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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... |
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