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PMC10614310
core_pubmed_pmc
Pharmacokinetics and metabolism of lidocaine HCl 2% with epinephrine in horses following a palmar digital nerve block
Pharmacokinetics and metabolism of lidocaine HCl 2% with epinephrine in horses following a palmar digital nerve block Abstract Background Lidocaine is a local anesthetic that is sometimes administered in combination with epinephrine. The addition of epinephrine increases the time lidocaine remains at the site of admini...
PMC9386913
core_pubmed_pmc
CC-99677, a novel, oral, selective covalent MK2 inhibitor, sustainably reduces pro-inflammatory cytokine production
CC-99677, a novel, oral, selective covalent MK2 inhibitor, sustainably reduces pro-inflammatory cytokine production Abstract Background Mitogen-activated protein kinase (MAPK)-activated protein kinase-2 (MK2) is activated downstream of p38 MAPK and regulates stability of mRNAs encoding inflammatory cytokines. CC-99677 ...
PMC3102322
core_pubmed_pmc
Pharmacokinetic-Pharmacodynamic Modeling of Metformin for the Treatment of Type II Diabetes Mellitus
Pharmacokinetic-Pharmacodynamic Modeling of Metformin for the Treatment of Type II Diabetes Mellitus Abstract Metformin is an antihyperglycemic agent commonly used for the treatment of Type II diabetes mellitus. However, its effects on patients are derived usually from clinical experiments. In this study, a dynamic mod...
PMC10508544
core_pubmed_pmc
Exposure‐safety and exposure‐efficacy analyses for tisotumab vedotin for patients with locally advanced or metastatic solid tumors
Exposure‐safety and exposure‐efficacy analyses for tisotumab vedotin for patients with locally advanced or metastatic solid tumors Abstract Abstract The antibody‐drug conjugate (ADC) tisotumab vedotin (TV) received accelerated approval from the US Food and Drug Administration for treatment of adults with recurrent or m...
PMC10302406
core_pubmed_pmc
Influence of Surface-Modification via PEGylation or Chitosanization of Lipidic Nanocarriers on In Vivo Pharmacokinetic/Pharmacodynamic Profiles of Apixaban
Influence of Surface-Modification via PEGylation or Chitosanization of Lipidic Nanocarriers on In Vivo Pharmacokinetic/Pharmacodynamic Profiles of Apixaban Abstract Abstract Nanostructured lipid carriers (NLCs) have been proven to significantly improve the bioavailability and efficacy of many drugs; however, they still...
PMC12845259
core_pubmed_pmc
Pharmacogenomics of CYP2D6, CYP2C19, CYP2C9, and Clinical Determinants of Fluoxetine–Norfluoxetine Pharmacokinetics in Real-World Clinical Conditions
Pharmacogenomics of CYP2D6, CYP2C19, CYP2C9, and Clinical Determinants of Fluoxetine–Norfluoxetine Pharmacokinetics in Real-World Clinical Conditions Abstract Abstract Background: Fluoxetine, a widely prescribed selective serotonin reuptake inhibitor, exhibits significant interindividual variability in pharmacokinetics...
PMC8332596
core_pubmed_pmc
Effects of Renal Impairment on the Pharmacokinetics of the Dual GIP and GLP-1 Receptor Agonist Tirzepatide
Effects of Renal Impairment on the Pharmacokinetics of the Dual GIP and GLP-1 Receptor Agonist Tirzepatide Abstract Abstract Background and Aims The pharmacokinetics (PK) and single-dose tolerability of tirzepatide, a dual glucose-dependent insulinotropic polypeptide and glucagon-like peptide-1 receptor agonist being d...
PMC11745869
core_pubmed_pmc
Pharmacogenetic and pharmacokinetic factors for dexmedetomidine-associated hemodynamic instability in pediatric patients
Pharmacogenetic and pharmacokinetic factors for dexmedetomidine-associated hemodynamic instability in pediatric patients Abstract Purpose The incidence of hemodynamic instability associated with dexmedetomidine (DEX) sedation has been reported to exceed 50%, with substantial inter-individual variability in response. Ge...
PMC5270291
core_pubmed_pmc
Model‐Based Characterization of the Pharmacokinetics of Pembrolizumab: A Humanized Anti–PD‐1 Monoclonal Antibody in Advanced Solid Tumors
Model‐Based Characterization of the Pharmacokinetics of Pembrolizumab: A Humanized Anti–PD‐1 Monoclonal Antibody in Advanced Solid Tumors Abstract Abstract Pembrolizumab, a potent antibody against programmed death 1 (PD‐1) receptor, has shown robust antitumor activity and manageable safety in patients with advanced sol...
PMC11091978
core_pubmed_pmc
Pharmacological Analysis of NLRP3 Inflammasome Inhibitor Sodium [(1,2,3,5,6,7-Hexahydro-s-indacen-4-yl)carbamoyl][(1-methyl-1 H -pyrazol-4-yl)({[(2 S )-oxolan-2-yl]methyl})sulfamoyl]azanide in Cellular and Mouse Models of Inflammation Provides a Translational Framework
Pharmacological Analysis of NLRP3 Inflammasome Inhibitor Sodium [(1,2,3,5,6,7-Hexahydro-s-indacen-4-yl)carbamoyl][(1-methyl-1 H -pyrazol-4-yl)({[(2 S )-oxolan-2-yl]methyl})sulfamoyl]azanide in Cellular and Mouse Models of Inflammation Provides a Translational Framework Abstract Abstract Interleukin (IL)-1β is an apex p...
PMC8437715
core_pubmed_pmc
Borneol influences the pharmacokinetics of florfenicol through regulation of cytochrome P450 1A2 (CYP1A2), CYP2C11, CYP3A1, and multidrug resistance 1 (MDR1) mRNA expression levels in rats
Borneol influences the pharmacokinetics of florfenicol through regulation of cytochrome P450 1A2 (CYP1A2), CYP2C11, CYP3A1, and multidrug resistance 1 (MDR1) mRNA expression levels in rats Abstract Borneol is a traditional Chinese medicine. In Chinese veterinary clinics, borneol and its related compounds are often used...
PMC7612567
core_pubmed_pmc
Pharmacodynamic Biomarkers for Quantifying the Mycobacterial Effect of High Doses of Rifampin in Patients with Rifampin-susceptible Pulmonary Tuberculosis
Pharmacodynamic Biomarkers for Quantifying the Mycobacterial Effect of High Doses of Rifampin in Patients with Rifampin-susceptible Pulmonary Tuberculosis Abstract Background Suboptimal drug exposure in patients with drug-susceptible tuberculosis (DS-TB) can drive treatment failure. Pharmacodynamics (PD) biomarkers suc...
PMC9053417
core_pubmed_pmc
Guideline recommendations for antimicrobial stewardship education for clinical nursing practice in hospitals: A scoping review
Guideline recommendations for antimicrobial stewardship education for clinical nursing practice in hospitals: A scoping review Abstract Background Antimicrobial stewardship (AMS) is a proactive healthcare intervention to improve patient outcomes by optimising antimicrobial use. Although nursing involvement is a recogni...
PMC11064479
core_pubmed_pmc
Assessing potential drug-drug interactions between clofazimine and other frequently used agents to treat drug-resistant tuberculosis
Assessing potential drug-drug interactions between clofazimine and other frequently used agents to treat drug-resistant tuberculosis Abstract ABSTRACT Clofazimine is included in drug regimens to treat rifampicin/drug-resistant tuberculosis (DR-TB), but there is little information about its interaction with other drugs ...
PMC5057500
core_pubmed_pmc
Phase II study of TP300 in patients with advanced gastric or gastro-oesophageal junction adenocarcinoma
Phase II study of TP300 in patients with advanced gastric or gastro-oesophageal junction adenocarcinoma Abstract Background TP300, a recently developed synthetic camptothecin analogue, is a highly selective topoisomerase I inhibitor. A phase I study showed good safety and tolerability. As camptothecins have proven acti...
PMC10975186
core_pubmed_pmc
Modeling Pharmacokinetics in Individual Patients Using Therapeutic Drug Monitoring and Artificial Population Quasi-Models: A Study with Piperacillin
Modeling Pharmacokinetics in Individual Patients Using Therapeutic Drug Monitoring and Artificial Population Quasi-Models: A Study with Piperacillin Abstract Population pharmacokinetic (pop-PK) models constructed for model-informed precision dosing often have limited utility due to the low number of patients recruited....
PMC8920108
core_pubmed_pmc
Lost in modelling and simulation?
Lost in modelling and simulation? Abstract Abstract Over the past few decades, physiologically-based pharmacokinetic modelling (PBPK) has been anticipated to be a powerful tool to improve the productivity of drug discovery and development. However, recently, multiple systematic evaluation studies independently suggeste...
PMC9666522
core_pubmed_pmc
Influence of tramadol on bacterial burden in the standard neutropenic thigh infection model
Influence of tramadol on bacterial burden in the standard neutropenic thigh infection model Abstract Abstract The neutropenic thigh infection model is one of the standard models in pharmacokinetic/ pharmacodynamic (PK/PD) characterization of novel antibacterials which are urgently needed due to the rise of antimicrobia...
PMC12751989
core_pubmed_pmc
A case report of wrist arthritis caused by Gemella haemolysans
A case report of wrist arthritis caused by Gemella haemolysans Abstract Abstract Background Septic wrist arthritis is rare and usually due to Staphylococcus aureus. Gemella haemolysans is exceptionally involved in osteoarticular infection, mainly reported in prosthetic infections or spondylodiscitis. Case presentation ...
PMC8232873
core_pubmed_pmc
Efficacy, Safety and Pharmacokinetic Results of a Phase III, Open-Label, Multicenter Study with a Plasma-Derived Von Willebrand Factor (VWF)/Factor VIII (FVIII) Concentrate in Pediatric Patients <12 Years of Age with Hemophilia A (SWIFTLY-HA Study)
Efficacy, Safety and Pharmacokinetic Results of a Phase III, Open-Label, Multicenter Study with a Plasma-Derived Von Willebrand Factor (VWF)/Factor VIII (FVIII) Concentrate in Pediatric Patients <12 Years of Age with Hemophilia A (SWIFTLY-HA Study) Abstract Abstract Background Plasma-derived von Willebrand factor/facto...
PMC7579269
core_pubmed_pmc
Tegaserod for the Treatment of Irritable Bowel Syndrome
Tegaserod for the Treatment of Irritable Bowel Syndrome Abstract Background: Tegaserod (Zelnorm®) is a 5-hydroxytryptamine (serotonin) type 4 receptor agonist for the treatment of hypomotility disorders of the lower gastrointestinal tract associated with the irritable bowel syndrome with constipation (IBS-C). Objective...
PMC12347757
core_pubmed_pmc
In Vitro Antimicrobial Activity of the Novel Antimicrobial Peptide OMN51 Against Multi-Drug-Resistant Pseudomonas aeruginosa Isolated from People with Cystic Fibrosis †
In Vitro Antimicrobial Activity of the Novel Antimicrobial Peptide OMN51 Against Multi-Drug-Resistant Pseudomonas aeruginosa Isolated from People with Cystic Fibrosis † Abstract Abstract Background: People with cystic fibrosis (pwCF) frequently suffer from chronic lung infections, with Pseudomonas aeruginosa being the ...
PMC10745500
core_pubmed_pmc
Engineering a New IFN-ApoA-I Fusion Protein with Low Toxicity and Prolonged Action
Engineering a New IFN-ApoA-I Fusion Protein with Low Toxicity and Prolonged Action Abstract Abstract Recombinant human interferon alpha-2b (rIFN) is widely used in antiviral and anticancer immunotherapy. However, the high efficiency of interferon therapy is accompanied by a number of side effects; this problem requires...
PMC7427305
core_pubmed_pmc
A phase I study of toripalimab, an anti‐PD‐1 antibody, in patients with refractory malignant solid tumors
A phase I study of toripalimab, an anti‐PD‐1 antibody, in patients with refractory malignant solid tumors Abstract Abstract Background Several programmed cell death ligand 1 (PD‐L1)/programmed cell death protein 1 (PD‐1) antibodies have been approved for cancer treatment worldwide. Their pharmacokinetic and pharmacodyn...
PMC10380404
core_pubmed_pmc
Glycosylation of Quercetin by Selected Entomopathogenic Filamentous Fungi and Prediction of Its Products’ Bioactivity
Glycosylation of Quercetin by Selected Entomopathogenic Filamentous Fungi and Prediction of Its Products’ Bioactivity Abstract Abstract Quercetin is the most abundant flavonoid in food products, including berries, apples, cauliflower, tea, cabbage, nuts, onions, red wine and fruit juices. It exhibits various biological...
PMC6488552
core_pubmed_pmc
Pharmacokinetic and Pharmacodynamic Properties of a Micro-Dose Nasal Spray Formulation of Desmopressin (AV002) in Healthy Water-Loaded Subjects
Pharmacokinetic and Pharmacodynamic Properties of a Micro-Dose Nasal Spray Formulation of Desmopressin (AV002) in Healthy Water-Loaded Subjects Abstract Abstract Purpose Antidiuretic therapy with desmopressin for nocturia has been hampered by formulations with high doses, low bioavailability and variable pharmacokineti...
PMC5867575
core_pubmed_pmc
Once Daily High Dose Tigecycline Is Optimal: Tigecycline PK/PD Parameters Predict Clinical Effectiveness
Once Daily High Dose Tigecycline Is Optimal: Tigecycline PK/PD Parameters Predict Clinical Effectiveness Abstract Abstract Objective: The clinical effectiveness of tigecycline depends on appropriate use, and PK/PD (pharmacokinetic/pharmacodynamic) parameters related to dose and dosing interval. Methods: In our 600-bed ...
PMC9045047
core_pubmed_pmc
Rationale and design of the CORE (COrticosteroids REvised) study: protocol
Rationale and design of the CORE (COrticosteroids REvised) study: protocol Abstract Abstract Introduction Corticosteroids are an important pillar in many anti-inflammatory and immunosuppressive treatment regimens and are available in natural and synthetic forms, which are considered equipotent if clinical bioequivalenc...
PMC8595241
core_pubmed_pmc
Methods to Develop an in silico Clinical Trial: Computational Head-to-Head Comparison of Lisdexamfetamine and Methylphenidate
Methods to Develop an in silico Clinical Trial: Computational Head-to-Head Comparison of Lisdexamfetamine and Methylphenidate Abstract Abstract Regulatory agencies encourage computer modeling and simulation to reduce the time and cost of clinical trials. Although still not classified in formal guidelines, system biolog...
PMC7534356
core_pubmed_pmc
Pharmacology, toxicity and pharmacokinetics of acetylshikonin: a review
Pharmacology, toxicity and pharmacokinetics of acetylshikonin: a review Abstract Abstract Context Acetylshikonin, a naphthoquinone derivative, is mainly extracted from some species of the family Boraginaceae, such as Lithospermum erythrorhizon Sieb. et Zucc., Arnebia euchroma (Royle) Johnst., and Arnebia guttata Bunge....
PMC2819250
core_pubmed_pmc
Random pharmacokinetic profiles of EC-MPS in children with autoimmune disease
Random pharmacokinetic profiles of EC-MPS in children with autoimmune disease Abstract Background Therapy with mycophenolate mofetil (MMF) has become a valuable therapeutic option in children with autoimmune disease. MMF prescription in children with autoimmune diseases differs from that in transplant recipients in ter...
PMC4225446
core_pubmed_pmc
Phase IIIb, open-label single-arm trial of darunavir/cobicistat (DRV/COBI): Week 48 subgroup analysis of HIV-1-infected treatment-nave adults
Phase IIIb, open-label single-arm trial of darunavir/cobicistat (DRV/COBI): Week 48 subgroup analysis of HIV-1-infected treatment-nave adults Abstract Abstract Introduction COBI, a PK enhancer with no ARV activity is a more selective cytochrome P450 (CYP)3A inhibitor than ritonavir (RTV), does not induce CYP isozymes, ...
PMC6394649
core_pubmed_pmc
Model-Based Conditional Weighted Residuals Analysis for Structural Model Assessment
Model-Based Conditional Weighted Residuals Analysis for Structural Model Assessment Abstract Abstract Nonlinear mixed effects models are widely used to describe longitudinal data to improve the efficiency of drug development process or increase the understanding of the studied disease. In such settings, the appropriate...
PMC8128736
core_pubmed_pmc
Towards Evidence-Based Weaning: a Mechanism-Based Pharmacometric Model to Characterize Iatrogenic Withdrawal Syndrome in Critically Ill Children
Towards Evidence-Based Weaning: a Mechanism-Based Pharmacometric Model to Characterize Iatrogenic Withdrawal Syndrome in Critically Ill Children Abstract For the management of iatrogenic withdrawal syndrome (IWS) in children, a quantitative understanding of the dynamics of IWS of commonly used opioids and sedatives is ...
PMC3210071
core_pubmed_pmc
Bioequivalence assessment of two formulations of ibuprofen
Bioequivalence assessment of two formulations of ibuprofen Abstract Abstract Background: This study assessed the relative bioavailability of two formulations of ibuprofen. The first formulation was Doloraz ® , produced by Al-Razi Pharmaceutical Company, Amman, Jordan. The second forumulation was Brufen ® , manufactured...
PMC10861969
core_pubmed_pmc
Population pharmacokinetic approach to guide personalized sertraline treatment in Chinese patients
Population pharmacokinetic approach to guide personalized sertraline treatment in Chinese patients Abstract Abstract Object: Sertraline is a first-line SSRI for the treatment of depression and has the same effectiveness along with a superior safety profile compared to other medications. There are few population pharmac...
PMC7843972
core_pubmed_pmc
Oral absorption and drug interaction kinetics of moxifloxacin in an animal model of weightlessness
Oral absorption and drug interaction kinetics of moxifloxacin in an animal model of weightlessness Abstract Abstract To investigate the effect of simulated weightlessness on the pharmacokinetics of orally administered moxifloxacin and the antacid Maalox or the antidiarrheal Pepto-Bismol using a tail-suspended (TS) rat ...
PMC4492733
core_pubmed_pmc
Pharmacodynamic assays to facilitate preclinical and clinical development of pre-mRNA splicing modulatory drug candidates
Pharmacodynamic assays to facilitate preclinical and clinical development of pre-mRNA splicing modulatory drug candidates Abstract The spliceosome has recently emerged as a new target for cancer chemotherapy and novel antitumor spliceosome targeted agents are under development. Here, we describe two types of novel phar...
PMC8311652
core_pubmed_pmc
Drugs and Epigenetic Molecular Functions. A Pharmacological Data Scientometric Analysis
Drugs and Epigenetic Molecular Functions. A Pharmacological Data Scientometric Analysis Abstract Interactions of drugs with the classical epigenetic mechanism of DNA methylation or histone modification are increasingly being elucidated mechanistically and used to develop novel classes of epigenetic therapeutics. A data...
PMC7496732
core_pubmed_pmc
Effect of Fremanezumab Monthly and Quarterly Doses on Efficacy Responses
Effect of Fremanezumab Monthly and Quarterly Doses on Efficacy Responses Abstract Objective Exposure‐response (E‐R) models were developed to provide a description of the time‐course of treatment effect for monthly and quarterly dosing regimens of fremanezumab. Background Fremanezumab is a monoclonal antibody for preven...
PMC3428607
core_pubmed_pmc
Pre-clinical pharmacokinetics and anti-chlamydial activity of salicylidene acylhydrazide inhibitors of bacterial type III secretion
Pre-clinical pharmacokinetics and anti-chlamydial activity of salicylidene acylhydrazide inhibitors of bacterial type III secretion Abstract Abstract Salicylidene acylhydrazides belong to a class of compounds shown to inhibit bacterial type III secretion (T3S) in pathogenic Gram-negative bacteria. This class of compoun...
PMC12588635
core_pubmed_pmc
Effect of CYP3A4 Methylation on Tacrolimus Pharmacokinetics
Effect of CYP3A4 Methylation on Tacrolimus Pharmacokinetics Abstract Supplemental Digital Content is Available in the Text. Key Words: tacrolimus, transplantation, liver, pharmacokinetics, therapeutic drug monitoring Abstract Background: Common genetic variants in CYP3A4 together only explain a limited amount of the va...
PMC9290614
core_pubmed_pmc
Population pharmacokinetic and exposure–response analysis of apremilast in Japanese subjects with moderate to severe psoriasis
Population pharmacokinetic and exposure–response analysis of apremilast in Japanese subjects with moderate to severe psoriasis Abstract Abstract Apremilast is an orally available phosphodiesterase 4 inhibitor used for the treatment of moderate to severe psoriasis. The aims of this analysis were to develop a population ...
PMC5641330
core_pubmed_pmc
Prediction of a Therapeutic Dose for Buagafuran, a Potent Anxiolytic Agent by Physiologically Based Pharmacokinetic/Pharmacodynamic Modeling Starting from Pharmacokinetics in Rats and Human
Prediction of a Therapeutic Dose for Buagafuran, a Potent Anxiolytic Agent by Physiologically Based Pharmacokinetic/Pharmacodynamic Modeling Starting from Pharmacokinetics in Rats and Human Abstract Physiologically based pharmacokinetic (PBPK)/pharmacodynamic (PD) models can contribute to animal-to-human extrapolation ...
PMC10803350
core_pubmed_pmc
GC–MS analysis, molecular docking, and pharmacokinetic studies of Multidentia crassa extracts’ compounds for analgesic and anti-inflammatory activities in dentistry
GC–MS analysis, molecular docking, and pharmacokinetic studies of Multidentia crassa extracts’ compounds for analgesic and anti-inflammatory activities in dentistry Abstract Abstract Plant extracts have been useful for oral health or dentistry. However, only a few evidence-based justifications exist. This study evaluat...
PMC11636752
core_pubmed_pmc
PBTK model-based analysis of CYP3A4 induction and the toxicokinetics of the pyrrolizidine alkaloid retrorsine in man
PBTK model-based analysis of CYP3A4 induction and the toxicokinetics of the pyrrolizidine alkaloid retrorsine in man Abstract Abstract Cytochrome P450 (CYP)3A4 induction by drugs and pesticides plays a critical role in the enhancement of pyrrolizidine alkaloid (PA) toxicity as it leads to increased formation of hepatot...
PMC7898862
core_pubmed_pmc
Phase I study of ABBV-428, a mesothelin-CD40 bispecific, in patients with advanced solid tumors
Phase I study of ABBV-428, a mesothelin-CD40 bispecific, in patients with advanced solid tumors Abstract Background CD40 agonist immunotherapy can potentially license antigen-presenting cells to promote antitumor T-cell activation and re-educate macrophages to destroy tumor stroma. Systemic administration of CD40 agoni...
PMC4703793
core_pubmed_pmc
Pharmacokinetic/Pharmacodynamic Correlation of Cefquinome Against Experimental Catheter-Associated Biofilm Infection Due to Staphylococcus aureus
Pharmacokinetic/Pharmacodynamic Correlation of Cefquinome Against Experimental Catheter-Associated Biofilm Infection Due to Staphylococcus aureus Abstract Biofilm formations play an important role in Staphylococcus aureus pathogenesis and contribute to antibiotic treatment failures in biofilm-associated infections. The...
PMC11536375
core_pubmed_pmc
Determining the optimum dose of remifentanil in combination with propofol for total intravenous anaesthesia in hysteroscopy under Narcotrend and SPI monitoring
Determining the optimum dose of remifentanil in combination with propofol for total intravenous anaesthesia in hysteroscopy under Narcotrend and SPI monitoring Abstract Abstract Background: Outpatient hysteroscopic surgery requires patients to be anaesthetised and recover quickly, and the drugs used must be safe and ef...
PMC8618356
core_pubmed_pmc
Optimization, Characterization and Pharmacokinetic Study of Meso-Tetraphenylporphyrin Metal Complex-Loaded PLGA Nanoparticles
Optimization, Characterization and Pharmacokinetic Study of Meso-Tetraphenylporphyrin Metal Complex-Loaded PLGA Nanoparticles Abstract Abstract The selection of technological parameters for nanoparticle formulation represents a complicated development phase. Therefore, the statistical analysis based on Box–Behnken meth...
PMC10145446
core_pubmed_pmc
Developing a Formulation Strategy Coupled with PBPK Modeling and Simulation for the Weakly Basic Drug Albendazole
Developing a Formulation Strategy Coupled with PBPK Modeling and Simulation for the Weakly Basic Drug Albendazole Abstract Albendazole (ABZ) is a weakly basic drug that undergoes extensive presystemic metabolism after oral administration and converts to its active form albendazole sulfoxide (ABZ_SO). The absorption of ...
PMC5459654
core_pubmed_pmc
Prevention of Surgical Site Infections and Biofilms: Pharmacokinetics of Subcutaneous Cefazolin and Metronidazole in a Tumescent Lidocaine Solution
Prevention of Surgical Site Infections and Biofilms: Pharmacokinetics of Subcutaneous Cefazolin and Metronidazole in a Tumescent Lidocaine Solution Abstract Supplemental Digital Content is available in the text. Abstract Background: Tumescent anesthesia antibiotic delivery (TAAD) consists of subcutaneous infiltration o...
PMC6304572
core_pubmed_pmc
Simultaneous Evaluation of the Influence of Panax ginseng on the Pharmacokinetics of Three Diester Alkaloids after Oral Administration of Aconiti Lateralis Radix in Rats Using UHPLC/QQQ-MS/MS
Simultaneous Evaluation of the Influence of Panax ginseng on the Pharmacokinetics of Three Diester Alkaloids after Oral Administration of Aconiti Lateralis Radix in Rats Using UHPLC/QQQ-MS/MS Abstract Abstract Objectives To investigate whether Panax ginseng ( P. ginseng ) could affect the metabolism of Diester Alkaloid...
PMC11079547
core_pubmed_pmc
Evaluation of potential drug–drug interactions with medical cannabis
Evaluation of potential drug–drug interactions with medical cannabis Abstract Abstract Cannabis–drug interactions have caused significant concerns, mainly due to their role in the cytochrome P450 (CYP) enzyme‐mediated metabolic pathway of numerous medications. A systematic review was conducted to gain an overview of th...
PMC5158093
core_pubmed_pmc
Relative Bioavailabilities of Lisdexamfetamine Dimesylate and d -Amphetamine in Healthy Adults in an Open-Label, Randomized, Crossover Study After Mixing Lisdexamfetamine Dimesylate With Food or Drink
Relative Bioavailabilities of Lisdexamfetamine Dimesylate and d -Amphetamine in Healthy Adults in an Open-Label, Randomized, Crossover Study After Mixing Lisdexamfetamine Dimesylate With Food or Drink Abstract Supplemental Digital Content is Available in the Text. Key Words: d -amphetamine, lisdexamfetamine, pharmacoki...
PMC11090672
core_pubmed_pmc
Advanced UPLC-MS/MS Method for the Quantification of SIPI6398 in Rat Plasma and Its Pharmacokinetic Characterization
Advanced UPLC-MS/MS Method for the Quantification of SIPI6398 in Rat Plasma and Its Pharmacokinetic Characterization Abstract SIPI6398 is a novel anti-schizophrenia agent with a new mechanism of action and demonstrates better target selectivity and safety compared to its competitors. However, few in vivo studies on the...
PMC3282610
core_pubmed_pmc
Self-microemulsifying drug-delivery system for improved oral bioavailability of probucol: preparation and evaluation
Self-microemulsifying drug-delivery system for improved oral bioavailability of probucol: preparation and evaluation Abstract The objective of our investigation was to design a self-microemulsifying drug-delivery system (SMEDDS) to improve the bioavailability of probucol. SMEDDS was composed of probucol, olive oil, Lau...
PMC7073791
core_pubmed_pmc
A first-in-human phase 1 dose escalation study of spartalizumab (PDR001), an anti–PD-1 antibody, in patients with advanced solid tumors
A first-in-human phase 1 dose escalation study of spartalizumab (PDR001), an anti–PD-1 antibody, in patients with advanced solid tumors Abstract Abstract Background Spartalizumab is a humanized IgG4κ monoclonal antibody that binds programmed death-1 (PD-1) and blocks its interaction with PD-L1 and PD-L2. This phase 1/2...
PMC6050661
core_pubmed_pmc
A quantitative systems pharmacology (QSP) model for Pneumocystis treatment in mice
A quantitative systems pharmacology (QSP) model for Pneumocystis treatment in mice Abstract Background The yeast-like fungi Pneumocystis, resides in lung alveoli and can cause a lethal infection known as Pneumocystis pneumonia (PCP) in hosts with impaired immune systems. Current therapies for PCP, such as trimethoprim-...
PMC9728581
core_pubmed_pmc
Population pharmacokinetics and dosing optimization of unbound teicoplanin in Chinese adult patients
Population pharmacokinetics and dosing optimization of unbound teicoplanin in Chinese adult patients Abstract Objectives: To develop a population pharmacokinetic (PopPK) model describing unbound teicoplanin concentrations in Chinese adult patients and perform Monte Carlo simulations to optimize the dosing regimens. Met...
PMC10388746
core_pubmed_pmc
An update on placental drug transport and its relevance to fetal drug exposure
An update on placental drug transport and its relevance to fetal drug exposure Abstract Abstract Pregnant women are often complicated with diseases that require treatment with medication. Most drugs administered to pregnant women are off-label without the necessary dose, efficacy, and safety information. Knowledge conc...
PMC5968095
core_pubmed_pmc
A Computational Workflow for Probabilistic Quantitative in Vitro to in Vivo Extrapolation
A Computational Workflow for Probabilistic Quantitative in Vitro to in Vivo Extrapolation Abstract Abstract A computational workflow was developed to facilitate the process of quantitative in vitro to in vivo extrapolation (QIVIVE), specifically the translation of in vitro concentration-response to in vivo dose-respons...
PMC11609414
core_pubmed_pmc
Research Progress on Cyclic-Peptide Functionalized Nanoparticles for Tumor-Penetrating Delivery
Research Progress on Cyclic-Peptide Functionalized Nanoparticles for Tumor-Penetrating Delivery Abstract Abstract A key challenge in cancer treatment is the effective delivery of drugs into deep regions of tumor tissues, which are impermeable due to abnormal vascular network, increased interstitial fluid pressure (IFP)...
PMC7874534
core_pubmed_pmc
Coexisting flavonoids and administration route effect on pharmacokinetics of Puerarin in MCAO rats
Coexisting flavonoids and administration route effect on pharmacokinetics of Puerarin in MCAO rats Abstract Abstract A pharmacokinetic comparison was made to evaluate the influence from other components in the Radix Puerariae Extract on pharmacokinetic behavior of Puerarin. Samples of blood and brain were collected by ...
PMC9343874
core_pubmed_pmc
Comparative Pharmacokinetics of Cinobufacini Capsule and Injection by UPLC-MS/MS
Comparative Pharmacokinetics of Cinobufacini Capsule and Injection by UPLC-MS/MS Abstract Abstract Cinobufacini capsule and injection are two different formulations from the same source, obtained from the extraction of the skin of Bufo bufo gargarizans Cantor, which have been approved by the Chinese State Food and Drug...
PMC8001859
core_pubmed_pmc
Physiologically Based Pharmacokinetic Modeling of Bupropion and Its Metabolites in a CYP2B6 Drug-Drug-Gene Interaction Network
Physiologically Based Pharmacokinetic Modeling of Bupropion and Its Metabolites in a CYP2B6 Drug-Drug-Gene Interaction Network Abstract Abstract The noradrenaline and dopamine reuptake inhibitor bupropion is metabolized by CYP2B6 and recommended by the FDA as the only sensitive substrate for clinical CYP2B6 drug–drug i...
PMC4317228
core_pubmed_pmc
Pharmacological and pharmacokinetic properties of JNJ-40411813, a positive allosteric modulator of the mGlu2 receptor
Pharmacological and pharmacokinetic properties of JNJ-40411813, a positive allosteric modulator of the mGlu2 receptor Abstract Abstract Compounds modulating metabotropic glutamate type 2 (mGlu2) receptor activity may have therapeutic benefits in treating psychiatric disorders like schizophrenia and anxiety. The pharmac...
PMC4238735
core_pubmed_pmc
Pharmacokinetics of Tedizolid Following Oral Administration: Single and Multiple Dose, Effect of Food, and Comparison of Two Solid Forms of the Prodrug
Pharmacokinetics of Tedizolid Following Oral Administration: Single and Multiple Dose, Effect of Food, and Comparison of Two Solid Forms of the Prodrug Abstract Objectives The single- and multiple-dose pharmacokinetics (PK) of tedizolid were examined after oral administration of tedizolid phosphate disodium (TPD), incl...
PMC9548535
core_pubmed_pmc
Development of a pediatric physiologically-based pharmacokinetic model to support recommended dosing of atezolizumab in children with solid tumors
Development of a pediatric physiologically-based pharmacokinetic model to support recommended dosing of atezolizumab in children with solid tumors Abstract Background: Atezolizumab has been studied in multiple indications for both pediatric and adult patient populations. Generally, clinical studies enrolling pediatric ...
PMC8451859
core_pubmed_pmc
Evaluation of Drug‐Drug Interaction Liability for Buprenorphine Extended‐Release Monthly Injection Administered by Subcutaneous Route
Evaluation of Drug‐Drug Interaction Liability for Buprenorphine Extended‐Release Monthly Injection Administered by Subcutaneous Route Abstract Abstract Buprenorphine extended‐release (BUP‐XR) formulation is a once‐monthly subcutaneous injection for the treatment of opioid use disorder (OUD). Buprenorphine undergoes ext...
PMC9905117
core_pubmed_pmc
Characterization of the metabolism of eupalinolide A and B by carboxylesterase and cytochrome P450 in human liver microsomes
Characterization of the metabolism of eupalinolide A and B by carboxylesterase and cytochrome P450 in human liver microsomes Abstract Abstract Eupalinolide A (EA; Z-configuration) and eupalinolide B (EB; E-configuration) are bioactive cis-trans isomers isolated from Eupatorii Lindleyani Herba that exert anti-inflammato...
PMC8894944
core_pubmed_pmc
Regression Analysis to Estimate the Factor VIII Activity of Patients with Hemophilia A Without Inhibitor who Received Emicizumab Therapy
Regression Analysis to Estimate the Factor VIII Activity of Patients with Hemophilia A Without Inhibitor who Received Emicizumab Therapy Abstract Abstract Background Emicizumab, a bispecific monoclonal antibody for hemophilia A (HA), has strong pharmacodynamic effects in several coagulation assays resulting in dosing d...
PMC2880336
core_pubmed_pmc
New anticoagulants for the prevention of venous thromboembolism
New anticoagulants for the prevention of venous thromboembolism Abstract Anticoagulant drugs have an essential role in the prevention and treatment of thromboembolic diseases. Currently available anticoagulants substantially reduce the incidence of thromboembolic events in a number of clinical conditions. However, thes...
PMC10481538
core_pubmed_pmc
Bioanalytical method validation and application to a phase 1, double-blind, randomized pharmacokinetic trial of a standardized Centella asiatica (L.) Urban water extract product in healthy older adults
Bioanalytical method validation and application to a phase 1, double-blind, randomized pharmacokinetic trial of a standardized Centella asiatica (L.) Urban water extract product in healthy older adults Abstract Introduction: Centella asiatica is an herbaceous plant reputed in Eastern medicine to improve memory. Preclin...
PMC4716579
core_pubmed_pmc
Semi‐Mechanism‐Based Population Pharmacokinetic Modeling of the Hedgehog Pathway Inhibitor Vismodegib
Semi‐Mechanism‐Based Population Pharmacokinetic Modeling of the Hedgehog Pathway Inhibitor Vismodegib Abstract Abstract Vismodegib, approved for the treatment of advanced basal cell carcinoma, has shown unique pharmacokinetic (PK) nonlinearity and binding to α1‐acid glycoprotein (AAG) in humans. A semi‐mechanism‐based ...
PMC9230074
core_pubmed_pmc
Development of Photoremovable Linkers as a Novel Strategy to Improve the Pharmacokinetics of Drug Conjugates and Their Potential Application in Antibody–Drug Conjugates for Cancer Therapy
Development of Photoremovable Linkers as a Novel Strategy to Improve the Pharmacokinetics of Drug Conjugates and Their Potential Application in Antibody–Drug Conjugates for Cancer Therapy Abstract Abstract Although there have been extensive research and progress on the discovery of anticancer drug over the years, the a...
PMC12337008
core_pubmed_pmc
Predictors of caspofungin exposure-response relationship: a retrospective cohort study on therapeutic drug monitoring parameters
Predictors of caspofungin exposure-response relationship: a retrospective cohort study on therapeutic drug monitoring parameters Abstract Introduction This study aimed to characterize the exposure-response relationship of caspofungin through analysis of trough serum concentration (Cmin) associated with clinical efficac...
PMC4266495
core_pubmed_pmc
Preparation, Pharmacokinetics, Biodistribution, Antitumor Efficacy and Safety of Lx2-32c-Containing Liposome
Preparation, Pharmacokinetics, Biodistribution, Antitumor Efficacy and Safety of Lx2-32c-Containing Liposome Abstract Lx2-32c is a novel taxane that has been demonstrated to have robust antitumor activity against different types of tumors including several paclitaxel-resistant neoplasms. Since the delivery vehicles for...
PMC6887677
core_pubmed_pmc
Role of equilibrative nucleoside transporter 1 (ENT1) in the disposition of cytarabine in mice
Role of equilibrative nucleoside transporter 1 (ENT1) in the disposition of cytarabine in mice Abstract Abstract Cytarabine (Ara‐C) is a nucleoside analog used in the treatment of acute myeloid leukemia (AML). Despite the many years of clinical use, the identity of the transporter(s) involved in the disposition of Ara‐...
PMC12382689
core_pubmed_pmc
Pharmacokinetics/Pharmacodynamics-Based Repositioning of Cefmetazole and Flomoxef in Extended-Spectrum β-Lactamase-Producing Enterobacterales Treatment: An Injectable Carbapenem-Sparing and Outpatient Strategy
Pharmacokinetics/Pharmacodynamics-Based Repositioning of Cefmetazole and Flomoxef in Extended-Spectrum β-Lactamase-Producing Enterobacterales Treatment: An Injectable Carbapenem-Sparing and Outpatient Strategy Abstract Infections caused by extended-spectrum β-lactamase-producing Enterobacterales (ESBL-Es) pose a signif...
PMC8375633
core_pubmed_pmc
Synchronous LC-MS/MS determination of pantoprazole and amitriptyline in rabbit plasma: application to comparative in vivo pharmacokinetic study of novel formulated effervescent granules with its marketed tablet dosage form
Synchronous LC-MS/MS determination of pantoprazole and amitriptyline in rabbit plasma: application to comparative in vivo pharmacokinetic study of novel formulated effervescent granules with its marketed tablet dosage form Abstract Abstract In the present study the bioavailability and pharmacokinetics properties of pan...
PMC11962002
core_pubmed_pmc
Traditional usages, chemical metabolites, pharmacological activities, and pharmacokinetics of Boesenbergia rotunda (L.) Mansf.: a comprehensive review
Traditional usages, chemical metabolites, pharmacological activities, and pharmacokinetics of Boesenbergia rotunda (L.) Mansf.: a comprehensive review Abstract Abstract Boesenbergia rotunda : (L.) Mansf. (family Zingiberaceae), also known as fingerroot, is a medicinal and food plant that is widely distributed in southe...
PMC3018506
core_pubmed_pmc
Private Drinking Water Wells as a Source of Exposure to Perfluorooctanoic Acid (PFOA) in Communities Surrounding a Fluoropolymer Production Facility
Private Drinking Water Wells as a Source of Exposure to Perfluorooctanoic Acid (PFOA) in Communities Surrounding a Fluoropolymer Production Facility Abstract Background The C8 Health Project was established in 2005 to collect data on perfluorooctanoic acid (PFOA, or C8) and human health in Ohio and West Virginia commun...
PMC5434340
core_pubmed_pmc
Pharmacodynamics of Isavuconazole for Invasive Mold Disease: Role of Galactomannan for Real-Time Monitoring of Therapeutic Response
Pharmacodynamics of Isavuconazole for Invasive Mold Disease: Role of Galactomannan for Real-Time Monitoring of Therapeutic Response Abstract Abstract Background. The ability to make early therapeutic decisions when treating invasive aspergillosis using changes in biomarkers as a surrogate for therapeutic response could...
PMC4174509
core_pubmed_pmc
Accuracy and Completeness of Drug Information in Wikipedia: A Comparison with Standard Textbooks of Pharmacology
Accuracy and Completeness of Drug Information in Wikipedia: A Comparison with Standard Textbooks of Pharmacology Abstract The online resource Wikipedia is increasingly used by students for knowledge acquisition and learning. However, the lack of a formal editorial review and the heterogeneous expertise of contributors ...
PMC6521589
core_pubmed_pmc
Developmental Pharmacokinetics and Safety of Ibuprofen and Its Enantiomers in the Conventional Pig as Potential Pediatric Animal Model
Developmental Pharmacokinetics and Safety of Ibuprofen and Its Enantiomers in the Conventional Pig as Potential Pediatric Animal Model Abstract Abstract Pediatric drug development, especially in disease areas that only affect children, can be stimulated by using juvenile animal models not only for general safety studie...
PMC9087011
core_pubmed_pmc
Innovative Randomized Phase I Study and Dosing Regimen Selection to Accelerate and Inform Pivotal COVID‐19 Trial of Nirmatrelvir
Innovative Randomized Phase I Study and Dosing Regimen Selection to Accelerate and Inform Pivotal COVID‐19 Trial of Nirmatrelvir Abstract Coronavirus disease 2019 (COVID‐19) is a continued leading cause of hospitalization and death. Safe, efficacious COVID‐19 antivirals are needed urgently. Nirmatrelvir (PF‐07321332), ...
PMC6615816
core_pubmed_pmc
Assessing the safety and pharmacokinetics of the monoclonal antibodies, VRC07-523LS and PGT121 in HIV negative women in South Africa: study protocol for the CAPRISA 012A randomised controlled phase I trial
Assessing the safety and pharmacokinetics of the monoclonal antibodies, VRC07-523LS and PGT121 in HIV negative women in South Africa: study protocol for the CAPRISA 012A randomised controlled phase I trial Abstract Abstract Introduction Despite extensive prevention campaigns and scale-up of antiretroviral therapy, HIV ...
PMC3293174
core_pubmed_pmc
Rationale, challenges, and participants in a Phase II trial of a botanical product for chronic hepatitis C
Rationale, challenges, and participants in a Phase II trial of a botanical product for chronic hepatitis C Abstract Abstract Background Chronic hepatitis C is associated with significant morbidity and mortality as a consequence of progression to cirrhosis, hepatocellular carcinoma, and liver failure. Current treatment ...
PMC3573806
core_pubmed_pmc
Formulation and in vitro and in vivo evaluation of film-coated montelukast sodium tablets using Opadry ® yellow 20A82938 on an industrial scale
Formulation and in vitro and in vivo evaluation of film-coated montelukast sodium tablets using Opadry ® yellow 20A82938 on an industrial scale Abstract Purpose: The aim of this study was to formulate stable film-coated montelukast sodium (MS) tablets using Opadry ® yellow 20A82938 (Montikast ® tablets) and to evaluate...
PMC5822840
core_pubmed_pmc
Drug–drug interactions involving antidepressants: focus on desvenlafaxine
Drug–drug interactions involving antidepressants: focus on desvenlafaxine Abstract Abstract Psychiatric and physical conditions often coexist, and there is robust evidence that associates the frequency of depression with single and multiple physical conditions. More than half of patients with depression may have at lea...
PMC6451710
core_pubmed_pmc
Impact of CYP3A4*22 on Pazopanib Pharmacokinetics in Cancer Patients
Impact of CYP3A4*22 on Pazopanib Pharmacokinetics in Cancer Patients Abstract Background and Objective As pazopanib plasma trough concentrations are correlated with treatment outcome, we explored whether single nucleotide polymorphisms in the elimination pathway of pazopanib affect systemic pazopanib concentrations. Me...
PMC5320447
core_pubmed_pmc
Scale up and pharmacokinetic study of a novel mutated chimeric tissue plasminogen activator (mt-PA) in rats
Scale up and pharmacokinetic study of a novel mutated chimeric tissue plasminogen activator (mt-PA) in rats Abstract Because of high mortality caused by cardiovascular diseases, various fibrinolytic agents with diverse pharmacokinetic and pharmacodynamic properties have been developed. A novel mutated chimeric tissue p...
PMC11579104
core_pubmed_pmc
A quantitative systems pharmacology model of plasma kallikrein-kinin system dysregulation in hereditary angioedema
A quantitative systems pharmacology model of plasma kallikrein-kinin system dysregulation in hereditary angioedema Abstract Abstract Hereditary angioedema (HAE) due to C1-inhibitor deficiency is a rare, debilitating, genetic disorder characterized by recurrent, unpredictable, attacks of edema. The clinical symptoms of ...
PMC5890720
core_pubmed_pmc
A model-informed preclinical approach for prediction of clinical pharmacodynamic interactions of anti-TB drug combinations
A model-informed preclinical approach for prediction of clinical pharmacodynamic interactions of anti-TB drug combinations Abstract Abstract Background Identification of pharmacodynamic interactions is not reasonable to carry out in a clinical setting for many reasons. The aim of this work was to develop a model-inform...
PMC7961457
core_pubmed_pmc
Rp-HPLC Determination of Quercetin in a Novel D-α-Tocopherol Polyethylene Glycol 1000 Succinate Based SNEDDS Formulation: Pharmacokinetics in Rat Plasma
Rp-HPLC Determination of Quercetin in a Novel D-α-Tocopherol Polyethylene Glycol 1000 Succinate Based SNEDDS Formulation: Pharmacokinetics in Rat Plasma Abstract Despite its proven efficacy in diverse metabolic disorders, quercetin (QU) for clinical use is still limited because of its low bioavailability. D-α-Tocophero...
PMC6989225
core_pubmed_pmc
Pharmacokinetics of fixed-dose combination of rosuvastatin 20 mg and ezetimibe 10 mg compared to concurrent administration of individual tablets in healthy Korean subjects
Pharmacokinetics of fixed-dose combination of rosuvastatin 20 mg and ezetimibe 10 mg compared to concurrent administration of individual tablets in healthy Korean subjects Abstract Abstract This study aimed to compare the pharmacokinetics of fixed-dose combination (FDC) tablet of rosuvastatin 20 mg/ezetimibe 10 mg with...
PMC7042483
core_pubmed_pmc
Percutaneous absorption and brain distribution facilitation of borneol on tetramethylpyrazine in a microemulsion-based transdermal therapeutic system
Percutaneous absorption and brain distribution facilitation of borneol on tetramethylpyrazine in a microemulsion-based transdermal therapeutic system Abstract In this study, we show that the percutaneous absorption and brain distribution of tetramethylpyrazine (TMP) is enhanced when combined with borneol (BN) in a micr...
PMC12843901
core_pubmed_pmc
Bacteriophage Therapy: Overcoming Antimicrobial Resistance Through Advanced Delivery Methods
Bacteriophage Therapy: Overcoming Antimicrobial Resistance Through Advanced Delivery Methods Abstract Abstract Microbial resistance to antibiotics necessitates the development of alternative treatments to address the challenges posed by severe bacterial infections. Bacteriophages are regaining clinical relevance, but t...
PMC8663851
core_pubmed_pmc
Development of a simple method for measuring tedizolid concentration in human serum using HPLC with a fluorescent detector
Development of a simple method for measuring tedizolid concentration in human serum using HPLC with a fluorescent detector Abstract Abstract The objective of the present study was to develop a method to measure tedizolid (TZD) concentration for studying target concentration intervention, pharmacokinetics, and pharmacod...