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PMC8604233
core_pubmed_pmc
The necessary conduct: Exploratory multiregional clinical trials in East Asia
The necessary conduct: Exploratory multiregional clinical trials in East Asia Abstract Abstract Various studies have highlighted the importance of ethnic differences. The consideration of ethnic differences in the field of individualized pharmacotherapy is imperative. Therefore, various organizations and networks acros...
PMC10796130
core_pubmed_pmc
A Parametric Time-to-Event Modelling of Recurrent Ischemic Stroke After Index Stroke Among Patients With and Without Diabetes Mellitus: Implementation of Temporal Validation of the Model
A Parametric Time-to-Event Modelling of Recurrent Ischemic Stroke After Index Stroke Among Patients With and Without Diabetes Mellitus: Implementation of Temporal Validation of the Model Abstract Abstract Objectives Compared with the first stroke, neurological impairment caused by stroke recurrence is more serious, mor...
PMC9286721
core_pubmed_pmc
Development and application of a pediatric mechanistic kidney model
Development and application of a pediatric mechanistic kidney model Abstract Abstract Pediatric physiologically‐based pharmacokinetic (P‐PBPK) models have been used to predict age related changes in the pharmacokinetics (PKs) of renally cleared drugs mainly in relation to changes in glomerular filtration rate. With eme...
PMC10819442
core_pubmed_pmc
Real-Time TDM-Guided Optimal Joint PK/PD Target Attainment of Continuous Infusion Piperacillin–Tazobactam Monotherapy Is an Effective Carbapenem-Sparing Strategy for Treating Non-Severe ESBL-Producing Enterobacterales Secondary Bloodstream Infections: Findings from a Prospective Pilot Study
Real-Time TDM-Guided Optimal Joint PK/PD Target Attainment of Continuous Infusion Piperacillin–Tazobactam Monotherapy Is an Effective Carbapenem-Sparing Strategy for Treating Non-Severe ESBL-Producing Enterobacterales Secondary Bloodstream Infections: Findings from a Prospective Pilot Study Abstract Abstract (1) Object...
PMC12766025
core_pubmed_pmc
Solidification of SNEDDS Using Mesoporous Carriers (2020–2025): A Review of Design, Biopharmaceutical Enhancement, and Therapeutic Impact
Solidification of SNEDDS Using Mesoporous Carriers (2020–2025): A Review of Design, Biopharmaceutical Enhancement, and Therapeutic Impact Abstract Abstract Self-nanoemulsifying drug delivery systems (SNEDDS) have been widely developed as a practical approach to enhance the bioavailability of poorly water-soluble drugs ...
PMC5261556
core_pubmed_pmc
Paclitaxel-loaded hyaluronan solid nanoemulsions for enhanced treatment efficacy in ovarian cancer
Paclitaxel-loaded hyaluronan solid nanoemulsions for enhanced treatment efficacy in ovarian cancer Abstract Abstract Paclitaxel-loaded hyaluronan solid nanoemulsions (PTX-HSNs) were successfully fabricated for the delivery of PTX to improve ovarian cancer treatment via active tumor targeting. PTX-HSNs were fabricated u...
PMC8302240
core_pubmed_pmc
Personalise vitamin D 3 using physiologically based pharmacokinetic modelling
Personalise vitamin D 3 using physiologically based pharmacokinetic modelling Abstract Abstract Plasma concentration of vitamin D 3 metabolite 25‐hydroxyvitamin D 3 (25(OH)D 3 ) is variable among individuals. The objective of this study is to establish an accurate model for 25(OH)D 3 pharmacokinetics (PKs) to support s...
PMC6365258
core_pubmed_pmc
What concentration of tranexamic acid is needed to inhibit fibrinolysis? A systematic review of pharmacodynamics studies
What concentration of tranexamic acid is needed to inhibit fibrinolysis? A systematic review of pharmacodynamics studies Abstract Supplemental Digital Content is available in the text Keywords: fibrinolysis, pharmacodynamics, systematic review, tissue plasminogen activator, tranexamic acid Abstract Intravenous tranexam...
PMC3299545
core_pubmed_pmc
Safety and efficacy of dual therapy with GSK233705 and salmeterol versus monotherapy with salmeterol, tiotropium, or placebo in a crossover pilot study in partially reversible COPD patients
Safety and efficacy of dual therapy with GSK233705 and salmeterol versus monotherapy with salmeterol, tiotropium, or placebo in a crossover pilot study in partially reversible COPD patients Abstract Background GSK233705 is an inhaled, long-acting muscarinic antagonist in development for the treatment of chronic obstruc...
PMC3155838
core_pubmed_pmc
Optimal designs for population pharmacokinetic studies of oral artesunate in patients with uncomplicated falciparum malaria
Optimal designs for population pharmacokinetic studies of oral artesunate in patients with uncomplicated falciparum malaria Abstract Abstract Background Currently, population pharmacokinetic (PK) studies of anti-malarial drugs are designed primarily by the logistical and ethical constraints of taking blood samples from...
PMC12299981
core_pubmed_pmc
Human Metabolism of Sirolimus Revisited
Human Metabolism of Sirolimus Revisited Abstract Abstract Background: Sirolimus (SRL, rapamycin) is a clinically important mTOR inhibitor used in immunosuppression, oncology, and cardiovascular drug-eluting devices. Despite its long-standing FDA approval, the human metabolic profile of SRL remains incompletely characte...
PMC8756085
core_pubmed_pmc
Effects of Mixing Energy Drinks With Alcohol on Driving-Related Skills
Effects of Mixing Energy Drinks With Alcohol on Driving-Related Skills Abstract Abstract Background Energy drinks (EDs) reduce sleepiness and fatigue and improve driving performance whereas alcohol does just the opposite. Although it is a trendy combination among young people, the effects of alcohol mixed with EDs on d...
PMC6156363
core_pubmed_pmc
The Modulatory Role of CYP3A4 in Dictamnine-Induced Hepatotoxicity
The Modulatory Role of CYP3A4 in Dictamnine-Induced Hepatotoxicity Abstract Abstract Dictamni Cortex (DC) has been reported to be associated with acute hepatitis in clinic and may lead to a selective sub-chronic hepatotoxicity in rats. Nevertheless, the potent toxic ingredient and the underlying mechanism remain unknow...
PMC9940175
core_pubmed_pmc
Effects of Two Different Doses of Ursodeoxycholic Acid on Indirect Hyperbilirubinemia in Neonates with Glucose-6-phosphate Dehydrogenase Deficiency Treated with Phototherapy: A Randomized Controlled Trial
Effects of Two Different Doses of Ursodeoxycholic Acid on Indirect Hyperbilirubinemia in Neonates with Glucose-6-phosphate Dehydrogenase Deficiency Treated with Phototherapy: A Randomized Controlled Trial Abstract Abstract Glucose-6-phosphate dehydrogenase (G6PD) deficiency is one of the causes of severe hyperbilirubin...
PMC12799588
core_pubmed_pmc
Pharmacological considerations for next-generation protein therapeutics in cardiovascular disease
Pharmacological considerations for next-generation protein therapeutics in cardiovascular disease Abstract Cardiovascular disease (CVD) remains the leading cause of death worldwide despite decades of therapeutic advances. Emerging insights into its etiology have revealed previously unappreciated cellular and molecular ...
PMC5667814
core_pubmed_pmc
Elimination kinetics of ceftiofur hydrochloride in milk after an 8-day extended intramammary administration in healthy and infected cows
Elimination kinetics of ceftiofur hydrochloride in milk after an 8-day extended intramammary administration in healthy and infected cows Abstract Abstract Ceftiofur hydrochloride (CEF) is occasionally used for the intramammary (IMM) treatment of mastitis. This extralabel manner could result in a drug-residue violation ...
PMC11382452
core_pubmed_pmc
Kinetics of fluoride after brushing with the no-rinse method
Kinetics of fluoride after brushing with the no-rinse method Abstract Background Fluoride plays a vital role in preventing dental caries, with its addition to oral care products significantly promoting oral hygiene. A no-rinse brushing method aims to increase fluoride retention in the oral cavity, as rinsing with water...
PMC5723699
core_pubmed_pmc
Randomized clinical study of safety, pharmacokinetics, and pharmacodynamics of RIPK 1 inhibitor GSK 2982772 in healthy volunteers
Randomized clinical study of safety, pharmacokinetics, and pharmacodynamics of RIPK 1 inhibitor GSK 2982772 in healthy volunteers Abstract Abstract GSK 2982772 is a highly selective inhibitor of receptor‐interacting protein kinase 1 ( RIPK 1) being developed to treat chronic inflammatory diseases. This first‐in‐human s...
PMC5983770
core_pubmed_pmc
Preferential Inhibition of Wnt/β-Catenin Signaling by Novel Benzimidazole Compounds in Triple-Negative Breast Cancer
Preferential Inhibition of Wnt/β-Catenin Signaling by Novel Benzimidazole Compounds in Triple-Negative Breast Cancer Abstract Abstract Wnt/β-catenin signaling is upregulated in triple-negative breast cancer (TNBC) compared to other breast cancer subtypes and normal tissues. Current Wnt/β-catenin inhibitors, such as nic...
PMC4269827
core_pubmed_pmc
In Silico Comparison Between Metoprolol Succinate and Bisoprolol on 24-Hour Systolic Blood Pressures
In Silico Comparison Between Metoprolol Succinate and Bisoprolol on 24-Hour Systolic Blood Pressures Abstract Abstract Objective To compare the effects of bisoprolol and metoprolol CR/ZOK (metoprolol succinate controlled release) on systolic blood pressure (bp sys ) over a 24-h period in an in silico model. Methods On ...
PMC4976878
core_pubmed_pmc
Brucella melitensis Methionyl-tRNA-Synthetase (MetRS), a Potential Drug Target for Brucellosis
Brucella melitensis Methionyl-tRNA-Synthetase (MetRS), a Potential Drug Target for Brucellosis Abstract Abstract We investigated Brucella melitensis methionyl-tRNA-synthetase ( Bm MetRS) with molecular, structural and phenotypic methods to learn if Bm MetRS is a promising target for brucellosis drug development. Recomb...
PMC10043734
core_pubmed_pmc
Change of metformin concentrations in the liver as a pharmacological target site of metformin after long-term combined treatment with ginseng berry extract
Change of metformin concentrations in the liver as a pharmacological target site of metformin after long-term combined treatment with ginseng berry extract Abstract Metformin as an oral glucose-lowering drug is used to treat type 2 diabetic mellitus. Considering the relatively high incidence of cardiovascular complicat...
PMC8934724
core_pubmed_pmc
A physiologically based pharmacokinetic model of clopidogrel in populations of European and Japanese ancestry: An evaluation of CYP2C19 activity
A physiologically based pharmacokinetic model of clopidogrel in populations of European and Japanese ancestry: An evaluation of CYP2C19 activity Abstract ABSTRACT Treatment response to clopidogrel is associated with CYP2C19 activity through the formation of the active H4 metabolite. The aims of this study were to devel...
PMC12022903
core_pubmed_pmc
Evaluation of drug-drug interaction between Suraxavir Marboxil (GP681) and itraconazole, and assessment of the impact of gene polymorphism
Evaluation of drug-drug interaction between Suraxavir Marboxil (GP681) and itraconazole, and assessment of the impact of gene polymorphism Abstract Introduction Suraxavir Marboxil (GP681) is a prodrug metabolized to GP1707D07, which inhibits influenza viral replication by targeting cap-dependent endonuclease through a ...
PMC5124745
core_pubmed_pmc
Pharmacokinetic Modeling of Paracetamol Uptake and Clearance in Zebrafish Larvae: Expanding the Allometric Scale in Vertebrates with Five Orders of Magnitude
Pharmacokinetic Modeling of Paracetamol Uptake and Clearance in Zebrafish Larvae: Expanding the Allometric Scale in Vertebrates with Five Orders of Magnitude Abstract Abstract Zebrafish larvae ( Danio rerio ) are increasingly used to translate findings regarding drug efficacy and safety from in vitro -based assays to v...
PMC10033950
core_pubmed_pmc
PK-PD Evaluation of Inhaled Microparticles loaded with Ciprofloxacin-Copper complex in a Rat Model of Chronic Pseudomonas aeruginosa Lung Infection.
PK-PD Evaluation of Inhaled Microparticles loaded with Ciprofloxacin-Copper complex in a Rat Model of Chronic Pseudomonas aeruginosa Lung Infection. Abstract Abstract The potential gain in efficacy of pulmonary administration over IV administration of some antibiotics such as ciprofloxacin (CIP) may be limited by the s...
PMC11567960
core_pubmed_pmc
Preclinical pharmacology characterization of HX009, a novel PD1 x CD47 Bi-specific antibody
Preclinical pharmacology characterization of HX009, a novel PD1 x CD47 Bi-specific antibody Abstract Abstract Certain immune-checkpoint inhibitors have a narrow therapeutic window (TW) as cancer therapeutics, and engineered dual-/multi-targeting agents could potentially widen the TW to bring true clinical benefits. We ...
PMC9328660
core_pubmed_pmc
Similar pharmacokinetics of three dosing regimens comprising two oral delayed‐release mesalamine formulations in healthy adult volunteers: Randomised, open‐label, parallel‐group study
Similar pharmacokinetics of three dosing regimens comprising two oral delayed‐release mesalamine formulations in healthy adult volunteers: Randomised, open‐label, parallel‐group study Abstract Abstract Aims Mesalamine is the first‐line therapy for treating mild‐to‐moderate ulcerative colitis. Multiple mesalamine formul...
PMC8541456
core_pubmed_pmc
Molecular Epidemiology, Antimicrobial Surveillance, and PK/PD Analysis to Guide the Treatment of Neisseria gonorrhoeae Infections
Molecular Epidemiology, Antimicrobial Surveillance, and PK/PD Analysis to Guide the Treatment of Neisseria gonorrhoeae Infections Abstract Abstract The aim of this study was to apply molecular epidemiology, antimicrobial surveillance, and PK/PD analysis to guide the antimicrobial treatment of gonococci infections in a ...
PMC4971058
core_pubmed_pmc
Veterinary Medicine Needs New Green Antimicrobial Drugs
Veterinary Medicine Needs New Green Antimicrobial Drugs Abstract Given that: (1) the worldwide consumption of antimicrobial drugs (AMDs) used in food-producing animals will increase over the coming decades; (2) the prudent use of AMDs will not suffice to stem the rise in human antimicrobial resistance (AMR) of animal o...
PMC12195082
core_pubmed_pmc
From Nature to Nanomedicine: Enhancing the Antitumor Efficacy of Rhein, Curcumin, and Resveratrol
From Nature to Nanomedicine: Enhancing the Antitumor Efficacy of Rhein, Curcumin, and Resveratrol Abstract Abstract Natural compounds have garnered increasing interest as potential antitumor agents due to their multifaceted biological activities and relatively low toxicity profiles. This review focuses on three well-st...
PMC3589659
core_pubmed_pmc
A Phase I, open-label, dose escalation study of afatinib, in a 3-week-on/1-week-off schedule in patients with advanced solid tumors
A Phase I, open-label, dose escalation study of afatinib, in a 3-week-on/1-week-off schedule in patients with advanced solid tumors Abstract Summary Background A Phase I study to determine the maximum tolerated dose (MTD) and pharmacokinetics of afatinib (BIBW 2992), a novel irreversible ErbB Family Blocker, administer...
PMC9760816
core_pubmed_pmc
Targeting cancer-related inflammation with non-steroidal anti-inflammatory drugs: Perspectives in pharmacogenomics
Targeting cancer-related inflammation with non-steroidal anti-inflammatory drugs: Perspectives in pharmacogenomics Abstract Abstract Inflammatory processes are essential for innate immunity and contribute to carcinogenesis in various malignancies, such as colorectal cancer, esophageal cancer and lung cancer. Pharmacoth...
PMC4757991
core_pubmed_pmc
The influence of pregnancy on the pharmacokinetic properties of artemisinin combination therapy (ACT): a systematic review
The influence of pregnancy on the pharmacokinetic properties of artemisinin combination therapy (ACT): a systematic review Abstract Abstract Background Pregnancy has been reported to alter the pharmacokinetic properties of anti-malarial drugs, including the different components of artemisinin-based combination therapy ...
PMC3940691
core_pubmed_pmc
Germline genetic variants in ABCB1 , ABCC1 , and ALDH1A1 and risk of hematological and gastrointestinal toxicities in a SWOG Phase III trial S0221 for breast cancer
Germline genetic variants in ABCB1 , ABCC1 , and ALDH1A1 and risk of hematological and gastrointestinal toxicities in a SWOG Phase III trial S0221 for breast cancer Abstract Hematological and gastrointestinal toxicities are common among patients treated with cyclophosphamide and doxorubicin for breast cancer. To examin...
PMC8663953
core_pubmed_pmc
Tuberculosis and pharmacological interactions: A narrative review
Tuberculosis and pharmacological interactions: A narrative review Abstract Even if major improvements in therapeutic regimens and treatment outcomes have been progressively achieved, tuberculosis (TB) remains the leading cause of death from a single infectious microorganism. To improve TB treatment success as well as p...
PMC4266249
core_pubmed_pmc
Pharmacokinetics and safety of dexlansoprazole MR in pediatric patients with symptomatic gastroesophageal reflux disease
Pharmacokinetics and safety of dexlansoprazole MR in pediatric patients with symptomatic gastroesophageal reflux disease Abstract Objective To evaluate the safety and pharmacokinetic profile of dexlansoprazole modified-release (MR) capsules in pediatric patients with symptomatic gastroesophageal reflux disease (GERD). ...
PMC10976559
core_pubmed_pmc
Synthetic exendin-4 disrupts responding to reward predictive incentive cues in male rats
Synthetic exendin-4 disrupts responding to reward predictive incentive cues in male rats Abstract Abstract Synthetic exendin-4 (EX4, exenatide), is a GLP-1 receptor agonist used clinically to treat glycemia in Type-2 diabetes mellitus. EX4 also promotes weight loss and alters food reward-seeking behaviors in part due t...
PMC3852277
core_pubmed_pmc
Long-acting methylphenidate formulations in the treatment of attention-deficit/hyperactivity disorder: a systematic review of head-to-head studies
Long-acting methylphenidate formulations in the treatment of attention-deficit/hyperactivity disorder: a systematic review of head-to-head studies Abstract Background The stimulant methylphenidate (MPH) has been a mainstay of treatment for attention-deficit/hyperactivity disorder (ADHD) for many years. Owing to the sho...
PMC11737169
core_pubmed_pmc
Risk of hemorrhagic fever with renal syndrome associated with meteorological factors in diverse epidemic regions: a nationwide longitudinal study in China
Risk of hemorrhagic fever with renal syndrome associated with meteorological factors in diverse epidemic regions: a nationwide longitudinal study in China Abstract Background Hemorrhagic fever with renal syndrome (HFRS) is a climate-sensitive zoonotic disease that poses a significant public health burden worldwide. Whi...
PMC5431734
core_pubmed_pmc
Preparation, characterization, and in vitro/vivo studies of oleanolic acid-loaded lactoferrin nanoparticles
Preparation, characterization, and in vitro/vivo studies of oleanolic acid-loaded lactoferrin nanoparticles Abstract Abstract Oleanolic acid (OA), a pentacyclic triterpene, is used to safely and economically treat hepatopathy. However, OA, a Biopharmaceutics Classification System IV category drug, has low bioavailabili...
PMC10818454
core_pubmed_pmc
The Development of an Oral Solution Containing Nirmatrelvir and Ritonavir and Assessment of Its Pharmacokinetics and Stability
The Development of an Oral Solution Containing Nirmatrelvir and Ritonavir and Assessment of Its Pharmacokinetics and Stability Abstract Abstract Paxlovid ® , a co-packaged medication comprised of separate tablets containing two active ingredients, nirmatrelvir (NRV) and ritonavir (RTV), exhibits good effectiveness agai...
PMC6553511
core_pubmed_pmc
Serum Concentrations and Pharmacokinetics of Tranexamic Acid after Two Means of Topical Administration in Massive Weight Loss Skin-Reducing Surgery
Serum Concentrations and Pharmacokinetics of Tranexamic Acid after Two Means of Topical Administration in Massive Weight Loss Skin-Reducing Surgery Abstract Supplemental Digital Content is available in the text. Background: Topical administration of tranexamic acid to reduce bleeding is receiving increasing attention, ...
PMC7032162
core_pubmed_pmc
Synthesis, characterization and in vivo evaluation of honokiol bisphosphate prodrugs protects against rats’ brain ischemia-reperfusion injury
Synthesis, characterization and in vivo evaluation of honokiol bisphosphate prodrugs protects against rats’ brain ischemia-reperfusion injury Abstract Honokiol (HK) usage is greatly restricted by its poor aqueous solubility and limited oral bioavailability. We synthesized and characterized a novel phosphate prodrug of ...
PMC6968681
core_pubmed_pmc
Identification of cytochrome P450 isoenzymes involved in the metabolism of 23-hydroxybetulinic acid in human liver microsomes
Identification of cytochrome P450 isoenzymes involved in the metabolism of 23-hydroxybetulinic acid in human liver microsomes Abstract Abstract Context 23-Hydroxybetulinic acid (23-HBA), a major active constituent of Pulsatilla chinensis (Bunge) Regel (Ranunculaceae), exhibits potential antitumor activity. Its metaboli...
PMC7937847
core_pubmed_pmc
Peptidyl and Non-Peptidyl Oral Glucagon-Like Peptide-1 Receptor Agonists
Peptidyl and Non-Peptidyl Oral Glucagon-Like Peptide-1 Receptor Agonists Abstract Glucagon-like peptide-1 (GLP-1) receptor agonists are efficacious glucose-lowering medications with salient benefits for body weight and cardiovascular events. This class of medications is now recommended as the top priority for patients ...
PMC3509643
core_pubmed_pmc
Pharmacological Evaluation and Preliminary Pharmacokinetics Studies of a New Diclofenac Prodrug without Gastric Ulceration Effect
Pharmacological Evaluation and Preliminary Pharmacokinetics Studies of a New Diclofenac Prodrug without Gastric Ulceration Effect Abstract Long-term nonsteroidal anti-inflammatory drugs (NSAIDs) therapy has been associated with several adverse effects such as gastric ulceration and cardiovascular events. Among the mole...
PMC7506178
core_pubmed_pmc
UPLC-MS/MS Measurement of the Effect of Isavuconazole, Itraconazole and Fluconazole on the Pharmacokinetics of Selinexor in Rats
UPLC-MS/MS Measurement of the Effect of Isavuconazole, Itraconazole and Fluconazole on the Pharmacokinetics of Selinexor in Rats Abstract Abstract Objective An ultra performance liquid chromatography tandem mass spectrometry (UPLC-MS/MS) method for the determination of selinexor was established to investigate the effec...
PMC11029161
core_pubmed_pmc
Pharmacokinetics and tissue residues of albendazole sulphoxide and its metabolites in donkey after intramuscular injection
Pharmacokinetics and tissue residues of albendazole sulphoxide and its metabolites in donkey after intramuscular injection Abstract Abstract Background Various anti‐parasitic drugs are used to control donkey parasitic diseases. The abuse of donkey drugs leads to the disposition of residues in the edible parts of treate...
PMC7927828
core_pubmed_pmc
Cerebrospinal Fluid Penetration of Ceftolozane-Tazobactam in Critically Ill Patients with an Indwelling External Ventricular Drain
Cerebrospinal Fluid Penetration of Ceftolozane-Tazobactam in Critically Ill Patients with an Indwelling External Ventricular Drain Abstract The aim of this study was to describe the pharmacokinetics of ceftolozane-tazobactam in plasma and cerebrospinal fluid (CSF) of infected critically ill patients. In a prospective o...
PMC4987405
core_pubmed_pmc
Effect of Moderate Hepatic Impairment on the Pharmacokinetics and Pharmacodynamics of Roxadustat, an Oral Hypoxia-Inducible Factor Prolyl Hydroxylase Inhibitor
Effect of Moderate Hepatic Impairment on the Pharmacokinetics and Pharmacodynamics of Roxadustat, an Oral Hypoxia-Inducible Factor Prolyl Hydroxylase Inhibitor Abstract Abstract Background and Objective Roxadustat is a hypoxia-inducible factor prolyl hydroxylase inhibitor in phase III development for the treatment of a...
PMC9147221
core_pubmed_pmc
Amphiphilic Poly- N -vinylpyrrolidone Nanoparticles as Carriers for Nonsteroidal, Anti-Inflammatory Drugs: Pharmacokinetic, Anti-Inflammatory, and Ulcerogenic Activity Study
Amphiphilic Poly- N -vinylpyrrolidone Nanoparticles as Carriers for Nonsteroidal, Anti-Inflammatory Drugs: Pharmacokinetic, Anti-Inflammatory, and Ulcerogenic Activity Study Abstract Nanoparticles are increasingly utilized as drug delivery agents. Previously, we have developed a drug delivery system based on amphiphili...
PMC5511303
core_pubmed_pmc
Pharmacokinetic Profile of a 2-Month Dose Regimen of Aripiprazole Lauroxil: A Phase I Study and a Population Pharmacokinetic Model
Pharmacokinetic Profile of a 2-Month Dose Regimen of Aripiprazole Lauroxil: A Phase I Study and a Population Pharmacokinetic Model Abstract Abstract Background Aripiprazole lauroxil (AL) is a long-acting injectable medication approved for the treatment of schizophrenia. Current AL regimens are 441 mg, 662 mg, and 882 m...
PMC10484623
core_pubmed_pmc
The impact of gene polymorphism and hepatic insufficiency on voriconazole dose adjustment in invasive fungal infection individuals
The impact of gene polymorphism and hepatic insufficiency on voriconazole dose adjustment in invasive fungal infection individuals Abstract Voriconazole (VRZ) is a broad-spectrum antifungal medication widely used to treat invasive fungal infections (IFI). The administration dosage and blood concentration of VRZ are inf...
PMC6165407
core_pubmed_pmc
Rational Use of Medicines in Neonates: Current Observations, Areas for Research and Perspectives
Rational Use of Medicines in Neonates: Current Observations, Areas for Research and Perspectives Abstract Abstract A focused reflection on rational medicines use in neonates is valuable and relevant, because indicators to assess rational medicines use are difficult to apply to neonates. Polypharmacy and exposure to ant...
PMC5767540
core_pubmed_pmc
Drug–Target Kinetics in Drug Discovery
Drug–Target Kinetics in Drug Discovery Abstract The development of therapies for the treatment of neurological cancer faces a number of major challenges including the synthesis of small molecule agents that can penetrate the blood-brain barrier (BBB). Given the likelihood that in many cases drug exposure will be lower ...
PMC12595851
core_pubmed_pmc
Pharmacokinetics, pharmacodynamics, and local tolerance at injection site of penicillin and gentamicin administered by intravenous regional limb perfusion in standing horses: comparison between weightbearing and flexed limbs
Pharmacokinetics, pharmacodynamics, and local tolerance at injection site of penicillin and gentamicin administered by intravenous regional limb perfusion in standing horses: comparison between weightbearing and flexed limbs Abstract Abstract Background Intravenous regional limb perfusion (IVRLP) of antibiotics is a th...
PMC8538870
core_pubmed_pmc
Data-Driven Modeling of the Cellular Pharmacokinetics of Degradable Chitosan-Based Nanoparticles
Data-Driven Modeling of the Cellular Pharmacokinetics of Degradable Chitosan-Based Nanoparticles Abstract Nanoparticle drug delivery vehicles introduce multiple pharmacokinetic processes, with the delivery, accumulation, and stability of the therapeutic molecule influenced by nanoscale processes. Therefore, considering...
PMC7238021
core_pubmed_pmc
Changing the Drug Delivery System: Does it Add to Non-Compliance Ramifications Control? A Simulation Study on the Pharmacokinetics and Pharmacodynamics of Atypical Antipsychotic Drug
Changing the Drug Delivery System: Does it Add to Non-Compliance Ramifications Control? A Simulation Study on the Pharmacokinetics and Pharmacodynamics of Atypical Antipsychotic Drug Abstract This study investigates the pharmacokinetic (PK) and pharmacodynamic (PD) consequences of shifting from Quetiapine fumarate imme...
PMC10508574
core_pubmed_pmc
Saliva as a noninvasive sampling matrix for therapeutic drug monitoring of intravenous busulfan in Chinese patients undergoing hematopoietic stem cell transplantation: A prospective population pharmacokinetic and simulation study
Saliva as a noninvasive sampling matrix for therapeutic drug monitoring of intravenous busulfan in Chinese patients undergoing hematopoietic stem cell transplantation: A prospective population pharmacokinetic and simulation study Abstract Abstract Therapeutic drug monitoring (TDM) of busulfan (BU) is currently performe...
PMC12711674
core_pubmed_pmc
Non-orthosteric inhibition of enolase 1 impedes growth of triple-negative breast cancer
Non-orthosteric inhibition of enolase 1 impedes growth of triple-negative breast cancer Abstract Summary Cancer cells exploit and overexpress glycolytic enzymes such as enolase 1 (ENO1) to sustain the Warburg effect, a hallmark of cancer metabolism, which makes ENO1 a compelling therapeutic target. Here, we demonstrate...
PMC7067721
core_pubmed_pmc
Extrapolation of Drug Clearance in Children ≤ 2 Years of Age from Empirical Models Using Data from Children (> 2 Years) and Adults
Extrapolation of Drug Clearance in Children ≤ 2 Years of Age from Empirical Models Using Data from Children (> 2 Years) and Adults Abstract Abstract Background The application of modeling and simulation approaches in clinical pharmacology studies has gained momentum over the last 20 years. Objectives The objective of t...
PMC10353446
core_pubmed_pmc
Pharmacokinetics of SPR206 in Plasma, Pulmonary Epithelial Lining Fluid, and Alveolar Macrophages following Intravenous Administration to Healthy Adult Subjects
Pharmacokinetics of SPR206 in Plasma, Pulmonary Epithelial Lining Fluid, and Alveolar Macrophages following Intravenous Administration to Healthy Adult Subjects Abstract ABSTRACT SPR206 is a next-generation polymyxin being developed for the treatment of multidrug-resistant (MDR) Gram-negative infections. This Phase 1 b...
PMC7211298
core_pubmed_pmc
Pharmacokinetic Evaluation by Modeling and Simulation Analysis of a Donepezil Patch Formulation in Healthy Male Volunteers
Pharmacokinetic Evaluation by Modeling and Simulation Analysis of a Donepezil Patch Formulation in Healthy Male Volunteers Abstract Introduction This study characterized the pharmacokinetics (PKs) of a donepezil patch formulation currently under development, using mixed effect modeling analysis, and explored optimal pa...
PMC8634185
core_pubmed_pmc
Danicopan: an oral complement factor D inhibitor for paroxysmal nocturnal hemoglobinuria
Danicopan: an oral complement factor D inhibitor for paroxysmal nocturnal hemoglobinuria Abstract Abstract Paroxysmal nocturnal hemoglobinuria (PNH) is characterized by complement-mediated intravascular hemolysis due to the absence of complement regulators CD55 and CD59 on affected erythrocytes. Danicopan is a first-in...
PMC12752375
core_pubmed_pmc
Factors affecting voriconazole pharmacokinetic variability in critically ill patients: a systematic review
Factors affecting voriconazole pharmacokinetic variability in critically ill patients: a systematic review Abstract Abstract Background The efficacy and toxicity of voriconazole, a broad-spectrum antifungal agent, are correlated with its trough concentration (C trough ). Patients hospitalised in the intensive care unit...
PMC4644137
core_pubmed_pmc
In silico evaluation of gadofosveset pharmacokinetics in different population groups using the Simcyp® simulator platform
In silico evaluation of gadofosveset pharmacokinetics in different population groups using the Simcyp® simulator platform Abstract Purpose Gadofosveset is a Gd-based contrast agent used for magnetic resonance imaging (MRI). Gadolinium kinetic distribution models are implemented in T1-weighted dynamic contrast-enhanced ...
PMC12439010
core_pubmed_pmc
Dose Optimization in Oncology Drug Development: Risk Factors for Postmarketing Requirements and Commitments
Dose Optimization in Oncology Drug Development: Risk Factors for Postmarketing Requirements and Commitments Abstract Abstract Optimal dosing of oncological drugs is historically determined based on the “higher is better” paradigm. However, a paradigm shift in optimal dose selection has occurred in the development of ne...
PMC6155365
core_pubmed_pmc
A Phase 3 Study of Micafungin Versus Amphotericin B Deoxycholate in Infants With Invasive Candidiasis
A Phase 3 Study of Micafungin Versus Amphotericin B Deoxycholate in Infants With Invasive Candidiasis Abstract Supplemental Digital Content is available in the text. Keywords: amphotericin B deoxycholate, infants, invasive candidiasis, micafungin, neonates Abstract Background: Amphotericin B deoxycholate (AmB-D) is sta...
PMC8423463
core_pubmed_pmc
Blood Parasite Load as an Early Marker to Predict Treatment Response in Visceral Leishmaniasis in Eastern Africa
Blood Parasite Load as an Early Marker to Predict Treatment Response in Visceral Leishmaniasis in Eastern Africa Abstract Abstract Background To expedite the development of new oral treatment regimens for visceral leishmaniasis (VL), there is a need for early markers to evaluate treatment response and predict long-term...
PMC5685150
core_pubmed_pmc
Population pharmacokinetics of pomalidomide in patients with relapsed or refractory multiple myeloma with various degrees of impaired renal function
Population pharmacokinetics of pomalidomide in patients with relapsed or refractory multiple myeloma with various degrees of impaired renal function Abstract Pomalidomide is an immunomodulatory drug for treatment of relapsed or refractory multiple myeloma (rrMM) in patients who often have comorbid renal conditions. To ...
PMC8205603
core_pubmed_pmc
Simultaneous Quantification of Pioglitazone and Omarigliptin in Rat Plasma by UHPLC-MS/MS and Its Application to Pharmacokinetic Study after Coadministration of the Two Drugs
Simultaneous Quantification of Pioglitazone and Omarigliptin in Rat Plasma by UHPLC-MS/MS and Its Application to Pharmacokinetic Study after Coadministration of the Two Drugs Abstract Combination therapy is a common approach for clinical treatment of type 2 diabetes mellitus, especially for patients with poor monothera...
PMC8197310
core_pubmed_pmc
C-11, a New Antiepileptic Drug Candidate: Evaluation of the Physicochemical Properties and Impact on the Protective Action of Selected Antiepileptic Drugs in the Mouse Maximal Electroshock-Induced Seizure Model
C-11, a New Antiepileptic Drug Candidate: Evaluation of the Physicochemical Properties and Impact on the Protective Action of Selected Antiepileptic Drugs in the Mouse Maximal Electroshock-Induced Seizure Model Abstract C-11 is a hybrid compound derived from 2-(2,5-dioxopyrrolidin-1-yl) propanamide, with a wide spectru...
PMC9574875
core_pubmed_pmc
Enhanced bioavailability and pharmacokinetics of a novel hybrid-hydrogel formulation of fisetin orally administered in healthy individuals: a randomised double-blinded comparative crossover study
Enhanced bioavailability and pharmacokinetics of a novel hybrid-hydrogel formulation of fisetin orally administered in healthy individuals: a randomised double-blinded comparative crossover study Abstract Fisetin, a polyphenol found in several fruits and vegetables, has shown potential health benefits in many pre-clini...
PMC5700339
core_pubmed_pmc
Exposure-Response Relationships for Isavuconazole in Patients with Invasive Aspergillosis and Other Filamentous Fungi
Exposure-Response Relationships for Isavuconazole in Patients with Invasive Aspergillosis and Other Filamentous Fungi Abstract ABSTRACT Isavuconazole, the active moiety of the water-soluble prodrug isavuconazonium sulfate, is a triazole antifungal agent for the treatment of invasive fungal infections. The purpose of th...
PMC5444125
core_pubmed_pmc
Experimental Models of Short Courses of Liposomal Amphotericin B for Induction Therapy for Cryptococcal Meningitis
Experimental Models of Short Courses of Liposomal Amphotericin B for Induction Therapy for Cryptococcal Meningitis Abstract ABSTRACT Cryptococcal meningoencephalitis is a rapidly lethal infection in immunocompromised patients. Induction regimens are usually administered for 2 weeks. The shortest effective period of ind...
PMC12515209
core_pubmed_pmc
Phase I results on the efficacy, safety and pharmacokinetics of lurbinectedin and irinotecan in advanced solid tumors
Phase I results on the efficacy, safety and pharmacokinetics of lurbinectedin and irinotecan in advanced solid tumors Abstract Abstract Lurbinectedin and irinotecan showed synergistic antitumor activity when combined in preclinical studies, and have non-completely overlapping toxicity profiles. A two-stage phase I/II t...
PMC8002238
core_pubmed_pmc
Pharmacokinetics and Pharmacogenetics of Cyclophosphamide in a Neonate and Infant Childhood Cancer Patient Population
Pharmacokinetics and Pharmacogenetics of Cyclophosphamide in a Neonate and Infant Childhood Cancer Patient Population Abstract Abstract Infants and young children represent an important but much understudied childhood cancer patient population. The pharmacokinetics and pharmacogenetics of the widely used anticancer pro...
PMC12583990
core_pubmed_pmc
A multifaceted review on extraction optimization, nanoformulation, and chemical modification approaches to enhance the yield, bioavailability, and health effects of xanthones
A multifaceted review on extraction optimization, nanoformulation, and chemical modification approaches to enhance the yield, bioavailability, and health effects of xanthones Abstract Abstract Xanthones, a class of polyphenolic bioactive compounds found abundantly in nature, possess a broad spectrum of pharmacological ...
PMC5452411
core_pubmed_pmc
Lymphatic delivery of etanercept via nanotopography improves response to collagen-induced arthritis
Lymphatic delivery of etanercept via nanotopography improves response to collagen-induced arthritis Abstract Abstract Background Evidence suggests lymphatic function mediates local rheumatoid arthritis (RA) flares. Yet biologics that target the immune system are dosed systemically via the subcutaneous (SC) administrati...
PMC12413699
core_pubmed_pmc
The effect of modified donanemab titration on amyloid-related imaging abnormalities with edema/effusions and amyloid reduction: 18-month results from TRAILBLAZER-ALZ 6
The effect of modified donanemab titration on amyloid-related imaging abnormalities with edema/effusions and amyloid reduction: 18-month results from TRAILBLAZER-ALZ 6 Abstract The TRAILBLAZER-ALZ 6 study ( NCT05738486 ) evaluated the effect of different donanemab dosing regimens on amyloid-related imaging abnormalitie...
PMC12041113
core_pubmed_pmc
Pharmacokinetics and Safety of Levofloxacin for Treatment of Rifampicin-Resistant Tuberculosis During Pregnancy and the Postpartum Period: Results from IMPAACT P1026s
Pharmacokinetics and Safety of Levofloxacin for Treatment of Rifampicin-Resistant Tuberculosis During Pregnancy and the Postpartum Period: Results from IMPAACT P1026s Abstract Abstract Background and Objective Treatment of rifampicin-resistant tuberculosis (RR-TB) often includes fluoroquinolones, but data on long-term ...
PMC12171110
core_pubmed_pmc
Safety, tolerability, pharmacokinetics, and pharmacodynamics of etrasimod in healthy Chinese adults: a randomized, double-blind, placebo-controlled dose-escalation phase 1 study
Safety, tolerability, pharmacokinetics, and pharmacodynamics of etrasimod in healthy Chinese adults: a randomized, double-blind, placebo-controlled dose-escalation phase 1 study Abstract Objectives Etrasimod is an investigational, oral, once-daily, selective S1P 1,4,5 receptor modulator in development for the treatment...
PMC6733935
core_pubmed_pmc
A convenient and efficient total solid-phase synthesis of DOTA-functionalized tumor-targeting peptides for PET imaging of cancer
A convenient and efficient total solid-phase synthesis of DOTA-functionalized tumor-targeting peptides for PET imaging of cancer Abstract Introduction An efficient and cost-effective synthesis of the metal chelating agents that couple to tumor-targeting peptides is required to enhance the process of preclinical researc...
PMC8061066
core_pubmed_pmc
Safety, pharmacokinetics and exploratory pro-cognitive effects of HTL0018318, a selective M 1 receptor agonist, in healthy younger adult and elderly subjects: a multiple ascending dose study
Safety, pharmacokinetics and exploratory pro-cognitive effects of HTL0018318, a selective M 1 receptor agonist, in healthy younger adult and elderly subjects: a multiple ascending dose study Abstract Abstract Background The cholinergic system and M 1 receptor remain an important target for symptomatic treatment of cogn...
PMC10651909
core_pubmed_pmc
Polysorbate 80 surface modified SLNs of formoterol suppress SNCA gene and mitochondrial oxidative stress in mice model of Parkinson’s disease
Polysorbate 80 surface modified SLNs of formoterol suppress SNCA gene and mitochondrial oxidative stress in mice model of Parkinson’s disease Abstract Abstract The present study hypothesises that the selective brain β2 receptor activation through β2-adrenoreceptor agonist (β2ARA), Formoterol (FMT), suppresses SNCA gene...
PMC10761411
core_pubmed_pmc
Combined in vivo metabolic effects of quetiapine and methadone in brain and blood of rats
Combined in vivo metabolic effects of quetiapine and methadone in brain and blood of rats Abstract Changes in pharmacokinetics and endogenous metabolites may underlie additive biological effects of concomitant use of antipsychotics and opioids. In this study, we employed untargeted metabolomics analysis and targeted an...
PMC7351633
core_pubmed_pmc
Evaluation of Bioequivalency and Pharmacokinetic Parameters for Two Formulations of Glimepiride 1-mg in Chinese Subjects
Evaluation of Bioequivalency and Pharmacokinetic Parameters for Two Formulations of Glimepiride 1-mg in Chinese Subjects Abstract Abstract Purpose Glimepiride, an FDA-approved oral hypoglycemic drug, is a long-acting sulfonylurea (SU), used for treating type 2 diabetes. The study aimed to evaluate the bioequivalence an...
PMC4169869
core_pubmed_pmc
Phase I study on the safety, pharmacokinetic profile, and efficacy of the combination of TSU-68, an oral antiangiogenic agent, and S-1 in patients with advanced hepatocellular carcinoma
Phase I study on the safety, pharmacokinetic profile, and efficacy of the combination of TSU-68, an oral antiangiogenic agent, and S-1 in patients with advanced hepatocellular carcinoma Abstract Summary Purpose We aimed to investigate the recommended dose for the combination of TSU-68, a multiple-receptor tyrosine kina...
PMC8632000
core_pubmed_pmc
Dose Tailoring of Vancomycin Through Population Pharmacokinetic Modeling Among Surgical Patients in Pakistan
Dose Tailoring of Vancomycin Through Population Pharmacokinetic Modeling Among Surgical Patients in Pakistan Abstract Abstract Background: Vancomycin is a narrow therapeutic agent, and it is necessary to optimize the dose to achieve safe therapeutic outcomes. The purpose of this study was to identify the significant co...
PMC11382693
core_pubmed_pmc
Automated regional citrate anticoagulation system based on individualized dosing models in nonliver failure patients undergoing PIRRT therapy
Automated regional citrate anticoagulation system based on individualized dosing models in nonliver failure patients undergoing PIRRT therapy Abstract Abstract Introduction Regional citrate anticoagulation is a preferred option for renal replacement therapy in critically ill patients. However, current implementations i...
PMC3700763
core_pubmed_pmc
First human dose-escalation study with remogliflozin etabonate, a selective inhibitor of the sodium-glucose transporter 2 (SGLT2), in healthy subjects and in subjects with type 2 diabetes mellitus
First human dose-escalation study with remogliflozin etabonate, a selective inhibitor of the sodium-glucose transporter 2 (SGLT2), in healthy subjects and in subjects with type 2 diabetes mellitus Abstract Abstract Background Remogliflozin etabonate (RE) is the prodrug of remogliflozin, a selective inhibitor of the ren...
PMC3433414
core_pubmed_pmc
Oral Administration of the Pimelic Diphenylamide HDAC Inhibitor HDACi 4b Is Unsuitable for Chronic Inhibition of HDAC Activity in the CNS In Vivo
Oral Administration of the Pimelic Diphenylamide HDAC Inhibitor HDACi 4b Is Unsuitable for Chronic Inhibition of HDAC Activity in the CNS In Vivo Abstract Histone deacetylase (HDAC) inhibitors have received considerable attention as potential therapeutics for a variety of cancers and neurological disorders. Recent publ...
PMC11078060
core_pubmed_pmc
Effect of food on selumetinib pharmacokinetics and gastrointestinal tolerability in adolescents with neurofibromatosis type 1-related plexiform neurofibromas
Effect of food on selumetinib pharmacokinetics and gastrointestinal tolerability in adolescents with neurofibromatosis type 1-related plexiform neurofibromas Abstract Abstract Background Selumetinib is approved for the treatment of pediatric patients with neurofibromatosis type 1 (NF1) who have symptomatic, inoperable ...
PMC11747864
core_pubmed_pmc
Pimobendan oral solution is bioequivalent to pimobendan chewable tablets in beagle dogs
Pimobendan oral solution is bioequivalent to pimobendan chewable tablets in beagle dogs Abstract Abstract Background Myxomatous mitral valve disease (MMVD) is frequently diagnosed in small breed dogs. Pimobendan oral solution has been developed to improve dosing accuracy in small and toy breed dogs. Hypothesis/Objectiv...
PMC6177617
core_pubmed_pmc
In vitro and in silico analysis of the effects of D 2 receptor antagonist target binding kinetics on the cellular response to fluctuating dopamine concentrations
In vitro and in silico analysis of the effects of D 2 receptor antagonist target binding kinetics on the cellular response to fluctuating dopamine concentrations Abstract Abstract Background and Purpose Target binding kinetics influence the time course of the drug effect (pharmacodynamics) both (i) directly, by affecti...
PMC12309307
core_pubmed_pmc
Polymorphisms in CYP3A5, CYP3A4 , and ABCB1 genes: implications for calcineurin inhibitors therapy in hematopoietic cell transplantation recipients—a systematic review
Polymorphisms in CYP3A5, CYP3A4 , and ABCB1 genes: implications for calcineurin inhibitors therapy in hematopoietic cell transplantation recipients—a systematic review Abstract Abstract This systematic review assessed the impact of CYP3A5 , CYP3A4 , and ABCB1 polymorphisms on the pharmacokinetics and clinical outcomes ...
PMC7537091
core_pubmed_pmc
The Weight of Evidence From Electrophysiology, Observational, and Cardiovascular End Point Studies Demonstrates the Safety of Azithromycin
The Weight of Evidence From Electrophysiology, Observational, and Cardiovascular End Point Studies Demonstrates the Safety of Azithromycin Abstract Increased use of azithromycin (AZ) in treating infections associated with coronavirus disease 2019 (COVID‐19) and reports of increased incidence of prolonged corrected QT (...
PMC7897192
core_pubmed_pmc
Current methods in translational cancer research
Current methods in translational cancer research Abstract Recent developments in pre-clinical screening tools, that more reliably predict the clinical effects and adverse events of candidate therapeutic agents, has ushered in a new era of drug development and screening. However, given the rapid pace with which these mo...
PMC11687205
core_pubmed_pmc
Aztreonam–avibactam: The dynamic duo against multidrug‐resistant gram‐negative pathogens
Aztreonam–avibactam: The dynamic duo against multidrug‐resistant gram‐negative pathogens Abstract Abstract Antimicrobial resistance poses a significant public health challenge, particularly with the rise of gram‐negative hospital‐acquired infections resistant to carbapenems. Aztreonam–avibactam (ATM–AVI) is a promising...