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PMC8825669
core_pubmed_pmc
Model-Based Efficacy and Toxicity Comparisons of Moxifloxacin for Multidrug-Resistant Tuberculosis
Model-Based Efficacy and Toxicity Comparisons of Moxifloxacin for Multidrug-Resistant Tuberculosis Abstract Abstract Background Moxifloxacin (MOX) is used as a first-choice drug to treat multidrug-resistant tuberculosis (MDR-TB); however, evidence-based dosing optimization should be strengthened by integrative analysis...
PMC9395533
core_pubmed_pmc
Estimating the time of last drinking from blood ethyl glucuronide and ethyl sulphate concentrations
Estimating the time of last drinking from blood ethyl glucuronide and ethyl sulphate concentrations Abstract The determination of length of time from the last drinking is critical for cases like drunk driving, sexual assault victims, and also postmortem suspected poisoning cases. The study was aimed to established a me...
PMC9466465
core_pubmed_pmc
Population pharmacokinetic study of pemetrexed in chinese primary advanced non-small cell lung carcinoma patients
Population pharmacokinetic study of pemetrexed in chinese primary advanced non-small cell lung carcinoma patients Abstract The purposes of this study were to identify physiological and genetic factors that contributed to variability of pemetrexed (PEM) exposure and to optimize the dosing regimens for Chinese non-small ...
PMC9401487
core_pubmed_pmc
Ceralasertib (AZD6738), an Oral ATR Kinase Inhibitor, in Combination with Carboplatin in Patients with Advanced Solid Tumors: A Phase I Study
Ceralasertib (AZD6738), an Oral ATR Kinase Inhibitor, in Combination with Carboplatin in Patients with Advanced Solid Tumors: A Phase I Study Abstract Abstract Purpose: This study reports the safety, tolerability, MTD, recommended phase II dose (RP2D), pharmacokinetic/pharmacodynamic profile, and preliminary antitumor ...
PMC5168502
core_pubmed_pmc
Understanding Lung Deposition of Alpha-1 Antitrypsin in Acute Experimental Mouse Lung Injury Model Using Fluorescence Microscopy
Understanding Lung Deposition of Alpha-1 Antitrypsin in Acute Experimental Mouse Lung Injury Model Using Fluorescence Microscopy Abstract Abstract Human plasma-derived α 1-antitrypsin (AAT) delivered by intravenous infusion is used as augmentation therapy in patients with emphysema who have a genetic mutation resulting...
PMC12148590
core_pubmed_pmc
Sex differences in discontinuations due to side effects of second-generation integrase strand transfer inhibitors: a systematic review and meta-analysis
Sex differences in discontinuations due to side effects of second-generation integrase strand transfer inhibitors: a systematic review and meta-analysis Abstract Summary Background Dolutegravir and bictegravir are frequently prescribed second-generation integrase strand transfer inhibitors. Although sex and gender infl...
PMC4987402
core_pubmed_pmc
Pharmacokinetic Bioequivalence of Two Inhaled Tiotropium Bromide Formulations in Healthy Volunteers
Pharmacokinetic Bioequivalence of Two Inhaled Tiotropium Bromide Formulations in Healthy Volunteers Abstract Abstract Background and Objective A novel tiotropium bromide monodose capsule dry powder inhaler (DPI) formulation and device have been developed. The formulation was based on a spray-dried matrix that enhances ...
PMC7884679
core_pubmed_pmc
A first-in-man phase 1 study of the DNA-dependent protein kinase inhibitor peposertib (formerly M3814) in patients with advanced solid tumours
A first-in-man phase 1 study of the DNA-dependent protein kinase inhibitor peposertib (formerly M3814) in patients with advanced solid tumours Abstract Background This open-label, phase 1 trial ( NCT02316197 ) aimed to determine the maximum-tolerated dose (MTD) and/or recommended phase 2 dose (RP2D) of peposertib (form...
PMC7032169
core_pubmed_pmc
Preparation and in vitro-in vivo evaluation of intestinal retention pellets of Berberine chloride to enhance hypoglycemic and lipid-lowing efficacy
Preparation and in vitro-in vivo evaluation of intestinal retention pellets of Berberine chloride to enhance hypoglycemic and lipid-lowing efficacy Abstract Abstract Berberine chloride (BBR) is a pharmacokinetic profile of drug with poor bioavailability but good therapeutic efficacy, which is closely related to the dis...
PMC8761718
core_pubmed_pmc
Characterization of the Population Pharmacokinetics of Moxidectin in Adults Infected with Strongyloides Stercoralis : Support for a Fixed-Dose Treatment Regimen
Characterization of the Population Pharmacokinetics of Moxidectin in Adults Infected with Strongyloides Stercoralis : Support for a Fixed-Dose Treatment Regimen Abstract Abstract Background Moxidectin has recently attracted attention as a novel candidate for the treatment of helminth infections, including Strongyloides...
PMC7152953
core_pubmed_pmc
Pharmacokinetic Comparisons of Naringenin and Naringenin-Nicotinamide Cocrystal in Rats by LC-MS/MS
Pharmacokinetic Comparisons of Naringenin and Naringenin-Nicotinamide Cocrystal in Rats by LC-MS/MS Abstract Abstract Naringenin (NAR), 4′,5,7-trihydroxydihydroflavone, has a wide range of pharmacological activities but shows poor water solubility and low bioavailability. The pharmacokinetics and bioavailability of nar...
PMC8249265
core_pubmed_pmc
Glomerular Filtration Rate in Asphyxiated Neonates Under Therapeutic Whole-Body Hypothermia, Quantified by Mannitol Clearance
Glomerular Filtration Rate in Asphyxiated Neonates Under Therapeutic Whole-Body Hypothermia, Quantified by Mannitol Clearance Abstract Background Therapeutic hypothermia (TH) is an established intervention to improve the outcome of neonates with moderate-to-severe hypoxic-ischemic encephalopathy resulting from perinata...
PMC5826151
core_pubmed_pmc
Relation between Skin Pharmacokinetics and Efficacy in AmBisome Treatment of Murine Cutaneous Leishmaniasis
Relation between Skin Pharmacokinetics and Efficacy in AmBisome Treatment of Murine Cutaneous Leishmaniasis Abstract ABSTRACT AmBisome (LAmB), a liposomal formulation of amphotericin B (AmB), is a second-line treatment for the parasitic skin disease cutaneous leishmaniasis (CL). Little is known about its tissue distrib...
PMC6150481
core_pubmed_pmc
Structural basis of antiviral activity of peptides from MPER of FIV gp36
Structural basis of antiviral activity of peptides from MPER of FIV gp36 Abstract Abstract Feline immunodeficiency virus (FIV) is a naturally occurring Lentivirus causing acquired immunodeficiency syndrome in felines. It is considered a useful non-primate model to study HIV infection, and to test anti-HIV vaccine. Simi...
PMC11770325
core_pubmed_pmc
Evaluation of the Effect of Loperamide on the Cardiac Repolarization Interval Using Exposure–Response Analysis
Evaluation of the Effect of Loperamide on the Cardiac Repolarization Interval Using Exposure–Response Analysis Abstract ABSTRACT This analysis assessed the relationship between the plasma concentrations of loperamide and its N ‐desmethyl loperamide meta‐ bolite (M1) and the potential QT interval prolongation at therape...
PMC10962649
core_pubmed_pmc
An acute herb–drug interaction of Magnoliae Officinalis Cortex with methotrexate via inhibiting multidrug resistance-associated protein 2
An acute herb–drug interaction of Magnoliae Officinalis Cortex with methotrexate via inhibiting multidrug resistance-associated protein 2 Abstract Abstract Magnoliae Officinalis Cortex (MOC), an herbal drug, contains polyphenolic lignans mainly magnolol (MN) and honokiol (HK). Methotrexate (MTX), a critical drug for ca...
PMC9283737
core_pubmed_pmc
Bioequivalence of two oral formulations of tebipenem pivoxil hydrobromide in healthy subjects
Bioequivalence of two oral formulations of tebipenem pivoxil hydrobromide in healthy subjects Abstract Abstract Tebipenem pivoxil hydrobromide (TBP‐PI‐HBr) is a novel oral carbapenem prodrug of tebipenem (TBP), the active moiety, currently in development for treating serious bacterial infections. This study assessed th...
PMC11646940
core_pubmed_pmc
Local depletion of large molecule drugs due to target binding in tissue interstitial space
Local depletion of large molecule drugs due to target binding in tissue interstitial space Abstract Abstract Drug–target binding determines a drug's pharmacodynamics but can also have a profound impact on a drug's pharmacokinetics, known as target‐mediated drug disposition (TMDD). TMDD models describe the influence of ...
PMC4418344
core_pubmed_pmc
Population Pharmacokinetics of Pomalidomide
Population Pharmacokinetics of Pomalidomide Abstract A population pharmacokinetic (PPK) model of pomalidomide was developed and the influence of demographic and disease-related covariates on PPK parameters was assessed based on data from 6 clinical trials of pomalidomide (dose range, 0.5–10 mg) in healthy participants ...
PMC7459987
core_pubmed_pmc
Pharmacokinetics of a Long-Acting Formulation of Oxytetracycline in Freshwater Crocodiles ( Crocodylus siamensis ) after Intramuscular Administration at Three Different Dosages
Pharmacokinetics of a Long-Acting Formulation of Oxytetracycline in Freshwater Crocodiles ( Crocodylus siamensis ) after Intramuscular Administration at Three Different Dosages Abstract Simple Summary The oxytetracycline long-acting formulation (OTC-LA) is used to treat sensitive pathogenic bacteria in the freshwater c...
PMC6470992
core_pubmed_pmc
Pharmacokinetics of a New Pharmaceutical Form of Vitamin D3 100,000 IU in Soft Capsule
Pharmacokinetics of a New Pharmaceutical Form of Vitamin D3 100,000 IU in Soft Capsule Abstract Vitamin D deficiency is frequent in the general population and both subjects and health professionals could benefit from a broader range of vitamin D3 formulations. We conducted a single-dose, open-label, parallel-group, ran...
PMC8932692
core_pubmed_pmc
Population pharmacokinetics and exposure‐response modeling analyses of guselkumab in patients with psoriatic arthritis
Population pharmacokinetics and exposure‐response modeling analyses of guselkumab in patients with psoriatic arthritis Abstract Abstract Guselkumab is an anti‐interleukin‐23 human monoclonal antibody effective in treating psoriatic arthritis (PsA). To characterize the pharmacokinetics (PKs) and exposure‐response relati...
PMC4467585
core_pubmed_pmc
Phase I Study of Ceritinib (LDK378) in Japanese Patients with Advanced, Anaplastic Lymphoma Kinase-Rearranged Non–Small-Cell Lung Cancer or Other Tumors
Phase I Study of Ceritinib (LDK378) in Japanese Patients with Advanced, Anaplastic Lymphoma Kinase-Rearranged Non–Small-Cell Lung Cancer or Other Tumors Abstract Abstract Introduction: Anaplastic lymphoma kinase (ALK)-rearranged non–small-cell lung cancer (NSCLC) is sensitive to ALK inhibitors, but resistance develops....
PMC7049745
core_pubmed_pmc
Comparative Assessment of Distribution Characteristics and Ocular Pharmacokinetics of Norvancomycin Between Continuous Topical Ocular Instillation and Hourly Administration of Eye Drop
Comparative Assessment of Distribution Characteristics and Ocular Pharmacokinetics of Norvancomycin Between Continuous Topical Ocular Instillation and Hourly Administration of Eye Drop Abstract Background The aim of this study was to compare the distribution characteristics and ocular pharmacokinetics of norvancomycin ...
PMC8550258
core_pubmed_pmc
Characterization of Plasma Protein Alterations in Pregnant and Postpartum Individuals Living With HIV to Support Physiologically-Based Pharmacokinetic Model Development
Characterization of Plasma Protein Alterations in Pregnant and Postpartum Individuals Living With HIV to Support Physiologically-Based Pharmacokinetic Model Development Abstract Background: Alterations in plasma protein concentrations in pregnant and postpartum individuals can influence antiretroviral (ARV) pharmacokin...
PMC9020367
core_pubmed_pmc
Race and sex associations with tacrolimus pharmacokinetics in stable kidney transplant recipients
Race and sex associations with tacrolimus pharmacokinetics in stable kidney transplant recipients Abstract Abstract Study Objective This study investigated race and sex differences in tacrolimus pharmacokinetics and pharmacodynamics in stable kidney transplant recipients. Design and Setting A cross‐sectional, open‐labe...
PMC7147088
core_pubmed_pmc
First-in-human study of anticancer immunotherapy drug candidate mobilan: safety, pharmacokinetics and pharmacodynamics in prostate cancer patients
First-in-human study of anticancer immunotherapy drug candidate mobilan: safety, pharmacokinetics and pharmacodynamics in prostate cancer patients Abstract Toll-like receptor 5 (TLR5) controls endogenous immune responses to pathogens and is a promising target for pharmacological stimulation of anti-tumor immunity. Mobi...
PMC12349950
core_pubmed_pmc
Population Pharmacokinetics of Rifampicin in Plasma and Cerebrospinal Fluid in Adults With Tuberculosis Meningitis
Population Pharmacokinetics of Rifampicin in Plasma and Cerebrospinal Fluid in Adults With Tuberculosis Meningitis Abstract Abstract Background Several ongoing clinical trials are evaluating high-dose rifampicin (up to 35 mg/kg) for tuberculous meningitis (TBM). However, rifampicin pharmacokinetics at higher doses is n...
PMC8808076
core_pubmed_pmc
High doses of favipiravir in two men survivors of Ebola virus disease carrying Ebola virus in semen in Guinea
High doses of favipiravir in two men survivors of Ebola virus disease carrying Ebola virus in semen in Guinea Abstract Abstract Background Persistence of Ebola virus (EBOV) in semen remains of deep concern, as sexual transmission of EBOV seems plausible up to 6 months after acute phase of Ebola virus disease (EVD). Fav...
PMC7536163
core_pubmed_pmc
Direct comparison of two extended half-life PEGylated recombinant FVIII products: a randomized, crossover pharmacokinetic study in patients with severe hemophilia A
Direct comparison of two extended half-life PEGylated recombinant FVIII products: a randomized, crossover pharmacokinetic study in patients with severe hemophilia A Abstract An open-label, crossover randomized study was performed to compare the pharmacokinetics (PK) of damoctocog alfa pegol and rurioctocog alfa pegol, ...
PMC10796587
core_pubmed_pmc
Nimodipine systemic exposure and outcomes following aneurysmal subarachnoid hemorrhage: a pilot prospective observational study (ASH-1 study)
Nimodipine systemic exposure and outcomes following aneurysmal subarachnoid hemorrhage: a pilot prospective observational study (ASH-1 study) Abstract Abstract Background Nimodipine improves outcomes following aneurysmal subarachnoid hemorrhage (aSAH). Guidelines recommend that all patients should receive a fixed-dose ...
PMC12777563
core_pubmed_pmc
Population pharmacokinetics and optimized dosing of piperacillin-tazobactam in hematological patients with febrile neutropenia
Population pharmacokinetics and optimized dosing of piperacillin-tazobactam in hematological patients with febrile neutropenia Abstract ABSTRACT Hematological patients with febrile neutropenia receiving piperacillin-tazobactam may experience pharmacokinetic alterations that compromise drug exposure. We aimed to charact...
PMC8637767
core_pubmed_pmc
Multimodal Imaging Technology Effectively Monitors HER2 Expression in Tumors Using Trastuzumab-Coupled Organic Nanoparticles in Patient-Derived Xenograft Mice Models
Multimodal Imaging Technology Effectively Monitors HER2 Expression in Tumors Using Trastuzumab-Coupled Organic Nanoparticles in Patient-Derived Xenograft Mice Models Abstract Abstract Trastuzumab is a monoclonal antibody targeting human epidermal growth factor 2 (HER2), which has been successfully used in the treatment...
PMC10985906
core_pubmed_pmc
Anticholinesterase activities of novel isoindolin-1,3-dione-based acetohydrazide derivatives: design, synthesis, biological evaluation, molecular dynamic study
Anticholinesterase activities of novel isoindolin-1,3-dione-based acetohydrazide derivatives: design, synthesis, biological evaluation, molecular dynamic study Abstract In pursuit of developing novel cholinesterase (ChE) inhibitors through molecular hybridization theory, a novel series of isoindolin-1,3-dione-based ace...
PMC8518673
core_pubmed_pmc
Evaluation of Pharmacokinetics, Safety, and Drug‐Drug Interactions of an Oral Suspension of Edaravone in Healthy Adults
Evaluation of Pharmacokinetics, Safety, and Drug‐Drug Interactions of an Oral Suspension of Edaravone in Healthy Adults Abstract Abstract Intravenous (IV) edaravone is approved as an amyotrophic lateral sclerosis (ALS) treatment. Because IV administration places a burden on patients, development of orally administered ...
PMC4446576
core_pubmed_pmc
A Novel Simultaneous Determination of Sarpogrelate and its Active Metabolite (M-1) in Human Plasma, Using Liquid Chromatography-Tandem Mass Spectrometry: Clinical Application
A Novel Simultaneous Determination of Sarpogrelate and its Active Metabolite (M-1) in Human Plasma, Using Liquid Chromatography-Tandem Mass Spectrometry: Clinical Application Abstract Background This study describes a novel analytical method for simultaneously determining sarpogrelate and its metabolite (M-1) in human ...
PMC9202863
core_pubmed_pmc
Permeability of dopamine D2 receptor agonist hordenine across the intestinal and blood-brain barrier in vitro
Permeability of dopamine D2 receptor agonist hordenine across the intestinal and blood-brain barrier in vitro Abstract Abstract Hordenine, a bioactive food compound, has several pharmacological properties and has recently been identified as a dopamine D2 receptor (D2R) agonist. Since the pharmacokinetic profile of hord...
PMC12842855
core_pubmed_pmc
Pharmacokinetics, pharmacodynamics, and safety interaction study of tunodafil hydrochloride and alcohol: A randomized, blinded, placebo‐controlled, three‐cycle crossover study in Chinese healthy men
Pharmacokinetics, pharmacodynamics, and safety interaction study of tunodafil hydrochloride and alcohol: A randomized, blinded, placebo‐controlled, three‐cycle crossover study in Chinese healthy men Abstract Abstract Objectives This study aimed to evaluate the pharmacodynamic effects of administering tunodafil hydrochl...
PMC10690594
core_pubmed_pmc
A mechanism-based pathway toward administering highly active N-phage cocktails
A mechanism-based pathway toward administering highly active N-phage cocktails Abstract Abstract Bacteriophage (phage) therapy is being explored as a possible response to the antimicrobial resistance public health emergency. Administering a mixture of different phage types as a cocktail is one proposed strategy for the...
PMC6020478
core_pubmed_pmc
Efficacy of Nivolumab in a Patient with Metastatic Renal Cell Carcinoma and End-Stage Renal Disease on Dialysis: Case Report and Literature Review
Efficacy of Nivolumab in a Patient with Metastatic Renal Cell Carcinoma and End-Stage Renal Disease on Dialysis: Case Report and Literature Review Abstract Abstract Treatment of patients with metastatic renal cell carcinoma (mRCC) and end-stage renal disease (ESRD) on dialysis poses a therapeutic challenge, particularl...
PMC10692660
core_pubmed_pmc
A pilot study of the pharmacokinetics of continuous magnesium infusion in critically ill patients
A pilot study of the pharmacokinetics of continuous magnesium infusion in critically ill patients Abstract Objective: The pharmacokinetics and haemodynamic effect of continuous magnesium infusion in non-cardiac intensive care unit (ICU) patients are poorly understood. We aimed to measure serum and urine magnesium level...
PMC11993281
core_pubmed_pmc
Dose‐Optimization of a Novel Co‐Formulated Triple Combination Antimalarial Therapy: Artemether‐Lumefantrine‐Amodiaquine
Dose‐Optimization of a Novel Co‐Formulated Triple Combination Antimalarial Therapy: Artemether‐Lumefantrine‐Amodiaquine Abstract Abstract Artemisinin‐based combination therapy (ACT) is the first‐line therapy for uncomplicated falciparum malaria, but artemisinin resistance in Asia and now sub‐Saharan Africa is threateni...
PMC3405235
core_pubmed_pmc
Effect of abiraterone acetate plus prednisone on the QT interval in patients with metastatic castration-resistant prostate cancer
Effect of abiraterone acetate plus prednisone on the QT interval in patients with metastatic castration-resistant prostate cancer Abstract Abstract Purpose Abiraterone is the active metabolite of the pro-drug abiraterone acetate (AA) and a selective inhibitor of CYP17, a key enzyme in testosterone synthesis, and improv...
PMC10191279
core_pubmed_pmc
Interspecies evaluation of a physiologically based pharmacokinetic model to predict the biodistribution dynamics of dendritic nanoparticles
Interspecies evaluation of a physiologically based pharmacokinetic model to predict the biodistribution dynamics of dendritic nanoparticles Abstract Abstract The exposure of a dendritic nanoparticle and its conjugated active pharmaceutical ingredient (API) was determined in mouse, rat and dog, with the aim of investiga...
PMC12502012
core_pubmed_pmc
Site‐Specific Antithrombotic Therapy: 24‐Month Outcomes of the Randomized DESyne BDS Plus Trial Using a Novel Triple‐Drug Eluting Coronary Implant With Two Anticoagulants and Sirolimus
Site‐Specific Antithrombotic Therapy: 24‐Month Outcomes of the Randomized DESyne BDS Plus Trial Using a Novel Triple‐Drug Eluting Coronary Implant With Two Anticoagulants and Sirolimus Abstract ABSTRACT Background DESyne BDS Plus represents a novel triple drug therapy (TRx) applied on a coronary stent platform eluting ...
PMC10349714
core_pubmed_pmc
Neuroprotective and nephroprotective effects of Ircinia sponge in polycyclic aromatic hydrocarbons (PAHs) induced toxicity in animal model: a pharmacological and computational approach
Neuroprotective and nephroprotective effects of Ircinia sponge in polycyclic aromatic hydrocarbons (PAHs) induced toxicity in animal model: a pharmacological and computational approach Abstract The present study investigated the neuroprotective and nephroprotective effects of the sponge Ircinia sp. ethyl acetate extrac...
PMC7151106
core_pubmed_pmc
Comparative Pharmacokinetics and Pharmacodynamics of a Novel Sodium-Glucose Cotransporter 2 Inhibitor, DWP16001, with Dapagliflozin and Ipragliflozin
Comparative Pharmacokinetics and Pharmacodynamics of a Novel Sodium-Glucose Cotransporter 2 Inhibitor, DWP16001, with Dapagliflozin and Ipragliflozin Abstract Since sodium-glucose cotransporter 2 (SGLT2) inhibitors reduced blood glucose level by inhibiting renal tubular glucose reabsorption mediated by SGLT2, we aimed ...
PMC6138480
core_pubmed_pmc
In vivo affinity and target engagement in skin and blood in a first‐time‐in‐human study of an anti‐oncostatin M monoclonal antibody
In vivo affinity and target engagement in skin and blood in a first‐time‐in‐human study of an anti‐oncostatin M monoclonal antibody Abstract Abstract Aims The oncostatin M (OSM) pathway drives fibrosis, inflammation and vasculopathy, and is a potential therapeutic target for inflammatory and fibrotic diseases. The aim ...
PMC9755920
core_pubmed_pmc
Applying interpretable machine learning workflow to evaluate exposure–response relationships for large‐molecule oncology drugs
Applying interpretable machine learning workflow to evaluate exposure–response relationships for large‐molecule oncology drugs Abstract Abstract The application of logistic regression (LR) and Cox Proportional Hazard (CoxPH) models are well‐established for evaluating exposure–response (E–R) relationship in large molecu...
PMC9123906
core_pubmed_pmc
Effects of Ethanolic Extract of Schisandra sphenanthera on the Pharmacokinetics of Rosuvastatin in Rats
Effects of Ethanolic Extract of Schisandra sphenanthera on the Pharmacokinetics of Rosuvastatin in Rats Abstract Purpose Wuzhi capsule (WZ) is a proprietary Chinese medicine prepared from the ethanolic extract of Schisandra sphenanthera that is commonly used to treat liver injury. Statins are widely used in patients wi...
PMC11360071
core_pubmed_pmc
Pharmacokinetic Simulation and Area under the Curve Estimation of Drugs Subject to Enterohepatic Circulation
Pharmacokinetic Simulation and Area under the Curve Estimation of Drugs Subject to Enterohepatic Circulation Abstract Abstract Enterohepatic circulation (EHC) is a complex process where drugs undergo secretion and reabsorption from the intestinal lumen multiple times, resulting in pharmacokinetic profiles with multiple...
PMC7487994
core_pubmed_pmc
Navafenterol (AZD8871) in patients with mild asthma: a randomised placebo-controlled phase I study evaluating the safety, tolerability, pharmacokinetics, and pharmacodynamics of single ascending doses of this novel inhaled long-acting dual-pharmacology bronchodilator
Navafenterol (AZD8871) in patients with mild asthma: a randomised placebo-controlled phase I study evaluating the safety, tolerability, pharmacokinetics, and pharmacodynamics of single ascending doses of this novel inhaled long-acting dual-pharmacology bronchodilator Abstract Abstract Background Navafenterol (AZD8871) ...
PMC10990017
core_pubmed_pmc
The novel rapid formulation of intravenous dantrolene (NPJ5008) versus standard dantrolene (Dantrium®)
The novel rapid formulation of intravenous dantrolene (NPJ5008) versus standard dantrolene (Dantrium®) Abstract Abstract BACKGROUND Delays in treating anaesthesia-induced malignant hyperthermia increase risks of complications and death. NPJ5008 is a novel formulation of the indicated treatment, dantrolene sodium, devel...
PMC9411916
core_pubmed_pmc
Randomised controlled trial of fosfomycin in neonatal sepsis: pharmacokinetics and safety in relation to sodium overload
Randomised controlled trial of fosfomycin in neonatal sepsis: pharmacokinetics and safety in relation to sodium overload Abstract Objective To assess pharmacokinetics and changes to sodium levels in addition to adverse events (AEs) associated with fosfomycin among neonates with clinical sepsis. Design A single-centre o...
PMC11251614
core_pubmed_pmc
Pharmacokinetics of isavuconazonium sulfate and its active metabolite isavuconazole in healthy dogs
Pharmacokinetics of isavuconazonium sulfate and its active metabolite isavuconazole in healthy dogs Abstract Abstract Invasive fungal infections (IFIs) are growing in importance in veterinary and human medicine. IFIs such as aspergillosis, blastomycosis, coccidioidomycosis and histoplasmosis remain challenging to treat...
PMC12631411
core_pubmed_pmc
A Comprehensive Review of Medicarpin: A Phytoalexin with Therapeutic Potential
A Comprehensive Review of Medicarpin: A Phytoalexin with Therapeutic Potential Abstract Initially, research on medicarpin focused on its role in crop protection, including gene modifications, allelopathic effects, antifungal potential, and biosynthetic mechanisms. Later, various biological activities were demonstrated ...
PMC10892536
core_pubmed_pmc
Establishment and Validation of a Transdermal Drug Delivery System for the Anti-Depressant Drug Citalopram Hydrobromide
Establishment and Validation of a Transdermal Drug Delivery System for the Anti-Depressant Drug Citalopram Hydrobromide Abstract To enhance the bioavailability and antihypertensive effect of the anti-depressant drug citalopram hydrobromide (CTH) we developed a sustained-release transdermal delivery system containing CT...
PMC6669232
core_pubmed_pmc
Effects of Comedication and Genetic Factors on the Population Pharmacokinetics of Lamotrigine: A Prospective Analysis in Chinese Patients With Epilepsy
Effects of Comedication and Genetic Factors on the Population Pharmacokinetics of Lamotrigine: A Prospective Analysis in Chinese Patients With Epilepsy Abstract Abstract Lamotrigine (LTG) is a second-generation anti-epileptic drug widely used for focal and generalized seizures in adults and children, and as a first-lin...
PMC3852160
core_pubmed_pmc
PKPD Modeling of VEGF, sVEGFR-2, sVEGFR-3, and sKIT as Predictors of Tumor Dynamics and Overall Survival Following Sunitinib Treatment in GIST
PKPD Modeling of VEGF, sVEGFR-2, sVEGFR-3, and sKIT as Predictors of Tumor Dynamics and Overall Survival Following Sunitinib Treatment in GIST Abstract The predictive value of longitudinal biomarker data (vascular endothelial growth factor (VEGF), soluble VEGF receptor (sVEGFR)-2, sVEGFR-3, and soluble stem cell factor...
PMC4631180
core_pubmed_pmc
Favipiravir inhibits acetaminophen sulfate formation but minimally affects systemic pharmacokinetics of acetaminophen
Favipiravir inhibits acetaminophen sulfate formation but minimally affects systemic pharmacokinetics of acetaminophen Abstract Aims The antiviral agent favipiravir is likely to be co‐prescribed with acetaminophen (paracetamol). The present study evaluated the possiblility of a pharmacokinetic interaction between favipi...
PMC5444153
core_pubmed_pmc
Efficacy, Safety, and Tolerability of Gepotidacin (GSK2140944) in the Treatment of Patients with Suspected or Confirmed Gram-Positive Acute Bacterial Skin and Skin Structure Infections
Efficacy, Safety, and Tolerability of Gepotidacin (GSK2140944) in the Treatment of Patients with Suspected or Confirmed Gram-Positive Acute Bacterial Skin and Skin Structure Infections Abstract ABSTRACT Gepotidacin is a novel, first-in-class, triazaacenaphthylene antibacterial agent which has in vitro activity against ...
PMC7433713
core_pubmed_pmc
Beyond Single Nucleotide Polymorphisms: CYP3A5 ∗ 3 ∗ 6 ∗ 7 Composite and ABCB1 Haplotype Associations to Tacrolimus Pharmacokinetics in Black and White Renal Transplant Recipients
Beyond Single Nucleotide Polymorphisms: CYP3A5 ∗ 3 ∗ 6 ∗ 7 Composite and ABCB1 Haplotype Associations to Tacrolimus Pharmacokinetics in Black and White Renal Transplant Recipients Abstract Abstract Interpatient variability in tacrolimus pharmacokinetics is attributed to metabolism by cytochrome P-450 3A5 (CYP3A5) isoen...
PMC9588345
core_pubmed_pmc
Mechanisms Underlying the Differences in the Pharmacokinetics of Six Active Constituents of Huangqi Liuyi Decoction between Normal and Diabetic Nephropathy Mouse Models
Mechanisms Underlying the Differences in the Pharmacokinetics of Six Active Constituents of Huangqi Liuyi Decoction between Normal and Diabetic Nephropathy Mouse Models Abstract The aim of this study was to explore the mechanisms underlying the differences in the pharmacokinetics of Huangqi Liuyi decoction extract (HQD...
PMC5431384
core_pubmed_pmc
Human Abuse Potential of an Abuse-Deterrent (AD), Extended-Release (ER) Morphine Product Candidate (Morphine-ADER Injection-Molded Tablets) versus Extended-Release Morphine Administered Orally in Nondependent Recreational Opioid Users
Human Abuse Potential of an Abuse-Deterrent (AD), Extended-Release (ER) Morphine Product Candidate (Morphine-ADER Injection-Molded Tablets) versus Extended-Release Morphine Administered Orally in Nondependent Recreational Opioid Users Abstract Objective . To compare the relative human abuse potential of intact and mani...
PMC6134777
core_pubmed_pmc
Cefepime dosing regimens in critically ill patients receiving continuous renal replacement therapy: a Monte Carlo simulation study
Cefepime dosing regimens in critically ill patients receiving continuous renal replacement therapy: a Monte Carlo simulation study Abstract Background Cefepime can be removed by continuous renal replacement therapy (CRRT) due to its pharmacokinetics. The purpose of this study is to define the optimal cefepime dosing re...
PMC9275503
core_pubmed_pmc
Preparation and in vitro and in vivo evaluation of an isoliquiritigenin-loaded ophthalmic nanoemulsion for the treatment of corneal neovascularization
Preparation and in vitro and in vivo evaluation of an isoliquiritigenin-loaded ophthalmic nanoemulsion for the treatment of corneal neovascularization Abstract Abstract Isoliquiritigenin (ISL), as a natural flavonoid, has been proven to have therapeutic potential for corneal neovascularization (CNV) treatment; however,...
PMC6271955
core_pubmed_pmc
Pharmacokinetics of BMEDA after Intravenous Administration in Beagle Dogs
Pharmacokinetics of BMEDA after Intravenous Administration in Beagle Dogs Abstract The pharmacokinetics of N , N -bis(2-mercapatoethly)- N ', N '-diethylenediamine (BMEDA), a molecule that can form a chelate with rhenium-188 ( 188 Re) to produce the 188 Re-BMEDA-liposomes, was studied. In this work, beagles received a ...
PMC8212730
core_pubmed_pmc
Population pharmacokinetic and exposure‐response analyses of ivosidenib in patients with IDH1 ‐mutant advanced hematologic malignancies
Population pharmacokinetic and exposure‐response analyses of ivosidenib in patients with IDH1 ‐mutant advanced hematologic malignancies Abstract Abstract Ivosidenib is a once daily (q.d.), orally available, potent mutant isocitrate dehydrogenase 1 (mIDH1) inhibitor approved for treatment of patients with relapsed or re...
PMC8464239
core_pubmed_pmc
Pharmacokinetics of zonisamide after oral single dosing and multiple‐dose escalation administration in domestic chickens ( Gallus gallus )
Pharmacokinetics of zonisamide after oral single dosing and multiple‐dose escalation administration in domestic chickens ( Gallus gallus ) Abstract Abstract Background There are few effective drugs for treatment of seizures in avian species. Objectives To investigate the pharmacokinetics and safety of zonisamide in chi...
PMC10525795
core_pubmed_pmc
Pharmacokinetics of Four Tyrosine Kinase Inhibitors in Adult and Paediatric Chronic Myeloid Leukaemia Patients
Pharmacokinetics of Four Tyrosine Kinase Inhibitors in Adult and Paediatric Chronic Myeloid Leukaemia Patients Abstract Tyrosine kinase inhibitors work by blocking the tyrosine kinases responsible for the dysregulation of intracellular signalling pathways in tumour cells. This study looked at the impact of age and sex ...
PMC11807123
core_pubmed_pmc
Development of highly bioactive long-acting recombinant porcine FSH for batch production management of sows
Development of highly bioactive long-acting recombinant porcine FSH for batch production management of sows Abstract To improve the economic benefits, exogenous hormones are used to control follicular development and synchronize ovulation in the batch flow management of gilts and weaned sows. Equine chorionic gonadotro...
PMC6466385
core_pubmed_pmc
A Three-Compartment Pharmacokinetic Model to Predict the Interstitial Concentration of Talaporfin Sodium in the Myocardium for Photodynamic Therapy: A Method Combining Measured Fluorescence and Analysis of the Compartmental Origin of the Fluorescence
A Three-Compartment Pharmacokinetic Model to Predict the Interstitial Concentration of Talaporfin Sodium in the Myocardium for Photodynamic Therapy: A Method Combining Measured Fluorescence and Analysis of the Compartmental Origin of the Fluorescence Abstract Abstract To evaluate the effectiveness of photodynamic thera...
PMC9572380
core_pubmed_pmc
Effect of Hydrophilic Polymers on the Release Rate and Pharmacokinetics of Acyclovir Tablets Obtained by Wet Granulation: In Vitro and In Vivo Assays
Effect of Hydrophilic Polymers on the Release Rate and Pharmacokinetics of Acyclovir Tablets Obtained by Wet Granulation: In Vitro and In Vivo Assays Abstract This study aims to evaluate the feasibility of producing acyclovir-containing modified release matrix tablets by a wet granulation method based on the type and c...
PMC10237096
core_pubmed_pmc
Assessment of delayed bleeding after endoscopic submucosal dissection of early-stage gastrointestinal tumors in patients receiving direct oral anticoagulants
Assessment of delayed bleeding after endoscopic submucosal dissection of early-stage gastrointestinal tumors in patients receiving direct oral anticoagulants Abstract Delayed bleeding is a major and serious adverse event of endoscopic submucosal dissection (ESD) for early-stage gastrointestinal tumors. The rate of post...
PMC10620511
core_pubmed_pmc
In vitro to clinical translation of combinatorial effects of doxorubicin and dexrazoxane in breast cancer: a mechanism-based pharmacokinetic/pharmacodynamic modeling approach
In vitro to clinical translation of combinatorial effects of doxorubicin and dexrazoxane in breast cancer: a mechanism-based pharmacokinetic/pharmacodynamic modeling approach Abstract Abstract Dexrazoxane (DEX) is the only drug clinically approved to treat Doxorubicin-induced cardiotoxicity (DIC), however its impact on...
PMC11912929
core_pubmed_pmc
Bioequivalence Study of Single-Pill Capsule Formulation of Amlodipine Plus Benazepril in Healthy Chinese Subjects Under Fasting and Fed Conditions
Bioequivalence Study of Single-Pill Capsule Formulation of Amlodipine Plus Benazepril in Healthy Chinese Subjects Under Fasting and Fed Conditions Abstract Abstract Background The aim of the study was to evaluate the pharmacokinetic (PK) properties and safety profiles of test and reference amlodipine/benazepril capsule...
PMC6615023
core_pubmed_pmc
Elaboration and characterization of curcumin-loaded Tri-CL-mPEG three-arm copolymeric nanoparticles by a microchannel technology
Elaboration and characterization of curcumin-loaded Tri-CL-mPEG three-arm copolymeric nanoparticles by a microchannel technology Abstract Abstract Purpose: Clinical applications of curcumin (Cur) have been greatly restricted due to its low solubility and poor systemic bioavailability. Three-arm amphiphilic copolymer tr...
PMC11897554
core_pubmed_pmc
Pharmacokinetic effect of disease severity and use of extracorporeal membrane oxygenation in critically ill Asian patients receiving vancomycin
Pharmacokinetic effect of disease severity and use of extracorporeal membrane oxygenation in critically ill Asian patients receiving vancomycin Abstract Abstract Purpose Vancomycin is an essential antibiotic for the treatment of severe gram-positive bacterial infections, including methicillin-resistant Staphylococcus a...
PMC12884172
core_pubmed_pmc
Ginseng and its active compounds in ovarian aging: mechanistic basis and translational prospects
Ginseng and its active compounds in ovarian aging: mechanistic basis and translational prospects Abstract Ovarian aging is characterized by follicular depletion and declining oocyte quality, encompassing both physiological age-related decline and pathological forms such as diminished ovarian reserve, premature ovarian ...
PMC10399172
core_pubmed_pmc
Application of Allometric Scaling to Nanochelator Pharmacokinetics
Application of Allometric Scaling to Nanochelator Pharmacokinetics Abstract Deferoxamine (DFO) is an effective FDA-approved iron chelator; however, its use is considerably limited by off-target toxicities and an extremely cumbersome dose regimen involving daily infusions. The recent development of a deferoxamine-based ...
PMC4224077
core_pubmed_pmc
Computational investigation of potential dosing schedules for a switch of medication from warfarin to rivaroxaban—an oral, direct Factor Xa inhibitor
Computational investigation of potential dosing schedules for a switch of medication from warfarin to rivaroxaban—an oral, direct Factor Xa inhibitor Abstract Abstract The long-lasting anticoagulant effect of vitamin K antagonists can be problematic in cases of adverse drug reactions or when patients are switched to an...
PMC10469630
core_pubmed_pmc
Microfluidic technology and simulation models in studying pharmacokinetics during pregnancy
Microfluidic technology and simulation models in studying pharmacokinetics during pregnancy Abstract Abstract Introduction: Preterm birth rates and maternal and neonatal mortality remain concerning global health issues, necessitating improved strategies for testing therapeutic compounds during pregnancy. Current 2D or ...
PMC5324257
core_pubmed_pmc
Malaria parasite clearance
Malaria parasite clearance Abstract Following anti-malarial drug treatment asexual malaria parasite killing and clearance appear to be first order processes. Damaged malaria parasites in circulating erythrocytes are removed from the circulation mainly by the spleen. Splenic clearance functions increase markedly in acut...
PMC11597675
core_pubmed_pmc
Principles and Biomedical Applications of Self-Assembled Peptides: Potential Treatment of Type 2 Diabetes Mellitus
Principles and Biomedical Applications of Self-Assembled Peptides: Potential Treatment of Type 2 Diabetes Mellitus Abstract Type 2 diabetes mellitus (T2DM) is the most prevalent metabolic disorder worldwide. There have been tremendous efforts to find a safe and prolonged effective therapy for its treatment. Peptide hor...
PMC6519757
core_pubmed_pmc
First‐in‐Human Phase I Study of MBC‐11, a Novel Bone‐Targeted Cytarabine‐Etidronate Conjugate in Patients with Cancer‐Induced Bone Disease
First‐in‐Human Phase I Study of MBC‐11, a Novel Bone‐Targeted Cytarabine‐Etidronate Conjugate in Patients with Cancer‐Induced Bone Disease Abstract Abstract Lessons Learned. Results are consistent with MBC‐11 targeting and treating cancer‐induced bone lesions by concentrating cytarabine and etidronate at the site of di...
PMC6875711
core_pubmed_pmc
Physiologically‐Based Pharmacokinetic Modeling vs. Allometric Scaling for the Prediction of Infliximab Pharmacokinetics in Pediatric Patients
Physiologically‐Based Pharmacokinetic Modeling vs. Allometric Scaling for the Prediction of Infliximab Pharmacokinetics in Pediatric Patients Abstract The comparative performances of physiologically‐based pharmacokinetic ( PBPK ) modeling and allometric scaling for predicting the pharmacokinetics (PKs) of large molecul...
PMC10234547
core_pubmed_pmc
Population pharmacokinetic model of ivermectin in mass drug administration against lymphatic filariasis
Population pharmacokinetic model of ivermectin in mass drug administration against lymphatic filariasis Abstract Background Ivermectin (IVM) is a broad–spectrum anthelmintic drug used to treat diseases caused by filarial worms, such as onchocerciasis and lymphatic filariasis (LF). IVM is part of a triple–drug therapy u...
PMC7442995
core_pubmed_pmc
Pharmacokinetics of Bismuth following Oral Administration of Wei Bi Mei in Healthy Chinese Volunteers
Pharmacokinetics of Bismuth following Oral Administration of Wei Bi Mei in Healthy Chinese Volunteers Abstract Abstract Background Bismuth-containing quadruple therapy achieves higher eradication rate of Helicobacter pylori . High level of bismuth in blood may result in damage of many organs. Wei Bi Mei is a new bismut...
PMC10812532
core_pubmed_pmc
Dosage Optimisation of Trimethoprim and Sulfamethoxazole for the Treatment of an Avian Pathogenic Strain of Escherichia coli in Broiler Chickens
Dosage Optimisation of Trimethoprim and Sulfamethoxazole for the Treatment of an Avian Pathogenic Strain of Escherichia coli in Broiler Chickens Abstract Based on pharmacokinetic studies carried out according to the methodologies defined by the European Medicines Agency (EMA) using mass spectrometry analysis, a new for...
PMC6441814
core_pubmed_pmc
Pharmacokinetic and pharmacodynamic integration of enrofloxacin against Salmonella Enteritidis after administering to broiler chicken by per-oral and intravenous routes
Pharmacokinetic and pharmacodynamic integration of enrofloxacin against Salmonella Enteritidis after administering to broiler chicken by per-oral and intravenous routes Abstract Abstract It is crucial to optimize the dose of fluoroquinolones to avoid antibiotic resistance and to attain clinical success. We undertook th...
PMC9293227
core_pubmed_pmc
Assessment of the Effect of Filgotinib on the Pharmacokinetics of Atorvastatin, Pravastatin, and Rosuvastatin in Healthy Adult Participants
Assessment of the Effect of Filgotinib on the Pharmacokinetics of Atorvastatin, Pravastatin, and Rosuvastatin in Healthy Adult Participants Abstract Abstract Filgotinib, an oral Janus kinase‐1 preferential inhibitor, is approved in Europe and Japan for adults with rheumatoid arthritis. Patients with rheumatoid arthriti...
PMC12174348
core_pubmed_pmc
Monoclonal humanized monovalent antibody blocking therapy for anti-NMDA receptor encephalitis
Monoclonal humanized monovalent antibody blocking therapy for anti-NMDA receptor encephalitis Abstract Abstract Anti-NMDA receptor (NMDAR) encephalitis is a devastating disease with severe psychiatric and neurological symptoms believed to be caused by pathogenic autoantibodies that bind to the N-terminal domain (NTD) o...
PMC10534867
core_pubmed_pmc
Topical Micro-Emulsion of 5-Fluorouracil by a Twin Screw Processor-Based Novel Continuous Manufacturing Process for the Treatment of Skin Cancer: Preparation and In Vitro and In Vivo Evaluations
Topical Micro-Emulsion of 5-Fluorouracil by a Twin Screw Processor-Based Novel Continuous Manufacturing Process for the Treatment of Skin Cancer: Preparation and In Vitro and In Vivo Evaluations Abstract 5-Fluorouracil (5-FU), a BCS class III drug, has low oral bioavailability and is cytotoxic in nature causing severe ...
PMC4249529
core_pubmed_pmc
Effects of Dosage, Comorbidities, and Food on Isoniazid Pharmacokinetics in Peruvian Tuberculosis Patients
Effects of Dosage, Comorbidities, and Food on Isoniazid Pharmacokinetics in Peruvian Tuberculosis Patients Abstract Poor response to tuberculosis (TB) therapy might be attributable to subtherapeutic levels in drug-compliant patients. Pharmacokinetic (PK) parameters can be affected by several factors, such as comorbidit...
PMC8775906
core_pubmed_pmc
Dosing Therapeutic Radiopharmaceuticals in Obese Patients
Dosing Therapeutic Radiopharmaceuticals in Obese Patients Abstract Abstract The prevalence of obesity has increased dramatically in the Western population. Obesity is known to influence not only the proportion of adipose tissue but also physiological processes that could alter drug pharmacokinetics. Yet, there are no s...
PMC8468506
core_pubmed_pmc
Direct Oral Anticoagulants in Patients with Obesity and Atrial Fibrillation: Position Paper of Italian National Association of Hospital Cardiologists (ANMCO)
Direct Oral Anticoagulants in Patients with Obesity and Atrial Fibrillation: Position Paper of Italian National Association of Hospital Cardiologists (ANMCO) Abstract Abstract The use of the direct oral anticoagulants dabigatran, rivaroxaban, apixaban and edoxaban (DOACs) offers some major advantages over warfarin and ...
PMC10044408
core_pubmed_pmc
Update on Therapeutic Drug Monitoring of Beta-Lactam Antibiotics in Critically Ill Patients—A Narrative Review
Update on Therapeutic Drug Monitoring of Beta-Lactam Antibiotics in Critically Ill Patients—A Narrative Review Abstract Beta-lactam antibiotics remain one of the most preferred groups of antibiotics in critical care due to their excellent safety profiles and their activity against a wide spectrum of pathogens. The corn...
PMC4370505
core_pubmed_pmc
Stabilization of Resveratrol in Blood Circulation by Conjugation to mPEG and mPEG-PLA Polymers: Investigation of Conjugate Linker and Polymer Composition on Stability, Metabolism, Antioxidant Activity and Pharmacokinetic Profile
Stabilization of Resveratrol in Blood Circulation by Conjugation to mPEG and mPEG-PLA Polymers: Investigation of Conjugate Linker and Polymer Composition on Stability, Metabolism, Antioxidant Activity and Pharmacokinetic Profile Abstract Abstract Resveratrol is naturally occurring phytochemical with diverse biological ...
PMC6156125
core_pubmed_pmc
Chemistry and Hypoglycemic Activity of GPR119 Agonist ZB-16
Chemistry and Hypoglycemic Activity of GPR119 Agonist ZB-16 Abstract This article is to highlight the chemical properties and primary pharmacology of novel GPR119 agonist ZB-16 and its analogs, which were rejected during the screening. Experiments were performed in vitro (specific activity, metabolism and cell toxicity...
PMC3858995
core_pubmed_pmc
Interaction of Acupuncture and Electroacupuncture on the Pharmacokinetics of Aspirin and the Effect of Brain Blood Flow in Rats
Interaction of Acupuncture and Electroacupuncture on the Pharmacokinetics of Aspirin and the Effect of Brain Blood Flow in Rats Abstract Acupuncture and electroacupuncture have been used to improve the brain and motor functions of poststroke patients, and aspirin is used for the prevention of stroke recurrence. Our hyp...