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PMC12776329
core_pubmed_pmc
Same class, different activity: Delamanid and pretomanid have comparable bactericidal activity but pretomanid potently inhibits Mycobacterium tuberculosis ribosomal rRNA synthesis
Same class, different activity: Delamanid and pretomanid have comparable bactericidal activity but pretomanid potently inhibits Mycobacterium tuberculosis ribosomal rRNA synthesis Abstract Abstract Background. The nitroimidazoles delamanid and pretomanid play an important role in contemporary tuberculosis treatment. It...
PMC9469699
core_pubmed_pmc
Longitudinal and time‐to‐event modeling for prognostic implications of radical surgery in retroperitoneal sarcoma
Longitudinal and time‐to‐event modeling for prognostic implications of radical surgery in retroperitoneal sarcoma Abstract Abstract Retroperitoneal sarcoma (RPS) is a rare malignancy which can be difficult to manage due to the variety of clinical behaviors. In this study, we aimed to develop a parametric modeling frame...
PMC11842063
core_pubmed_pmc
Pharmacokinetic Aspects of Hydroxychloroquine and Its Relationship to Efficacy in Immunoglobulin A Nephropathy
Pharmacokinetic Aspects of Hydroxychloroquine and Its Relationship to Efficacy in Immunoglobulin A Nephropathy Abstract Abstract Introduction Hydroxychloroquine (HCQ) is recommended for Chinese patients with immunoglobulin A nephropathy (IgAN). This study aimed to investigate the pharmacokinetics of HCQ in the treatmen...
PMC9171976
core_pubmed_pmc
Effects of Soy Isoflavones and Green Tea Extract on Simvastatin Pharmacokinetics and Influence of the SLCO1B1 521T > C Polymorphism
Effects of Soy Isoflavones and Green Tea Extract on Simvastatin Pharmacokinetics and Influence of the SLCO1B1 521T > C Polymorphism Abstract Abstract Objectives Green tea and soy products are extensively consumed by many people and they may influence the activity of drug metabolizing enzymes and drug transporters to re...
PMC7038309
core_pubmed_pmc
A Randomized Controlled Trial of Three- versus Five-Day Artemether-Lumefantrine Regimens for Treatment of Uncomplicated Plasmodium falciparum Malaria in Pregnancy in Africa
A Randomized Controlled Trial of Three- versus Five-Day Artemether-Lumefantrine Regimens for Treatment of Uncomplicated Plasmodium falciparum Malaria in Pregnancy in Africa Abstract Artemether-lumefantrine antimalarial efficacy in pregnancy could be compromised by reduced drug exposure. Population-based simulations sug...
PMC7349017
core_pubmed_pmc
Association of NUDT15 c.415C>T and FPGS 2572C>T Variants with the Risk of Early Hematologic Toxicity During 6-MP and Low-Dose Methotrexate-Based Maintenance Therapy in Indian Patients with Acute Lymphoblastic Leukemia
Association of NUDT15 c.415C>T and FPGS 2572C>T Variants with the Risk of Early Hematologic Toxicity During 6-MP and Low-Dose Methotrexate-Based Maintenance Therapy in Indian Patients with Acute Lymphoblastic Leukemia Abstract Genetic variants influencing the pharmacokinetics and/or pharmacodynamics of the chemotherape...
PMC8339067
core_pubmed_pmc
Phase 1b clinical trial of ado-trastuzumab emtansine and ribociclib for HER2-positive metastatic breast cancer
Phase 1b clinical trial of ado-trastuzumab emtansine and ribociclib for HER2-positive metastatic breast cancer Abstract Abstract Patients with HER2+ metastatic breast cancer are often treated with a multitude of therapies in the metastatic setting, and additional strategies to prolong responses to anti-HER2 therapies a...
PMC12135251
core_pubmed_pmc
Integrative investigation on Hippocratea africana root: insights from cardio-protective, anti-oxidative stress activities, isolation, GC/MS, and pharmacological significance profiling
Integrative investigation on Hippocratea africana root: insights from cardio-protective, anti-oxidative stress activities, isolation, GC/MS, and pharmacological significance profiling Abstract Abstract Background Hippocratea africana root is scientifically used in cardiotoxicity treatment; therefore, this study was des...
PMC4232785
core_pubmed_pmc
RP-HPTLC Retention Data in Correlation with the In-silico ADME Properties of a Series of s-triazine Derivatives
RP-HPTLC Retention Data in Correlation with the In-silico ADME Properties of a Series of s-triazine Derivatives Abstract The properties relevant to pharmacokinetics and pharmacodynamics of four series of synthesized s -triazine derivatives have been studied by Quantitative structure-retention relationship (QSRR) approa...
PMC9444296
core_pubmed_pmc
Evaluation of Physicochemical Properties, Pharmacokinetics, Biodistribution, Toxicity, and Contrast-Enhanced Cancer MRI of a Cancer-Targeting Contrast Agent, MT218
Evaluation of Physicochemical Properties, Pharmacokinetics, Biodistribution, Toxicity, and Contrast-Enhanced Cancer MRI of a Cancer-Targeting Contrast Agent, MT218 Abstract Objectives Preclinical assessments were performed according to the US Food and Drug Administration guidelines to determine the physicochemical prop...
PMC5498639
core_pubmed_pmc
N-[ 11 C]Methyl-AMD3465 PET as a Tool for In Vivo Measurement of Chemokine Receptor 4 (CXCR4) Occupancy by Therapeutic Drugs
N-[ 11 C]Methyl-AMD3465 PET as a Tool for In Vivo Measurement of Chemokine Receptor 4 (CXCR4) Occupancy by Therapeutic Drugs Abstract Abstract Purpose Chemokine receptor 4 (CXCR4) is overexpressed in many cancers and a potential drug target. We have recently developed the tracer N-[ 11 C]methyl-AMD3465 for imaging of C...
PMC10864932
core_pubmed_pmc
Physiologically‐based pharmacokinetic model of sparsentan to evaluate drug–drug interaction potential
Physiologically‐based pharmacokinetic model of sparsentan to evaluate drug–drug interaction potential Abstract Abstract Sparsentan is a dual endothelin/angiotensin II receptor antagonist indicated to reduce proteinuria in patients with primary IgA nephropathy at high risk of disease progression. In vitro data indicate ...
PMC5010191
core_pubmed_pmc
Long-Term Efficacy, Safety, and Pharmacokinetics of Drisapersen in Duchenne Muscular Dystrophy: Results from an Open-Label Extension Study
Long-Term Efficacy, Safety, and Pharmacokinetics of Drisapersen in Duchenne Muscular Dystrophy: Results from an Open-Label Extension Study Abstract Background Drisapersen induces exon 51 skipping during dystrophin pre-mRNA splicing and allows synthesis of partially functional dystrophin in Duchenne muscular dystrophy (...
PMC11268257
core_pubmed_pmc
Discovery and development of ANV419, an IL-2/anti-IL-2 antibody fusion protein with potent CD8+ T and natural killer cell-stimulating capacity for cancer immunotherapy
Discovery and development of ANV419, an IL-2/anti-IL-2 antibody fusion protein with potent CD8+ T and natural killer cell-stimulating capacity for cancer immunotherapy Abstract ABSTRACT Novel engineered IL-2 agonists strive to increase the therapeutic window of aldesleukin (human IL-2) by increasing selectivity toward ...
PMC11387447
core_pubmed_pmc
Pharmacokinetic interaction between regorafenib and atorvastatin in rats
Pharmacokinetic interaction between regorafenib and atorvastatin in rats Abstract Abstract Background Regorafenib is used in the treatment of colorectal cancer and hepatocellular carcinoma. Due to the co-morbidity of hyperlipidemia in these conditions, statins, including atorvastatin, are used as potential adjuvant the...
PMC3731826
core_pubmed_pmc
Quantitative Systems Pharmacology Model of NO Metabolome and Methemoglobin Following Long-Term Infusion of Sodium Nitrite in Humans
Quantitative Systems Pharmacology Model of NO Metabolome and Methemoglobin Following Long-Term Infusion of Sodium Nitrite in Humans Abstract A long-term sodium nitrite infusion is intended for the treatment of vascular disorders. Phase I data demonstrated a significant nonlinear dose-exposure-toxicity relationship with...
PMC8779485
core_pubmed_pmc
Implementation and Comparison of Two Pharmacometric Tools for Model-Based Therapeutic Drug Monitoring and Precision Dosing of Daptomycin
Implementation and Comparison of Two Pharmacometric Tools for Model-Based Therapeutic Drug Monitoring and Precision Dosing of Daptomycin Abstract Daptomycin is a candidate for therapeutic drug monitoring (TDM). The objectives of this work were to implement and compare two pharmacometric tools for daptomycin TDM and pre...
PMC9300831
core_pubmed_pmc
External Evaluation of Population Pharmacokinetic Models of Busulfan in Chinese Adult Hematopoietic Stem Cell Transplantation Recipients
External Evaluation of Population Pharmacokinetic Models of Busulfan in Chinese Adult Hematopoietic Stem Cell Transplantation Recipients Abstract Objective: Busulfan (BU) is a bi-functional DNA-alkylating agent used in patients undergoing hematopoietic stem cell transplantation (HSCT). Over the last decades, several po...
PMC10576855
core_pubmed_pmc
IMM47, a humanized monoclonal antibody that targets CD24, exhibits exceptional anti-tumor efficacy by blocking the CD24/Siglec-10 interaction and can be used as monotherapy or in combination with anti-PD1 antibodies for cancer immunotherapy
IMM47, a humanized monoclonal antibody that targets CD24, exhibits exceptional anti-tumor efficacy by blocking the CD24/Siglec-10 interaction and can be used as monotherapy or in combination with anti-PD1 antibodies for cancer immunotherapy Abstract Abstract This study evaluates the anti-tumor mechanism of IMM47, a hum...
PMC10865773
core_pubmed_pmc
Comparison of Blood Concentration and Weight-Based Heparin and Protamine Dosing Strategies for Cardiopulmonary Bypass: A Systematic Review and Meta-Analysis
Comparison of Blood Concentration and Weight-Based Heparin and Protamine Dosing Strategies for Cardiopulmonary Bypass: A Systematic Review and Meta-Analysis Abstract Background: The conventional method of heparin and protamine management during cardiopulmonary bypass (CPB) is based on total body weight which fails to a...
PMC5084669
core_pubmed_pmc
Patritumab plus trastuzumab and paclitaxel in human epidermal growth factor receptor 2‐overexpressing metastatic breast cancer
Patritumab plus trastuzumab and paclitaxel in human epidermal growth factor receptor 2‐overexpressing metastatic breast cancer Abstract Human epidermal growth factor receptor 3 ( HER 3) expression in lung and breast cancers has a negative impact on survival. Patritumab, a human anti‐ HER 3 m A b, has shown anticancer a...
PMC10681430
core_pubmed_pmc
A multistate modeling and simulation framework to learn dose–response of oncology drugs: Application to bintrafusp alfa in non‐small cell lung cancer
A multistate modeling and simulation framework to learn dose–response of oncology drugs: Application to bintrafusp alfa in non‐small cell lung cancer Abstract Abstract The dose/exposure‐efficacy analyses are often conducted separately for oncology end points like best overall response, progression‐free survival (PFS) a...
PMC11215536
core_pubmed_pmc
Skin pharmacokinetics of miltefosine in the treatment of post-kala-azar dermal leishmaniasis in South Asia
Skin pharmacokinetics of miltefosine in the treatment of post-kala-azar dermal leishmaniasis in South Asia Abstract Abstract Introduction Post-kala-azar dermal leishmaniasis (PKDL) arises as a dermal complication following a visceral leishmaniasis (VL) infection. Current treatment options for PKDL are unsatisfactory, a...
PMC4327740
core_pubmed_pmc
Citrus aurantium increases seizure latency to PTZ induced seizures in zebrafish thru NMDA and mGluR's I and II
Citrus aurantium increases seizure latency to PTZ induced seizures in zebrafish thru NMDA and mGluR's I and II Abstract Abstract Epilepsy is a serious neurological condition and pharmacotherapy is not effective for all patients and causes serious adverse effects and pharmacokinetic and pharmacodynamic interactions. Nat...
PMC12787564
core_pubmed_pmc
A Star-PEGylation Strategy to Improve Testosterone Pharmacokinetics
A Star-PEGylation Strategy to Improve Testosterone Pharmacokinetics Abstract Abstract Testosterone, an androgenic steroid hormone, regulates primary sexual characteristics and influences mood, cognition, social behavior, and sexual function. Deficiency, caused by factors such as aging and genetics, is linked to multipl...
PMC3916444
core_pubmed_pmc
Enhanced antitumor activity of realgar mediated by milling it to nanosize
Enhanced antitumor activity of realgar mediated by milling it to nanosize Abstract Realgar is a poorly water-soluble compound that exhibits poor bioavailability. To improve this, the authors reduced the particle size of realgar to nanoscale by high-energy ball milling and optimized the preparation process under which (...
PMC12507653
core_pubmed_pmc
Precision dosing of amikacin in term neonates using pharmacometric approach
Precision dosing of amikacin in term neonates using pharmacometric approach Abstract Background Maintaining amikacin concentrations within a specific therapeutic window is crucial to avoid sub-therapeutic or toxic levels. This study aimed to design a dosing nomogram for amikacin in neonates using a Population Pharmacok...
PMC7221111
core_pubmed_pmc
Assessment of Vancomycin Pharmacokinetics and Dose Regimen Optimisation in Preterm Neonates
Assessment of Vancomycin Pharmacokinetics and Dose Regimen Optimisation in Preterm Neonates Abstract Abstract Background The pharmacokinetics of vancomycin, a drug used for the treatment of methicillin-resistant Staphylococcus aureus (MRSA), varies between paediatric and adult patients. Objective The objective of this ...
PMC12206278
core_pubmed_pmc
Sublingual Crushed Levodopa for Parkinson’s Disease Management of a Lewy Body Dementia Patient With Dysphagia: A Case Report
Sublingual Crushed Levodopa for Parkinson’s Disease Management of a Lewy Body Dementia Patient With Dysphagia: A Case Report Abstract Levodopa/carbidopa is the cornerstone treatment for Parkinson’s disease (PD), but in patients with dysphagia, there are limited options for the routes of administration. Traditional meth...
PMC12901222
core_pubmed_pmc
A mathematical model to simulate the biological action of Infliximab on TNF- \documentclass[12pt]{minimal} \usepackage{amsmath} \usepackage{wasysym} \usepackage{amsfonts} \usepackage{amssymb} \usepackage{amsbsy} \usepackage{mathrsfs} \usepackage{upgreek} \setlength{\oddsidemargin}{-69pt} \begin{document}$$\alpha $$\end...
A mathematical model to simulate the biological action of Infliximab on TNF- \documentclass[12pt]{minimal} \usepackage{amsmath} \usepackage{wasysym} \usepackage{amsfonts} \usepackage{amssymb} \usepackage{amsbsy} \usepackage{mathrsfs} \usepackage{upgreek} \setlength{\oddsidemargin}{-69pt} \begin{document}$$\alpha $$\end...
PMC11284584
core_pubmed_pmc
Interest in antibiotic pharmacokinetic modelling in the context of optimising dosing and reducing resistance: bibliometric analysis
Interest in antibiotic pharmacokinetic modelling in the context of optimising dosing and reducing resistance: bibliometric analysis Abstract Abstract Background In the era of problems with resistant bacteria strains, pharmacokinetic (PK) modelling offers ways to optimise antibiotic therapy and minimise the risk of resi...
PMC10122091
core_pubmed_pmc
In Silico Interactions of Natural and Synthetic Compounds with Key Proteins Involved in Alzheimer’s Disease: Prospects for Designing New Therapeutics Compound
In Silico Interactions of Natural and Synthetic Compounds with Key Proteins Involved in Alzheimer’s Disease: Prospects for Designing New Therapeutics Compound Abstract Memory impairment is a result of multiple factors including amyloid-beta (Aβ) accumulation. Several receptors are mediated for Aβ transport and signalin...
PMC9278964
core_pubmed_pmc
Engineering of a trispecific tumor-targeted immunotherapy incorporating 4-1BB co-stimulation and PD-L1 blockade
Engineering of a trispecific tumor-targeted immunotherapy incorporating 4-1BB co-stimulation and PD-L1 blockade Abstract ABSTRACT Co-stimulatory 4–1BB receptors on tumor-infiltrating T cells are a compelling target for overcoming resistance to immune checkpoint inhibitors, but initial clinical studies of 4–1BB agonist ...
PMC4647865
core_pubmed_pmc
Characterization of the relationship between dose and blood eosinophil response following subcutaneous administration of mepolizumab
Characterization of the relationship between dose and blood eosinophil response following subcutaneous administration of mepolizumab Abstract Objective: Mepolizumab is a humanized IgG1 monoclonal antibody that blocks human IL-5 from binding to the IL-5 receptor, which is mainly expressed on eosinophils. Eosinophils are...
PMC11106167
core_pubmed_pmc
Tacrolimus Variability and Clinical Outcomes in the Early Post-lung Transplantation Period: Oral Versus Continuous Intravenous Administration
Tacrolimus Variability and Clinical Outcomes in the Early Post-lung Transplantation Period: Oral Versus Continuous Intravenous Administration Abstract Background and Objective High variability in tacrolimus pharmacokinetics directly after lung transplantation (LuTx) may increase the risk for acute kidney injury (AKI) a...
PMC6209770
core_pubmed_pmc
HBK-17, a 5-HT 1A Receptor Ligand With Anxiolytic-Like Activity, Preferentially Activates ß-Arrestin Signaling
HBK-17, a 5-HT 1A Receptor Ligand With Anxiolytic-Like Activity, Preferentially Activates ß-Arrestin Signaling Abstract Numerous studies have proven that both stimulation and blockade of 5-HT 1A and the blockade of 5-HT 7 receptors might cause the anxiolytic-like effects. Biased agonists selectively activate specific s...
PMC12866562
core_pubmed_pmc
Synergistic antiarrhythmic mechanism of I Na-L and RyR2 blockade: normalization of pathological calcium cycling and CaMKII signaling
Synergistic antiarrhythmic mechanism of I Na-L and RyR2 blockade: normalization of pathological calcium cycling and CaMKII signaling Abstract Abstract Background Arrhythmias represent a leading cause of mortality among individuals with cardiovascular diseases. Considering the failure of antiarrhythmic drugs targeting s...
PMC9079914
core_pubmed_pmc
An open‐label randomized study of the relative absorption of gastro‐resistant risedronate taken fasted or with food versus immediate‐release risedronate
An open‐label randomized study of the relative absorption of gastro‐resistant risedronate taken fasted or with food versus immediate‐release risedronate Abstract Abstract Patients with osteoporosis often take oral bisphosphonates with food, rendering these medications ineffective. This study compared the relative absor...
PMC12625168
core_pubmed_pmc
Population Pharmacokinetic Modeling and Pediatric Exposure of Dexamethasone Sodium Phosphate Encapsulated in Erythrocytes (eDSP) Administered Monthly for Treatment of Neurological Symptoms of Patients With Ataxia Telangiectasia
Population Pharmacokinetic Modeling and Pediatric Exposure of Dexamethasone Sodium Phosphate Encapsulated in Erythrocytes (eDSP) Administered Monthly for Treatment of Neurological Symptoms of Patients With Ataxia Telangiectasia Abstract ABSTRACT The EryDex System (EDS) is a drug/device combination, which has been teste...
PMC8072471
core_pubmed_pmc
Pharmacokinetic and Pharmacodynamic Considerations in Relation to Calcineurin Usage in Elderly Kidney Transplant Recipients
Pharmacokinetic and Pharmacodynamic Considerations in Relation to Calcineurin Usage in Elderly Kidney Transplant Recipients Abstract Abstract This review summarizes how possible age-related changes in tacrolimus and cyclosporine pharmacokinetics and pharmacodynamics may influence drug dosing and monitoring in the elder...
PMC6566825
core_pubmed_pmc
Glucose Tolerance Test and Pharmacokinetic Study of Kaempferia parviflora Extract in Healthy Subjects
Glucose Tolerance Test and Pharmacokinetic Study of Kaempferia parviflora Extract in Healthy Subjects Abstract Abstract Kaempferia parviflora Wall. ex Baker (KP), Krachaidam in Thai or Thai ginseng, is a herbal medicine that has many potential pharmacological effects. The effect of KP extract on blood glucose level in ...
PMC4937653
core_pubmed_pmc
Individual and population pharmacokinetic compartment analysis: a graphic procedure for quantification of predictive performance
Individual and population pharmacokinetic compartment analysis: a graphic procedure for quantification of predictive performance Abstract Objectives Pharmacokinetic studies are important for optimizing of drug dosing, but requires proper validation of the used pharmacokinetic procedures. However, simple and reliable st...
PMC7889459
core_pubmed_pmc
An integrated virtual screening of compounds from Carica papaya leaves against multiple protein targets of SARS-Coronavirus-2
An integrated virtual screening of compounds from Carica papaya leaves against multiple protein targets of SARS-Coronavirus-2 Abstract The pandemic of SARS-Coronavirus-2 (Coronavirus-19) has been progressing by the increasing trend of the cases as well as deaths with neither vaccine nor drug is rationally used to stop ...
PMC9126436
core_pubmed_pmc
Pharmacokinetic Evaluation of a Single 5-Gram Bolus of Creatine Monohydrate Versus Two Other Creatine-Containing Investigational Products
Pharmacokinetic Evaluation of a Single 5-Gram Bolus of Creatine Monohydrate Versus Two Other Creatine-Containing Investigational Products Abstract The purpose of this study was to determine the relative pharmacokinetics of creatine monohydrate delivered as a formula or as a pure powder (all mixed in solution). A single...
PMC5108434
core_pubmed_pmc
Phase I study of pegylated interferon‐alpha‐2b as an adjuvant therapy in Japanese patients with malignant melanoma
Phase I study of pegylated interferon‐alpha‐2b as an adjuvant therapy in Japanese patients with malignant melanoma Abstract Abstract In the adjuvant setting for malignant melanoma, interferon (IFN)‐α‐2b and pegylated (PEG) IFN‐α‐2b were approved in several countries including the USA before these were approved in Japan...
PMC12805088
core_pubmed_pmc
Preclinical characterisation of the protective capacity of an anti-nucleoprotein hRSV monoclonal antibody
Preclinical characterisation of the protective capacity of an anti-nucleoprotein hRSV monoclonal antibody Abstract Summary Background The human respiratory syncytial virus (hRSV) is a pathogen of global concern, causing significant morbidity and mortality, mainly in preterm infants. To date, all licenced monoclonal ant...
PMC5863893
core_pubmed_pmc
Current perspectives on the role of the pharmacist in heart failure management
Current perspectives on the role of the pharmacist in heart failure management Abstract Abstract Pharmacists play an important role within a multidisciplinary health care team in the care of patients with heart failure (HF). It has been evaluated and documented that pharmacists providing medication reconciliation espec...
PMC7470133
core_pubmed_pmc
Dissolving microneedles for transdermal delivery of huperzine A for the treatment of Alzheimer's disease
Dissolving microneedles for transdermal delivery of huperzine A for the treatment of Alzheimer's disease Abstract Abstract Increasingly attention has been paid to the transdermal drug delivery systems with microneedles owing to their excellent compliance, high efficiency, and controllable drug release, therefore, becom...
PMC12357863
core_pubmed_pmc
Randomized phase I trial outcomes show safe and sustainable inhibition of classical and lectin complement pathways by empasiprubart
Randomized phase I trial outcomes show safe and sustainable inhibition of classical and lectin complement pathways by empasiprubart Abstract Activation of classical and lectin complement pathways contributes to several human diseases. Empasiprubart is a humanized recycling monoclonal antibody that inhibits both pathway...
PMC12842561
core_pubmed_pmc
Angiopoietin-like Protein 3 (ANGPTL3) Targeting in the Management of Dyslipidemias
Angiopoietin-like Protein 3 (ANGPTL3) Targeting in the Management of Dyslipidemias Abstract Cardiovascular disease (CVD) remains the leading cause of morbidity and mortality, despite advances in pharmacological prevention and treatment. The burden of CVD necessitates implementing the treatment of risk factors including...
PMC12180466
core_pubmed_pmc
Platelet Membrane-Based Nanoparticles for Targeted Delivery of Deferoxamine to Alleviate Brain Injury Induced by Ischemic Stroke
Platelet Membrane-Based Nanoparticles for Targeted Delivery of Deferoxamine to Alleviate Brain Injury Induced by Ischemic Stroke Abstract Background Timely thrombolysis serves as the primary therapeutic approach for ischemic stroke, one of the most serious global public health problems, although reperfusion can cause s...
PMC5743916
core_pubmed_pmc
Pharmacokinetics of Conventional and Long-Acting Oxytetracycline Preparations in Kilis Goat
Pharmacokinetics of Conventional and Long-Acting Oxytetracycline Preparations in Kilis Goat Abstract The pharmacokinetics of conventional and long-acting (LA) oxytetracycline (OTC), widely used broad-spectrum antibacterial drugs in veterinary medicine, were evaluated in Kilis goats at single dosage of 20 mg/kg body wei...
PMC6656793
core_pubmed_pmc
Automated proper lumping for simplification of linear physiologically based pharmacokinetic systems
Automated proper lumping for simplification of linear physiologically based pharmacokinetic systems Abstract Physiologically based pharmacokinetic (PBPK) models are an important type of systems model used commonly in drug development before commencement of first-in-human studies. Due to structural complexity, these mod...
PMC9373154
core_pubmed_pmc
A Phase 2 Study of Pimodivir (JNJ-63623872) in Combination With Oseltamivir in Elderly and Nonelderly Adults Hospitalized With Influenza A Infection: OPAL Study
A Phase 2 Study of Pimodivir (JNJ-63623872) in Combination With Oseltamivir in Elderly and Nonelderly Adults Hospitalized With Influenza A Infection: OPAL Study Abstract Abstract Background Both the elderly and individuals with comorbidities are at increased risk of developing influenza-related complications. Novel inf...
PMC10728082
core_pubmed_pmc
Randomized phase II study of preoperative afatinib in untreated head and neck cancers: predictive and pharmacodynamic biomarkers of activity
Randomized phase II study of preoperative afatinib in untreated head and neck cancers: predictive and pharmacodynamic biomarkers of activity Abstract Abstract There is no strong and reliable predictive biomarker in head and neck squamous cell carcinoma (HNSCC) for EGFR inhibitors. We aimed to identify predictive and ph...
PMC10120766
core_pubmed_pmc
nlive: an R Package to facilitate the application of the sigmoidal and random changepoint mixed models
nlive: an R Package to facilitate the application of the sigmoidal and random changepoint mixed models Abstract Abstract Background: The use of mixed effect models with a specific functional form such as the Sigmoidal Mixed Model and the Piecewise Mixed Model (or Changepoint Mixed Model) with abrupt or smooth random ch...
PMC4150925
core_pubmed_pmc
Modeling and Simulation of Count Data
Modeling and Simulation of Count Data Abstract Count data, or number of events per time interval, are discrete data arising from repeated time to event observations. Their mean count, or piecewise constant event rate, can be evaluated by discrete probability distributions from the Poisson model family. Clinical trial d...
PMC8096738
core_pubmed_pmc
Hot liquid extrusion assisted drug-cyclodextrin complexation: a novel continuous manufacturing method for solubility and bioavailability enhancement of drugs
Hot liquid extrusion assisted drug-cyclodextrin complexation: a novel continuous manufacturing method for solubility and bioavailability enhancement of drugs Abstract Abstract In this study, drug-cyclodextrin (CD) complexes were prepared using hot liquid extrusion (HLE) process with an aim to improve solubility and bio...
PMC12030500
core_pubmed_pmc
Exploring the Pharmacokinetics of Drugs in Disabled Saudi Patients: A Systematic Review
Exploring the Pharmacokinetics of Drugs in Disabled Saudi Patients: A Systematic Review Abstract Abstract Background/Objectives : Disability is a term that involves mental, intellectual, or sensory impairment resulting in the loss of one’s ability to walk or perform the activities necessary to live in a society. This s...
PMC10196427
core_pubmed_pmc
Regulatory utility of physiologically based pharmacokinetic modeling for assessing food impact in bioequivalence studies: A workshop summary report
Regulatory utility of physiologically based pharmacokinetic modeling for assessing food impact in bioequivalence studies: A workshop summary report Abstract Abstract This workshop report summarizes the presentations and panel discussion related to the use of physiologically based pharmacokinetic (PBPK) modeling approac...
PMC5270302
core_pubmed_pmc
Model‐Based Population Pharmacokinetic Analysis of Nivolumab in Patients With Solid Tumors
Model‐Based Population Pharmacokinetic Analysis of Nivolumab in Patients With Solid Tumors Abstract Abstract Nivolumab is a fully human monoclonal antibody that inhibits programmed death‐1 activation. The clinical pharmacology profile of nivolumab was analyzed by a population pharmacokinetics model that assessed covari...
PMC12890303
core_pubmed_pmc
UPLC-QDA combined with pharmacology and chemometrics to analyze the correlation between the processing technology and color of Siegesbeckiae herba
UPLC-QDA combined with pharmacology and chemometrics to analyze the correlation between the processing technology and color of Siegesbeckiae herba Abstract In the Chinese Pharmacopoeia (2025 Edition), it is reported that Siegesbeckiae herba (SH) can be processed via a single herb preparation, demonstrating significant ...
PMC8836664
core_pubmed_pmc
Single and Multiple Dose PK–PD Characterization for Carisoprodol. Part I: Pharmacokinetics, Metabolites, and 2C19 Phenotype Influence. Double-Blind, Placebo-Controlled Clinical Trial in Healthy Volunteers
Single and Multiple Dose PK–PD Characterization for Carisoprodol. Part I: Pharmacokinetics, Metabolites, and 2C19 Phenotype Influence. Double-Blind, Placebo-Controlled Clinical Trial in Healthy Volunteers Abstract Carisoprodol was authorised in 1959 without a full pharmacokinetic–pharmacodynamic (PK–PD) characterisatio...
PMC8343403
core_pubmed_pmc
An automated approach to identify scientific publications reporting pharmacokinetic parameters
An automated approach to identify scientific publications reporting pharmacokinetic parameters Abstract Abstract Pharmacokinetic (PK) predictions of new chemical entities are aided by prior knowledge from other compounds. The development of robust algorithms that improve preclinical and clinical phases of drug developm...
PMC12592298
core_pubmed_pmc
An automated pipeline to generate initial estimates for population Pharmacokinetic base models
An automated pipeline to generate initial estimates for population Pharmacokinetic base models Abstract Abstract Nonlinear mixed-effects models rely on adequate initial parameter estimates for efficient parameter optimization. Poor initial estimates can result in failed model convergence or termination with incorrect p...
PMC5755306
core_pubmed_pmc
Pharmacokinetics comparison of two pegylated interferon alfa formulations in healthy volunteers
Pharmacokinetics comparison of two pegylated interferon alfa formulations in healthy volunteers Abstract Abstract Background Several countries have used pegylation technology to improve the pharmacokinetic properties of essential drugs. Recently, a novel interferon alfa-2b protein conjugated to four-branched 12 kDa pol...
PMC12503756
core_pubmed_pmc
Efficacy and Safety of Glibenclamide on Functional Outcomes and Cerebral Edema following Ischemic and Hemorrhagic Stroke: A Systematic Review and Meta-Analysis of Randomized Controlled Trials
Efficacy and Safety of Glibenclamide on Functional Outcomes and Cerebral Edema following Ischemic and Hemorrhagic Stroke: A Systematic Review and Meta-Analysis of Randomized Controlled Trials Abstract Abstract Objective This systematic review and meta-analysis aimed to evaluate the clinical and radiological outcomes of...
PMC2809265
core_pubmed_pmc
U-500 Regular Insulin
U-500 Regular Insulin Abstract Abstract OBJECTIVE To describe the clinical experience and the pharmacokinetics of U-500 regular insulin in severely insulin-resistant obese type 2 diabetic patients. RESEARCH DESIGN AND METHODS Patients requiring >200 units of insulin with A1C levels >8.0% were switched to U-500 regular ...
PMC4406150
core_pubmed_pmc
Phase 1, Open-Label, Dose Escalation, Safety, and Pharmacokinetics Study of ME-344 as a Single Agent in Patients With Refractory Solid Tumors
Phase 1, Open-Label, Dose Escalation, Safety, and Pharmacokinetics Study of ME-344 as a Single Agent in Patients With Refractory Solid Tumors Abstract Abstract Background The current phase 1, open-label, dose escalation study was conducted to establish the safety, tolerability, pharmacokinetic profile, and preliminary ...
PMC7485652
core_pubmed_pmc
Role of Glucuronidation Pathway in Quetiapine Metabolism: An In vivo Drug–Drug Interaction Study between Quetiapine and Probenecid
Role of Glucuronidation Pathway in Quetiapine Metabolism: An In vivo Drug–Drug Interaction Study between Quetiapine and Probenecid Abstract Background: Uridine 5'-diphospho-glucuronosyltransferase (UGT) enzymes play a significant role in the metabolism of quetiapine, and coadministration with a UGT inhibitor/inducer dr...
PMC6856026
core_pubmed_pmc
Requirements to Establishing Confidence in Physiologically Based Pharmacokinetic (PBPK) Models and Overcoming Some of the Challenges to Meeting Them
Requirements to Establishing Confidence in Physiologically Based Pharmacokinetic (PBPK) Models and Overcoming Some of the Challenges to Meeting Them Abstract When scientifically well-founded, the mechanistic basis of physiologically based pharmacokinetic (PBPK) models can help reduce the uncertainty and increase confid...
PMC7448837
core_pubmed_pmc
Pharmacokinetics, Pharmacodynamics, and Safety of Nivolumab in Patients With Sepsis-Induced Immunosuppression: A Multicenter, Open-Label Phase 1/2 Study
Pharmacokinetics, Pharmacodynamics, and Safety of Nivolumab in Patients With Sepsis-Induced Immunosuppression: A Multicenter, Open-Label Phase 1/2 Study Abstract ABSTRACT Background: Sepsis often induces an immunosuppressive state, which is associated with high mortality rates. Immunostimulation may be beneficial for s...
PMC9609639
core_pubmed_pmc
Evaluating and Improving Neonatal Gentamicin Pharmacokinetic Models Using Aggregated Routine Clinical Care Data
Evaluating and Improving Neonatal Gentamicin Pharmacokinetic Models Using Aggregated Routine Clinical Care Data Abstract Abstract Model-informed precision dosing (MIPD) can aid dose decision-making for drugs such as gentamicin that have high inter-individual variability, a narrow therapeutic window, and a high risk of ...
PMC9544602
core_pubmed_pmc
Population pharmacokinetic‐pharmacodynamic modelling of platelet time‐courses following administration of abrocitinib
Population pharmacokinetic‐pharmacodynamic modelling of platelet time‐courses following administration of abrocitinib Abstract Aims Abrocitinib is a selective Janus kinase 1 inhibitor for the treatment of moderate‐to‐severe atopic dermatitis. Herein we describe the time‐course of drug‐induced platelet reduction followi...
PMC9020506
core_pubmed_pmc
Medication Appropriateness, Polypharmacy, and Drug-Drug Interactions in Ambulatory Elderly Patients with Cardiovascular Diseases at Tikur Anbessa Specialized Hospital, Ethiopia
Medication Appropriateness, Polypharmacy, and Drug-Drug Interactions in Ambulatory Elderly Patients with Cardiovascular Diseases at Tikur Anbessa Specialized Hospital, Ethiopia Abstract Abstract Background Appropriate prescribing is often challenging in geriatric patients due to age-related pharmacokinetic and pharmaco...
PMC5957549
core_pubmed_pmc
Vaccine-driven pharmacodynamic dissection and mitigation of Captagon psychoactivity
Vaccine-driven pharmacodynamic dissection and mitigation of Captagon psychoactivity Abstract SUMMARY PARAGRAPH Fenethylline, also known as Captagon, is a synthetic psychoactive stimulant that has recently been linked to substance use disorder and ‘pharmacoterrorism’ in the Middle East. 1 – 4 Although fenethylline share...
PMC9610933
core_pubmed_pmc
Simulation-Based Gastrointestinal Endoscopy Sedations: A Novel Validation to Multidrug Pharmacodynamic Modeling
Simulation-Based Gastrointestinal Endoscopy Sedations: A Novel Validation to Multidrug Pharmacodynamic Modeling Abstract Abstract Pharmacodynamic models have described the interactions between anesthetics. Applying the models to clinical practice is still problematic due to inherent limitations: 1. modeling conditions ...
PMC11358351
core_pubmed_pmc
Treatment Targets Should Influence Choice of Infliximab Dose Intensification Strategy in Inflammatory Bowel Disease: A Pharmacokinetic Simulation Study
Treatment Targets Should Influence Choice of Infliximab Dose Intensification Strategy in Inflammatory Bowel Disease: A Pharmacokinetic Simulation Study Abstract Background The optimal infliximab dose intensification strategy to address loss of response associated with subtherapeutic infliximab trough levels remains unc...
PMC6720019
core_pubmed_pmc
In vitro inhibitory effects of kaempferitrin on human liver cytochrome P450 enzymes
In vitro inhibitory effects of kaempferitrin on human liver cytochrome P450 enzymes Abstract Abstract Context: Kaempferitrinis (KF) is a bioactive flavonoid and possesses numerous pharmacological activities. However, whether KF affects the activity of human liver cytochrome P450 (CYP) enzymes remains unclear. Objective...
PMC12388929
core_pubmed_pmc
A Novel Iodine–Dextrin Complex Exhibits No Acute or Subacute Toxicity and Enhances Azithromycin Efficacy in an LPS-Induced Sepsis Model
A Novel Iodine–Dextrin Complex Exhibits No Acute or Subacute Toxicity and Enhances Azithromycin Efficacy in an LPS-Induced Sepsis Model Abstract Background/Objectives: Our work was designed to study the physicochemical properties, safety profile, pharmacokinetics, and prophylactic efficacy of an original iodine–dextrin...
PMC8607796
core_pubmed_pmc
Carbon fullerene and nanotube are probable binders to multiple targets of SARS-CoV-2: Insights from computational modeling and molecular dynamic simulation studies
Carbon fullerene and nanotube are probable binders to multiple targets of SARS-CoV-2: Insights from computational modeling and molecular dynamic simulation studies Abstract Abstract The present study aimed to predict the binding potential of carbon nanotube and nano fullerene towards multiple targets of SARS-CoV-2. Bas...
PMC9501058
core_pubmed_pmc
Clinical Effectiveness and Pharmacokinetics of Dalbavancin in Treatment-Experienced Patients with Skin, Osteoarticular, or Vascular Infections
Clinical Effectiveness and Pharmacokinetics of Dalbavancin in Treatment-Experienced Patients with Skin, Osteoarticular, or Vascular Infections Abstract Dalbavancin (DBV) is a lipoglycopeptide approved for the treatment of Gram-positive infections of the skin and skin-associated structures (ABSSSIs). Currently, its off-...
PMC12605441
core_pubmed_pmc
A Multicentric Clinical Study to Evaluate Pharmacokinetics, Efficacy, and Safety of Immune Globulin Subcutaneous 20% Weekly/Biweekly Dosing in Treatment-Experienced Patients and Loading/Weekly Maintenance Dosing in Treatment-Naïve Patients with Primary Immunodeficiency
A Multicentric Clinical Study to Evaluate Pharmacokinetics, Efficacy, and Safety of Immune Globulin Subcutaneous 20% Weekly/Biweekly Dosing in Treatment-Experienced Patients and Loading/Weekly Maintenance Dosing in Treatment-Naïve Patients with Primary Immunodeficiency Abstract Intravenous immunoglobulin (IVIG) therapy...
PMC9160848
core_pubmed_pmc
A randomised, crossover, clinical study to assess nicotine pharmacokinetics and subjective effects of the BIDI ® stick ENDS compared with combustible cigarettes and a comparator ENDS in adult smokers
A randomised, crossover, clinical study to assess nicotine pharmacokinetics and subjective effects of the BIDI ® stick ENDS compared with combustible cigarettes and a comparator ENDS in adult smokers Abstract Background Nicotine pharmacokinetic assessments of electronic nicotine delivery systems (ENDS) are crucial to u...
PMC12510059
core_pubmed_pmc
Synthesis and characterization of a functional benzoylecgonine – bovine serum albumin conjugate for quantification of a humanized monoclonal anti-cocaine antibody
Synthesis and characterization of a functional benzoylecgonine – bovine serum albumin conjugate for quantification of a humanized monoclonal anti-cocaine antibody Abstract Abstract We have developed a humanized monoclonal anti-cocaine antibody (h2E2), as a potential solution for cocaine use disorder. A key milestone wa...
PMC4735029
core_pubmed_pmc
Intake of a fermented soymilk beverage containing moderate levels of isoflavone aglycones enhances bioavailability of isoflavones in healthy premenopausal Japanese women: a double-blind, placebo-controlled, single-dose, crossover trial
Intake of a fermented soymilk beverage containing moderate levels of isoflavone aglycones enhances bioavailability of isoflavones in healthy premenopausal Japanese women: a double-blind, placebo-controlled, single-dose, crossover trial Abstract Abstract This study aimed to investigate the bioavailability of serum isofl...
PMC5603097
core_pubmed_pmc
Vemurafenib plus cobimetinib in unresectable stage IIIc or stage IV melanoma: response monitoring and resistance prediction with positron emission tomography and tumor characteristics (REPOSIT): study protocol of a phase II, open-label, multicenter study
Vemurafenib plus cobimetinib in unresectable stage IIIc or stage IV melanoma: response monitoring and resistance prediction with positron emission tomography and tumor characteristics (REPOSIT): study protocol of a phase II, open-label, multicenter study Abstract Background In patients with BRAFV600 mutated unresectabl...
PMC7558639
core_pubmed_pmc
A Tumor-Immune Interaction Model for Synergistic Combinations of Anti PD-L1 and Ionizing Irradiation Treatment
A Tumor-Immune Interaction Model for Synergistic Combinations of Anti PD-L1 and Ionizing Irradiation Treatment Abstract Abstract Combination therapy with immune checkpoint blockade and ionizing irradiation therapy (IR) generates a synergistic effect to inhibit tumor growth better than either therapy does alone. We mode...
PMC4220649
core_pubmed_pmc
Phase 1 dose-escalation study of IV ixazomib, an investigational proteasome inhibitor, in patients with relapsed/refractory lymphoma
Phase 1 dose-escalation study of IV ixazomib, an investigational proteasome inhibitor, in patients with relapsed/refractory lymphoma Abstract Abstract Ixazomib is an investigational proteasome inhibitor that has shown preclinical activity in lymphoma models. This phase 1 study assessed the safety, tolerability, maximum...
PMC10299594
core_pubmed_pmc
Pharmacokinetics and Tissue Distribution of Bee Venom-Derived Phospholipase A2 Using a Sandwich ELISA after Subcutaneous Injection of New Composition Bee Venom in Rats
Pharmacokinetics and Tissue Distribution of Bee Venom-Derived Phospholipase A2 Using a Sandwich ELISA after Subcutaneous Injection of New Composition Bee Venom in Rats Abstract Abstract Bee venom is a traditional drug used to treat the nervous system, musculoskeletal system, and autoimmune diseases. A previous study fo...
PMC6843445
core_pubmed_pmc
Pharmacokinetic Properties of Fluorescently Labelled Hydroxypropyl-Beta-Cyclodextrin
Pharmacokinetic Properties of Fluorescently Labelled Hydroxypropyl-Beta-Cyclodextrin Abstract Abstract 2-Hydroxypropyl-beta-cyclodextrin (HPBCD) is utilized in the formulation of pharmaceutical products and recently orphan designation was granted for the treatment of Niemann–Pick disease, type C. The exact mechanism of...
PMC5424766
core_pubmed_pmc
A phase 2 trial of long-acting TransCon growth hormone in adult GH deficiency
A phase 2 trial of long-acting TransCon growth hormone in adult GH deficiency Abstract Abstract TransCon growth hormone is a sustained-release human growth hormone prodrug under development in which unmodified growth hormone is transiently linked to a carrier molecule. It is intended as an alternative to daily growth h...
PMC10955036
core_pubmed_pmc
New advances in management and treatment of cardiac implantable electronic devices infections
New advances in management and treatment of cardiac implantable electronic devices infections Abstract Cardiac implantable electronic devices (CIED) are increasingly used worldwide, and infection of these devices remains one of the most feared complications. CIED infections (CDIs) represent a challenge for physicians a...
PMC9514206
core_pubmed_pmc
Commentary: Population pharmacokinetics of colistin sulfate in critically ill patients: Exposure and clinical efficacy
Commentary: Population pharmacokinetics of colistin sulfate in critically ill patients: Exposure and clinical efficacy Modeling Pharmacokinetic/pharmacodynamic modeling Yu et al. had developed a population pharmacokinetic model for colistin sulfate, and the model only accounts for intravenous administration. But 52.4% ...
PMC3502186
core_pubmed_pmc
PEGylation Extends Circulation Half-Life While Preserving In Vitro and In Vivo Activity of Tissue Inhibitor of Metalloproteinases-1 (TIMP-1)
PEGylation Extends Circulation Half-Life While Preserving In Vitro and In Vivo Activity of Tissue Inhibitor of Metalloproteinases-1 (TIMP-1) Abstract Abstract Excess proteolytic activity of matrix metalloproteinases (MMPs) contributes to the development of arthritis, cardiovascular diseases and cancer progression, impl...
PMC12112076
core_pubmed_pmc
Discovery and Functional Validation of EP3 Receptor Ligands with Therapeutic Potential in Cardiovascular Disease
Discovery and Functional Validation of EP3 Receptor Ligands with Therapeutic Potential in Cardiovascular Disease Abstract Abstract The prostaglandin E2 receptor EP3 is emerging as a promising therapeutic target in cardiovascular diseases because of its involvement in vascular inflammation, platelet aggregation, and vas...
PMC12966204
core_pubmed_pmc
Window of opportunity study measuring defactinib and avutometinib delivery in glioblastomas
Window of opportunity study measuring defactinib and avutometinib delivery in glioblastomas Abstract Purpose Glioblastoma (GBM) is the most common malignant brain tumor in adults, and durable control or cure with current standard or investigational therapies is rare. Therefore, novel approaches are needed. This explora...
PMC6680430
core_pubmed_pmc
Quantitative Prediction of Human Pharmacokinetics and Pharmacodynamics of CKD519, a Potent Inhibitor of Cholesteryl Ester Transfer Protein (CETP)
Quantitative Prediction of Human Pharmacokinetics and Pharmacodynamics of CKD519, a Potent Inhibitor of Cholesteryl Ester Transfer Protein (CETP) Abstract CKD519, a selective inhibitor of cholesteryl ester transfer protein(CETP), is undergoing development as an oral agent for the treatment of primary hypercholesterolem...
PMC11557210
core_pubmed_pmc
Japanese Mucuna pruriens (Hasshou Beans) Showed Fast-acting and Long-lasting Effects in Parkinson's Disease
Japanese Mucuna pruriens (Hasshou Beans) Showed Fast-acting and Long-lasting Effects in Parkinson's Disease Abstract Objective Mucuna pruriens (MP) is a legume whose seeds contain levodopa (LD), which has potential therapeutic effects against Parkinson's disease (PD). However, further research is needed to thoroughly e...
PMC8129711
core_pubmed_pmc
Translational pharmacokinetic‐pharmacodynamic modeling of preclinical and clinical data of the oral MET inhibitor tepotinib to determine the recommended phase II dose
Translational pharmacokinetic‐pharmacodynamic modeling of preclinical and clinical data of the oral MET inhibitor tepotinib to determine the recommended phase II dose Abstract Abstract Tepotinib is a highly selective and potent MET inhibitor in development for the treatment of patients with solid tumors. Given the favo...