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PMC6222889
core_pubmed_pmc
An Ultra-High Performance Liquid Chromatography with Tandem Mass Spectrometry Method for Determination of 10 Alkaloids in Beagle Dog Plasma after the Oral Administration of the Corydalis yanhusuo W.T. Wang Extract and Yuanhuzhitong Tablets
An Ultra-High Performance Liquid Chromatography with Tandem Mass Spectrometry Method for Determination of 10 Alkaloids in Beagle Dog Plasma after the Oral Administration of the Corydalis yanhusuo W.T. Wang Extract and Yuanhuzhitong Tablets Abstract Abstract This study has developed a sensitive and simple ultra-high per...
PMC6147689
core_pubmed_pmc
Comparison between prefilled syringe and autoinjector devices on patient-reported experiences and pharmacokinetics in galcanezumab studies
Comparison between prefilled syringe and autoinjector devices on patient-reported experiences and pharmacokinetics in galcanezumab studies Abstract Abstract Purpose The aim of this study was to compare the usability and patient-rated experiences of an autoinjector with a prefilled syringe in patients with migraine, who...
PMC12243904
core_pubmed_pmc
Tramadol overdose in total knee arthroplasty: A case report
Tramadol overdose in total knee arthroplasty: A case report Abstract BACKGROUND Tramadol is a synthetic opioid analgesic commonly employed in postoperative pain control due to its moderate efficacy and comparatively favorable safety profile. Nonetheless, overdose can result in significant adverse effects, notably centr...
PMC12538123
core_pubmed_pmc
Polygenic scores and antidepressant treatment outcomes in major depression: a critical integrative review
Polygenic scores and antidepressant treatment outcomes in major depression: a critical integrative review Abstract Abstract Major depressive disorder (MDD) shows a large heterogeneity in antidepressant treatment outcome, a variability explained in part by common-variant liability captured by polygenic scores (PGSs). We...
PMC8970962
core_pubmed_pmc
Comparative Pharmacokinetic Study of Three Major Bioactive Components in the Normal and Different Courses of Liver-Stagnation and Spleen-Deficiency Syndrome Depressive Rats after Intragastric Administration of Zhi-Zi-Hou-Po Decoction
Comparative Pharmacokinetic Study of Three Major Bioactive Components in the Normal and Different Courses of Liver-Stagnation and Spleen-Deficiency Syndrome Depressive Rats after Intragastric Administration of Zhi-Zi-Hou-Po Decoction Abstract To reveal the pharmacokinetic process of narirutin, naringin, and honokiol in...
PMC10097767
core_pubmed_pmc
Dose Rationale of Nasal Glucagon in Japanese Pediatric Patients with Diabetes Using Pharmacokinetic/Pharmacodynamic Modeling and Simulation
Dose Rationale of Nasal Glucagon in Japanese Pediatric Patients with Diabetes Using Pharmacokinetic/Pharmacodynamic Modeling and Simulation Abstract Abstract Background Nasal glucagon (NG) 3 mg is approved in Japan to treat hypoglycemia in pediatric patients with diabetes, but an NG clinical study has not been performe...
PMC11154777
core_pubmed_pmc
Phase 2 study of the efficacy and safety of ponsegromab in patients with cancer cachexia: PROACC‐1 study design
Phase 2 study of the efficacy and safety of ponsegromab in patients with cancer cachexia: PROACC‐1 study design Abstract Abstract Background Cancer cachexia is a multifactorial metabolic wasting syndrome characterized by anorexia, unintentional loss of weight involving both skeletal muscle and adipose tissues, progress...
PMC5013402
core_pubmed_pmc
Impact of symptomatic upper respiratory tract infections on insulin absorption and action of Technosphere inhaled insulin
Impact of symptomatic upper respiratory tract infections on insulin absorption and action of Technosphere inhaled insulin Abstract Objective Uncomplicated, acute upper respiratory tract infections (URTIs) occur in patients with diabetes at a similar frequency to the general population. This study ( NCT00642681 ) invest...
PMC3271538
core_pubmed_pmc
The peak bispectral index time cannot predict early phase propofol pharmacodynamics with effect site-controlled infusion algorithm
The peak bispectral index time cannot predict early phase propofol pharmacodynamics with effect site-controlled infusion algorithm Abstract Objectives: The plasma-effect site equilibration rate constant (ke0) of propofol was determined with peak bispectral index (BIS) time (T PEAK ) in our previous study. The present s...
PMC4533485
core_pubmed_pmc
A Multicenter Phase I/II Study of the BCNU Implant (Gliadel ® Wafer) for Japanese Patients with Malignant Gliomas
A Multicenter Phase I/II Study of the BCNU Implant (Gliadel ® Wafer) for Japanese Patients with Malignant Gliomas Abstract Abstract Carmustine (BCNU) implants (Gliadel ® Wafer, Eisai Inc., New Jersey, USA) for the treatment of malignant gliomas (MGs) were shown to enhance overall survival in comparison to placebo in co...
PMC7811513
core_pubmed_pmc
Cross-species analysis of hepatic cytochrome P450 and transport protein expression
Cross-species analysis of hepatic cytochrome P450 and transport protein expression Abstract Most drugs and xenobiotics are metabolized in the liver. Amongst others, different cytochrome P450 (CYP) enzymes catalyze the metabolic conversion of foreign compounds, and various transport proteins are engaged in the excretion...
PMC8157589
core_pubmed_pmc
Comparative Gene Signature of (−)-Oleocanthal Formulation Treatments in Heterogeneous Triple Negative Breast Tumor Models: Oncological Therapeutic Target Insights
Comparative Gene Signature of (−)-Oleocanthal Formulation Treatments in Heterogeneous Triple Negative Breast Tumor Models: Oncological Therapeutic Target Insights Abstract Abstract Triple negative breast cancer (TNBC) heterogeneity and limited therapeutic options confer its phenotypic aggressiveness. The discovery of a...
PMC7785372
core_pubmed_pmc
An UPLC-MS/MS Method for Determination of Osimertinib in Rat Plasma: Application to Investigating the Effect of Ginsenoside Rg3 on the Pharmacokinetics of Osimertinib
An UPLC-MS/MS Method for Determination of Osimertinib in Rat Plasma: Application to Investigating the Effect of Ginsenoside Rg3 on the Pharmacokinetics of Osimertinib Abstract Osimertinib is a novel oral, potent, and irreversible epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) for treatment of adv...
PMC6770293
core_pubmed_pmc
Overview of the Anticancer Profile of Avenanthramides from Oat
Overview of the Anticancer Profile of Avenanthramides from Oat Abstract Abstract Cancer represents one of the leading causes of death worldwide. Progresses in treatment of cancer have continued at a rapid pace. However, undesirable side effects and drug resistance remain major challenges for therapeutic success. Natura...
PMC10491600
core_pubmed_pmc
Structural variation of the coding and non-coding human pharmacogenome
Structural variation of the coding and non-coding human pharmacogenome Abstract Genetic variants in drug targets and genes encoding factors involved in drug absorption, distribution, metabolism and excretion (ADME) can have pronounced impacts on drug pharmacokinetics, response, and toxicity. While the landscape of gene...
PMC7364767
core_pubmed_pmc
Evaluation of the Switch From Amiodarone to Dronedarone in Patients With Atrial Fibrillation: Results of the ARTEMIS AF Studies
Evaluation of the Switch From Amiodarone to Dronedarone in Patients With Atrial Fibrillation: Results of the ARTEMIS AF Studies Abstract Abstract Background: Switching between antiarrhythmic drugs is timed to minimize arrhythmia recurrence and adverse reactions. Dronedarone and amiodarone have similar electrophysiologi...
PMC7813410
core_pubmed_pmc
Intraperitoneal insulin administration in pigs: effect on circulating insulin and glucose levels
Intraperitoneal insulin administration in pigs: effect on circulating insulin and glucose levels Abstract Introduction The effect of intraperitoneal insulin infusion has limited evidence in the literature. Therefore, the aim of the study was to investigate the pharmacokinetics and pharmacodynamics of different intraper...
PMC11745150
core_pubmed_pmc
Red Yeast Rice or Lovastatin? A Comparative Evaluation of Safety and Efficacy Through a Multifaceted Approach
Red Yeast Rice or Lovastatin? A Comparative Evaluation of Safety and Efficacy Through a Multifaceted Approach Abstract ABSTRACT The increasing use of red yeast rice (RYR) as a natural supplement to manage blood cholesterol levels is driven by its active compound, monacolin K (MK), which is chemically identical to the s...
PMC3766776
core_pubmed_pmc
The determinants of propofol induction time in anesthesia
The determinants of propofol induction time in anesthesia Abstract Background The required dose of anesthetics is generally smaller in patients with low cardiac output (CO). A high CO decreases the blood concentration of anesthetics during induction and maintenance of anesthesia. However, a high CO may also shorten the...
PMC8009217
core_pubmed_pmc
Effects of the combination of second-generation antipsychotics on serum concentrations of aripiprazole and dehydroaripiprazole in Chinese patients with schizophrenia
Effects of the combination of second-generation antipsychotics on serum concentrations of aripiprazole and dehydroaripiprazole in Chinese patients with schizophrenia Abstract Background Aripiprazole (ARI) is often prescribed alone or in combination with other second-generation antipsychotics (SGAs) to treat patients wi...
PMC7927832
core_pubmed_pmc
Population Pharmacokinetic Properties of Antituberculosis Drugs in Vietnamese Children with Tuberculous Meningitis
Population Pharmacokinetic Properties of Antituberculosis Drugs in Vietnamese Children with Tuberculous Meningitis Abstract Optimal dosing of children with tuberculous meningitis (TBM) remains uncertain and is currently based on the treatment of pulmonary tuberculosis in adults. This study aimed to investigate the popu...
PMC12458661
core_pubmed_pmc
Pharmacokinetics and pharmacodynamics of inhaled molgramostim in healthy people
Pharmacokinetics and pharmacodynamics of inhaled molgramostim in healthy people Abstract Abstract Background Inhaled molgramostim, a form of recombinant human granulocyte–macrophage colony stimulating factor (GM-CSF), is a promising investigational pharmacotherapy for autoimmune pulmonary alveolar proteinosis (aPAP); h...
PMC11200783
core_pubmed_pmc
Meropenem/Vaborbactam—A Mechanistic Review for Insight into Future Development of Combinational Therapies
Meropenem/Vaborbactam—A Mechanistic Review for Insight into Future Development of Combinational Therapies Abstract Abstract Beta-lactam antibiotics have been a major climacteric in medicine for being the first bactericidal compound available for clinical use. They have continually been prescribed since their developmen...
PMC10916370
core_pubmed_pmc
Limitations of antifungal prophylaxis in preventing invasive Candida surgical site infections after liver transplant surgery
Limitations of antifungal prophylaxis in preventing invasive Candida surgical site infections after liver transplant surgery Abstract ABSTRACT Invasive primary Candida surgical site infections (IP-SSIs) are a common complication of liver transplantation, and targeted antifungal prophylaxis is an efficient strategy to l...
PMC7691413
core_pubmed_pmc
Population Pharmacokinetic Model of Plasma and Cellular Mycophenolic Acid in Kidney Transplant Patients from the CIMTRE Study
Population Pharmacokinetic Model of Plasma and Cellular Mycophenolic Acid in Kidney Transplant Patients from the CIMTRE Study Abstract Background and Objective Mycophenolate mofetil is widely used in kidney transplant recipients. Mycophenolate mofetil is hydrolysed by blood esterases to mycophenolic acid (MPA), the act...
PMC9643401
core_pubmed_pmc
Pharmacokinetics and efficacy of topical inserts containing tenofovir alafenamide fumarate and elvitegravir administered rectally in macaques
Pharmacokinetics and efficacy of topical inserts containing tenofovir alafenamide fumarate and elvitegravir administered rectally in macaques Abstract Summary Background Topical on-demand forms for HIV pre-exposure prophylaxis (PrEP) may be a desirable alternative for people that prefer not to use daily PrEP. CONRAD ha...
PMC6437518
core_pubmed_pmc
DSM265 at 400 Milligrams Clears Asexual Stage Parasites but Not Mature Gametocytes from the Blood of Healthy Subjects Experimentally Infected with Plasmodium falciparum
DSM265 at 400 Milligrams Clears Asexual Stage Parasites but Not Mature Gametocytes from the Blood of Healthy Subjects Experimentally Infected with Plasmodium falciparum Abstract DSM265 is a novel antimalarial drug in clinical development that acts as a selective inhibitor of Plasmodium dihydroorotate dehydrogenase. In ...
PMC8415261
core_pubmed_pmc
Case Report: Low Hematocrit Leading to Tacrolimus Toxicity
Case Report: Low Hematocrit Leading to Tacrolimus Toxicity Abstract Abstract Tacrolimus is a calcineurin inhibitor characterized by a narrow therapeutic index and high intra- and inter-individual pharmacokinetic variability. Therapeutic drug monitoring in whole-blood is the standard monitoring procedure. However, tacro...
PMC9065877
core_pubmed_pmc
Safety, tolerability and pharmacokinetics of the oligomer modulator anle138b with exposure levels sufficient for therapeutic efficacy in a murine Parkinson model: A randomised, double-blind, placebo-controlled phase 1a trial
Safety, tolerability and pharmacokinetics of the oligomer modulator anle138b with exposure levels sufficient for therapeutic efficacy in a murine Parkinson model: A randomised, double-blind, placebo-controlled phase 1a trial Abstract Summary Background Synucleinopathies such as Parkinson ´s disease (PD), Dementia with ...
PMC10386916
core_pubmed_pmc
A Randomized Open-Label Study of Relugolix Alone or Relugolix Combination Therapy in Premenopausal Women
A Randomized Open-Label Study of Relugolix Alone or Relugolix Combination Therapy in Premenopausal Women Abstract Background and Objective Relugolix is a gonadotropin-releasing hormone receptor antagonist. Relugolix 40-mg monotherapy is associated with vasomotor symptoms and long-term bone mineral density loss due to h...
PMC6522587
core_pubmed_pmc
A Retrospective Analysis of Probability of Target Attainment in Community-Acquired Pneumonia: Ceftaroline Fosamil Versus Comparators
A Retrospective Analysis of Probability of Target Attainment in Community-Acquired Pneumonia: Ceftaroline Fosamil Versus Comparators Abstract Introduction This retrospective analysis compares the probability of target attainment (PTA) for ceftriaxone, levofloxacin and ceftaroline fosamil against Staphylococcus aureus ,...
PMC4825616
core_pubmed_pmc
Rapid Quantitative Pharmacodynamic Imaging with Bayesian Estimation
Rapid Quantitative Pharmacodynamic Imaging with Bayesian Estimation Abstract We recently described rapid quantitative pharmacodynamic imaging, a novel method for estimating sensitivity of a biological system to a drug. We tested its accuracy in simulated biological signals with varying receptor sensitivity and varying ...
PMC8304466
core_pubmed_pmc
Simplified and Rapid Determination of Primaquine and 5,6-Orthoquinone Primaquine by UHPLC-MS/MS: Its Application to a Pharmacokinetic Study
Simplified and Rapid Determination of Primaquine and 5,6-Orthoquinone Primaquine by UHPLC-MS/MS: Its Application to a Pharmacokinetic Study Abstract Abstract The method for the determination of primaquine (PQ) and 5,6-orthoquinone primaquine (5,6-PQ), the representative marker for PQ active metabolites, via CYP2D6 in h...
PMC6099598
core_pubmed_pmc
Upregulation of UDP-Glucuronosyltransferases 1a1 and 1a7 Are Involved in Altered Puerarin Pharmacokinetics in Type II Diabetic Rats
Upregulation of UDP-Glucuronosyltransferases 1a1 and 1a7 Are Involved in Altered Puerarin Pharmacokinetics in Type II Diabetic Rats Abstract Puerarin is an isoflavonoid extracted from Pueraria lobata roots, and displays a broad range of pharmacological activities, including antidiabetic activity. However, information a...
PMC6402189
core_pubmed_pmc
Single‐Dose and Multiple‐Dose Pharmacokinetics of Vaniprevir in Healthy Men
Single‐Dose and Multiple‐Dose Pharmacokinetics of Vaniprevir in Healthy Men Abstract Abstract Vaniprevir is an inhibitor of the hepatitis C virus (HCV) NS3/4A protease. The aim of these double‐blind, placebo‐controlled phase I studies was to evaluate the safety and pharmacokinetics of vaniprevir in healthy male volunte...
PMC4556830
core_pubmed_pmc
The Effect of MGCD0103 on CYP450 Isoforms Activity of Rats by Cocktail Method
The Effect of MGCD0103 on CYP450 Isoforms Activity of Rats by Cocktail Method Abstract Abstract MGCD0103, an isotype-selective histone deacetylase inhibitor (HDACi), has been clinically evaluated for the treatment of hematologic malignancies and advanced solid tumors, alone and in combination with standard-of-care agen...
PMC7010620
core_pubmed_pmc
Multi-scale modeling of drug binding kinetics to predict drug efficacy
Multi-scale modeling of drug binding kinetics to predict drug efficacy Abstract Abstract Optimizing drug therapies for any disease requires a solid understanding of pharmacokinetics (the drug concentration at a given time point in different body compartments) and pharmacodynamics (the effect a drug has at a given conce...
PMC5762451
core_pubmed_pmc
The pharmacokinetic study of rutin in rat plasma based on an electrochemically reduced graphene oxide modified sensor ☆
The pharmacokinetic study of rutin in rat plasma based on an electrochemically reduced graphene oxide modified sensor ☆ Abstract Abstract An electrochemical method based on a directly electrochemically reduced graphene oxide (ERGO) film coated on a glassy carbon electrode (GCE) was developed for the rapid and convenien...
PMC7187626
core_pubmed_pmc
A Single-Dose Combination Study with the Experimental Antimalarials Artefenomel and DSM265 To Determine Safety and Antimalarial Activity against Blood-Stage Plasmodium falciparum in Healthy Volunteers
A Single-Dose Combination Study with the Experimental Antimalarials Artefenomel and DSM265 To Determine Safety and Antimalarial Activity against Blood-Stage Plasmodium falciparum in Healthy Volunteers Abstract Artefenomel and DSM265 are two new compounds that have been shown to be well tolerated and effective when admi...
PMC5351339
core_pubmed_pmc
Characterizing Class‐Specific Exposure‐Viral Load Suppression Response of HIV Antiretrovirals Using A Model‐Based Meta‐Analysis
Characterizing Class‐Specific Exposure‐Viral Load Suppression Response of HIV Antiretrovirals Using A Model‐Based Meta‐Analysis Abstract Abstract We applied model‐based meta‐analysis of viral suppression as a function of drug exposure and in vitro potency for short‐term monotherapy in human immunodeficiency virus type ...
PMC10794428
core_pubmed_pmc
A minimal PBPK model to accelerate preclinical development of drugs against tuberculosis
A minimal PBPK model to accelerate preclinical development of drugs against tuberculosis Abstract Abstract Introduction: Understanding drug exposure at disease target sites is pivotal to profiling new drug candidates in terms of tolerability and efficacy. Such quantification is particularly tedious for anti-tuberculosi...
PMC4171595
core_pubmed_pmc
Midazolam Pharmacokinetics in Morbidly Obese Patients Following Semi-Simultaneous Oral and Intravenous Administration: A Comparison with Healthy Volunteers
Midazolam Pharmacokinetics in Morbidly Obese Patients Following Semi-Simultaneous Oral and Intravenous Administration: A Comparison with Healthy Volunteers Abstract Abstract Background While in vitro and animal studies have shown reduced cytochrome P450 (CYP) 3A activity due to obesity, clinical studies in (morbidly) o...
PMC9922681
core_pubmed_pmc
Analytical approaches for determination of COVID-19 candidate drugs in human biological matrices
Analytical approaches for determination of COVID-19 candidate drugs in human biological matrices Abstract Abstract Since the outbreak of the COVID-19 pandemic, the use of antiviral and other available drugs has been considered to combat or reduce the clinical symptoms of patients. In this regard, it would be necessary ...
PMC8550736
core_pubmed_pmc
OptiDose: Computing the Individualized Optimal Drug Dosing Regimen Using Optimal Control
OptiDose: Computing the Individualized Optimal Drug Dosing Regimen Using Optimal Control Abstract Providing the optimal dosing strategy of a drug for an individual patient is an important task in pharmaceutical sciences and daily clinical application. We developed and validated an optimal dosing algorithm (OptiDose) th...
PMC11632551
core_pubmed_pmc
Impact of potential multiple drug-drug interactions on the adverse event profile of patients with hepatitis C treated with pangenotypic direct-acting antivirals in Spain
Impact of potential multiple drug-drug interactions on the adverse event profile of patients with hepatitis C treated with pangenotypic direct-acting antivirals in Spain Abstract Abstract Objectives: Direct-acting antivirals (DAAs) share pharmacokinetic pathways with many comedications commonly administered to patients...
PMC7939511
core_pubmed_pmc
Individualized Vancomycin Dosing with Therapeutic Drug Monitoring and Pharmacokinetic Consultation Service: A Large-Scale Retrospective Observational Study
Individualized Vancomycin Dosing with Therapeutic Drug Monitoring and Pharmacokinetic Consultation Service: A Large-Scale Retrospective Observational Study Abstract Abstract Background To date, outcome data with a large sample size and data regarding the clinical outcomes of pharmacokinetic-guided (PK) dosing of vancom...
PMC12486805
core_pubmed_pmc
Preclinical evaluation of tridecaptin M: in vitro and in vivo efficacy against colistin-resistant Gram-negative bacterial pathogens and pharmacokinetics
Preclinical evaluation of tridecaptin M: in vitro and in vivo efficacy against colistin-resistant Gram-negative bacterial pathogens and pharmacokinetics Abstract ABSTRACT The escalating threat of antimicrobial resistance (AMR), particularly among gram-negative pathogens, necessitates the development of novel therapeuti...
PMC12402880
core_pubmed_pmc
Bioequivalence of a Donepezil/Memantine 10/20 mg Fixed‐Dose Combination Versus Single‐Component Tablets in Healthy Korean Males
Bioequivalence of a Donepezil/Memantine 10/20 mg Fixed‐Dose Combination Versus Single‐Component Tablets in Healthy Korean Males Abstract Abstract A fixed‐dose combination (FDC) tablet formulation of donepezil/memantine (10/20 mg) was developed to improve medication compliance in patients with Alzheimer's disease (AD). ...
PMC12872115
core_pubmed_pmc
Stochastic Gates for Covariate Selection in Population Pharmacokinetics Modeling
Stochastic Gates for Covariate Selection in Population Pharmacokinetics Modeling Abstract ABSTRACT Covariate selection in population pharmacokinetics modeling is essential for understanding interindividual variability in drug response and optimizing dosing. Traditional stepwise covariate modeling is often time‐consumin...
PMC7605398
core_pubmed_pmc
Brigatinib Versus Crizotinib in Advanced ALK Inhibitor–Naive ALK-Positive Non–Small Cell Lung Cancer: Second Interim Analysis of the Phase III ALTA-1L Trial
Brigatinib Versus Crizotinib in Advanced ALK Inhibitor–Naive ALK-Positive Non–Small Cell Lung Cancer: Second Interim Analysis of the Phase III ALTA-1L Trial Abstract PURPOSE Brigatinib, a next-generation anaplastic lymphoma kinase (ALK) inhibitor, demonstrated superior progression-free survival (PFS) and improved healt...
PMC11492913
core_pubmed_pmc
Preliminary Study on Pharmacokinetics and Antitumor Pharmacodynamics of Folic Acid Modified Crebanine Polyethyleneglycol-Polylactic Acid Hydroxyacetic Acid Copolymer Nanoparticles
Preliminary Study on Pharmacokinetics and Antitumor Pharmacodynamics of Folic Acid Modified Crebanine Polyethyleneglycol-Polylactic Acid Hydroxyacetic Acid Copolymer Nanoparticles Abstract Abstract Purpose Liver cancer is associated significantly with morbidity and mortality. The combination of low-intensity ultrasound...
PMC8960550
core_pubmed_pmc
Adverse Reactions in a Phase 1 Trial of the Anti-Malarial DM1157: An Example of Pharmacokinetic Modeling and Simulation Guiding Clinical Trial Decisions
Adverse Reactions in a Phase 1 Trial of the Anti-Malarial DM1157: An Example of Pharmacokinetic Modeling and Simulation Guiding Clinical Trial Decisions Abstract Introduction There is an urgent need to develop new drugs to treat malaria due to increasing resistance to first-line therapeutics targeting the causative org...
PMC8110997
core_pubmed_pmc
Structural analogues in herbal medicine ginseng hit a shared target to achieve cumulative bioactivity
Structural analogues in herbal medicine ginseng hit a shared target to achieve cumulative bioactivity Abstract By a pilot trial on investigating immunomodulatory activity and target of ginsenosides, the major bioactive components of ginseng, here we report that structural analogues in herbal medicines hit a shared targ...
PMC4695179
core_pubmed_pmc
Suppression of Rituximab-resistant B-cell lymphoma with a novel multi-component anti-CD20 mAb nanocluster
Suppression of Rituximab-resistant B-cell lymphoma with a novel multi-component anti-CD20 mAb nanocluster Abstract Abstract Although the anti-CD20 antibody Rituximab has revolutionized the treatment of Non-Hodgkin Lymphoma (NHL), resistance to treatment still existed. Thus, strategies for suppressing Rituximab-resistan...
PMC10748103
core_pubmed_pmc
In Vitro Screening of Antimicrobial and Anti-Coagulant Activities, ADME Profiling, and Molecular Docking Study of Citrus limon L. and Citrus paradisi L. Cold-Pressed Volatile Oils
In Vitro Screening of Antimicrobial and Anti-Coagulant Activities, ADME Profiling, and Molecular Docking Study of Citrus limon L. and Citrus paradisi L. Cold-Pressed Volatile Oils Abstract Abstract Citrus , which belongs to the Rutaceae family, is a very widespread genus in the Mediterranean Basin. In Tunisia, various ...
PMC8312709
core_pubmed_pmc
Physiologically Based Pharmacokinetic Models Are Effective Support for Pediatric Drug Development
Physiologically Based Pharmacokinetic Models Are Effective Support for Pediatric Drug Development Abstract Abstract Pediatric drug development faces many difficulties. Traditionally, pediatric drug doses are simply calculated linearly based on the body weight, age, and body surface area of adults. Due to the ontogeny o...
PMC12790504
core_pubmed_pmc
Can Alpha-Glucosidase Activity in Plasma or Leukocytes Serve as a Biomarker for Future Gene Therapy in Classic Infantile Pompe Disease?
Can Alpha-Glucosidase Activity in Plasma or Leukocytes Serve as a Biomarker for Future Gene Therapy in Classic Infantile Pompe Disease? Abstract We studied alpha-glucosidase activity in plasma and leukocytes after an infusion of 40 mg/kg of recombinant alglucosidase alpha in patients with classic infantile Pompe diseas...
PMC5114325
core_pubmed_pmc
Pharmacokinetic and pharmacodynamic study of doxorubicin in children with cancer: results of a “European Pediatric Oncology Off-patents Medicines Consortium” trial
Pharmacokinetic and pharmacodynamic study of doxorubicin in children with cancer: results of a “European Pediatric Oncology Off-patents Medicines Consortium” trial Abstract Abstract Purpose Doxorubicin is a key component in many pediatric oncology treatment regimens; still pharmacology data on which current dosing regi...
PMC12135528
core_pubmed_pmc
Determining an appropriate fosfomycin (ZTI-01) dosing regimen in pneumonia patients by utilizing minimal PBPK modeling and target attainment analysis
Determining an appropriate fosfomycin (ZTI-01) dosing regimen in pneumonia patients by utilizing minimal PBPK modeling and target attainment analysis Abstract ABSTRACT Fosfomycin, a broad-spectrum antibiotic used for uncomplicated cystitis, represents a potential promising candidate in combating resistant pneumonia. To...
PMC8480901
core_pubmed_pmc
Anti-inflammatory activity of lefamulin versus azithromycin and dexamethasone in vivo and in vitro in a lipopolysaccharide-induced lung neutrophilia mouse model
Anti-inflammatory activity of lefamulin versus azithromycin and dexamethasone in vivo and in vitro in a lipopolysaccharide-induced lung neutrophilia mouse model Abstract Abstract Several antibiotics demonstrate both antibacterial and anti-inflammatory/immunomodulatory activities and are used to treat inflammatory pulmo...
PMC5525741
core_pubmed_pmc
[ 177 Lu]pentixather: Comprehensive Preclinical Characterization of a First CXCR4-directed Endoradiotherapeutic Agent
[ 177 Lu]pentixather: Comprehensive Preclinical Characterization of a First CXCR4-directed Endoradiotherapeutic Agent Abstract Purpose: Based on the clinical relevance of the chemokine receptor 4 (CXCR4) as a molecular target in cancer and on the success of [ 68 Ga]pentixafor as an imaging probe for high-contrast visua...
PMC8674255
core_pubmed_pmc
Safety and tolerability of asunercept plus standard radiotherapy/temozolomide in Asian patients with newly-diagnosed glioblastoma: a phase I study
Safety and tolerability of asunercept plus standard radiotherapy/temozolomide in Asian patients with newly-diagnosed glioblastoma: a phase I study Abstract Asunercept (company code APG101 [Apogenix AG]; company code CAN008 [CANbridge Pharmaceuticals]) is a novel glycosylated fusion protein that has shown promising effe...
PMC10281928
core_pubmed_pmc
Invasive Mold Infections in Children: Navigating Troubled Waters with a Broken Compass
Invasive Mold Infections in Children: Navigating Troubled Waters with a Broken Compass Abstract Abstract Incidence of invasive mold infections in children, while rare, is increasing as the population of high-risk patients expands, including premature infants, pediatric patients undergoing treatment for hematological ma...
PMC9605490
core_pubmed_pmc
Opposite Response to Vitamin K Antagonists: A Report of Two Cases and Systematic Review of Literature
Opposite Response to Vitamin K Antagonists: A Report of Two Cases and Systematic Review of Literature Abstract Vitamin K antagonists (VKAs) are used in the prophylaxis and treatment of thromboembolic disorders. Despite a high efficacy, their narrow therapeutic window and high response variability hamper their managemen...
PMC9942414
core_pubmed_pmc
The Alzheimer’s disease-linked protease BACE1 modulates neuronal IL-6 signaling through shedding of the receptor gp130
The Alzheimer’s disease-linked protease BACE1 modulates neuronal IL-6 signaling through shedding of the receptor gp130 Abstract Abstract Background The protease BACE1 is a major drug target for Alzheimer’s disease, but chronic BACE1 inhibition is associated with non-progressive cognitive worsening that may be caused by...
PMC11878927
core_pubmed_pmc
Identifying novel inhibitors against drug-resistant mutant CYP-51 Candida albicans : A computational study to combat fungal infections
Identifying novel inhibitors against drug-resistant mutant CYP-51 Candida albicans : A computational study to combat fungal infections Abstract Candida albicans (C. albicans) is an opportunistic pathogen in immunocompromised individuals and a normal inhabitant of the oral cavity, throat, gastrointestinal tract, and gen...
PMC6544603
core_pubmed_pmc
Towards a Generic Tool for Prediction of Meropenem Systemic and Infection-Site Exposure: A Physiologically Based Pharmacokinetic Model for Adult Patients with Pneumonia
Towards a Generic Tool for Prediction of Meropenem Systemic and Infection-Site Exposure: A Physiologically Based Pharmacokinetic Model for Adult Patients with Pneumonia Abstract Objective The objective of this study was to develop a physiologically based pharmacokinetic model for meropenem using a retrograde approach, ...
PMC7099768
core_pubmed_pmc
A positron emission tomography imaging study to confirm target engagement in the lungs of patients with idiopathic pulmonary fibrosis following a single dose of a novel inhaled αvβ6 integrin inhibitor
A positron emission tomography imaging study to confirm target engagement in the lungs of patients with idiopathic pulmonary fibrosis following a single dose of a novel inhaled αvβ6 integrin inhibitor Abstract Abstract Background Idiopathic pulmonary fibrosis (IPF) is a chronic, progressive lung disease with poor progn...
PMC12055767
core_pubmed_pmc
Comprehensive characterisation of the active ingredients of Smilax glabra Roxb based on chemical fingerprinting, metabolic fingerprinting and pharmacodynamic fingerprinting
Comprehensive characterisation of the active ingredients of Smilax glabra Roxb based on chemical fingerprinting, metabolic fingerprinting and pharmacodynamic fingerprinting Abstract Background Smilax glabra Roxb (SGR) is a traditional Chinese medicine known for its medicinal and edible properties, with a long history o...
PMC6780994
core_pubmed_pmc
Evaluation and use of an anti‐cynomolgus monkey CD79b surrogate antibody–drug conjugate to enable clinical development of polatuzumab vedotin
Evaluation and use of an anti‐cynomolgus monkey CD79b surrogate antibody–drug conjugate to enable clinical development of polatuzumab vedotin Abstract Abstract Background and Purpose Polatuzumab vedotin is an antibody–drug conjugate (ADC) being developed for non‐Hodgkin's lymphoma. It contains a humanized anti‐CD79b Ig...
PMC11243415
core_pubmed_pmc
The Impact of Chemical Modifications on the Interferon-Inducing and Antiproliferative Activity of Short Double-Stranded Immunostimulating RNA
The Impact of Chemical Modifications on the Interferon-Inducing and Antiproliferative Activity of Short Double-Stranded Immunostimulating RNA Abstract Abstract A short 19 bp dsRNA with 3′-trinucleotide overhangs acting as immunostimulating RNA (isRNA) demonstrated strong antiproliferative action against cancer cells, i...
PMC3946503
core_pubmed_pmc
Impact of the Smoothened Inhibitor, IPI-926, on Smoothened Ciliary Localization and Hedgehog Pathway Activity
Impact of the Smoothened Inhibitor, IPI-926, on Smoothened Ciliary Localization and Hedgehog Pathway Activity Abstract Abstract A requisite step for canonical Hedgehog (Hh) pathway activation by Sonic Hedgehog (Shh) ligand is accumulation of Smoothened (Smo) to the primary cilium (PC). Activation of the Hh pathway has ...
PMC4430595
core_pubmed_pmc
Pharmacokinetics of intravenous telavancin in healthy subjects with varying degrees of renal impairment
Pharmacokinetics of intravenous telavancin in healthy subjects with varying degrees of renal impairment Abstract Purpose We evaluated the effect of renal impairment (RI) on the pharmacokinetics of telavancin and hydroxypropylbetadex (excipient in the telavancin drug product). Methods Adults with normal, mild, moderate ...
PMC12699107
core_pubmed_pmc
Volume kinetics of lactated Ringer's solution in adult horses
Volume kinetics of lactated Ringer's solution in adult horses Abstract Abstract Background Fluid therapy in horses is primarily empirical. Evidence‐based quantification of the disposition of intravenous (IV) crystalloids used in clinical practice could enhance the effectiveness of fluid therapy. Objectives To determine...
PMC4156447
core_pubmed_pmc
Slow clearance of Plasmodium vivax with chloroquine amongst children younger than six months of age in the Brazilian Amazon
Slow clearance of Plasmodium vivax with chloroquine amongst children younger than six months of age in the Brazilian Amazon Abstract Abstract Plasmodium vivax is the most widespread parasite causing malaria, being especially prevalent in the Americas and Southeast Asia. Children are one of the most affected populations...
PMC3133529
core_pubmed_pmc
Pharmacokinetics of ligustrazine ethosome patch in rats and anti-myocardial ischemia and anti-ischemic reperfusion injury effect
Pharmacokinetics of ligustrazine ethosome patch in rats and anti-myocardial ischemia and anti-ischemic reperfusion injury effect Abstract The objective of this study was to investigate the pharmacokinetics of the ligustrazine ethosome patch and antimyocardial ischemia and anti-ischemic reperfusion injury effect. Male S...
PMC12406652
core_pubmed_pmc
Safety and pharmacokinetics of single and multiple doses of ledaborbactam etzadroxil with or without ceftibuten in healthy volunteers
Safety and pharmacokinetics of single and multiple doses of ledaborbactam etzadroxil with or without ceftibuten in healthy volunteers Abstract ABSTRACT Ledaborbactam etzadroxil (LED-E), a novel oral prodrug that converts to the active β-lactamase inhibitor (BLI) ledaborbactam (LED), is being developed in combination wi...
PMC6945443
core_pubmed_pmc
Safety, tolerability, and pharmacokinetics of repeated oral doses of 2-hydroxybenzylamine acetate in healthy volunteers: a double-blind, randomized, placebo-controlled clinical trial
Safety, tolerability, and pharmacokinetics of repeated oral doses of 2-hydroxybenzylamine acetate in healthy volunteers: a double-blind, randomized, placebo-controlled clinical trial Abstract Abstract Background 2-Hydroxybenzylamine (2-HOBA) is a selective dicarbonyl electrophile scavenger being developed as a nutritio...
PMC5908290
core_pubmed_pmc
Cisplatin liposome and 6-amino nicotinamide combination to overcome drug resistance in ovarian cancer cells
Cisplatin liposome and 6-amino nicotinamide combination to overcome drug resistance in ovarian cancer cells Abstract Ovarian cancer is an aggressive and lethal cancer usually treated by cytoreductive surgery followed by chemotherapy. Unfortunately, after an initial response, many patients relapse owing mainly to the de...
PMC7600512
core_pubmed_pmc
Kava as a Clinical Nutrient: Promises and Challenges
Kava as a Clinical Nutrient: Promises and Challenges Abstract Kava beverages are typically prepared from the root of Piper methysticum. They have been consumed among Pacific Islanders for centuries. Kava extract preparations were once used as herbal drugs to treat anxiety in Europe. Kava is also marketed as a dietary s...
PMC8349217
core_pubmed_pmc
LPS-Induced Inflammation Affects Midazolam Clearance in Juvenile Mice in an Age-Dependent Manner
LPS-Induced Inflammation Affects Midazolam Clearance in Juvenile Mice in an Age-Dependent Manner Abstract Purpose Inflammation has a significant impact on CYP3A activity. We hypothesized that this effect might be age dependent. Our objective was to conduct a population pharmacokinetic study of midazolam in mice at diff...
PMC8778670
core_pubmed_pmc
Identification of an Orally Bioavailable, Brain-Penetrant Compound with Selectivity for the Cannabinoid Type 2 Receptor
Identification of an Orally Bioavailable, Brain-Penetrant Compound with Selectivity for the Cannabinoid Type 2 Receptor Abstract Abstract Modulation of the endocannabinoid system (ECS) is of great interest for its therapeutic relevance in several pathophysiological processes. The CB2 subtype is largely localized to imm...
PMC12794297
core_pubmed_pmc
Impact of structure and formulation changes on the function of insulin products
Impact of structure and formulation changes on the function of insulin products Abstract Abstract Insulin has played an important role in the treatment of diabetes since its discovery in the early 1920s. Initially derived from animal sources, insulin production underwent significant changes with the advent of recombina...
PMC2906415
core_pubmed_pmc
The pharmacokinetic profile of a novel fixed-dose combination tablet of ibuprofen and paracetamol
The pharmacokinetic profile of a novel fixed-dose combination tablet of ibuprofen and paracetamol Abstract Abstract Background Ibuprofen and paracetamol differ in their mode of action and related therapeutic effects, suggesting that combined administration may offer improved analgesia. Reported here are the results of ...
PMC9290518
core_pubmed_pmc
Association Between Use of Pharmacokinetic‐Interacting Drugs and Effectiveness and Safety of Direct Acting Oral Anticoagulants: Nested Case‐Control Study
Association Between Use of Pharmacokinetic‐Interacting Drugs and Effectiveness and Safety of Direct Acting Oral Anticoagulants: Nested Case‐Control Study Abstract Concomitant use of direct oral anticoagulants (DOACs) and medications with inhibition/induction effect on P‐gp/CYP3A might increase risk of bleeding/treatmen...
PMC11859385
core_pubmed_pmc
Ustekinumab Drug Clearance Is Better Associated with Disease Control than Serum Trough Concentrations in a Prospective Cohort of Inflammatory Bowel Disease †
Ustekinumab Drug Clearance Is Better Associated with Disease Control than Serum Trough Concentrations in a Prospective Cohort of Inflammatory Bowel Disease † Abstract Background/Objectives : This study aimed to compare the association of ustekinumab (UST) drug clearance (CL) and trough drug concentrations with disease ...
PMC9865105
core_pubmed_pmc
A Mechanistic Pharmacodynamic Modeling Framework for the Assessment and Optimization of Proteolysis Targeting Chimeras (PROTACs)
A Mechanistic Pharmacodynamic Modeling Framework for the Assessment and Optimization of Proteolysis Targeting Chimeras (PROTACs) Abstract Abstract The field of targeted protein degradation is growing exponentially. Yet, there is an unmet need for pharmacokinetic/pharmacodynamic models that provide mechanistic insights,...
PMC5762213
core_pubmed_pmc
Simultaneous determination of four Sudan dyes in rat blood by UFLC–MS/MS and its application to a pharmacokinetic study in rats ☆
Simultaneous determination of four Sudan dyes in rat blood by UFLC–MS/MS and its application to a pharmacokinetic study in rats ☆ Abstract Abstract A rapid and sensitive method based on ultrafast liquid chromatography–tandem mass spectrometry was developed and validated for simultaneous determination of Sudan I, Sudan ...
PMC12064575
core_pubmed_pmc
Variability in Meropenem Distribution and Clearance in Children with Sepsis: Population-Based Pharmacokinetics with Assessment of Renal Biomarkers
Variability in Meropenem Distribution and Clearance in Children with Sepsis: Population-Based Pharmacokinetics with Assessment of Renal Biomarkers Abstract Abstract Background and Objective Meropenem dosing to achieve therapeutic exposure in critically ill children with sepsis is challenging due to a spectrum of renal ...
PMC8354861
core_pubmed_pmc
Potency and pharmacokinetics of GS-441524 derivatives against SARS-CoV-2
Potency and pharmacokinetics of GS-441524 derivatives against SARS-CoV-2 Abstract Abstract The nucleoside metabolite of remdesivir, GS-441524 displays potent anti-SARS-CoV-2 efficacy, and is being evaluated in clinical as an oral antiviral therapeutic for COVID-19. However, this nucleoside has a poor oral bioavailabili...
PMC7256114
core_pubmed_pmc
First‐in‐human clinical trial to assess the safety, tolerability and pharmacokinetics of P218, a novel candidate for malaria chemoprotection
First‐in‐human clinical trial to assess the safety, tolerability and pharmacokinetics of P218, a novel candidate for malaria chemoprotection Abstract Abstract Aims This first‐in‐human clinical trial of P218, a novel dihydrofolate reductase inhibitor antimalarial candidate, assessed safety, tolerability, pharmacokinetic...
PMC9010279
core_pubmed_pmc
The anti‐C5a antibody vilobelimab efficiently inhibits C5a in patients with severe COVID‐19
The anti‐C5a antibody vilobelimab efficiently inhibits C5a in patients with severe COVID‐19 Abstract Abstract Recently, we reported the phase II portion of the adaptive phase II/III PANAMO trial exploring potential benefit and safety of selectively blocking C5a with the monoclonal antibody vilobelimab (IFX‐1) in patien...
PMC12853142
core_pubmed_pmc
Population Physiologically‐Based Pharmacokinetic Modeling to Determine Ontogeny: A Quantitative Clinical Pharmacology Example in Pediatric Rare Disease
Population Physiologically‐Based Pharmacokinetic Modeling to Determine Ontogeny: A Quantitative Clinical Pharmacology Example in Pediatric Rare Disease Abstract ABSTRACT Pediatric physiologically‐based pharmacokinetic (PBPK) modelling plays an increasing role in selecting doses in children and addressing clinical pharm...
PMC11458656
core_pubmed_pmc
Model-informed dose optimization of mycophenolic acid in pediatric kidney transplant patients
Model-informed dose optimization of mycophenolic acid in pediatric kidney transplant patients Abstract Purpose We aimed to develop and evaluate a population PK model of mycophenolic acid (MPA) in pediatric kidney transplant patients to aid MPA dose optimization. Methods Data were collected from pediatric kidney transpl...
PMC7148462
core_pubmed_pmc
Population Pharmacokinetic Modeling and Pharmacodynamic Target Attainment Simulation of Piperacillin/Tazobactam for Dosing Optimization in Late Elderly Patients with Pneumonia
Population Pharmacokinetic Modeling and Pharmacodynamic Target Attainment Simulation of Piperacillin/Tazobactam for Dosing Optimization in Late Elderly Patients with Pneumonia Abstract Abstract The aim of this study was to develop a population pharmacokinetic model for piperacillin (PIPC)/tazobactam (TAZ) in late elder...
PMC7860071
core_pubmed_pmc
Preclinical Pharmacokinetic Interaction and Histopathological Analyses of Hedyotis diffusa on Sorafenib in Rats
Preclinical Pharmacokinetic Interaction and Histopathological Analyses of Hedyotis diffusa on Sorafenib in Rats Abstract Abstract Sorafenib is one of the most effective target therapeutic agents for patients with late-stage hepatocellular carcinoma. To seek possible alternative adjuvant agents to enhance the efficacy a...
PMC9283751
core_pubmed_pmc
Pharmacokinetics of apixaban and tacrolimus or cyclosporine in kidney and lung transplant recipients
Pharmacokinetics of apixaban and tacrolimus or cyclosporine in kidney and lung transplant recipients Abstract Abstract Apixaban is frequently used off‐label in transplant recipients. However, a potential drug interaction exists with the calcineurin inhibitors. We conducted an open‐label drug–drug interaction study to d...
PMC3356703
core_pubmed_pmc
Update on a Pharmacokinetic-Centric Alternative Tier II Program for MMT—Part II: Physiologically Based Pharmacokinetic Modeling and Manganese Risk Assessment
Update on a Pharmacokinetic-Centric Alternative Tier II Program for MMT—Part II: Physiologically Based Pharmacokinetic Modeling and Manganese Risk Assessment Abstract Recently, a variety of physiologically based pharmacokinetic (PBPK) models have been developed for the essential element manganese. This paper reviews th...
PMC5156571
core_pubmed_pmc
Voriconazole Composited Polyvinyl Alcohol/Hydroxypropyl-β-Cyclodextrin Nanofibers for Ophthalmic Delivery
Voriconazole Composited Polyvinyl Alcohol/Hydroxypropyl-β-Cyclodextrin Nanofibers for Ophthalmic Delivery Abstract Abstract Voriconazole (VRC) incorporated in composited polyvinyl alcohol (PVA)/hydroxypropyl-β-cyclodextrin (HPβCD) blended nanofibers were produced via electrospinning for efficient ophthalmic delivery. T...
PMC3230563
core_pubmed_pmc
Oral fondaparinux: use of lipid nanocapsules as nanocarriers and in vivo pharmacokinetic study
Oral fondaparinux: use of lipid nanocapsules as nanocarriers and in vivo pharmacokinetic study Abstract Abstract Oral anticoagulant therapy could be advanced using lipid-based nanoparticulate systems. This study examined lipid nanocapsules for their oral absorption potential as the first step in developing oral fondapa...