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PMC10928666
core_pubmed_pmc
Defining the pharmacokinetic/pharmacodynamic index of piperacillin/tazobactam within a hollow-fibre infection model to determine target attainment in intensive care patients
Defining the pharmacokinetic/pharmacodynamic index of piperacillin/tazobactam within a hollow-fibre infection model to determine target attainment in intensive care patients Abstract Abstract Background It is important to optimize dosing schemes of antibiotics to maximize the probability of therapeutic success. The rec...
PMC12285040
core_pubmed_pmc
Pharmacokinetic study of voriconazole administered orally at 50 mg/kg in nursehound sharks ( Scyliorhinus stellaris ) and udulate skates ( Raja undulata )
Pharmacokinetic study of voriconazole administered orally at 50 mg/kg in nursehound sharks ( Scyliorhinus stellaris ) and udulate skates ( Raja undulata ) Abstract Background Fungal diseases represent an ongoing problem for elasmobranchs kept under human care worldwide. When present, mycoses often lead to high mortalit...
PMC10674484
core_pubmed_pmc
A Spectroscopic and Molecular Dynamics Study on the Aggregation Properties of a Lipopeptide Analogue of Liraglutide, a Therapeutic Peptide against Diabetes Type 2
A Spectroscopic and Molecular Dynamics Study on the Aggregation Properties of a Lipopeptide Analogue of Liraglutide, a Therapeutic Peptide against Diabetes Type 2 Abstract The pharmacokinetics of peptide drugs are strongly affected by their aggregation properties and the morphology of the nanostructures they form in th...
PMC10652050
core_pubmed_pmc
Effects of Cross-linked Hyaluronic Acid in a Rat Model of Vestibular and Cochlear Toxicity
Effects of Cross-linked Hyaluronic Acid in a Rat Model of Vestibular and Cochlear Toxicity Abstract Objective: To investigate the effects of cross-linked hyaluronic acid (CLHA) in an experimental model of vestibulotoxicity and cochleotoxicity. Methods: Twenty-eight female Wistar albino rats (200–250 g) were divided int...
PMC6208487
core_pubmed_pmc
Pharmacokinetic and bioequivalence study comparing a fimasartan/rosuvastatin fixed-dose combination with the concomitant administration of fimasartan and rosuvastatin in healthy subjects
Pharmacokinetic and bioequivalence study comparing a fimasartan/rosuvastatin fixed-dose combination with the concomitant administration of fimasartan and rosuvastatin in healthy subjects Abstract Abstract Purpose A new fixed-dose combination (FDC) formulation of 120 mg fimasartan and 20 mg rosuvastatin was developed to...
PMC7419247
core_pubmed_pmc
Antimalarials as Antivirals for COVID-19: Believe it or Not!
Antimalarials as Antivirals for COVID-19: Believe it or Not! Abstract Abstract Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is a novel coronavirus responsible for the coronavirus disease -19 (COVID-19). Since December 2019, SARS-CoV-2 has infected millions of people worldwide, leaving hundreds of thousa...
PMC10233350
core_pubmed_pmc
Preclinical Profile of BYON3521 Predicts an Effective and Safe MET Antibody–Drug Conjugate
Preclinical Profile of BYON3521 Predicts an Effective and Safe MET Antibody–Drug Conjugate Abstract Abstract MET, the cell-surface receptor for the hepatocyte growth factor/scatter factor, which is widely overexpressed in various solid cancer types, is an attractive target for the development of antibody-based therapeu...
PMC12466686
core_pubmed_pmc
Impact of Obesity on Serum Concentrations of Vancomycin Administered as Continuous Infusion and on Clinical Outcomes in Critically Ill Patients—A Retrospective Observational Study
Impact of Obesity on Serum Concentrations of Vancomycin Administered as Continuous Infusion and on Clinical Outcomes in Critically Ill Patients—A Retrospective Observational Study Abstract Abstract Background/Objectives: Vancomycin is a commonly used antibiotic in critically ill patients with severe methicillin-resista...
PMC6066355
core_pubmed_pmc
Probing the binding site of novel selective positive allosteric modulators at the M 1 muscarinic acetylcholine receptor
Probing the binding site of novel selective positive allosteric modulators at the M 1 muscarinic acetylcholine receptor Abstract Subtype-selective allosteric modulation of the M 1 muscarinic acetylcholine (ACh) receptor (M 1 mAChR) is an attractive approach for the treatment of numerous disorders, including cognitive d...
PMC4562162
core_pubmed_pmc
Analysis of “On/Off” Kinetics of a CETP Inhibitor Using a Mechanistic Model of Lipoprotein Metabolism and Kinetics
Analysis of “On/Off” Kinetics of a CETP Inhibitor Using a Mechanistic Model of Lipoprotein Metabolism and Kinetics Abstract RG7232 is a potent inhibitor of cholesteryl-ester transfer protein (CETP). Daily oral administration of RG7232 produces a dose- and time-dependent increase in high-density lipoprotein-cholesterol ...
PMC10253699
core_pubmed_pmc
The Combination of a Human Biomimetic Liver Microphysiology System with BIOLOGXsym, a Quantitative Systems Toxicology (QST) Modeling Platform for Macromolecules, Provides Mechanistic Understanding of Tocilizumab- and GGF2-Induced Liver Injury
The Combination of a Human Biomimetic Liver Microphysiology System with BIOLOGXsym, a Quantitative Systems Toxicology (QST) Modeling Platform for Macromolecules, Provides Mechanistic Understanding of Tocilizumab- and GGF2-Induced Liver Injury Abstract Biologics address a range of unmet clinical needs, but the occurrenc...
PMC11064583
core_pubmed_pmc
First-in-human trial evaluating safety and pharmacokinetics of AT-752, a novel nucleotide prodrug with pan-serotype activity against dengue virus
First-in-human trial evaluating safety and pharmacokinetics of AT-752, a novel nucleotide prodrug with pan-serotype activity against dengue virus Abstract ABSTRACT AT-752 is a novel guanosine nucleotide prodrug inhibitor of the dengue virus (DENV) polymerase with sub-micromolar, pan-serotype antiviral activity. This ph...
PMC6151743
core_pubmed_pmc
Alterations in Pharmacokinetics of Gemcitabine and Erlotinib by Concurrent Administration of Hyangsayukgunja-Tang, a Gastroprotective Herbal Medicine
Alterations in Pharmacokinetics of Gemcitabine and Erlotinib by Concurrent Administration of Hyangsayukgunja-Tang, a Gastroprotective Herbal Medicine Abstract Abstract Gemcitabine and erlotinib are the chemotherapeutic agents used in the treatment of various cancers and their combination is being accepted as a first-li...
PMC11683174
core_pubmed_pmc
A Model‐Based Approach Supporting Abacavir/Dolutegravir/Lamivudine Fixed‐Dose Combination Approval in Children Living with HIV‐1
A Model‐Based Approach Supporting Abacavir/Dolutegravir/Lamivudine Fixed‐Dose Combination Approval in Children Living with HIV‐1 Abstract Abstract In March 2022, the US Food and Drug Administration expanded indications of TRIUMEQ, a once‐daily fixed‐dose combination (FDC) containing abacavir (ABC), dolutegravir (DTG), ...
PMC4644344
core_pubmed_pmc
Paracetamol pharmacokinetics and metabolism in young women
Paracetamol pharmacokinetics and metabolism in young women Abstract Abstract Background There is relevant between individual variability in paracetamol clearance in young women. In this pooled study, we focused on the population pharmacokinetic profile of intravenous paracetamol metabolism and its covariates in young w...
PMC11677246
core_pubmed_pmc
Vedolizumab Clearance as a Surrogate Marker for Remission in Inflammatory Bowel Disease Patients: Insights from Real-World Pharmacokinetics
Vedolizumab Clearance as a Surrogate Marker for Remission in Inflammatory Bowel Disease Patients: Insights from Real-World Pharmacokinetics Abstract Abstract Background/Objectives: Vedolizumab (VDZ) is approved in the treatment of patients with moderate to severe ulcerative colitis (UC) or Crohn’s disease (CD). VDZ exh...
PMC7459528
core_pubmed_pmc
Clinical Experience with High-Dose Polymyxin B against Carbapenem-Resistant Gram-Negative Bacterial Infections—A Cohort Study
Clinical Experience with High-Dose Polymyxin B against Carbapenem-Resistant Gram-Negative Bacterial Infections—A Cohort Study Abstract Population pharmacokinetic studies have suggested that high polymyxin B (PMB) doses (≥30,000 IU/kg/day) can improve bacterial kill in carbapenem-resistant Gram-negative bacteria (CR-GNB...
PMC4196769
core_pubmed_pmc
Simultaneous pharmacokinetic and pharmacodynamic analysis of 5α-reductase inhibitors and androgens by liquid chromatography tandem mass spectrometry
Simultaneous pharmacokinetic and pharmacodynamic analysis of 5α-reductase inhibitors and androgens by liquid chromatography tandem mass spectrometry Abstract Benign prostatic hyperplasia and prostate cancer can be treated with the 5α-reductase inhibitors, finasteride and dutasteride, when pharmacodynamic biomarkers are...
PMC3494447
core_pubmed_pmc
Phase I trial of axitinib combined with platinum doublets in patients with advanced non-small cell lung cancer and other solid tumours
Phase I trial of axitinib combined with platinum doublets in patients with advanced non-small cell lung cancer and other solid tumours Abstract Background: This phase I dose-finding trial evaluated safety, efficacy and pharmacokinetics of axitinib, a potent and selective second-generation inhibitor of vascular endothel...
PMC9592989
core_pubmed_pmc
Determination of (-)-epigallocatechin-3-gallate octaacetate and its metabolites in plasma of rats for pharmacokinetic study by ultra-performance-liquid-chromatography coupled to quadrupole-time-of-flight-mass-spectrometry
Determination of (-)-epigallocatechin-3-gallate octaacetate and its metabolites in plasma of rats for pharmacokinetic study by ultra-performance-liquid-chromatography coupled to quadrupole-time-of-flight-mass-spectrometry Abstract (-)-Epigallocatechin-gallate octaacetate (pro-EGCG), a prodrug of epigallocatechin-gallat...
PMC3060062
core_pubmed_pmc
Effects of Anti-VEGF on Predicted Antibody Biodistribution: Roles of Vascular Volume, Interstitial Volume, and Blood Flow
Effects of Anti-VEGF on Predicted Antibody Biodistribution: Roles of Vascular Volume, Interstitial Volume, and Blood Flow Abstract Abstract Background The identification of clinically meaningful and predictive models of disposition kinetics for cancer therapeutics is an ongoing pursuit in drug development. In particula...
PMC5318325
core_pubmed_pmc
Salvia (Sage): A Review of its Potential Cognitive-Enhancing and Protective Effects
Salvia (Sage): A Review of its Potential Cognitive-Enhancing and Protective Effects Abstract Abstract Genus Salvia , commonly known as sage, is the largest genus in the Lamiaceae family. It comprises many species traditionally used as brain-enhancing tonics. In vitro and animal studies have confirmed that several Salvi...
PMC12746526
core_pubmed_pmc
Clinical Implementation of Pharmacogenomics and Drug–Drug Interaction Screening in a German Academic Teaching Hospital and Outpatient Follow‐Up
Clinical Implementation of Pharmacogenomics and Drug–Drug Interaction Screening in a German Academic Teaching Hospital and Outpatient Follow‐Up Abstract Abstract Pharmacogenomics (PGx) helps to explain variability in drug response, including adverse drug reactions. Functional variants in genes affecting drug absorption...
PMC7511474
core_pubmed_pmc
A Phase 1, Randomised, Placebo-Controlled, Dose Escalation Study to Investigate the Safety, Tolerability and Pharmacokinetics of Cannabidiol in Fed Healthy Volunteers
A Phase 1, Randomised, Placebo-Controlled, Dose Escalation Study to Investigate the Safety, Tolerability and Pharmacokinetics of Cannabidiol in Fed Healthy Volunteers Abstract Abstract Background There is increasing interest in the use of purified cannabidiol (CBD) as a treatment for a wide range of conditions due to i...
PMC3383212
core_pubmed_pmc
Randomized, Crossover and Single-Dose Bioquivalence Study of Two Oral Desogestrel Formulations (Film-Coated Tablets of 75 μg) in Healthy Female Volunteers
Randomized, Crossover and Single-Dose Bioquivalence Study of Two Oral Desogestrel Formulations (Film-Coated Tablets of 75 μg) in Healthy Female Volunteers Abstract Despite the increase in the substitution of branded medicinal product with generic drugs, this is a controversial issue for some pharmacological groups (suc...
PMC5008228
core_pubmed_pmc
Nilotinib Effects in Parkinson’s disease and Dementia with Lewy bodies
Nilotinib Effects in Parkinson’s disease and Dementia with Lewy bodies Abstract Abstract Background : We evaluated the effects of low doses of the tyrosine kinase Abelson (Abl) inhibitor Nilotinib, on safety and pharmacokinetics in Parkinson’s disease dementia or dementia with Lewy bodies. Objectives : The primary outc...
PMC4602263
core_pubmed_pmc
Preclinical characterisation of the GM-CSF receptor as a therapeutic target in rheumatoid arthritis
Preclinical characterisation of the GM-CSF receptor as a therapeutic target in rheumatoid arthritis Abstract Abstract Objective Previous work has suggested that the granulocyte macrophage colony stimulating factor (GM-CSF)–GM-CSF receptor α axis (GM-CSFRα) may provide a new therapeutic target for the treatment of rheum...
PMC5214901
core_pubmed_pmc
Prediction of pharmacokinetics and drug-drug interaction potential using physiologically based pharmacokinetic (PBPK) modeling approach: A case study of caffeine and ciprofloxacin
Prediction of pharmacokinetics and drug-drug interaction potential using physiologically based pharmacokinetic (PBPK) modeling approach: A case study of caffeine and ciprofloxacin Abstract Abstract Over the last decade, physiologically based pharmacokinetics (PBPK) application has been extended significantly not only t...
PMC6698876
core_pubmed_pmc
Hydrophilic Auristatin Glycoside Payload Enables Improved Antibody-Drug Conjugate Efficacy and Biocompatibility
Hydrophilic Auristatin Glycoside Payload Enables Improved Antibody-Drug Conjugate Efficacy and Biocompatibility Abstract Abstract Antibody-drug conjugates (ADCs) offer a combination of antibody therapy and specific delivery of potent small-molecule payloads to target cells. The properties of the ADC molecule are determ...
PMC3828008
core_pubmed_pmc
Use of a Biomarker in Exposure–Response Analysis to Support Dose Selection for Fingolimod
Use of a Biomarker in Exposure–Response Analysis to Support Dose Selection for Fingolimod Abstract Abstract Fingolimod 0.5 mg q.d. (once daily) has been approved for the treatment of patients with relapsing and remitting forms of multiple sclerosis (RRMS). Fingolimod at two doses (0.5 and 1.25 mg) showed superior effec...
PMC7066278
core_pubmed_pmc
Clinical pharmacological study of dotinurad administered to male and female elderly or young subjects
Clinical pharmacological study of dotinurad administered to male and female elderly or young subjects Abstract Abstract Background Dotinurad is a novel selective urate reabsorption inhibitor (SURI) that selectively inhibits the reabsorption of uric acid in renal tubules and promotes the excretion of uric acid into urin...
PMC7524330
core_pubmed_pmc
Insights from pharmacokinetic models of host-microbiome drug metabolism
Insights from pharmacokinetic models of host-microbiome drug metabolism Abstract ABSTRACT Increasing evidence suggests a role of the gut microbiota in patients’ response to medicinal drugs. In our recent study, we combined genomics of human gut commensals and gnotobiotic animal experiments to quantify microbiota and ho...
PMC10565488
core_pubmed_pmc
Harder, better, faster, stronger? Retrospective chart review of adverse events of interactions between adaptogens and antidepressant drugs
Harder, better, faster, stronger? Retrospective chart review of adverse events of interactions between adaptogens and antidepressant drugs Abstract Aim: We aimed to systematically evaluate the prevalence and clinical characteristics of adverse events associated with the adaptogens and antidepressant drug interactions i...
PMC11191901
core_pubmed_pmc
Pharmacodynamic Effect of mTOR Inhibition-based Immunosuppressive Therapy on T- and B-cell Subsets After Renal Transplantation
Pharmacodynamic Effect of mTOR Inhibition-based Immunosuppressive Therapy on T- and B-cell Subsets After Renal Transplantation Abstract Background. The mammalian target of rapamycin inhibitor (mTORi) therapy after kidney transplantation is solely monitored pharmacokinetically, not necessarily reflecting PI3K-Akt-mTOR p...
PMC12579708
core_pubmed_pmc
Pharmacokinetic Bridging Between an Autoinjector and a Prefilled Syringe Following Subcutaneous Administration of Mirikizumab in Healthy Participants
Pharmacokinetic Bridging Between an Autoinjector and a Prefilled Syringe Following Subcutaneous Administration of Mirikizumab in Healthy Participants Abstract Abstract Introduction Mirikizumab, a humanized anti-interleukin-23p19 monoclonal antibody, is approved for the treatment of moderate-to-severe ulcerative colitis...
PMC11155669
core_pubmed_pmc
Mathematical modeling of endogenous and exogenously administered T cell recirculation in mouse and its application to pharmacokinetic studies of cell therapies
Mathematical modeling of endogenous and exogenously administered T cell recirculation in mouse and its application to pharmacokinetic studies of cell therapies Abstract Introduction In vivo T cell migration has been of interest to scientists for the past 60 years. T cell kinetics are important in the understanding of t...
PMC6938617
core_pubmed_pmc
A phase I/II study of epertinib plus trastuzumab with or without chemotherapy in patients with HER2-positive metastatic breast cancer
A phase I/II study of epertinib plus trastuzumab with or without chemotherapy in patients with HER2-positive metastatic breast cancer Abstract Abstract Background Epertinib (S-222611) is a potent reversible inhibitor of HER2, EGFR and HER4. This trial evaluated the safety, tolerability, pharmacokinetics and antitumour ...
PMC5655746
core_pubmed_pmc
Effect of Hepatic Impairment on Eluxadoline Pharmacokinetics
Effect of Hepatic Impairment on Eluxadoline Pharmacokinetics Methods Study Design Investigational review boards (Schulman Associates IRB, Sunrise, Florida, and Independent IRB, Inc, Plantation, Florida) approved the study protocol. All volunteers provided written, informed consent, which was reviewed and approved by th...
PMC12001262
core_pubmed_pmc
Comprehensive Parent‐Metabolite PBPK/PD Modeling Insights Into Methotrexate Personalized Dosing Strategies in Patients With Rheumatoid Arthritis
Comprehensive Parent‐Metabolite PBPK/PD Modeling Insights Into Methotrexate Personalized Dosing Strategies in Patients With Rheumatoid Arthritis Abstract ABSTRACT Rheumatoid arthritis (RA) is a major public health concern, which can cause serious outcomes. Low‐dose methotrexate (MTX) is a cornerstone in RA treatment, b...
PMC10349193
core_pubmed_pmc
Development of a PBPK model to quantitatively understand absorption and disposition mechanism and support future clinical trials for PB‐201
Development of a PBPK model to quantitatively understand absorption and disposition mechanism and support future clinical trials for PB‐201 Abstract Abstract PB‐201 is the second glucokinase activator in the world to enter the phase III clinical trials for the treatment of type 2 diabetes mellitus (T2DM). Combined with...
PMC8092503
core_pubmed_pmc
Population Pharmacokinetic and Pharmacokinetic/Pharmacodynamic Analyses of Cefiderocol, a Parenteral Siderophore Cephalosporin, in Patients with Pneumonia, Bloodstream Infection/Sepsis, or Complicated Urinary Tract Infection
Population Pharmacokinetic and Pharmacokinetic/Pharmacodynamic Analyses of Cefiderocol, a Parenteral Siderophore Cephalosporin, in Patients with Pneumonia, Bloodstream Infection/Sepsis, or Complicated Urinary Tract Infection Abstract Cefiderocol is a novel siderophore cephalosporin with antibacterial activity against G...
PMC11263075
core_pubmed_pmc
The atypical antipsychotics and sexual dysfunction: a pharmacovigilance-pharmacodynamic study
The atypical antipsychotics and sexual dysfunction: a pharmacovigilance-pharmacodynamic study Abstract Abstract Background Atypical antipsychotics (AAPs)-induced sexual dysfunction (SD) is a frequent issue in clinical practice, often underestimated by clinicians and not extensively researched. The current study aimed t...
PMC7587530
core_pubmed_pmc
Modeling of Chemoperfusion vs. Intravenous Administration of Cisplatin in Wistar Rats: Adsorption and Tissue Distribution
Modeling of Chemoperfusion vs. Intravenous Administration of Cisplatin in Wistar Rats: Adsorption and Tissue Distribution Abstract Abstract Hyperthermic intraperitoneal chemoperfusion (HIPEC) is an established form of locoregional chemotherapy of peritoneum tumors. However, its efficacy and safety status remain a contr...
PMC7842207
core_pubmed_pmc
Pharmacokinetics and pharmacodynamics of hydroxychloroquine in hospitalized patients with COVID-19
Pharmacokinetics and pharmacodynamics of hydroxychloroquine in hospitalized patients with COVID-19 Abstract Background Hydroxychloroquine (HCQ) dosage required to reach circulating levels that inhibit SARS-Cov-2 are extrapolated from pharmacokinetic data in non-COVID-19 patients. Methods We performed a population-pharm...
PMC4495062
core_pubmed_pmc
Pharmacokinetics of Active Components of Yokukansan, a Traditional Japanese Herbal Medicine after a Single Oral Administration to Healthy Japanese Volunteers: A Cross-Over, Randomized Study
Pharmacokinetics of Active Components of Yokukansan, a Traditional Japanese Herbal Medicine after a Single Oral Administration to Healthy Japanese Volunteers: A Cross-Over, Randomized Study Abstract Context Yokukansan (YKS) is a traditional Japanese herbal medicine called kampo medicine in Japan. Its extract comprises ...
PMC7284780
core_pubmed_pmc
Vascular Drug Delivery Using Carrier Red Blood Cells: Focus on RBC Surface Loading and Pharmacokinetics
Vascular Drug Delivery Using Carrier Red Blood Cells: Focus on RBC Surface Loading and Pharmacokinetics Abstract Abstract Red blood cells (RBC) have great potential as drug delivery systems, capable of producing unprecedented changes in pharmacokinetics, pharmacodynamics, and immunogenicity. Despite this great potentia...
PMC7833544
core_pubmed_pmc
Aerosol Inhalation Delivery of Triazavirin in Mice: Outlooks for Advanced Therapy Against Novel Viral Infections
Aerosol Inhalation Delivery of Triazavirin in Mice: Outlooks for Advanced Therapy Against Novel Viral Infections Abstract Abstract Under pandemic-caused emergency, evaluation of the potential of existing antiviral drugs for the treatment of COVID-19 is relevant. Triazavirin, an antiviral drug developed in Russia for pe...
PMC11169242
core_pubmed_pmc
Whole body physiology model to simulate respiratory depression of fentanyl and associated naloxone reversal
Whole body physiology model to simulate respiratory depression of fentanyl and associated naloxone reversal Abstract Abstract Background Opioid use in the United States and abroad is an endemic part of society with yearly increases in overdose rates and deaths. In response, the use of the safe and effective reversal ag...
PMC11728601
core_pubmed_pmc
LC-MS/MS-Based Concurrent Quantification of Cannabidiol and Melatonin in Mouse Plasma to Elucidate Complex PK Interactions
LC-MS/MS-Based Concurrent Quantification of Cannabidiol and Melatonin in Mouse Plasma to Elucidate Complex PK Interactions Abstract Objective: This study aimed to develop a quantitative analytical method for the simultaneous determination of cannabidiol (CBD) and melatonin (MT) in mouse plasma using the protein precipi...
PMC7222999
core_pubmed_pmc
Development of Population and Bayesian Models for Applied Use in Patients Receiving Cefepime
Development of Population and Bayesian Models for Applied Use in Patients Receiving Cefepime Abstract Abstract Background and Objective Understanding pharmacokinetic disposition of cefepime, a β-lactam antibiotic, is crucial for developing regimens to achieve optimal exposure and improved clinical outcomes. This study ...
PMC5874816
core_pubmed_pmc
Determination of Tangeretin in Rat Plasma: Assessment of Its Clearance and Absolute Oral Bioavailability
Determination of Tangeretin in Rat Plasma: Assessment of Its Clearance and Absolute Oral Bioavailability Abstract Abstract Tangeretin (TAN) is a dietary polymethoxylated flavone that possesses a broad scope of pharmacological activities. A simple high-performance liquid chromatography (HPLC) method was developed and va...
PMC6097164
core_pubmed_pmc
Sacubitril/valsartan: A novel angiotensin receptor-neprilysin inhibitor
Sacubitril/valsartan: A novel angiotensin receptor-neprilysin inhibitor Abstract Abstract Objective To describe the efficacy, superiority and safety profile of the first-in-class angiotensin receptor-neprilysin inhibitor “Sacubitril/Valsartan” as compared to angiotensin-converting enzyme inhibitors (ACEi) and angiotens...
PMC11678360
core_pubmed_pmc
Spanlastic Nano-Vesicles: A Novel Approach to Improve the Dissolution, Bioavailability, and Pharmacokinetic Behavior of Famotidine
Spanlastic Nano-Vesicles: A Novel Approach to Improve the Dissolution, Bioavailability, and Pharmacokinetic Behavior of Famotidine Abstract Abstract Background/Objectives : Drugs exhibiting poor aqueous solubility present a challenge to efficient delivery to the site of action. Spanlastics (a nano, surfactant-based dru...
PMC10046071
core_pubmed_pmc
Therapeutic Drug Monitoring in Oncohematological Patients: A Fast and Accurate HPLC-UV Method for the Quantification of Nilotinib in Human Plasma and Its Clinical Application
Therapeutic Drug Monitoring in Oncohematological Patients: A Fast and Accurate HPLC-UV Method for the Quantification of Nilotinib in Human Plasma and Its Clinical Application Abstract Nilotinib, a second-generation tyrosine kinase inhibitor, has demonstrated clinical activity in chronic myeloid leukemia. As an exposure...
PMC10669433
core_pubmed_pmc
Long-Term Suppressive Therapeutic-Drug-Monitoring-Guided Dalbavancin Therapy for Cardiovascular Prosthetic Infections
Long-Term Suppressive Therapeutic-Drug-Monitoring-Guided Dalbavancin Therapy for Cardiovascular Prosthetic Infections Abstract Dalbavancin represents a promising treatment for cardiovascular prosthetic infections due to its prolonged half-life, bactericidal activity, large spectrum of activity, and excellent biofilm pe...
PMC6454753
core_pubmed_pmc
Methods to account for uncertainties in exposure assessment in studies of environmental exposures
Methods to account for uncertainties in exposure assessment in studies of environmental exposures Abstract Background Accurate exposure estimation in environmental epidemiological studies is crucial for health risk assessment. Failure to account for uncertainties in exposure estimation could lead to biased results in e...
PMC4374761
core_pubmed_pmc
Pharmacokinetics and Metabolism of 4R-Cembranoid
Pharmacokinetics and Metabolism of 4R-Cembranoid Abstract Abstract 4R-cembranoid (4R) is a natural cyclic diterpenoid found in tobacco leaves that displays neuroprotective activity. 4R protects against NMDA, paraoxon (POX), and diisopropylfluorophosphate (DFP) damage in rat hippocampal slices and against DFP in rats in...
PMC9772593
core_pubmed_pmc
Clazakizumab for the treatment of chronic active antibody-mediated rejection (AMR) in kidney transplant recipients: Phase 3 IMAGINE study rationale and design
Clazakizumab for the treatment of chronic active antibody-mediated rejection (AMR) in kidney transplant recipients: Phase 3 IMAGINE study rationale and design Abstract Abstract Background Chronic active antibody-mediated rejection (AMR) is a major cause of graft loss with no approved drugs for its treatment. Currently,...
PMC11938029
core_pubmed_pmc
Determining the Multivalent Effects of d -Peptide-Based Radiotracers
Determining the Multivalent Effects of d -Peptide-Based Radiotracers Abstract Dextrorotary ( d ) peptides, composed of d -amino acids, are hyper-resistant to proteolytic hydrolysis, making them valuable ligands with excellent in vivo stability for radiopharmaceutical development. Multimerization is a well-established s...
PMC6161084
core_pubmed_pmc
Simultaneous Determination of Chlorogenic Acid Isomers and Metabolites in Rat Plasma Using LC-MS/MS and Its Application to A Pharmacokinetic Study Following Oral Administration of Stauntonia Hexaphylla Leaf Extract (YRA-1909) to Rats
Simultaneous Determination of Chlorogenic Acid Isomers and Metabolites in Rat Plasma Using LC-MS/MS and Its Application to A Pharmacokinetic Study Following Oral Administration of Stauntonia Hexaphylla Leaf Extract (YRA-1909) to Rats Abstract Abstract Stauntonia hexaphylla leaf extract (YRA-1909), which is widely used ...
PMC9315759
core_pubmed_pmc
Model Re-Estimation: An Alternative for Poor Predictive Performance during External Evaluations? Example of Gentamicin in Critically Ill Patients
Model Re-Estimation: An Alternative for Poor Predictive Performance during External Evaluations? Example of Gentamicin in Critically Ill Patients Abstract Abstract Background: An external evaluation is crucial before clinical applications; however, only a few gentamicin population pharmacokinetic (PopPK) models for cri...
PMC11179501
core_pubmed_pmc
Therapeutic strategies during cenobamate treatment initiation: Delphi panel recommendations
Therapeutic strategies during cenobamate treatment initiation: Delphi panel recommendations Abstract The goal of epilepsy treatment is seizure freedom, typically with antiseizure medication (ASM). If patients fail to attain seizure control despite two trials of appropriately chosen ASMs at adequate doses, they are clas...
PMC9095552
core_pubmed_pmc
Microdosing as a Potential Tool to Enhance Clinical Development of Novel Antibiotics: A Tissue and Plasma PK Feasibility Study with Ciprofloxacin
Microdosing as a Potential Tool to Enhance Clinical Development of Novel Antibiotics: A Tissue and Plasma PK Feasibility Study with Ciprofloxacin Abstract Abstract Background and Objective In microdose studies, drug pharmacokinetics is measured in humans after administration of subtherapeutic doses. While previous micr...
PMC11321260
core_pubmed_pmc
Rapid-Test Kit for Cardiac Troponin I: A Reliable Enzyme-Linked-Immuno-Substrate-Assay-Based Biosensor for Daily-Use Naked-Eye Detection and Pharmacokinetic Studies for Myocardial Infarction in Cardiovascular Disease
Rapid-Test Kit for Cardiac Troponin I: A Reliable Enzyme-Linked-Immuno-Substrate-Assay-Based Biosensor for Daily-Use Naked-Eye Detection and Pharmacokinetic Studies for Myocardial Infarction in Cardiovascular Disease Abstract Abstract Myocardial infarction (MI) is a severe cardiovascular event that can lead to death. C...
PMC7582154
core_pubmed_pmc
Population pharmacokinetics of levodopa gel infusion in Parkinson’s disease: effects of entacapone infusion and genetic polymorphism
Population pharmacokinetics of levodopa gel infusion in Parkinson’s disease: effects of entacapone infusion and genetic polymorphism Abstract Abstract Levodopa-entacapone-carbidopa intestinal gel (LECIG) provides continuous drug delivery through intrajejunal infusion. The aim of this study was to characterize the popul...
PMC10999626
core_pubmed_pmc
Kinetic modeling of the plasma pharmacokinetic profiles of ADAMTS13 fragment and its Fc-fusion counterpart in mice
Kinetic modeling of the plasma pharmacokinetic profiles of ADAMTS13 fragment and its Fc-fusion counterpart in mice Abstract Introduction: Fusion of the fragment crystallizable (Fc) to protein therapeutics is commonly used to extend the circulation time by enhancing neonatal Fc-receptor (FcRn)-mediated endosomal recycli...
PMC8738623
core_pubmed_pmc
An Integrated Pharmacokinetic–Pharmacodynamic–Pharmacoeconomic Modeling Method to Evaluate Treatments for Adults with Schizophrenia
An Integrated Pharmacokinetic–Pharmacodynamic–Pharmacoeconomic Modeling Method to Evaluate Treatments for Adults with Schizophrenia Abstract Introduction Schizophrenia is a chronic mental disorder that worsens with each relapse. Long-acting injectable (LAI) antipsychotics may prevent the exacerbation of symptoms and oc...
PMC8582029
core_pubmed_pmc
New Antagonists of the Membrane Androgen Receptor OXER1 from the ZINC Natural Product Database
New Antagonists of the Membrane Androgen Receptor OXER1 from the ZINC Natural Product Database Abstract Abstract OXER1 (oxoeicosanoid receptor 1) was deorphanized in 1993 and found to be the specific receptor for the arachidonic acid metabolite 5-oxo-ETE. Recently, we have reported that androgen binds to this receptor ...
PMC8998519
core_pubmed_pmc
Optimization and Validation of Dosage Regimen for Ceftiofur against Pasteurella multocida in Swine by Physiological Based Pharmacokinetic–Pharmacodynamic Model
Optimization and Validation of Dosage Regimen for Ceftiofur against Pasteurella multocida in Swine by Physiological Based Pharmacokinetic–Pharmacodynamic Model Abstract Model informed drug development is a valuable tool for drug development and clinical application due to its ability to integrate variability and uncert...
PMC4618643
core_pubmed_pmc
Randomized pharmacokinetic and drug–drug interaction studies of ceftazidime, avibactam, and metronidazole in healthy subjects
Randomized pharmacokinetic and drug–drug interaction studies of ceftazidime, avibactam, and metronidazole in healthy subjects Abstract We assessed pharmacokinetic and safety profiles of ceftazidime–avibactam administered ± metronidazole, and whether drug–drug interactions exist between ceftazidime and avibactam, or cef...
PMC10973044
core_pubmed_pmc
Mathematical modeling in autoimmune diseases: from theory to clinical application
Mathematical modeling in autoimmune diseases: from theory to clinical application Abstract Abstract The research & development (R&D) of novel therapeutic agents for the treatment of autoimmune diseases is challenged by highly complex pathogenesis and multiple etiologies of these conditions. The number of targeted thera...
PMC6516654
core_pubmed_pmc
Vancomycin pharmacokinetic model development in patients on intermittent online hemodiafiltration
Vancomycin pharmacokinetic model development in patients on intermittent online hemodiafiltration Abstract Background Vancomycin is frequently used in hemodialysis (HD) and in hemodiafiltration (HDF) patients and is usually administered in the last 30 or 60 minutes of a dialysis session. Vancomycin pharmacokinetics are...
PMC10144240
core_pubmed_pmc
Pharmacokinetic/Pharmacodynamic Analysis of Oral Calcium Fosfomycin: Are Urine Levels Sufficient to Ensure Efficacy for Urinary Tract Infections?
Pharmacokinetic/Pharmacodynamic Analysis of Oral Calcium Fosfomycin: Are Urine Levels Sufficient to Ensure Efficacy for Urinary Tract Infections? Abstract Urinary tract infections (UTIs) are extremely common and a major driver for the use of antimicrobials. Calcium fosfomycin is an old antibiotic indicated for the trea...
PMC9785946
core_pubmed_pmc
Bioorthogonal Chemistry Approach for the Theranostics of GRPR-Expressing Cancers
Bioorthogonal Chemistry Approach for the Theranostics of GRPR-Expressing Cancers Abstract Several gastrin-releasing peptide receptor (GRPR) antagonists with improved in vivo behavior have been recently developed and tested in the clinic. However, despite the generally mild side effects of peptide receptor radionuclide ...
PMC9698835
core_pubmed_pmc
Evaluation and Validation of the Limited Sampling Strategy of Polymyxin B in Patients with Multidrug-Resistant Gram-Negative Infection
Evaluation and Validation of the Limited Sampling Strategy of Polymyxin B in Patients with Multidrug-Resistant Gram-Negative Infection Abstract Abstract Polymyxin B (PMB) is the final option for treating multidrug-resistant Gram-negative bacterial infections. The acceptable pharmacokinetic/pharmacodynamic target is an ...
PMC5964640
core_pubmed_pmc
Pharmacological effects of N -[2-[[2-[2-[(2,6-dichlorophenyl)amino]phenyl]acetyl]oxy]ethyl]hyaluronamide (diclofenac Etalhyaluronate, SI-613), a novel sodium hyaluronate derivative chemically linked with diclofenac
Pharmacological effects of N -[2-[[2-[2-[(2,6-dichlorophenyl)amino]phenyl]acetyl]oxy]ethyl]hyaluronamide (diclofenac Etalhyaluronate, SI-613), a novel sodium hyaluronate derivative chemically linked with diclofenac Abstract Background Osteoarthritis (OA) is the most common joint disorder worldwide and one of the leadin...
PMC6017276
core_pubmed_pmc
A Sample and Sensitive HPLC-MS/MS Method for Simultaneous Determination of Ziyuglycoside I and Its Metabolite Ziyuglycoside II in Rat Pharmacokinetics
A Sample and Sensitive HPLC-MS/MS Method for Simultaneous Determination of Ziyuglycoside I and Its Metabolite Ziyuglycoside II in Rat Pharmacokinetics Abstract Abstract Ziyuglycoside I (ZGS1) is a promising drug candidate for the treatment of leucopenia. Currently, information on ZGS1 and its in vivo metabolite ziyugly...
PMC5116218
core_pubmed_pmc
Effects of continuous renal replacement therapy on linezolid pharmacokinetic/pharmacodynamics: a systematic review
Effects of continuous renal replacement therapy on linezolid pharmacokinetic/pharmacodynamics: a systematic review Abstract Background Major alterations in linezolid pharmacokinetic/pharmacodynamic (PK/PD) parameters might be expected in critically ill septic patients with acute kidney injury (AKI) who are undergoing c...
PMC4755158
core_pubmed_pmc
Evaluation of regional gastrointestinal absorption of edoxaban using the enterion capsule
Evaluation of regional gastrointestinal absorption of edoxaban using the enterion capsule Abstract Abstract Two studies in healthy subjects assessed the absorption of edoxaban when delivered to specific locations within the gastrointestinal tract using Enterion capsules. In study 1 (single‐dose, 4‐way crossover), 8 par...
PMC9069401
core_pubmed_pmc
Anthelmintics nitazoxanide protects against experimental hyperlipidemia and hepatic steatosis in hamsters and mice
Anthelmintics nitazoxanide protects against experimental hyperlipidemia and hepatic steatosis in hamsters and mice Abstract Abstract Lipid metabolism disorders contribute to hyperlipidemia and hepatic steatosis. It is ideal to develop drugs simultaneous improving both hyperlipidemia and hepatic steatosis. Nitazoxanide ...
PMC11566214
core_pubmed_pmc
Dose Optimization of Fluconazole After Initial Treatment Failure in Pulmonary Cryptococcosis in an Obese Patient with Type 2 Diabetes and Cirrhosis: A Case Report
Dose Optimization of Fluconazole After Initial Treatment Failure in Pulmonary Cryptococcosis in an Obese Patient with Type 2 Diabetes and Cirrhosis: A Case Report Abstract Abstract Background Pulmonary cryptococcosis is a fungal infection of the lungs, particularly challenging to treat in patients with multiple comorbi...
PMC12103360
core_pubmed_pmc
Preclinical pharmacokinetics and in vitro ADME properties of PAT-1102: a novel HDAC inhibitor for cancer therapy
Preclinical pharmacokinetics and in vitro ADME properties of PAT-1102: a novel HDAC inhibitor for cancer therapy Abstract Background Histone deacetylases (HDAC) are involved in chromatin remodelling, and histone deacetylases inhibitors have become the interest of research and shown promising antitumor effects against v...
PMC9290918
core_pubmed_pmc
Hyperhydration with cisplatin does not influence pemetrexed exposure
Hyperhydration with cisplatin does not influence pemetrexed exposure Abstract Abstract Pemetrexed is a cytotoxic drug for first‐line treatment of lung cancer. It is often combined with other anticancer drugs such as cisplatin or carboplatin. In clinical practice, hyperhydration regimens are applied to overcome cisplati...
PMC11359040
core_pubmed_pmc
Long-Circulating and Brain-Targeted Liposomes Loaded with Isoliquiritigenin: Formation, Characterization, Pharmacokinetics, and Distribution
Long-Circulating and Brain-Targeted Liposomes Loaded with Isoliquiritigenin: Formation, Characterization, Pharmacokinetics, and Distribution Abstract Isoliquiritigenin (ISL) has excellent neuroprotective effects. However, its limitations, including poor solubility, low bioavailability, and low accumulation in the brain...
PMC12511467
core_pubmed_pmc
Optimizing Polymyxin B Therapy in Critical Care: Pharmacokinetic Insights and Clinical Outcomes in a Retrospective Cohort Study
Optimizing Polymyxin B Therapy in Critical Care: Pharmacokinetic Insights and Clinical Outcomes in a Retrospective Cohort Study Abstract Abstract Introduction Carbapenem-resistant Gram-negative bacteria pose significant global health threats due to high infection rates and limited treatment options. Polymyxin B (PMB) h...
PMC9008396
core_pubmed_pmc
Molecular docking unveils the potential of andrographolide derivatives against COVID-19: an in silico approach
Molecular docking unveils the potential of andrographolide derivatives against COVID-19: an in silico approach Abstract Abstract Background The recent severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2) infection cause high mortality and there is an emergency need to develop a specific drug to treat the novel ...
PMC5297880
core_pubmed_pmc
Pharmacokinetic Interaction Between Isavuconazole and a Fixed‐Dose Combination of Lopinavir 400 mg/Ritonavir 100 mg in Healthy Subjects
Pharmacokinetic Interaction Between Isavuconazole and a Fixed‐Dose Combination of Lopinavir 400 mg/Ritonavir 100 mg in Healthy Subjects Abstract Abstract This phase 1, open‐label study evaluated the pharmacokinetic effects of coadministration of the antifungal agent, isavuconazole (administered as its water‐soluble pro...
PMC10895678
core_pubmed_pmc
Azetidines Kill Multidrug-Resistant Mycobacterium tuberculosis without Detectable Resistance by Blocking Mycolate Assembly
Azetidines Kill Multidrug-Resistant Mycobacterium tuberculosis without Detectable Resistance by Blocking Mycolate Assembly Abstract Tuberculosis (TB) is the leading cause of global morbidity and mortality resulting from infectious disease, with over 10.6 million new cases and 1.4 million deaths in 2021. This global eme...
PMC12270367
core_pubmed_pmc
Evaluation of Polar Substituted Schiff Bases and 1,2,3‐Triazole Hybrids as Anticancer Agents
Evaluation of Polar Substituted Schiff Bases and 1,2,3‐Triazole Hybrids as Anticancer Agents Abstract ABSTRACT Polar substituted Schiff bases and 1,2,3‐triazole hybrids ( 2 – 6 ) were successfully synthesized by Schiff base condensation reaction between the previously synthesized triazole 1 and series of polar substitu...
PMC10339078
core_pubmed_pmc
A Phase I Randomized Trial of Once‐Daily Versus Twice‐Daily Recombinant Human Parathyroid Hormone (1‐84) for Hypoparathyroidism
A Phase I Randomized Trial of Once‐Daily Versus Twice‐Daily Recombinant Human Parathyroid Hormone (1‐84) for Hypoparathyroidism Abstract ABSTRACT Recombinant human parathyroid hormone (1‐84), rhPTH(1‐84), is an approved adjunctive treatment to oral calcium and active vitamin D for adult patients with hypoparathyroidism...
PMC4701937
core_pubmed_pmc
The Human Experience with Intravenous Levodopa
The Human Experience with Intravenous Levodopa Abstract Objective: To compile a comprehensive summary of published human experience with levodopa given intravenously, with a focus on information required by regulatory agencies. Background: While safe intravenous (IV) use of levodopa has been documented for over 50 year...
PMC7003282
core_pubmed_pmc
The Effect of Grapefruit Juice on the Pharmacokinetics of Tadalafil in Rats
The Effect of Grapefruit Juice on the Pharmacokinetics of Tadalafil in Rats Abstract Abstract We developed and validated a novel, sensitive, selective, and inexpensive high-performance liquid chromatography (HPLC) method for the determination of tadalafil in rats plasma and to investigate the effect of grapefruit juice...
PMC5609896
core_pubmed_pmc
Preclinical testing of the glycogen synthase kinase-3β inhibitor tideglusib for rhabdomyosarcoma
Preclinical testing of the glycogen synthase kinase-3β inhibitor tideglusib for rhabdomyosarcoma Abstract Abstract Rhabdomyosarcoma (RMS) is the most common childhood soft tissue sarcoma. RMS often arise from myogenic precursors and displays a poorly differentiated skeletal muscle phenotype most closely resembling rege...
PMC8222533
core_pubmed_pmc
Pharmacokinetics and Immunogenicity of Frunevetmab in Osteoarthritic Cats Following Intravenous and Subcutaneous Administration
Pharmacokinetics and Immunogenicity of Frunevetmab in Osteoarthritic Cats Following Intravenous and Subcutaneous Administration Abstract Osteoarthritis and other degenerative joint diseases are common causes of chronic pain in cats. Frunevetmab is a felinized monoclonal antibody that binds to nerve growth factor (NGF) ...
PMC11849668
core_pubmed_pmc
A randomized, double-blind, Phase 1, single- and multiple-dose placebo-controlled study of the safety and pharmacokinetics of IN-006, an inhaled antibody treatment for COVID-19 in healthy volunteers
A randomized, double-blind, Phase 1, single- and multiple-dose placebo-controlled study of the safety and pharmacokinetics of IN-006, an inhaled antibody treatment for COVID-19 in healthy volunteers Abstract Summary Background Although COVID-19 is predominantly a respiratory tract infection, current antibody treatments...
PMC8739320
core_pubmed_pmc
Population pharmacokinetic and exposure–response analyses of elotuzumab plus pomalidomide and dexamethasone for relapsed and refractory multiple myeloma
Population pharmacokinetic and exposure–response analyses of elotuzumab plus pomalidomide and dexamethasone for relapsed and refractory multiple myeloma Abstract Purpose Elotuzumab plus pomalidomide/dexamethasone (E-Pd) demonstrated efficacy and safety in relapsed and refractory multiple myeloma (RRMM). The clinical ph...
PMC7952625
core_pubmed_pmc
Discovering Potential RNA Dependent RNA Polymerase Inhibitors as Prospective Drugs Against COVID-19: An in silico Approach
Discovering Potential RNA Dependent RNA Polymerase Inhibitors as Prospective Drugs Against COVID-19: An in silico Approach Abstract Abstract COVID-19, caused by Severe Acute Respiratory Syndrome Corona Virus 2, is declared a Global Pandemic by WHO in early 2020. In the present situation, though more than 180 vaccine ca...
PMC12182795
core_pubmed_pmc
Clinical relevance and methodological approach for the assessment of drug–drug interactions in cancer patients: a position statement from the Italian Association of Medical Oncology (AIOM) and the Italian Society of Pharmacology (SIF)
Clinical relevance and methodological approach for the assessment of drug–drug interactions in cancer patients: a position statement from the Italian Association of Medical Oncology (AIOM) and the Italian Society of Pharmacology (SIF) Abstract Abstract Background Drug–drug interactions (DDIs) are a critical challenge i...
PMC8241142
core_pubmed_pmc
Biomimetic synthesis of proline-derivative templated mesoporous silica for increasing the brain distribution of diazepam and improving the pharmacodynamics of nimesulide
Biomimetic synthesis of proline-derivative templated mesoporous silica for increasing the brain distribution of diazepam and improving the pharmacodynamics of nimesulide Abstract Abstract Herein a new kind of proline-derivative templated mesoporous silica with curved channels (CMS) was biomimetically synthesized and ap...
PMC12881174
core_pubmed_pmc
Platform Assessment of Concentration–QTc Relationship Across GalNAc–siRNA Molecules
Platform Assessment of Concentration–QTc Relationship Across GalNAc–siRNA Molecules Abstract Background GalNAc-conjugated short interfering RNAs (GalNAc–siRNAs) lack a biologically plausible mechanism for QT/QTc prolongation based on their unique physicochemical and absorption, distribution, metabolism, and excretion (...