id
stringlengths
9
11
source
stringclasses
1 value
title
stringlengths
15
560
text
stringlengths
2k
153k
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...