat... |
PMC11920646 | core_pubmed_pmc | Novel selective glucocorticoid receptor modulator GRM-01 demonstrates dissociation of anti-inflammatory effects from adverse effects on glucose and bone metabolism | Novel selective glucocorticoid receptor modulator GRM-01 demonstrates dissociation of anti-inflammatory effects from adverse effects on glucose and bone metabolism Abstract Introduction The development of selective GR agonist and modulators (SEGRAMs) aimed to minimize the adverse effects of chronic glucocorticoid treat... |
PMC7564881 | core_pubmed_pmc | A Simplified Iohexol-Based Method to Measure Renal Function in Sheep Models of Renal Disease | A Simplified Iohexol-Based Method to Measure Renal Function in Sheep Models of Renal Disease Abstract Abstract Sheep are highly adequate models for human renal diseases because of their many similarities in the histology and physiology of kidney and pathogenesis of kidney diseases. However, the lack of a simple method ... |
PMC9365822 | core_pubmed_pmc | The unique second wave phenomenon in contrast enhanced ultrasound imaging with nanobubbles | The unique second wave phenomenon in contrast enhanced ultrasound imaging with nanobubbles Abstract Investigation of nanobubble (NB) pharmacokinetics in contrast-enhanced ultrasound (CEUS) at the pixel level shows a unique phenomenon where the first pass of the contrast agent bolus is accompanied by a second wave. This... |
PMC12317694 | core_pubmed_pmc | Identification of potential inhibitors of the main protease from feline infectious peritonitis virus using molecular docking and dynamic simulation approaches | Identification of potential inhibitors of the main protease from feline infectious peritonitis virus using molecular docking and dynamic simulation approaches Abstract Abstract Background Feline infectious peritonitis virus (FIPV) is one of cats’ most serious viral infections. The FIPV infection induces a complicated s... |
PMC5531494 | core_pubmed_pmc | Target specificity, in vivo pharmacokinetics, and efficacy of the putative STAT3 inhibitor LY5 in osteosarcoma, Ewing's sarcoma, and rhabdomyosarcoma | Target specificity, in vivo pharmacokinetics, and efficacy of the putative STAT3 inhibitor LY5 in osteosarcoma, Ewing's sarcoma, and rhabdomyosarcoma Abstract Background STAT3 is a transcription factor involved in cytokine and receptor kinase signal transduction that is aberrantly activated in a variety of sarcomas, pr... |
PMC4948726 | core_pubmed_pmc | Population pharmacokinetic modeling of glibenclamide in poorly controlled South African type 2 diabetic subjects | Population pharmacokinetic modeling of glibenclamide in poorly controlled South African type 2 diabetic subjects Abstract Aim The aim of this study was to describe the pharmacokinetics (PK) of glibenclamide in poorly controlled South African type 2 diabetic subjects using noncompartmental and model-based methods. Metho... |
PMC6723750 | core_pubmed_pmc | Pharmacokinetics of Intravitreal Anti-VEGF Drugs in Age-Related Macular Degeneration | Pharmacokinetics of Intravitreal Anti-VEGF Drugs in Age-Related Macular Degeneration Abstract Abstract Intravitreal administration of anti-vascular endothelial growth factor (VEGF) antibodies has become the standard treatment for Age-Related Macular Degeneration; however, the knowledge of their pharmacokinetics is limi... |
PMC3261979 | core_pubmed_pmc | A Mechanistic Modeling Framework for Predicting Metabolic Interactions in Complex Mixtures | A Mechanistic Modeling Framework for Predicting Metabolic Interactions in Complex Mixtures Abstract Abstract Background: Computational modeling of the absorption, distribution, metabolism, and excretion of chemicals is now theoretically able to describe metabolic interactions in realistic mixtures of tens to hundreds o... |
PMC11684029 | core_pubmed_pmc | Discovery of VU6024578/BI02982816: An mGlu 1 Positive Allosteric Modulator with Efficacy in Preclinical Antipsychotic and Cognition Models | Discovery of VU6024578/BI02982816: An mGlu 1 Positive Allosteric Modulator with Efficacy in Preclinical Antipsychotic and Cognition Models Abstract Herein, we report progress toward a metabotropic glutamate receptor subtype 1 (mGlu 1 ) positive allosteric modulator (PAM) clinical candidate and the discovery of VU602457... |
PMC6615779 | core_pubmed_pmc | RAIN study: a protocol for a randomised controlled trial evaluating efficacy, safety and cost-effectiveness of intravenous-to-oral antibiotic switch therapy in neonates with a probable bacterial infection | RAIN study: a protocol for a randomised controlled trial evaluating efficacy, safety and cost-effectiveness of intravenous-to-oral antibiotic switch therapy in neonates with a probable bacterial infection Abstract Abstract Introduction High morbidity and mortality rates of proven bacterial infection are the main reason... |
PMC11825552 | core_pubmed_pmc | Population pharmacokinetic model of tranexamic acid in patients who undergo cardiac surgery with cardiopulmonary bypass | Population pharmacokinetic model of tranexamic acid in patients who undergo cardiac surgery with cardiopulmonary bypass Abstract Purpose Tranexamic acid (TXA) is widely used as an antifibrinolytic drug. However, studies to determine the optimal blood concentration of TXA have produced inconsistent results. During cardi... |
PMC6194917 | core_pubmed_pmc | Training a Drug to Do New Tricks: Insights on Stability of Meropenem Administered as a Continuous Infusion | Training a Drug to Do New Tricks: Insights on Stability of Meropenem Administered as a Continuous Infusion Abstract Abstract Background: The antibiotic armamentarium used to combat multi-drug resistant organisms (MDROs) include carbapenems. Continuous infusion (CI) dosing is frequently employed to maximize beta-lactam ... |
PMC12418826 | core_pubmed_pmc | Pharmacometric modeling of lipid nanoparticle-encapsulated mRNA therapeutics and vaccines: A systematic review | Pharmacometric modeling of lipid nanoparticle-encapsulated mRNA therapeutics and vaccines: A systematic review Abstract Abstract Significant progress has been made in the development of lipid nanoparticle (LNP)-encapsulated messenger RNA (mRNA)-based modalities with numerous candidates entering clinical trials. These n... |
PMC11728219 | core_pubmed_pmc | Efficacy of the Once-Daily Tacrolimus Formulation LCPT Compared to the Immediate-Release Formulation in Preventing Early Post-Transplant Diabetes in High-Risk Kidney Transplant Patients: A Randomized, Controlled, Open-Label Pilot Study (EUDRACT: 2017-000718-52) | Efficacy of the Once-Daily Tacrolimus Formulation LCPT Compared to the Immediate-Release Formulation in Preventing Early Post-Transplant Diabetes in High-Risk Kidney Transplant Patients: A Randomized, Controlled, Open-Label Pilot Study (EUDRACT: 2017-000718-52) Abstract Abstract Background/Objectives : Post-transplant ... |
PMC8154366 | core_pubmed_pmc | Lifetime Accumulation of Microplastic in Children and Adults | Lifetime Accumulation of Microplastic in Children and Adults Abstract Human exposure to microplastic is recognized as a global problem, but the uncertainty, variability, and lifetime accumulation are unresolved. We provide a probabilistic lifetime exposure model for children and adults, which accounts for intake via ei... |
PMC8858223 | core_pubmed_pmc | Novel inhibitors of phosphorylation independent activity of GRK2 modulate cAMP signaling | Novel inhibitors of phosphorylation independent activity of GRK2 modulate cAMP signaling Abstract Abstract G protein‐coupled receptors kinase 2 (GRK2) plays a major role in receptor regulation and, as a consequence, in cell biology and physiology. GRK2‐mediated receptor desensitization is performed by its kinase domain... |
PMC7823305 | core_pubmed_pmc | Food–Drug Interactions with Fruit Juices | Food–Drug Interactions with Fruit Juices Abstract Fruit juices contain a large number of phytochemicals that, in combination with certain drugs, can cause food–drug interactions that can be clinically significant and lead to adverse events. The mechanisms behind such interactions are in most cases related to phytochemi... |
PMC8841492 | core_pubmed_pmc | Adapting regulatory drug‐drug interaction guidance to design clinical pharmacokinetic natural product‐drug interaction studies: A NaPDI Center recommended approach | Adapting regulatory drug‐drug interaction guidance to design clinical pharmacokinetic natural product‐drug interaction studies: A NaPDI Center recommended approach Abstract Abstract Pharmacokinetic drug interactions precipitated by botanical and other natural products (NPs) remain critically understudied. Investigating... |
PMC10223897 | core_pubmed_pmc | A phase I study comparing the biosimilarity of the pharmacokinetics and safety of recombinant humanized anti-vascular endothelial growth factor monoclonal antibody injection with Avastin ® in healthy Chinese male subjects | A phase I study comparing the biosimilarity of the pharmacokinetics and safety of recombinant humanized anti-vascular endothelial growth factor monoclonal antibody injection with Avastin ® in healthy Chinese male subjects Abstract Abstract Background The biosimilar landscape for malignancies continues to grow, with sev... |
PMC11252542 | core_pubmed_pmc | Individualized, dynamic, and full-course vancomycin dosing prediction: a study on the customized dose model | Individualized, dynamic, and full-course vancomycin dosing prediction: a study on the customized dose model Abstract Abstract Purpose The single-point trough-based therapeutic drug monitoring (TDM) and Bayesian forecasting approaches are still limited in individualized and dynamic vancomycin delivery. Until recently, t... |
PMC8505376 | core_pubmed_pmc | Current Ceftriaxone Dose Recommendations are Adequate for Most Critically Ill Children: Results of a Population Pharmacokinetic Modeling and Simulation Study | Current Ceftriaxone Dose Recommendations are Adequate for Most Critically Ill Children: Results of a Population Pharmacokinetic Modeling and Simulation Study Abstract Abstract Background and Objective Ceftriaxone is a cornerstone antibiotic for critically ill children with severe infections. Despite its widespread use,... |
PMC10497097 | core_pubmed_pmc | In vitro Antimicrobial Activity and Dose Optimization of Eravacycline and Other Tetracycline Derivatives Against Levofloxacin-Non-Susceptible and/or Trimethoprim-Sulfamethoxazole-Resistant Stenotrophomonas maltophilia | In vitro Antimicrobial Activity and Dose Optimization of Eravacycline and Other Tetracycline Derivatives Against Levofloxacin-Non-Susceptible and/or Trimethoprim-Sulfamethoxazole-Resistant Stenotrophomonas maltophilia Abstract Abstract Purpose To better guide clinical use, we determined the in vitro antimicrobial activ... |
PMC12851796 | core_pubmed_pmc | Midkine as a therapeutic node in NF1-driven neuro-oncology: Biology, biomarkers, and translational strategies | Midkine as a therapeutic node in NF1-driven neuro-oncology: Biology, biomarkers, and translational strategies Abstract Abstract Neurofibromatosis type 1 (NF1) produces a permissive neuro-oncologic milieu by disabling neurofibromin’s GTPase-activating control over RAS, thereby exaggerating RAF–MEK–ERK and PI3K–AKT signa... |
PMC10725263 | core_pubmed_pmc | Physiologically based mechanistic insight into differential risk of valproate hepatotoxicity between children and adults: A focus on ontogeny impact | Physiologically based mechanistic insight into differential risk of valproate hepatotoxicity between children and adults: A focus on ontogeny impact Abstract Abstract The anticonvulsant valproic acid (VPA) despite complex pharmacokinetics has been in clinical use for nearly 6 decades. Previous reports indicated neonate... |
PMC2898707 | core_pubmed_pmc | Use of silkworms for identification of drug candidates having appropriate pharmacokinetics from plant sources | Use of silkworms for identification of drug candidates having appropriate pharmacokinetics from plant sources Abstract Abstract Background We use silkworms to evaluate therapeutic effects of drug candidates. Our previous reports have revealed that there are common mechanisms of pharmacokinetics of chemicals in silkworm... |
PMC5398698 | core_pubmed_pmc | Uncovering the molecular and physiological processes of anticancer leads binding human serum albumin: A physical insight into drug efficacy | Uncovering the molecular and physiological processes of anticancer leads binding human serum albumin: A physical insight into drug efficacy Abstract Abstract Human serum albumin (HSA) has its ability to bind drug molecules and influence their efficacies. Although anticancer leads NSC48693 and NSC290956 functioned at th... |
PMC8365785 | core_pubmed_pmc | A randomised, placebo-controlled study of RIPK1 inhibitor GSK2982772 in patients with active ulcerative colitis | A randomised, placebo-controlled study of RIPK1 inhibitor GSK2982772 in patients with active ulcerative colitis Abstract Objective Tumour necrosis factor signalling via the receptor-interacting protein kinase 1 (RIPK1) pathway regulates colonic inflammation suggesting that RIPK1 inhibition may be a potential therapeuti... |
PMC8614878 | core_pubmed_pmc | Dose Optimization of Vancomycin for Critically Ill Patients Undergoing CVVH: A Prospective Population PK/PD Analysis | Dose Optimization of Vancomycin for Critically Ill Patients Undergoing CVVH: A Prospective Population PK/PD Analysis Abstract The optimal dose of vancomycin in critically ill patients receiving continuous venovenous hemofiltration (CVVH) remains unclear. The objective of this study was to identify factors that signific... |
PMC5110709 | core_pubmed_pmc | Improving the estimation of parameter uncertainty distributions in nonlinear mixed effects models using sampling importance resampling | Improving the estimation of parameter uncertainty distributions in nonlinear mixed effects models using sampling importance resampling Abstract Taking parameter uncertainty into account is key to make drug development decisions such as testing whether trial endpoints meet defined criteria. Currently used methods for as... |
PMC11054576 | core_pubmed_pmc | Dietary Influence on Drug Efficacy: A Comprehensive Review of Ketogenic Diet–Pharmacotherapy Interactions | Dietary Influence on Drug Efficacy: A Comprehensive Review of Ketogenic Diet–Pharmacotherapy Interactions Abstract It is widely acknowledged that the ketogenic diet (KD) has positive physiological effects as well as therapeutic benefits, particularly in the treatment of chronic diseases. Maintaining nutritional ketosis... |
PMC5733816 | core_pubmed_pmc | Safety and Tolerability Study of an Intravenously Administered Small Interfering Ribonucleic Acid (siRNA) Post On-Pump Cardiothoracic Surgery in Patients at Risk of Acute Kidney Injury | Safety and Tolerability Study of an Intravenously Administered Small Interfering Ribonucleic Acid (siRNA) Post On-Pump Cardiothoracic Surgery in Patients at Risk of Acute Kidney Injury Abstract Abstract Introduction Patients undergoing on-pump cardiac surgery are at an increased risk of acute kidney injury. QPI-1002, a... |
PMC3622027 | core_pubmed_pmc | Glucose-Reducing Effect of the ORMD-0801 Oral Insulin Preparation in Patients with Uncontrolled Type 1 Diabetes: A Pilot Study | Glucose-Reducing Effect of the ORMD-0801 Oral Insulin Preparation in Patients with Uncontrolled Type 1 Diabetes: A Pilot Study Abstract The unpredictable behavior of uncontrolled type 1 diabetes often involves frequent swings in blood glucose levels that impact maintenance of a daily routine. An intensified insulin reg... |
PMC5808105 | core_pubmed_pmc | Sublingual Administration of Sildenafil Oro-dispersible Film: New Profiles of Drug Tolerability and Pharmacokinetics for PDE5 Inhibitors | Sublingual Administration of Sildenafil Oro-dispersible Film: New Profiles of Drug Tolerability and Pharmacokinetics for PDE5 Inhibitors Abstract Abstract Objective: Type 5 phosphodiesterase inhibitors (PDE5i) are efficient drugs used for treatment of erectile dysfunction (ED); however, a large discontinuation rate due... |
PMC8892098 | core_pubmed_pmc | Emerging nanoformulation strategies for phytocompounds and applications from drug delivery to phototherapy to imaging | Emerging nanoformulation strategies for phytocompounds and applications from drug delivery to phototherapy to imaging Abstract Over thousands of years, natural bioactive compounds derived from plants (bioactive phytocompounds, BPCs) have been used worldwide to address human health issues. Today, they are a significant ... |
PMC12114922 | core_pubmed_pmc | Population Pharmacokinetics of Risperidone and Paliperidone in Schizophrenia: A Systematic Review | Population Pharmacokinetics of Risperidone and Paliperidone in Schizophrenia: A Systematic Review Abstract Background: The primary treatment of schizophrenia is pharmacotherapy with antipsychotic agents, such as risperidone and paliperidone. Population pharmacokinetic (PopPK) modelling plays a crucial role in optimisin... |
PMC9571880 | core_pubmed_pmc | Polygonum capitatum , the Hmong Medicinal Flora: A Comprehensive Review of Its Phytochemical, Pharmacological and Pharmacokinetic Characteristics | Polygonum capitatum , the Hmong Medicinal Flora: A Comprehensive Review of Its Phytochemical, Pharmacological and Pharmacokinetic Characteristics Abstract Abstract Polygonum capitatum , known as “Tou Hua Liao” (Chinese name), is a crucial source of Hmong medicinal plants that has benefited human health for a long time.... |
PMC3529624 | core_pubmed_pmc | Effect of renal impairment on the pharmacokinetics of prucalopride: a single- dose open-label Phase I study | Effect of renal impairment on the pharmacokinetics of prucalopride: a single- dose open-label Phase I study Abstract Objective To evaluate the pharmacokinetics of prucalopride in individuals with renal impairment (RI). Methods This open-label Phase I study (ClinicalTrials.gov identifier: NCT01674192 ) enrolled men and ... |
PMC12944365 | core_pubmed_pmc | Influence of CYP2D6 , CYP2C19 , and CYP2C9 Pharmacogenetics and Clinical Factors on Dose-Normalized Venlafaxine/O-Desmethylvenlafaxine Metabolic Ratio in Spanish Patients | Influence of CYP2D6 , CYP2C19 , and CYP2C9 Pharmacogenetics and Clinical Factors on Dose-Normalized Venlafaxine/O-Desmethylvenlafaxine Metabolic Ratio in Spanish Patients Abstract Background/Objectives : Venlafaxine has been reported to exhibit significant interindividual pharmacokinetic heterogeneity across population... |
PMC3622689 | core_pubmed_pmc | Single Cell Analysis of Drug Distribution by Intravital Imaging | Single Cell Analysis of Drug Distribution by Intravital Imaging Abstract Abstract Recent advances in the field of intravital imaging have for the first time allowed us to conduct pharmacokinetic and pharmacodynamic studies at the single cell level in live animal models. Due to these advances, there is now a critical ne... |
PMC11512831 | core_pubmed_pmc | Dose Individualisation of Antimicrobials from a Pharmacometric Standpoint: The Current Landscape | Dose Individualisation of Antimicrobials from a Pharmacometric Standpoint: The Current Landscape Abstract Successful antimicrobial therapy depends on achieving optimal drug concentrations within individual patients. Inter-patient variability in pharmacokinetics (PK) and differences in pathogen susceptibility (reflected... |
PMC8714187 | core_pubmed_pmc | Pharmacodynamics of Linezolid Plus Fosfomycin Against Vancomycin–Resistant Enterococcus faecium in a Hollow Fiber Infection Model | Pharmacodynamics of Linezolid Plus Fosfomycin Against Vancomycin–Resistant Enterococcus faecium in a Hollow Fiber Infection Model Abstract The optimal therapy for severe infections caused by vancomycin-resistant Enterococcus faecium (VREfm) remains unclear, but the combination of linezolid and fosfomycin may be a good ... |
PMC11259592 | core_pubmed_pmc | Demystifying physiologically based pharmacokinetic modelling among non-modelers towards model-informed medicine use in under-served populations. | Demystifying physiologically based pharmacokinetic modelling among non-modelers towards model-informed medicine use in under-served populations. Abstract Abstract Physiologically based pharmacokinetic (PBPK) models represent computational technology to characterize drug behavior within the context of detailed human phy... |
PMC10932481 | core_pubmed_pmc | Anti-thymic stromal lymphopoietin monoclonal antibody in patients with chronic rhinosinusitis with nasal polyps (DUBHE): Rationale and design of a multicenter, randomized, double-blind, placebo-controlled study | Anti-thymic stromal lymphopoietin monoclonal antibody in patients with chronic rhinosinusitis with nasal polyps (DUBHE): Rationale and design of a multicenter, randomized, double-blind, placebo-controlled study Abstract Background: Chronic rhinosinusitis with nasal polyps (CRSwNP) has a complex pathogenesis and is diff... |
PMC4789266 | core_pubmed_pmc | Bioequivalence study between two formulations of ciclosporin A (Cyclavance® oral solution and Atopica® soft capsules) following a single oral administration to dogs | Bioequivalence study between two formulations of ciclosporin A (Cyclavance® oral solution and Atopica® soft capsules) following a single oral administration to dogs Abstract Background Ciclosporin is a selective immunomodulator used for the treatment of atopic dermatitis in dogs . A new 100 mg/ml oral solution formulat... |
PMC12822413 | core_pubmed_pmc | TSHR‐Targeting Nucleic Acid Aptamer Treats Graves' Ophthalmopathy via Novel Allosteric Inhibition | TSHR‐Targeting Nucleic Acid Aptamer Treats Graves' Ophthalmopathy via Novel Allosteric Inhibition Abstract Abstract Graves' ophthalmopathy (GO) is an autoimmune disorder marked by orbital inflammation and tissue remodeling, leading to irreversible disfigurement and vision loss. The current first‐line glucocorticoid the... |
PMC11134298 | core_pubmed_pmc | Deciphering the Efficacy of β-Lactams in the Face of Metallo-β-Lactamase-Derived Resistance in Enterobacterales: Supraphysiologic Zinc in the Broth Is the Culprit | Deciphering the Efficacy of β-Lactams in the Face of Metallo-β-Lactamase-Derived Resistance in Enterobacterales: Supraphysiologic Zinc in the Broth Is the Culprit Abstract Abstract Background In vitro–in vivo discordance in β-lactams’ activities against metallo-ß-lactamase (MBL)-producing Enterobacterales has been desc... |
PMC5805805 | core_pubmed_pmc | A phase Ib study of everolimus combined with metformin for patients with advanced cancer | A phase Ib study of everolimus combined with metformin for patients with advanced cancer Abstract Summary Background The efficacy to monotherapy with the mTOR inhibitor everolimus in advanced cancer is often limited due to therapy resistance. Combining everolimus with metformin may decrease the chance of therapy resist... |
PMC10249992 | core_pubmed_pmc | Analysis of Dynamic Efficacy Endpoints of the Nix-TB Trial | Analysis of Dynamic Efficacy Endpoints of the Nix-TB Trial Abstract Abstract Background Safer, better, and shorter treatments for multidrug-resistant (MDR) and extensively drug-resistant (XDR) tuberculosis (TB) are an urgent global health need. The phase 3 clinical trial Nix-TB ( NCT02333799 ) tested a 6-month treatmen... |
PMC3572369 | core_pubmed_pmc | Population pharmacokinetics of phenytoin after intravenous administration of fosphenytoin sodium in pediatric patients, adult patients, and healthy volunteers | Population pharmacokinetics of phenytoin after intravenous administration of fosphenytoin sodium in pediatric patients, adult patients, and healthy volunteers Abstract Abstract Purpose We performed a population pharmacokinetic analysis of phenytoin after intravenous administration of fosphenytoin sodium in healthy, neu... |
PMC11597739 | core_pubmed_pmc | Quantifying Withanolides in Plasma: Pharmacokinetic Studies and Analytical Methods | Quantifying Withanolides in Plasma: Pharmacokinetic Studies and Analytical Methods Abstract Abstract Withania somnifera (common name: ashwagandha; WS) is an Ayurvedic botanical that has become popular for its reputed effects on stress and insomnia. Research into the bioactive compounds responsible for the biological ef... |
PMC9621185 | core_pubmed_pmc | First-in-human study of an OX40 (ivuxolimab) and 4-1BB (utomilumab) agonistic antibody combination in patients with advanced solid tumors | First-in-human study of an OX40 (ivuxolimab) and 4-1BB (utomilumab) agonistic antibody combination in patients with advanced solid tumors Abstract Abstract Background Ivuxolimab (PF-04518600) and utomilumab (PF-05082566) are humanized agonistic IgG2 monoclonal antibodies against OX40 and 4-1BB, respectively. This first... |
PMC8298214 | core_pubmed_pmc | Pharmacokinetics of Intraperitoneally Delivered Glucagon in Pigs: A Hypothesis of First Pass Metabolism | Pharmacokinetics of Intraperitoneally Delivered Glucagon in Pigs: A Hypothesis of First Pass Metabolism Abstract Background and Objective Artificial pancreases administering low-dose glucagon in addition to insulin have the scope to improve glucose control in patients with diabetes mellitus type 1. If such a device wer... |
PMC7064168 | core_pubmed_pmc | Brain Shuttle Neprilysin reduces central Amyloid-β levels | Brain Shuttle Neprilysin reduces central Amyloid-β levels Abstract Reducing Amyloid β (Aβ) in the brain is of fundamental importance for advancing the therapeutics for Alzheimer`s disease. The endogenous metallopeptidase neprilysin (NEP) has been identified as one of the key Aβ-degrading enzymes. Delivery of NEP to the... |
PMC8187380 | core_pubmed_pmc | Lipophilic nanocrystal prodrug-release defines the extended pharmacokinetic profiles of a year-long cabotegravir | Lipophilic nanocrystal prodrug-release defines the extended pharmacokinetic profiles of a year-long cabotegravir Abstract A once every eight-week cabotegravir (CAB) long-acting parenteral is more effective than daily oral emtricitabine and tenofovir disoproxil fumarate in preventing human immunodeficiency virus type on... |
PMC5552226 | core_pubmed_pmc | Safety, Tolerability and Pharmacokinetics of Single Doses of Oxytocin Administered via an Inhaled Route in Healthy Females: Randomized, Single-blind, Phase 1 Study ☆ | Safety, Tolerability and Pharmacokinetics of Single Doses of Oxytocin Administered via an Inhaled Route in Healthy Females: Randomized, Single-blind, Phase 1 Study ☆ Abstract Abstract Background The utility of intramuscular (IM) oxytocin for the prevention of postpartum hemorrhage in resource-poor settings is limited b... |
PMC4402032 | core_pubmed_pmc | Safety, pharmacokinetics, and pharmacodynamics of TV-1380, a novel mutated butyrylcholinesterase treatment for cocaine addiction, after single and multiple intramuscular injections in healthy subjects | Safety, pharmacokinetics, and pharmacodynamics of TV-1380, a novel mutated butyrylcholinesterase treatment for cocaine addiction, after single and multiple intramuscular injections in healthy subjects Abstract Human plasma butyrylcholinesterase (BChE) contributes to cocaine metabolism and has been considered for use in... |
PMC4124067 | core_pubmed_pmc | 2′-(2-bromohexadecanoyl)-paclitaxel conjugate nanoparticles for the treatment of non-small cell lung cancer in an orthotopic xenograft mouse model | 2′-(2-bromohexadecanoyl)-paclitaxel conjugate nanoparticles for the treatment of non-small cell lung cancer in an orthotopic xenograft mouse model Abstract Abstract A nanoparticle (NP) formulation with 2′-(2-bromohexadecanoyl)-paclitaxel (Br-16-PX) conjugate was developed in these studies for the treatment of non-small... |
PMC5309263 | core_pubmed_pmc | Clinical outcomes of extended versus intermittent administration of piperacillin/tazobactam for the treatment of hospital-acquired pneumonia: a randomized controlled trial | Clinical outcomes of extended versus intermittent administration of piperacillin/tazobactam for the treatment of hospital-acquired pneumonia: a randomized controlled trial Abstract The purpose of this study was to assess the pharmacokinetic (PK) characteristics, clinical efficiency, and pharmacoeconomic parameters of p... |
PMC12234323 | core_pubmed_pmc | Gene polymorphisms associated with immunosuppressant adverse effects in systemic lupus erythematosus: a narrative review | Gene polymorphisms associated with immunosuppressant adverse effects in systemic lupus erythematosus: a narrative review Abstract Abstract Systemic Lupus Erythematosus (SLE) is an autoimmune disease that often requires treatment with immunosuppressant drugs to manage symptoms and prevent organ damage. However, the use ... |
PMC6935022 | core_pubmed_pmc | Verteporfin-Loaded Anisotropic Poly(Beta-Amino Ester)-Based Micelles Demonstrate Brain Cancer-Selective Cytotoxicity and Enhanced Pharmacokinetics | Verteporfin-Loaded Anisotropic Poly(Beta-Amino Ester)-Based Micelles Demonstrate Brain Cancer-Selective Cytotoxicity and Enhanced Pharmacokinetics Abstract Abstract Background Nanomedicine can improve traditional therapies by enhancing the controlled release of drugs at targeted tissues in the body. However, there stil... |
PMC8256662 | core_pubmed_pmc | In silico investigation on the inhibitory effect of fungal secondary metabolites on RNA dependent RNA polymerase of SARS-CoV-II: A docking and molecular dynamic simulation study | In silico investigation on the inhibitory effect of fungal secondary metabolites on RNA dependent RNA polymerase of SARS-CoV-II: A docking and molecular dynamic simulation study Abstract Abstract The newly emerged Coronavirus Disease 2019 (COVID-19) rapidly outspread worldwide and now is one of the biggest infectious p... |
PMC6993976 | core_pubmed_pmc | Insulin BBB pharmacokinetics in young apoE male and female transgenic mice | Insulin BBB pharmacokinetics in young apoE male and female transgenic mice Abstract In addition to age, apolipoprotein E4 (E4), female sex, or a combination of both synergistically increase the risk for the development of Alzheimer’s disease (AD). Why these risk factors predispose an individual to developing AD later i... |
PMC6707405 | core_pubmed_pmc | Screening Bioactive Compounds of Siraitia grosvenorii by Immobilized β 2 -Adrenergic Receptor Chromatography and Druggability Evaluation | Screening Bioactive Compounds of Siraitia grosvenorii by Immobilized β 2 -Adrenergic Receptor Chromatography and Druggability Evaluation Abstract As the first and key step of traditional Chinese medicine (TCM)-guided drug development, lead discovery necessitates continuous exploration of new methodology for screening b... |
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