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PMC7403243
core_pubmed_pmc
Pharmacokinetics of tigecycline in critically ill patients with liver failure defined by maximal liver function capacity test (LiMAx)
Pharmacokinetics of tigecycline in critically ill patients with liver failure defined by maximal liver function capacity test (LiMAx) Abstract Abstract Background In critically ill patients, tigecycline (TGC) remains an important therapeutic option due to its efficacy against multiresistant Gram-positive and Gram-negat...
PMC12961726
core_pubmed_pmc
Absolute Bioavailability and Absorption, Distribution, Metabolism, and Excretion of [ 14 C]Xevinapant, a Potent, Oral, Small‐Molecule IAP Inhibitor
Absolute Bioavailability and Absorption, Distribution, Metabolism, and Excretion of [ 14 C]Xevinapant, a Potent, Oral, Small‐Molecule IAP Inhibitor Abstract Abstract This Phase 1, open‐label, 2‐part, single‐dose study aimed to investigate the pharmacokinetics, metabolism, and excretion of xevinapant, a small molecule i...
PMC5988656
core_pubmed_pmc
Phase I studies of AZD1208, a proviral integration Moloney virus kinase inhibitor in solid and haematological cancers
Phase I studies of AZD1208, a proviral integration Moloney virus kinase inhibitor in solid and haematological cancers Abstract Abstract Background Proviral integration Moloney virus (PIM) kinases (PIM1, 2 and 3) are overexpressed in several tumour types and contribute to oncogenesis. AZD1208 is a potent ATP-competitive...
PMC3831742
core_pubmed_pmc
Enhanced tumor uptake, biodistribution and pharmacokinetics of etoposide loaded nanoparticles in Dalton's lymphoma tumor bearing mice
Enhanced tumor uptake, biodistribution and pharmacokinetics of etoposide loaded nanoparticles in Dalton's lymphoma tumor bearing mice Abstract Background: Nanotechnology plays a remarkable role in the field of the treatment of Lymphomas associated with tumor. Objective: The purpose of this study is to determine and to ...
PMC12055241
core_pubmed_pmc
Nutraceuticals Targeting Cannabinoid Receptor 1 and Transient Receptor Potential Vanilloid 1 for Pain Relief: A Computational Screening Approach
Nutraceuticals Targeting Cannabinoid Receptor 1 and Transient Receptor Potential Vanilloid 1 for Pain Relief: A Computational Screening Approach Abstract Abstract Objective: This study examined the binding affinities and therapeutic potential of natural products targeting pain-related receptors using molecular docking ...
PMC11893389
core_pubmed_pmc
Dose determination of VV116 in COVID-19 patients with severe liver dysfunction: a case report
Dose determination of VV116 in COVID-19 patients with severe liver dysfunction: a case report Abstract Abstract VV116 is an oral antiviral drug against SARS-CoV-2, known for its favorable efficacy and safety profile. But its application in patients with severe liver dysfunction has not been evaluated. Here, we report a...
PMC8538324
core_pubmed_pmc
Preparation and In Vitro/In Vivo Evaluation of Orally Disintegrating/Modified-Release Praziquantel Tablets
Preparation and In Vitro/In Vivo Evaluation of Orally Disintegrating/Modified-Release Praziquantel Tablets Abstract This study was designed to develop orally disintegrating/sustained-release praziquantel (PZQ) tablets using the hot-melt extrusion (HME) technique and direct compression, and subsequently evaluate their r...
PMC9372422
core_pubmed_pmc
An association study of ABCG2 rs2231142 on the concentrations of allopurinol and its metabolites
An association study of ABCG2 rs2231142 on the concentrations of allopurinol and its metabolites Abstract Abstract ABCG2 is a gene that codes for the human breast cancer resistance protein (BCRP). It is established that rs2231142 G>T, a single nucleotide polymorphism of the ABCG2 gene, is associated with gout and poor ...
PMC9538685
core_pubmed_pmc
Comparative assessment of viral dynamic models for SARS‐CoV‐2 for pharmacodynamic assessment in early treatment trials
Comparative assessment of viral dynamic models for SARS‐CoV‐2 for pharmacodynamic assessment in early treatment trials Abstract Pharmacometric analyses of time series viral load data may detect drug effects with greater power than approaches using single time points. Because SARS‐CoV‐2 viral load rapidly rises and then...
PMC9116664
core_pubmed_pmc
Factors affecting prolonged time to extubation in patients given remimazolam
Factors affecting prolonged time to extubation in patients given remimazolam Abstract Abstract Purpose To analyze the cause of prolonged recovery from general anesthesia with remimazolam. Methods We studied 65 patients under general anesthesia with remimazolam. According to time to extubation, patients were divided int...
PMC10311644
core_pubmed_pmc
Cannabidiol and cannabis-inspired terpene blends have acute prosocial effects in the BTBR mouse model of autism spectrum disorder
Cannabidiol and cannabis-inspired terpene blends have acute prosocial effects in the BTBR mouse model of autism spectrum disorder Abstract Abstract Introduction Cannabidiol (CBD) is a non-intoxicating phytocannabinoid with increasing popularity due to its purported therapeutic efficacy for numerous off-label conditions...
PMC3910012
core_pubmed_pmc
A Systems Pharmacology Perspective on the Clinical Development of Fatty Acid Amide Hydrolase Inhibitors for Pain
A Systems Pharmacology Perspective on the Clinical Development of Fatty Acid Amide Hydrolase Inhibitors for Pain Abstract Abstract The level of the endocannabinoid anandamide is controlled by fatty acid amide hydrolase (FAAH). In 2011, PF-04457845, an irreversible inhibitor of FAAH, was progressed to phase II clinical ...
PMC12391005
core_pubmed_pmc
Nano-enabled strategies for targeted immunotherapy in gastrointestinal cancers
Nano-enabled strategies for targeted immunotherapy in gastrointestinal cancers Abstract Abstract Gastrointestinal (GI) cancers remain a leading cause of global cancer morbidity and mortality, demanding novel therapeutic strategies that overcome existing limitations. Nanomedicine has recently emerged as a transformative...
PMC12214474
core_pubmed_pmc
A Systematic Review of SNPs Screening for Platinum-Related Pharmacodynamics and Pharmacokinetics Genes in Non-Small Cell Lung Cancer for Precision Medicine
A Systematic Review of SNPs Screening for Platinum-Related Pharmacodynamics and Pharmacokinetics Genes in Non-Small Cell Lung Cancer for Precision Medicine Abstract Introduction Traditional treatments for non-small cell lung cancer (NSCLC), such as chemotherapy, especially platinum-based regimens, often lack efficacy d...
PMC5826143
core_pubmed_pmc
Pharmacokinetics, Safety, and Tolerability of Cefiderocol, a Novel Siderophore Cephalosporin for Gram-Negative Bacteria, in Healthy Subjects
Pharmacokinetics, Safety, and Tolerability of Cefiderocol, a Novel Siderophore Cephalosporin for Gram-Negative Bacteria, in Healthy Subjects Abstract ABSTRACT Cefiderocol is a novel parenteral siderophore cephalosporin that shows potent efficacy against various Gram-negative bacteria, including carbapenem-resistant str...
PMC7004678
core_pubmed_pmc
Platelet inhibitory activity, tolerability, and safety of vicagrel, a novel thienopyridine P2Y12 inhibitor
Platelet inhibitory activity, tolerability, and safety of vicagrel, a novel thienopyridine P2Y12 inhibitor Abstract Abstract Vicagrel is a new antiplatelet pro-drug based on clopidogrel sulfur lactone metabolites. The purpose of the study was to evaluate the safety, tolerability, and pharmacodynamics (PD) of vicagrel i...
PMC7682210
core_pubmed_pmc
Gut-on-chip: Recreating human intestine in vitro
Gut-on-chip: Recreating human intestine in vitro Abstract Abstract The human gut is important for food digestion and absorption, as well as a venue for a large number of microorganisms that coexist with the host. Although numerous in vitro models have been proposed to study intestinal pathology or interactions between ...
PMC9652168
core_pubmed_pmc
Optimising the Nadroparin Dose for Thromboprophylaxis During Hemodialysis by Developing a Population Pharmacodynamic Model Using Anti-Xa Levels
Optimising the Nadroparin Dose for Thromboprophylaxis During Hemodialysis by Developing a Population Pharmacodynamic Model Using Anti-Xa Levels Abstract Abstract Introduction The optimal nadroparin dose in patients undergoing hemodialysis is difficult to determine in clinical practice. Anti-Xa levels ≥ 0.4 IU/mL and < ...
PMC4986685
core_pubmed_pmc
Pharmacokinetic and pharmacodynamic interactions between metformin and a novel dipeptidyl peptidase-4 inhibitor, evogliptin, in healthy subjects
Pharmacokinetic and pharmacodynamic interactions between metformin and a novel dipeptidyl peptidase-4 inhibitor, evogliptin, in healthy subjects Abstract Evogliptin is a newly developed dipeptidyl peptidase-4 (DPP-4) inhibitor, which is expected to be combined with metformin for treating type 2 diabetes mellitus. We in...
PMC8348688
core_pubmed_pmc
Application of Experimental Design Methodologies in the Enantioseparation of Pharmaceuticals by Capillary Electrophoresis: A Review
Application of Experimental Design Methodologies in the Enantioseparation of Pharmaceuticals by Capillary Electrophoresis: A Review Abstract Abstract Chirality is one of the major issues in pharmaceutical research and industry. Capillary electrophoresis (CE) is an interesting alternative to the more frequently used chr...
PMC7577020
core_pubmed_pmc
Development of a Pharmacokinetic Model Describing Neonatal Fc Receptor‐Mediated Recycling of HL2351, a Novel Hybrid Fc‐Fused Interleukin‐1 Receptor Antagonist, to Optimize Dosage Regimen
Development of a Pharmacokinetic Model Describing Neonatal Fc Receptor‐Mediated Recycling of HL2351, a Novel Hybrid Fc‐Fused Interleukin‐1 Receptor Antagonist, to Optimize Dosage Regimen Abstract HL2351 (hIL‐1Ra‐hyFc) is a novel recombinant protein formed by the fusion of two human interleukin‐1 receptor antagonist com...
PMC12619860
core_pubmed_pmc
Quantitative Evaluation of Nemolizumab Pharmacokinetics and Efficacy in Prurigo Nodularis: A Population Pharmacokinetics and Model-Based Meta-analysis Approach
Quantitative Evaluation of Nemolizumab Pharmacokinetics and Efficacy in Prurigo Nodularis: A Population Pharmacokinetics and Model-Based Meta-analysis Approach Abstract Abstract Introduction Nemolizumab is a humanized monoclonal antibody targeting interleukin-31 receptor A. It has shown efficacy in treating patients wi...
PMC3828003
core_pubmed_pmc
Quantitative assessment of minimal effective concentration of erythropoiesis-stimulating agents
Quantitative assessment of minimal effective concentration of erythropoiesis-stimulating agents Abstract Abstract Minimal effective concentration (MEC) was proposed to explain why subcutaneous (SC) administration of erythropoietin (EPO) induces a higher hemoglobin (HGB) increase than intravenous (IV) administration. It...
PMC11388511
core_pubmed_pmc
Recent advances in Scutellariae radix : A comprehensive review on ethnobotanical uses, processing, phytochemistry, pharmacological effects, quality control and influence factors of biosynthesis
Recent advances in Scutellariae radix : A comprehensive review on ethnobotanical uses, processing, phytochemistry, pharmacological effects, quality control and influence factors of biosynthesis Abstract Background Scutellariae radix (SR) is the dried root of Scutellaria baicalensis Georgi. It has a long history of ethn...
PMC8510464
core_pubmed_pmc
Optimization of Hyaluronate-Based Liposomes to Augment the Oral Delivery and the Bioavailability of Berberine
Optimization of Hyaluronate-Based Liposomes to Augment the Oral Delivery and the Bioavailability of Berberine Abstract Various perspectives had been utilized to enhance the poor intestinal permeability and bioavailability of drugs with low water solubility. Berberine (Brb) is a unique molecule that possesses multiple t...
PMC10373654
core_pubmed_pmc
Targeted Nanocarriers Co-Opting Pulmonary Intravascular Leukocytes for Drug Delivery to the Injured Brain
Targeted Nanocarriers Co-Opting Pulmonary Intravascular Leukocytes for Drug Delivery to the Injured Brain Abstract Abstract Ex vivo -loaded white blood cells (WBC) can transfer cargo to pathological foci in the central nervous system (CNS). Here we tested affinity ligand driven in vivo loading of WBC in order to bypass...
PMC12001255
core_pubmed_pmc
Population Pharmacokinetics and Pharmacodynamics of Sotalol Following Expedited Intravenous Loading in Patients With Atrial Arrhythmias
Population Pharmacokinetics and Pharmacodynamics of Sotalol Following Expedited Intravenous Loading in Patients With Atrial Arrhythmias Abstract ABSTRACT Sotalol, a class III antiarrhythmic agent, is used to maintain sinus rhythm in patients with atrial fibrillation or atrial flutter (AFIB/AFL). Despite its efficacy, s...
PMC5884649
core_pubmed_pmc
Grape seed procyanidin extract against lung cancer: the role of microrna-106b, bioavailability, and bioactivity
Grape seed procyanidin extract against lung cancer: the role of microrna-106b, bioavailability, and bioactivity Abstract Abstract MiR-106b is an oncomir and a potential target for anti-cancer therapy. We hypothesize that grape seed procyanidin extract (GSE) exerts antineoplastic effects on lung cancer through modulatio...
PMC12551005
core_pubmed_pmc
Impact of Sampling Strategy and Population Model on Bayesian Estimates of Vancomycin AUC in Patients with BMI > 40 kg/m 2 : A Single-Center Retrospective Study
Impact of Sampling Strategy and Population Model on Bayesian Estimates of Vancomycin AUC in Patients with BMI > 40 kg/m 2 : A Single-Center Retrospective Study Abstract Background/Objectives : Growing evidence supports the use of a single trough concentration, rather than both a peak and trough, to estimate the 24 h ar...
PMC4532868
core_pubmed_pmc
Beneficial Effects of the mTOR Inhibitor Everolimus in Patients with Advanced Medullary Thyroid Carcinoma: Subgroup Results of a Phase II Trial
Beneficial Effects of the mTOR Inhibitor Everolimus in Patients with Advanced Medullary Thyroid Carcinoma: Subgroup Results of a Phase II Trial Abstract Objective . Until recently, advanced medullary thyroid cancer (MTC) had few treatment options except surgery. The mTOR inhibitor everolimus has shown encouraging resul...
PMC7839014
core_pubmed_pmc
Interspecies Scaling of Antibody–Drug Conjugates (ADC) for the Prediction of Human Clearance
Interspecies Scaling of Antibody–Drug Conjugates (ADC) for the Prediction of Human Clearance Abstract Abstract Allometric scaling is a useful tool for the extrapolation of pharmacokinetic parameters from animals to humans. The objective of this study was to predict human clearance of antibody–drug conjugates (ADC) allo...
PMC4283607
core_pubmed_pmc
Prediction of the Pharmacokinetics, Pharmacodynamics, and Efficacy of a Monoclonal Antibody, Using a Physiologically Based Pharmacokinetic FcRn Model
Prediction of the Pharmacokinetics, Pharmacodynamics, and Efficacy of a Monoclonal Antibody, Using a Physiologically Based Pharmacokinetic FcRn Model Abstract Abstract Although advantages of physiologically based pharmacokinetic models (PBPK) are now well established, PBPK models that are linked to pharmacodynamic (PD)...
PMC10150366
core_pubmed_pmc
Discovery of an In Vivo Chemical Probe for BCL6 Inhibition by Optimization of Tricyclic Quinolinones
Discovery of an In Vivo Chemical Probe for BCL6 Inhibition by Optimization of Tricyclic Quinolinones Abstract B-cell lymphoma 6 (BCL6) is a transcriptional repressor and oncogenic driver of diffuse large B-cell lymphoma (DLBCL). Here, we report the optimization of our previously reported tricyclic quinolinone series fo...
PMC10035397
core_pubmed_pmc
Clinical Pharmacology and Determinants of Response to UCART19, an Allogeneic Anti-CD19 CAR-T Cell Product, in Adult B-cell Acute Lymphoblastic Leukemia
Clinical Pharmacology and Determinants of Response to UCART19, an Allogeneic Anti-CD19 CAR-T Cell Product, in Adult B-cell Acute Lymphoblastic Leukemia Abstract Abstract Background: UCART19 1 is an “off-the-shelf” genome-edited anti-CD19 chimeric antigen receptor (CAR)-T cell product, manufactured from unrelated health...
PMC10368397
core_pubmed_pmc
A single-arm study design with non-inferiority and superiority time-to-event endpoints: a tool for proof-of-concept and de-intensification strategies in breast cancer
A single-arm study design with non-inferiority and superiority time-to-event endpoints: a tool for proof-of-concept and de-intensification strategies in breast cancer Abstract Abstract De-escalation trials in oncology evaluate therapies that aim to improve the quality of life of patients with low-risk cancer by avoidin...
PMC9025904
core_pubmed_pmc
Application of In Vivo Imaging Techniques and Diagnostic Tools in Oral Drug Delivery Research
Application of In Vivo Imaging Techniques and Diagnostic Tools in Oral Drug Delivery Research Abstract Abstract Drug absorption following oral administration is determined by complex and dynamic interactions between gastrointestinal (GI) physiology, the drug, and its formulation. Since many of these interactions are no...
PMC12313456
core_pubmed_pmc
Establishment and validation of downsized hollow-fibre infection model and pharmacokinetics/pharmacodynamics analysis of VAN on Enterococcus faecium
Establishment and validation of downsized hollow-fibre infection model and pharmacokinetics/pharmacodynamics analysis of VAN on Enterococcus faecium Abstract Abstract Objectives This study clarified the target values of VAN against Enterococcus faecium using pharmacokinetics/pharmacodynamics (PK/PD) analysis and compar...
PMC8235681
core_pubmed_pmc
Formulation of Chewable Tablets Containing Carbamazepine-β-cyclodextrin Inclusion Complex and F-Melt Disintegration Excipient. The Mathematical Modeling of the Release Kinetics of Carbamazepine
Formulation of Chewable Tablets Containing Carbamazepine-β-cyclodextrin Inclusion Complex and F-Melt Disintegration Excipient. The Mathematical Modeling of the Release Kinetics of Carbamazepine Abstract Due to its low solubility, carbamazepine (CBZ) exhibits slow and incomplete release in the gastrointestinal tract and...
PMC10853758
core_pubmed_pmc
Assessment of the effects of amphiphilic poly (N‑vinylpyrrolidone) nanoparticles loaded with bortezomib on glioblastoma cell lines and zebrafish embryos
Assessment of the effects of amphiphilic poly (N‑vinylpyrrolidone) nanoparticles loaded with bortezomib on glioblastoma cell lines and zebrafish embryos Abstract Abstract Proteasome inhibitor bortezomib is an anticancer agent approved for treatment of multiple myeloma and mantle cell lymphoma. However, its application ...
PMC11739748
core_pubmed_pmc
French‐Speaking Network of Pharmacogenetics ( RNPGx ) Recommendations for Clinical Use of Mavacamten
French‐Speaking Network of Pharmacogenetics ( RNPGx ) Recommendations for Clinical Use of Mavacamten Abstract Mavacamten, the first drug in the class of β‐cardiac myosin modulator, is used for the treatment of patients with hypertrophic cardiomyopathy. This orally administered drug demonstrates wide interpatient variab...
PMC12863268
core_pubmed_pmc
Bictegravir concentrations in breastmilk of healthy, lactating women without HIV
Bictegravir concentrations in breastmilk of healthy, lactating women without HIV Abstract Abstract Introduction Risk of transmission of HIV through breastfeeding is minimal in case of maternal viral suppression due to antiretroviral therapy. However, to what extent antiretroviral drugs transfer into breastmilk is not f...
PMC10610255
core_pubmed_pmc
Predictive Potential of C max Bioequivalence in Pilot Bioavailability/Bioequivalence Studies, through the Alternative ƒ 2 Similarity Factor Method
Predictive Potential of C max Bioequivalence in Pilot Bioavailability/Bioequivalence Studies, through the Alternative ƒ 2 Similarity Factor Method Abstract Abstract Pilot bioavailability/bioequivalence (BA/BE) studies are downsized trials that can be conducted prior to the definitive pivotal trial. In these trials, 12 ...
PMC9495775
core_pubmed_pmc
Nanocarrier System: State-of-the-Art in Oral Delivery of Astaxanthin
Nanocarrier System: State-of-the-Art in Oral Delivery of Astaxanthin Abstract Abstract Astaxanthin (3,3′-dihydroxy-4,4′-diketo-β-β carotene), which belongs to the xanthophyll class, has shown potential biological activity in in vitro and in vivo models including as a potent antioxidant, anti-lipid peroxidation and card...
PMC9907514
core_pubmed_pmc
Pharmacokinetic-Pharmacodynamic Determinants of Clinical Outcomes for Rifampin-Resistant Tuberculosis: A Multisite Prospective Cohort Study
Pharmacokinetic-Pharmacodynamic Determinants of Clinical Outcomes for Rifampin-Resistant Tuberculosis: A Multisite Prospective Cohort Study Abstract Abstract Background Rifampin-resistant and/or multidrug-resistant tuberculosis (RR/MDR-TB) treatment requires multiple drugs, and outcomes remain suboptimal. Some drugs ar...
PMC9314311
core_pubmed_pmc
Applications of Model-Based Meta-Analysis in Drug Development
Applications of Model-Based Meta-Analysis in Drug Development Abstract Abstract Model-based meta-analysis (MBMA) is a quantitative approach that leverages published summary data along with internal data and can be applied to inform key drug development decisions, including the benefit-risk assessment of a treatment und...
PMC10959350
core_pubmed_pmc
Synthesis, molecular docking analysis, molecular dynamic simulation, ADMET, DFT, and drug likeness studies: Novel Indeno[1,2- b ]pyrrol-4(1 H )-one as SARS-CoV-2 main protease inhibitors
Synthesis, molecular docking analysis, molecular dynamic simulation, ADMET, DFT, and drug likeness studies: Novel Indeno[1,2- b ]pyrrol-4(1 H )-one as SARS-CoV-2 main protease inhibitors Abstract Abstract Background The COVID-19 pandemic began in 2019 as a result of the advent of a novel coronavirus, SARS-CoV-2. At pre...
PMC6609328
core_pubmed_pmc
Preparation, characterization, and pharmacodynamics of insulin-loaded fumaryl diketopiperazine microparticle dry powder inhalation
Preparation, characterization, and pharmacodynamics of insulin-loaded fumaryl diketopiperazine microparticle dry powder inhalation Abstract Abstract Purpose: With the increase of population aging and the proportion of overweight and obese, a growing number of people are suffering from diabetes. Insulin (INS) as the mos...
PMC12242390
core_pubmed_pmc
Web-based automated therapeutic drug monitoring application for precision medicine in tuberculosis management
Web-based automated therapeutic drug monitoring application for precision medicine in tuberculosis management Abstract Abstract Tuberculosis (TB) remains one of the leading causes of infectious disease-related deaths worldwide. Model-informed precision dosing-based therapeutic drug monitoring (TDM) is a promising strat...
PMC9780949
core_pubmed_pmc
Agmatine Administration Effects on Equine Gastric Ulceration and Lameness
Agmatine Administration Effects on Equine Gastric Ulceration and Lameness Abstract Osteoarthritis (OA) accounts for up to 60% of equine lameness. Agmatine, a decarboxylated arginine, may be a viable option for OA management, based on reports of its analgesic properties. Six adult thoroughbred horses, with lameness attr...
PMC5756253
core_pubmed_pmc
Florfenicol pharmacokinetics following intravenous and oral administrations and its elimination after oral and bath administrations in common carp (Cyprinus carpio)
Florfenicol pharmacokinetics following intravenous and oral administrations and its elimination after oral and bath administrations in common carp (Cyprinus carpio) Abstract The aim of this study was to evaluate pharmacokinetic profiles of florfenicol after a single dose of intravenous (5.00 mg kg -1 body weight) and o...
PMC7811375
core_pubmed_pmc
Preparation and Characterization of Tacrolimus-Loaded SLNs in situ Gel for Ocular Drug Delivery for the Treatment of Immune Conjunctivitis
Preparation and Characterization of Tacrolimus-Loaded SLNs in situ Gel for Ocular Drug Delivery for the Treatment of Immune Conjunctivitis Abstract Abstract Background The aim of this study is to develop a novel in situ gel of tacrolimus-loaded SLNs (solid lipid nanoparticles) for ocular drug delivery. Methods The opti...
PMC12303425
core_pubmed_pmc
A bibliometric analysis of the published studies in ciprofol research
A bibliometric analysis of the published studies in ciprofol research Abstract Objective: Ciprofol (HSK-3486), a novel intravenous anesthetic with structural similarities to propofol, has shown promising pharmacokinetic (PK) and pharmacodynamic (PD) profiles; however, clinical data regarding its efficacy and safety rem...
PMC6941357
core_pubmed_pmc
An in vitro toolbox to accelerate anti-malarial drug discovery and development
An in vitro toolbox to accelerate anti-malarial drug discovery and development Abstract Abstract Background Modelling and simulation are being increasingly utilized to support the discovery and development of new anti-malarial drugs. These approaches require reliable in vitro data for physicochemical properties, permea...
PMC5735248
core_pubmed_pmc
The Evaluation of Pharmacodynamics and Pharmacokinetics of Anti-thrombin DNA Aptamer RA-36
The Evaluation of Pharmacodynamics and Pharmacokinetics of Anti-thrombin DNA Aptamer RA-36 Abstract Abstract Anticoagulants are a vital class of drugs, which are applied for short-term surgical procedures, and for long-term treatments for thrombosis prevention in high risk groups. Several anticoagulant drugs are commer...
PMC9653025
core_pubmed_pmc
Comparative Pharmacokinetics and Safety of Imrecoxib, a Novel Selective Cyclooxygenase-2 Inhibitor, in Elderly Healthy Subjects
Comparative Pharmacokinetics and Safety of Imrecoxib, a Novel Selective Cyclooxygenase-2 Inhibitor, in Elderly Healthy Subjects Abstract Background Imrecoxib is a novel and moderately selective cyclooxygenase-2 inhibitor with properties of anti-inflammation and alleviating pain, which is widely applied in osteoarthriti...
PMC7927141
core_pubmed_pmc
In Vitro and In Vivo Studies on HPMA-Based Polymeric Micelles Loaded with Curcumin
In Vitro and In Vivo Studies on HPMA-Based Polymeric Micelles Loaded with Curcumin Abstract Abstract Curcumin-loaded polymeric micelles composed of poly(ethylene glycol)- b -poly( N -2-benzoyloxypropyl methacrylamide) (mPEG- b -p(HPMA-Bz)) were prepared to solubilize and improve the pharmacokinetics of curcumin. Curcum...
PMC9440320
core_pubmed_pmc
Pharmacokinetics of Oral Rebaudioside A in Patients with Type 2 Diabetes Mellitus and Its Effects on Glucose Homeostasis: A Placebo-Controlled Crossover Trial
Pharmacokinetics of Oral Rebaudioside A in Patients with Type 2 Diabetes Mellitus and Its Effects on Glucose Homeostasis: A Placebo-Controlled Crossover Trial Abstract Abstract Background and Objectives Rebaudioside A, a steviol glycoside, is deglycosylated by intestinal microflora prior to the absorption of steviol an...
PMC11563007
core_pubmed_pmc
Ocular Pharmacokinetics of Faricimab Following Intravitreal Administration in Patients With Retinal Disease
Ocular Pharmacokinetics of Faricimab Following Intravitreal Administration in Patients With Retinal Disease Abstract Abstract Purpose To characterize faricimab ocular and systemic pharmacokinetics (PK) in patients with neovascular age-related macular degeneration (nAMD) or diabetic macular edema (DME) and to assess the...
PMC10719471
core_pubmed_pmc
Dose selection for biological enzyme replacement therapy indicated for inborn errors of metabolism
Dose selection for biological enzyme replacement therapy indicated for inborn errors of metabolism Abstract Abstract This paper summarizes key features of the dose‐finding strategies used in the development of 11 approved new molecular entities that are first‐in‐class enzyme replacement therapy (ERT), with a goal to ga...
PMC6373189
core_pubmed_pmc
Exposure–response relationship of olaratumab for survival outcomes and safety when combined with doxorubicin in patients with soft tissue sarcoma
Exposure–response relationship of olaratumab for survival outcomes and safety when combined with doxorubicin in patients with soft tissue sarcoma Abstract Abstract Purpose Olaratumab is a recombinant human IgG1 monoclonal antibody against PGDFRα. Olaratumab plus doxorubicin improved survivalversus doxorubicin in an ope...
PMC11083769
core_pubmed_pmc
Characterization and pharmacokinetics of cinnamon and star anise compound essential oil pellets prepared via centrifugal granulation technology
Characterization and pharmacokinetics of cinnamon and star anise compound essential oil pellets prepared via centrifugal granulation technology Abstract Cinnamon and star anise essential oils are extracted from natural plants and provide a theoretical basis for the development and clinical application of compound essen...
PMC3797132
core_pubmed_pmc
SLCO1B1 and SLC19A1 Gene Variants and Irinotecan-Induced Rapid Response and Survival: A Prospective Multicenter Pharmacogenetics Study of Metastatic Colorectal Cancer
SLCO1B1 and SLC19A1 Gene Variants and Irinotecan-Induced Rapid Response and Survival: A Prospective Multicenter Pharmacogenetics Study of Metastatic Colorectal Cancer Abstract Abstract Background Rapid response to chemotherapy in metastatic colorectal cancer (mCRC) patients (response within 12 weeks of chemotherapy) ma...
PMC7018138
core_pubmed_pmc
Safety and effectiveness of a novel neuroprotectant, KUS121, in patients with non-arteritic central retinal artery occlusion: An open-label, non-randomized, first-in-humans, phase 1/2 trial
Safety and effectiveness of a novel neuroprotectant, KUS121, in patients with non-arteritic central retinal artery occlusion: An open-label, non-randomized, first-in-humans, phase 1/2 trial Abstract Kyoto University Substance (KUS) 121, an ATPase inhibitor of valosin-containing protein, is a novel neuroprotectant. We t...
PMC7126458
core_pubmed_pmc
Development of an SPE–HPLC–MS method for simultaneous determination and pharmacokinetic study of bioactive constituents of Yu Ping Feng San in rat plasma after oral administration
Development of an SPE–HPLC–MS method for simultaneous determination and pharmacokinetic study of bioactive constituents of Yu Ping Feng San in rat plasma after oral administration Abstract Abstract Ethnopharmacological relevance Yu Ping Feng San ( YPFS , in Chinese: Jade Windscreen Powder), a well-known traditional Chi...
PMC7846798
core_pubmed_pmc
Population pharmacokinetic modeling and clinical application of vancomycin in Chinese patients hospitalized in intensive care units
Population pharmacokinetic modeling and clinical application of vancomycin in Chinese patients hospitalized in intensive care units Abstract Abstract Management of vancomycin administration for intensive care units (ICU) patients remains a challenge. The aim of this study was to describe a population pharmacokinetic mo...
PMC9589670
core_pubmed_pmc
Phase 3 Study of Subcutaneous Versus Intravenous Ravulizumab in Eculizumab-Experienced Adult Patients with PNH: Primary Analysis and 1-Year Follow-Up
Phase 3 Study of Subcutaneous Versus Intravenous Ravulizumab in Eculizumab-Experienced Adult Patients with PNH: Primary Analysis and 1-Year Follow-Up Abstract Abstract Introduction This study compared the pharmacokinetics (PK) of the ravulizumab on-body delivery system for subcutaneous (SUBQ) administration with intrav...
PMC11921222
core_pubmed_pmc
Liver microsomal protein content and activity in patients with hepatocellular carcinoma and cirrhosis: implications for the in vivo prediction of individual hepatic clearance
Liver microsomal protein content and activity in patients with hepatocellular carcinoma and cirrhosis: implications for the in vivo prediction of individual hepatic clearance Abstract Background The hepatic metabolism of patients with hepatocellular carcinoma and cirrhosis (HCCC) may differ from that of patients with h...
PMC12300021
core_pubmed_pmc
Pharmacogenomics and Pharmacometabolomics in Precision Tramadol Prescribing for Enhanced Pain Management: Evidence from QBB and EMR Data
Pharmacogenomics and Pharmacometabolomics in Precision Tramadol Prescribing for Enhanced Pain Management: Evidence from QBB and EMR Data Abstract Background/Objectives : Tramadol is an opioid frequently prescribed for moderate to severe pain and has seen a global increase in use. This presents numerous challenges in cl...
PMC6117064
core_pubmed_pmc
Optimization of carvedilol solid lipid nanoparticles: An approach to control the release and enhance the oral bioavailability on rabbits
Optimization of carvedilol solid lipid nanoparticles: An approach to control the release and enhance the oral bioavailability on rabbits Abstract Solid lipid nanoparticles (SLNs) are prospective carriers for oral delivery of poorly soluble drugs with low bioavailability. Therefore, the study aimed at developing carvedi...
PMC7056828
core_pubmed_pmc
Local Irradiation Modulates the Pharmacokinetics of Metabolites in 5-Fluorouracil—Radiotherapy–Pharmacokinetics Phenomenon
Local Irradiation Modulates the Pharmacokinetics of Metabolites in 5-Fluorouracil—Radiotherapy–Pharmacokinetics Phenomenon Abstract Abstract Background The effects of radiotherapy (RT) on the pharmacokinetics (PK) of 5-FU and 5-fluoro-5,6-dihydro-uracil (5-FDHU) were investigated by animal experiments. Methods Whole-pe...
PMC12511455
core_pubmed_pmc
Impact of Esomeprazole, Ciprofloxacin and Their Combination on Cervical Cancer Cell Line Proliferation: A Focus on Heat Shock Protein 70 Modulation
Impact of Esomeprazole, Ciprofloxacin and Their Combination on Cervical Cancer Cell Line Proliferation: A Focus on Heat Shock Protein 70 Modulation Abstract Objective: This investigation aimed to evaluate the combined efficacy of ciprofloxacin and esomeprazole in inhibiting cervical cancer proliferation and their capac...
PMC12660969
core_pubmed_pmc
In-silico identification of novel Cis-aconitate decarboxylase inhibitors as potential anti-inflammatory agents using molecular docking and dynamics
In-silico identification of novel Cis-aconitate decarboxylase inhibitors as potential anti-inflammatory agents using molecular docking and dynamics Abstract Abstract Cis-aconitate decarboxylase (CAD), also known as ACOD1 or IRG1, catalyzes the conversion of cis-aconitate to itaconate, playing a pivotal role in innate i...
PMC9167409
core_pubmed_pmc
Evaluation of the Pharmacokinetics and Safety of AMG 986 Tablet and Capsule Formulations in Healthy Adult Subjects: A Phase I, Open-Label, Randomized Study
Evaluation of the Pharmacokinetics and Safety of AMG 986 Tablet and Capsule Formulations in Healthy Adult Subjects: A Phase I, Open-Label, Randomized Study Abstract Background and objective AMG 986 is a first-in-class, novel apelin receptor small molecule agonist initially developed for the treatment of heart failure. ...
PMC3161034
core_pubmed_pmc
Safety and pharmacokinetics of motesanib in combination with gemcitabine and erlotinib for the treatment of solid tumors: a phase 1b study
Safety and pharmacokinetics of motesanib in combination with gemcitabine and erlotinib for the treatment of solid tumors: a phase 1b study Abstract Abstract Background This phase 1b study assessed the maximum tolerated dose (MTD), safety, and pharmacokinetics of motesanib (a small-molecule antagonist of VEGF receptors ...
PMC12854121
core_pubmed_pmc
Brexpiprazole for the Treatment of Agitation Associated with Dementia due to Alzheimer’s Disease: Clinical Perspectives
Brexpiprazole for the Treatment of Agitation Associated with Dementia due to Alzheimer’s Disease: Clinical Perspectives Abstract Abstract Dementia is a neuropsychiatric disorder that primarily affects the elderly, leading to a widespread decline in cognitive function and significant impairment of occupational, social, ...
PMC10106704
core_pubmed_pmc
Factors influencing bioequivalence evaluation of insulin biosimilars based on a structural equation model
Factors influencing bioequivalence evaluation of insulin biosimilars based on a structural equation model Abstract Abstract Objective: This study aimed to explore the factors affecting the bioequivalence of test and reference insulin preparations so as to provide a scientific basis for the consistency evaluation of the...
PMC5701170
core_pubmed_pmc
Population pharmacokinetics of remifentanil in critically ill patients receiving extracorporeal membrane oxygenation
Population pharmacokinetics of remifentanil in critically ill patients receiving extracorporeal membrane oxygenation Abstract Extracorporeal membrane oxygenation (ECMO) is associated with pharmacokinetic (PK) changes of drugs. It presents considerable challenges to providing optimal dosing regimens for patients receivi...
PMC6590348
core_pubmed_pmc
Safety Exposure‐Response Analysis for Daclatasvir, Asunaprevir, and Beclabuvir Combinations in HCV‐Infected Subjects
Safety Exposure‐Response Analysis for Daclatasvir, Asunaprevir, and Beclabuvir Combinations in HCV‐Infected Subjects Abstract Abstract The combination regimen of daclatasvir, asunaprevir, and beclabuvir has been developed for the treatment of hepatitis C virus infection. The objectives of this analysis were to characte...
PMC3513230
core_pubmed_pmc
Pharmacogenomic considerations in opioid analgesia
Pharmacogenomic considerations in opioid analgesia Abstract Abstract Translating pharmacogenetics to clinical practice has been particularly challenging in the context of pain, due to the complexity of this multifaceted phenotype and the overall subjective nature of pain perception and response to analgesia. Overall, n...
PMC6955905
core_pubmed_pmc
Optical Biosensors for Therapeutic Drug Monitoring
Optical Biosensors for Therapeutic Drug Monitoring Abstract Therapeutic drug monitoring (TDM) is a fundamental tool when administering drugs that have a limited dosage or high toxicity, which could endanger the lives of patients. To carry out this monitoring, one can use different biological fluids, including blood, pl...
PMC12950048
core_pubmed_pmc
Safety, Tolerability, and Pharmacokinetics of Subcutaneous Extended-Release Injectable Olanzapine in Patients with Schizophrenia and Schizoaffective Disorder
Safety, Tolerability, and Pharmacokinetics of Subcutaneous Extended-Release Injectable Olanzapine in Patients with Schizophrenia and Schizoaffective Disorder Abstract Abstract Background and Objective This study evaluated the pharmacokinetics (PK), safety, and tolerability of TV-44749 in patients with schizophrenia or ...
PMC7131995
core_pubmed_pmc
Vedolizumab in the Treatment of Ulcerative Colitis: An Evidence-Based Review of Safety, Efficacy, and Place of Therapy
Vedolizumab in the Treatment of Ulcerative Colitis: An Evidence-Based Review of Safety, Efficacy, and Place of Therapy Abstract Abstract Introduction Selective blockade of the integrins and mucosal adhesion molecules is a promising therapeutic strategy for ulcerative colitis (UC). Vedolizumab (VDZ), a humanized IgG1 mo...
PMC6034206
core_pubmed_pmc
A randomized trial comparing the pharmacology of magnesium sulfate when used to treat severe preeclampsia with serial intravenous boluses versus a continuous intravenous infusion
A randomized trial comparing the pharmacology of magnesium sulfate when used to treat severe preeclampsia with serial intravenous boluses versus a continuous intravenous infusion Abstract Background Magnesium sulfate is the preferred pharmacological intervention for the prevention and treatment of eclamptic seizures in...
PMC6679487
core_pubmed_pmc
Pharmacokinetics of furosemide in thoroughbred horses subjected to supramaximal treadmill exercise with and without controlled access to water
Pharmacokinetics of furosemide in thoroughbred horses subjected to supramaximal treadmill exercise with and without controlled access to water Abstract Background The primary objective of this study was to assess the disposition of furosemide in Thoroughbred horses treated intravenously with 1 mg/kg of furosemide 4 and...
PMC9854724
core_pubmed_pmc
Continuous Infusion of High Doses of Cefepime in Intensive Care Unit: Assessment of Steady-State Plasma Level and Incidence on Neurotoxicity
Continuous Infusion of High Doses of Cefepime in Intensive Care Unit: Assessment of Steady-State Plasma Level and Incidence on Neurotoxicity Abstract Continuous infusion (CI) with high doses of cefepime is recommended in the empirical antimicrobial regimen of critically ill patients with suspected Gram-negative sepsis....
PMC11706422
core_pubmed_pmc
The population pharmacokinetics of dolutegravir co‐administered with rifampicin in Thai people living with HIV : Assessment of alternative dosing regimens
The population pharmacokinetics of dolutegravir co‐administered with rifampicin in Thai people living with HIV : Assessment of alternative dosing regimens Abstract Abstract Tuberculosis is the most common opportunistic infection in individuals with HIV, and rifampicin is crucial in the treatment of tuberculosis. Drug–d...
PMC9402746
core_pubmed_pmc
A phase I dose escalation, dose expansion and pharmacokinetic trial of gemcitabine and alisertib in advanced solid tumors and pancreatic cancer
A phase I dose escalation, dose expansion and pharmacokinetic trial of gemcitabine and alisertib in advanced solid tumors and pancreatic cancer Abstract Abstract Purpose Aurora Kinase A (AKA) inhibition with gemcitabine represents a potentially synergistic cancer treatment strategy via mitotic catastrophe. The feasibil...
PMC6327122
core_pubmed_pmc
Pharmacokinetic and Pharmacodynamic Relationship of Blinatumomab in Patients with Non-Hodgkin Lymphoma
Pharmacokinetic and Pharmacodynamic Relationship of Blinatumomab in Patients with Non-Hodgkin Lymphoma Abstract Background: Blinatumomab is a bispecific T-cell engager (BiTE®) antibody construct targeting CD3ε on T cells and CD19 on B cells. We describe the relationship between pharmacokinetics (PK) of blinatumomab and...
PMC3970917
core_pubmed_pmc
A randomized, placebo-controlled, four-period crossover, definitive QT study of the effects of APF530 exposure, high-dose intravenous granisetron, and moxifloxacin on QTc prolongation
A randomized, placebo-controlled, four-period crossover, definitive QT study of the effects of APF530 exposure, high-dose intravenous granisetron, and moxifloxacin on QTc prolongation Abstract Background Regulatory concern about potential QT-interval prolongation by serotonin-receptor antagonist antiemetics prompted pr...
PMC12736187
core_pubmed_pmc
Laser-Ablated Gold Nanoparticles as Tunable Contrast Agents for Preclinical Imaging
Laser-Ablated Gold Nanoparticles as Tunable Contrast Agents for Preclinical Imaging Abstract Femtosecond laser-ablated gold nanoparticles (AuNPs) offer a unique platform for developing novel cost-effective contrast agents due to their ultraclean, surfactant-free synthesis and precisely tunable surface properties. This ...
PMC9146796
core_pubmed_pmc
The Effect of Dynamic, In Vivo-like Oxaliplatin on HCT116 Spheroids in a Cancer-on-Chip Model Is Representative of the Response in Xenografts
The Effect of Dynamic, In Vivo-like Oxaliplatin on HCT116 Spheroids in a Cancer-on-Chip Model Is Representative of the Response in Xenografts Abstract Abstract The cancer xenograft model in which human cancer cells are implanted in a mouse is one of the most used preclinical models to test the efficacy of novel cancer ...
PMC6102536
core_pubmed_pmc
A Metabolism-Based Synergy for Total Coumarin Extract of Radix Angelicae Dahuricae and Ligustrazine on Migraine Treatment in Rats
A Metabolism-Based Synergy for Total Coumarin Extract of Radix Angelicae Dahuricae and Ligustrazine on Migraine Treatment in Rats Abstract Abstract Radix Angelicae dahuricae , containing coumarins, which might affect cytochrome P450 enzyme (CYP450) activity, has been co-administered with ligustrazine, a substrate of CY...
PMC5931243
core_pubmed_pmc
Rapid acting fentanyl formulations in breakthrough pain in cancer. Drug selection by means of the System of Objectified Judgement Analysis
Rapid acting fentanyl formulations in breakthrough pain in cancer. Drug selection by means of the System of Objectified Judgement Analysis Abstract Drug selection of rapid acting fentanyl formulations in the treatment of breakthrough pain in patients with cancer is performed by the System of Objectified Judgement Analy...
PMC9804975
core_pubmed_pmc
Analysis of fibrinogen concentrate pharmacokinetics and dosing for bleeds and surgery in adults, adolescents, and children with congenital afibrinogenaemia and hypofibrinogenaemia
Analysis of fibrinogen concentrate pharmacokinetics and dosing for bleeds and surgery in adults, adolescents, and children with congenital afibrinogenaemia and hypofibrinogenaemia Abstract Abstract Introduction Congenital afibrinogenaemia and hypofibrinogenaemia are rare coagulation disorders where clotting is impaired...
PMC12888882
core_pubmed_pmc
In vitro PK/PD modeling and simulation to accurately assess the antimicrobial activity of tigecycline against Mycobacterium abscessus
In vitro PK/PD modeling and simulation to accurately assess the antimicrobial activity of tigecycline against Mycobacterium abscessus Abstract ABSTRACT Conventional in vitro susceptibility testing methods may underestimate the bactericidal activity of antibiotics that are chemically unstable in aqueous media, thereby l...
PMC5980303
core_pubmed_pmc
Integrated Population Pharmacokinetic Analysis of Rivaroxaban Across Multiple Patient Populations
Integrated Population Pharmacokinetic Analysis of Rivaroxaban Across Multiple Patient Populations Abstract Abstract The population pharmacokinetics (PK) of rivaroxaban have been evaluated in several population‐specific models. We developed an integrated population PK model using pooled data from 4,918 patients in 7 cli...
PMC11222247
core_pubmed_pmc
PEGylation renders carnosine resistant to hydrolysis by serum carnosinase and increases renal carnosine levels
PEGylation renders carnosine resistant to hydrolysis by serum carnosinase and increases renal carnosine levels Abstract Abstract Carnosine’s protective effect in rodent models of glycoxidative stress have provided a rational for translation of these findings in therapeutic concepts in patient with diabetic kidney disea...
PMC12926690
core_pubmed_pmc
Pharmacokinetics of Perampanel in Danish Paediatric Patients With Epilepsy Based on Therapeutic Drug Monitoring
Pharmacokinetics of Perampanel in Danish Paediatric Patients With Epilepsy Based on Therapeutic Drug Monitoring Abstract ABSTRACT We aimed to quantify inter‐ and intra‐patient variability in serum perampanel concentrations and assess whether concentrations predict efficacy or tolerability. We conducted a retrospective ...
PMC7237702
core_pubmed_pmc
Network Pharmacology-Based Approach Uncovers the Mechanism of GuanXinNing Tablet for Treating Thrombus by MAPKs Signal Pathway
Network Pharmacology-Based Approach Uncovers the Mechanism of GuanXinNing Tablet for Treating Thrombus by MAPKs Signal Pathway Abstract Abstract Background GuanXinNing tablet (GXNT), a traditional Chinese patent medicine, has been found to have remarkable antithrombotic effects and can effectively inhibit pro-thromboti...
PMC8520863
core_pubmed_pmc
Phase I study of napabucasin in combination with FOLFIRI + bevacizumab in Japanese patients with metastatic colorectal cancer
Phase I study of napabucasin in combination with FOLFIRI + bevacizumab in Japanese patients with metastatic colorectal cancer Abstract Background Napabucasin is an oral NAD(P)H:quinone oxidoreductase 1 bioactivatable agent that generates reactive oxygen species, is hypothesised to affect multiple oncogenic cellular pat...