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PMC9794061
core_pubmed_pmc
Carotenoids as potential inhibitors of TNFα in COVID-19 treatment
Carotenoids as potential inhibitors of TNFα in COVID-19 treatment Abstract Abstract Tumor necrosis factor-alpha (TNF-α) is a multifunctional pro-inflammatory cytokine, responsible for autoimmune and inflammatory disorders. In COVID-19 patients, increased TNF-α concentration may provoke inflammatory cascade and induce t...
PMC7997453
core_pubmed_pmc
Investigation of the Impact of CYP3A5 Polymorphism on Drug–Drug Interaction between Tacrolimus and Schisantherin A/Schisandrin A Based on Physiologically-Based Pharmacokinetic Modeling
Investigation of the Impact of CYP3A5 Polymorphism on Drug–Drug Interaction between Tacrolimus and Schisantherin A/Schisandrin A Based on Physiologically-Based Pharmacokinetic Modeling Abstract Abstract Wuzhi capsule (WZC) is commonly prescribed with tacrolimus in China to ease drug-induced hepatotoxicity. Two abundant...
PMC5588692
core_pubmed_pmc
A pilot clinical trial of recombinant human angiotensin-converting enzyme 2 in acute respiratory distress syndrome
A pilot clinical trial of recombinant human angiotensin-converting enzyme 2 in acute respiratory distress syndrome Abstract Abstract Background Renin-angiotensin system (RAS) signaling and angiotensin-converting enzyme 2 (ACE2) have been implicated in the pathogenesis of acute respiratory distress syndrome (ARDS). We p...
PMC11373224
core_pubmed_pmc
Evaluation of a Bayesian hierarchical pharmacokinetic–pharmacodynamic model for predicting parasitological outcomes in Phase 2 studies of new antimalarial drugs
Evaluation of a Bayesian hierarchical pharmacokinetic–pharmacodynamic model for predicting parasitological outcomes in Phase 2 studies of new antimalarial drugs Abstract ABSTRACT The rise of multidrug-resistant malaria requires accelerated development of novel antimalarial drugs. Pharmacokinetic–pharmacodynamic (PK-PD)...
PMC5044985
core_pubmed_pmc
Radiolabeled tirofiban – a potential radiopharmaceutical for detection of deep venous thrombosis
Radiolabeled tirofiban – a potential radiopharmaceutical for detection of deep venous thrombosis Abstract Abstract Aim The aim of this study was to investigate the possibility of using 99m technetium ( 99m Tc)-labeled tirofiban (a reversible antagonist of glycoprotein IIb/IIIa) for detection of deep venous thrombosis (...
PMC8898728
core_pubmed_pmc
A phase 1 trial of xentuzumab, an IGF‐neutralizing antibody, in Japanese patients with advanced solid tumors
A phase 1 trial of xentuzumab, an IGF‐neutralizing antibody, in Japanese patients with advanced solid tumors Abstract Abstract Xentuzumab is an insulin‐like growth factor (IGF) ligand‐neutralizing antibody. This phase 1 trial assessed xentuzumab in Japanese patients with solid tumors. Patients aged ≥20 y old with solid...
PMC11846607
core_pubmed_pmc
Integrating early response biomarkers in pharmacokinetic models: A novel method to individualize the initial infliximab dose in patients with Crohn's disease
Integrating early response biomarkers in pharmacokinetic models: A novel method to individualize the initial infliximab dose in patients with Crohn's disease Abstract Abstract The use of model‐informed precision dosing to personalize infliximab has been shown to improve both the acquisition of concentration targets and...
PMC4931208
core_pubmed_pmc
Insulin degludec/insulin aspart in Japanese patients with type 1 diabetes mellitus: Distinct prandial and basal glucose‐lowering effects
Insulin degludec/insulin aspart in Japanese patients with type 1 diabetes mellitus: Distinct prandial and basal glucose‐lowering effects Abstract Abstract Aims/Introduction Insulin degludec/insulin aspart ( ID egAsp) is a soluble co‐formulation of long‐acting insulin degludec ( ID eg) and rapid‐acting insulin aspart ( ...
PMC4922823
core_pubmed_pmc
A stabilizer-free and organic solvent-free method to prepare 10-hydroxycamptothecin nanocrystals: in vitro and in vivo evaluation
A stabilizer-free and organic solvent-free method to prepare 10-hydroxycamptothecin nanocrystals: in vitro and in vivo evaluation Abstract Abstract 10-Hydroxycamptothecin (10-HCPT) is a promising anticancer drug with a wide spectrum of antitumor activities. Due to its poor solubility, the carboxylate form that shows hi...
PMC5768281
core_pubmed_pmc
A double-blind, placebo-controlled, single ascending-dose study of remyelinating antibody rHIgM22 in people with multiple sclerosis
A double-blind, placebo-controlled, single ascending-dose study of remyelinating antibody rHIgM22 in people with multiple sclerosis Abstract Short abstract Objective The objective of this paper is to assess, in individuals with clinically stable multiple sclerosis (MS), the safety, tolerability, pharmacokinetics (PK) a...
PMC11784183
core_pubmed_pmc
Identification of an antibiotic from an HTS targeting EF-Tu:tRNA interaction: a prospective topical treatment for MRSA skin infections
Identification of an antibiotic from an HTS targeting EF-Tu:tRNA interaction: a prospective topical treatment for MRSA skin infections Abstract ABSTRACT Because of the urgent need for new antibiotics to treat drug-resistant bacterial pathogens, we employed an assay that rapidly screens large quantities of compounds for...
PMC12498278
core_pubmed_pmc
Multi-omics pan-cancer profiling of CDK2 and in silico identification of plant-derived inhibitors using machine learning approaches
Multi-omics pan-cancer profiling of CDK2 and in silico identification of plant-derived inhibitors using machine learning approaches Abstract Abstract Cancer is a complex disease characterized by uncontrolled cell proliferation, often driven by dysregulated cyclin-dependent kinases (CDKs), particularly CDK2, which plays...
PMC9146265
core_pubmed_pmc
In Silico Evaluation of Paxlovid’s Pharmacometrics for SARS-CoV-2: A Multiscale Approach
In Silico Evaluation of Paxlovid’s Pharmacometrics for SARS-CoV-2: A Multiscale Approach Abstract Paxlovid is a promising, orally bioavailable novel drug for SARS-CoV-2 with excellent safety profiles. Our main goal here is to explore the pharmacometric features of this new antiviral. To provide a detailed assessment of...
PMC12587542
core_pubmed_pmc
Metronidazole exposure–response and safety in infants
Metronidazole exposure–response and safety in infants Abstract ABSTRACT The nitroimidazole antibiotic, metronidazole, is frequently prescribed to infants with serious intra-abdominal infections, and multiple dosing recommendations exist. We sought to evaluate the extent to which metronidazole doses and associated expos...
PMC12493022
core_pubmed_pmc
Recent Advances in Bioanalytical Methods for Quantification and Pharmacokinetic Analyses of Antibody–Drug Conjugates
Recent Advances in Bioanalytical Methods for Quantification and Pharmacokinetic Analyses of Antibody–Drug Conjugates Abstract Antibody–drug conjugates (ADCs) represent a rapidly expanding class of therapeutics, uniquely combining the specificity of monoclonal antibodies with the potency of cytotoxic small-molecule payl...
PMC9726673
core_pubmed_pmc
Self-nanoemulsifying drug delivery system (SNEDDS) mediated improved oral bioavailability of thymoquinone: optimization, characterization, pharmacokinetic, and hepatotoxicity studies
Self-nanoemulsifying drug delivery system (SNEDDS) mediated improved oral bioavailability of thymoquinone: optimization, characterization, pharmacokinetic, and hepatotoxicity studies Abstract Abstract Thymoquinone (TQ) is an antioxidant, anti-inflammatory, and hepatoprotective compound obtained from the black seed oil ...
PMC11385303
core_pubmed_pmc
Population pharmacokinetics study of tacrolimus in liver transplant recipients: a comparison between patients with or without liver cancer before surgery
Population pharmacokinetics study of tacrolimus in liver transplant recipients: a comparison between patients with or without liver cancer before surgery Abstract Abstract Background and Objective The main challenge for immunosuppressive therapy using tacrolimus in liver transplantation is the considerable variability ...
PMC12300842
core_pubmed_pmc
Quantification of Total and Unbound Selinexor Concentrations in Human Plasma by a Fully Validated Liquid Chromatography-Tandem Mass Spectrometry Method
Quantification of Total and Unbound Selinexor Concentrations in Human Plasma by a Fully Validated Liquid Chromatography-Tandem Mass Spectrometry Method Abstract Abstract Background/Objectives: Selinexor is a selective nuclear-export inhibitor approved for hematologic malignancies, characterized by extensive plasma prot...
PMC12567236
core_pubmed_pmc
Emerging Insulin Analogues: A Glimpse into How Insulin Analogues May Look in the near Future
Emerging Insulin Analogues: A Glimpse into How Insulin Analogues May Look in the near Future Abstract Abstract The use of insulin as a treatment for diabetes mellitus has been marred by several challenges. These setbacks incurred in an attempt to better manage diabetes, together with past innovative strategies, have en...
PMC4964463
core_pubmed_pmc
Chemical Structure-Biological Activity Models for Pharmacophores’ 3D-Interactions
Chemical Structure-Biological Activity Models for Pharmacophores’ 3D-Interactions Abstract Within medicinal chemistry nowadays, the so-called pharmaco-dynamics seeks for qualitative (for understanding) and quantitative (for predicting) mechanisms/models by which given chemical structure or series of congeners actively ...
PMC12710188
core_pubmed_pmc
AZP2006 in Progressive Supranuclear Palsy: Outcomes from a Phase 2a Multicenter, Randomized Trial, and Open‐Label Extension on Safety, Biomarkers, and Disease Progression
AZP2006 in Progressive Supranuclear Palsy: Outcomes from a Phase 2a Multicenter, Randomized Trial, and Open‐Label Extension on Safety, Biomarkers, and Disease Progression Abstract Abstract Objectives The aim was to evaluate the safety, tolerability, pharmacokinetics, and potential clinical efficacy of AZP2006, an oral ...
PMC7677109
core_pubmed_pmc
Traces pilot pharmacokinetic study dataset
Traces pilot pharmacokinetic study dataset Abstract The dataset displays the pharmacokinetics data obtained from the TRACES pilot study. The nine patients included were undergoing haemorrhagic caesarean section (blood loss > 800 mL) and receiving a single i.v dose of tranexamic acid (0.5, 1 or 2 g over 1 min). The data...
PMC3979827
core_pubmed_pmc
Pharmacokinetics and Pharmacodynamics of ASKP1240, a Fully Human Anti-CD40 Antibody, in Normal and Renal Transplanted Cynomolgus Monkeys
Pharmacokinetics and Pharmacodynamics of ASKP1240, a Fully Human Anti-CD40 Antibody, in Normal and Renal Transplanted Cynomolgus Monkeys Abstract Background The purpose of this study was to evaluate the serum concentration of ASKP1240 (pharmacokinetics [PK]) and the CD40 occupancy of ASKP1240 (pharmacodynamics [PD]) in...
PMC3249195
core_pubmed_pmc
Do CYP2D6 genotypes reflect oxycodone requirements for cancer patients treated for cancer pain? A cross-sectional multicentre study
Do CYP2D6 genotypes reflect oxycodone requirements for cancer patients treated for cancer pain? A cross-sectional multicentre study Abstract Objective Opioids are recommended by the World Health Organization for moderate to severe cancer pain. Oxycodone is one of the most commonly used opioids and is metabolized in the...
PMC12020506
core_pubmed_pmc
Design of a Phase 3, Global, Multicenter, Randomized, Placebo-Controlled, Double-Blind Study of Nipocalimab in Pregnancies at Risk for Severe Hemolytic Disease of the Fetus and Newborn
Design of a Phase 3, Global, Multicenter, Randomized, Placebo-Controlled, Double-Blind Study of Nipocalimab in Pregnancies at Risk for Severe Hemolytic Disease of the Fetus and Newborn Abstract Abstract Objective Nipocalimab is a neonatal fragment crystallizable (Fc) receptor (FcRn)—blocking monoclonal antibody that in...
PMC7264731
core_pubmed_pmc
Chloroquine Dosing Recommendations for Pediatric COVID‐19 Supported by Modeling and Simulation
Chloroquine Dosing Recommendations for Pediatric COVID‐19 Supported by Modeling and Simulation Abstract As chloroquine (CHQ) is part of the Dutch Centre for Infectious Disease Control coronavirus disease 2019 (COVID‐19) experimental treatment guideline, pediatric dosing guidelines are needed. Recent pediatric data sugg...
PMC9948638
core_pubmed_pmc
A Multifunctional, Highly Biocompatible, and Double-Triggering Caramelized Nanotheranostic System Loaded with Fe 3 O 4 and DOX for Combined Chemo-Photothermal Therapy and Real-Time Magnetic Resonance Imaging Monitoring of Triple Negative Breast Cancer
A Multifunctional, Highly Biocompatible, and Double-Triggering Caramelized Nanotheranostic System Loaded with Fe 3 O 4 and DOX for Combined Chemo-Photothermal Therapy and Real-Time Magnetic Resonance Imaging Monitoring of Triple Negative Breast Cancer Abstract Abstract Purpose Owing to lack of specific molecular target...
PMC11469156
core_pubmed_pmc
Engineering Lipid Spherulites for the Sustained Release of Highly Dosed Small Hydrophilic Compounds
Engineering Lipid Spherulites for the Sustained Release of Highly Dosed Small Hydrophilic Compounds Abstract Abstract Currently, there is a lack of parenteral sustained release formulations for the delivery of highly dosed small hydrophilic drugs. Therefore, parenteral lipid spherulites are engineered capable of entrap...
PMC10135101
core_pubmed_pmc
Population Pharmacokinetic Study of Benzylpenicillin in Critically Unwell Adults
Population Pharmacokinetic Study of Benzylpenicillin in Critically Unwell Adults Abstract Pharmacokinetics are highly variable in critical illness, and suboptimal antibiotic exposure is associated with treatment failure. Benzylpenicillin is a commonly used beta-lactam antibiotic, and pharmacokinetic data of its use in ...
PMC11892205
core_pubmed_pmc
Evaluation of direct oral anticoagulant continuation versus switching to a parenteral anticoagulant in critically ill patients: a retrospective cohort study
Evaluation of direct oral anticoagulant continuation versus switching to a parenteral anticoagulant in critically ill patients: a retrospective cohort study Abstract Background Direct oral anticoagulants (DOACs) are widely used as first-line agents in various clinical settings. However, there is very little evidence re...
PMC7831708
core_pubmed_pmc
Preclinical PET imaging with the novel human antibody 89 Zr-DFO-REGN3504 sensitively detects PD-L1 expression in tumors and normal tissues
Preclinical PET imaging with the novel human antibody 89 Zr-DFO-REGN3504 sensitively detects PD-L1 expression in tumors and normal tissues Abstract Background Programmed cell death protein 1/programmed death-ligand 1 (PD-1/PD-L1) blocking antibodies including cemiplimab have generated profound clinical activity across ...
PMC4640888
core_pubmed_pmc
Discovery and Characterization of a Potent Interleukin-6 Binding Peptide with Neutralizing Activity In Vivo
Discovery and Characterization of a Potent Interleukin-6 Binding Peptide with Neutralizing Activity In Vivo Abstract Abstract Interleukin-6 (IL-6) is an important member of the cytokine superfamily, exerting pleiotropic actions on many physiological processes. Over-production of IL-6 is a hallmark of immune-mediated in...
PMC8103611
core_pubmed_pmc
Toxicology and Pharmacokinetics Study of Intradiscal Injection of Simvastatin in Rabbits
Toxicology and Pharmacokinetics Study of Intradiscal Injection of Simvastatin in Rabbits Abstract Abstract To test the pharmacokinetics and toxicology of whole organs and tissues after intradiscal injection of simvastatin in rabbits. To provide the information needed to support human clinical trials. Twelve male and tw...
PMC6709424
core_pubmed_pmc
ATLAS mPBPK: A MATLAB‐Based Tool for Modeling and Simulation of Minimal Physiologically‐Based Pharmacokinetic Models
ATLAS mPBPK: A MATLAB‐Based Tool for Modeling and Simulation of Minimal Physiologically‐Based Pharmacokinetic Models Abstract Abstract Minimal physiologically‐based pharmacokinetic (mPBPK) models are frequently used to model plasma pharmacokinetic (PK) data and utilize and yield physiologically relevant parameters. Com...
PMC10251242
core_pubmed_pmc
Efficacy and Safety of the Aflibercept Biosimilar SB15 in Neovascular Age-Related Macular Degeneration
Efficacy and Safety of the Aflibercept Biosimilar SB15 in Neovascular Age-Related Macular Degeneration Abstract Key Points Question Does SB15, a proposed aflibercept biosimilar, have equivalent best-corrected visual acuity (BCVA) outcomes and a similar safety profile to reference aflibercept (AFL) in patients with neov...
PMC12735765
core_pubmed_pmc
A Unified Approach to Synthesizing Four Linezolid Metabolites That May Cause Thrombocytopenia
A Unified Approach to Synthesizing Four Linezolid Metabolites That May Cause Thrombocytopenia Abstract Abstract Background/Objectives : Linezolid is a first-in-class oxazolidinone antibiotic that exhibits activity against Gram-positive pathogens, including methicillin-resistant Staphylococcus aureus and vancomycin-resi...
PMC10063562
core_pubmed_pmc
Metabolic profiling, antioxidant, and enzyme inhibition potential of Iris pseudacorus L. from Egypt and Japan: A comparative study
Metabolic profiling, antioxidant, and enzyme inhibition potential of Iris pseudacorus L. from Egypt and Japan: A comparative study Abstract Genus Iris comprises numerous and diverse phytoconstituents displaying marked biological activities. The rhizomes, and aerial parts of Iris pseudacorus L. cultivars from Egypt and ...
PMC12351382
core_pubmed_pmc
Fibrinography and thrombography (thrombodynamics-4D) in atrial fibrillation assessment of direct oral anticoagulants in geriatrics patients aged 80 years and older receiving direct oral anticoagulant therapy
Fibrinography and thrombography (thrombodynamics-4D) in atrial fibrillation assessment of direct oral anticoagulants in geriatrics patients aged 80 years and older receiving direct oral anticoagulant therapy Abstract Background Scarce data are available on pharmacodynamic (PD) variability in very elderly patients recei...
PMC9135479
core_pubmed_pmc
Pharmacokinetic, Hemostatic, and Anticancer Properties of a Low-Anticoagulant Bovine Heparin
Pharmacokinetic, Hemostatic, and Anticancer Properties of a Low-Anticoagulant Bovine Heparin Abstract Abstract Heparin is a centennial anticoagulant drug broadly employed for treatment and prophylaxis of thromboembolic conditions. Although unfractionated heparin (UFH) has already been shown to have remarkable pharmacol...
PMC7438813
core_pubmed_pmc
Effect of Elagolix Exposure on Clinical Efficacy End Points in Phase III Trials in Women With Endometriosis‐Associated Pain: An Application of Markov Model
Effect of Elagolix Exposure on Clinical Efficacy End Points in Phase III Trials in Women With Endometriosis‐Associated Pain: An Application of Markov Model Abstract Elagolix is an oral gonadotropin‐releasing hormone antagonist approved by the US Food and Drug Administration (FDA) for the management of moderate‐to‐sever...
PMC9784610
core_pubmed_pmc
A Randomized, Triple-Blind, Comparator-Controlled Parallel Study Investigating the Pharmacokinetics of Cannabidiol and Tetrahydrocannabinol in a Novel Delivery System, Solutech, in Association with Cannabis Use History
A Randomized, Triple-Blind, Comparator-Controlled Parallel Study Investigating the Pharmacokinetics of Cannabidiol and Tetrahydrocannabinol in a Novel Delivery System, Solutech, in Association with Cannabis Use History Abstract Background: An oral route of administration for tetrahydrocannabinol (Δ 9 -THC) and cannabid...
PMC9855104
core_pubmed_pmc
Use of High-Dose Nebulized Colistimethate in Patients with Colistin-Only Susceptible Acinetobacter baumannii VAP: Clinical, Pharmacokinetic and Microbiome Features
Use of High-Dose Nebulized Colistimethate in Patients with Colistin-Only Susceptible Acinetobacter baumannii VAP: Clinical, Pharmacokinetic and Microbiome Features Abstract (1) Background: Colistin-only susceptible (COS) Acinetobacter baumannii (AB) ventilator-associated pneumonia (VAP) represents a clinical challenge ...
PMC3004594
core_pubmed_pmc
Uses and benefits of omega-3 ethyl esters in patients with cardiovascular disease
Uses and benefits of omega-3 ethyl esters in patients with cardiovascular disease Abstract Much evidence on the favorable effects of omega-3 ethyl esters on cardiovascular morbidity and mortality has been obtained in studies performed in healthy subjects and in different clinical settings. Here the clinical effects of ...
PMC12961800
core_pubmed_pmc
Attenuated hemodynamic response to adjunct vasopressin in obese septic shock patients: a physiological or dose-dependent effect?
Attenuated hemodynamic response to adjunct vasopressin in obese septic shock patients: a physiological or dose-dependent effect? Abstract Introduction Obesity is increasingly prevalent in ICU patients, often requiring adjusted dosing due to altered drug pharmacodynamics. Arginine vasopressin (AVP) is used adjunctively ...
PMC8891103
core_pubmed_pmc
Finerenone Dose–Exposure–Serum Potassium Response Analysis of FIDELIO-DKD Phase III: The Role of Dosing, Titration, and Inclusion Criteria
Finerenone Dose–Exposure–Serum Potassium Response Analysis of FIDELIO-DKD Phase III: The Role of Dosing, Titration, and Inclusion Criteria Abstract Abstract Background Finerenone is a nonsteroidal selective mineralocorticoid receptor antagonist (MRA) that demonstrated efficacy in delaying the progression of chronic kid...
PMC11856320
core_pubmed_pmc
Clinical safety and pharmacokinetics of a novel oral niclosamide formulation compared with marketed niclosamide chewing tablets in healthy volunteers: A three-part randomized, double-blind, placebo-controlled trial
Clinical safety and pharmacokinetics of a novel oral niclosamide formulation compared with marketed niclosamide chewing tablets in healthy volunteers: A three-part randomized, double-blind, placebo-controlled trial Abstract Aim Niclosamide is an established anthelmintic substance and a promising candidate for treating ...
PMC11320124
core_pubmed_pmc
Digital colloid-enhanced Raman spectroscopy for the pharmacokinetic detection of bioorthogonal drugs †
Digital colloid-enhanced Raman spectroscopy for the pharmacokinetic detection of bioorthogonal drugs † Abstract Bioorthogonal drug molecules are currently gaining prominence for their excellent efficacy, safety and metabolic stability. Pharmacokinetic study is critical for understanding their mechanisms and guiding pha...
PMC5024774
core_pubmed_pmc
Exposure-response analysis to assess the concentration–QTc relationship of CC-122
Exposure-response analysis to assess the concentration–QTc relationship of CC-122 Abstract CC-122 hydrochloride is a novel pleiotropic pathway modifier compound that binds cereblon, a substrate receptor of the Cullin 4 RING E3 ubiquitin ligase complex. CC-122 has multiple activities including modulation of immune cells...
PMC10296693
core_pubmed_pmc
Pharmacological Characterization of P626, a Novel Dual Adenosine A 2A /A 2B Receptor Antagonist, on Synaptic Plasticity and during an Ischemic-like Insult in CA1 Rat Hippocampus
Pharmacological Characterization of P626, a Novel Dual Adenosine A 2A /A 2B Receptor Antagonist, on Synaptic Plasticity and during an Ischemic-like Insult in CA1 Rat Hippocampus Abstract Abstract In recent years, the use of multi-target compounds has become an increasingly pursued strategy to treat complex pathologies,...
PMC9050788
core_pubmed_pmc
Assessment of the Effects of Inhibition or Induction of CYP2C19 and CYP2C9 Enzymes, or Inhibition of OAT3, on the Pharmacokinetics of Abrocitinib and Its Metabolites in Healthy Individuals
Assessment of the Effects of Inhibition or Induction of CYP2C19 and CYP2C9 Enzymes, or Inhibition of OAT3, on the Pharmacokinetics of Abrocitinib and Its Metabolites in Healthy Individuals Abstract Abstract Background and Objective Abrocitinib is a Janus kinase 1-selective inhibitor for the treatment of moderate-to-sev...
PMC11338093
core_pubmed_pmc
Inhibitor of apoptosis proteins (IAP) inhibitor APG-1387 monotherapy or in combination with programmed cell death 1 (PD-1) inhibitor toripalimab in patients with advanced solid tumors: results from two phase I trials
Inhibitor of apoptosis proteins (IAP) inhibitor APG-1387 monotherapy or in combination with programmed cell death 1 (PD-1) inhibitor toripalimab in patients with advanced solid tumors: results from two phase I trials Abstract Abstract Background APG-1387 is a novel second mitochondrial-derived activator of caspases mim...
PMC7677484
core_pubmed_pmc
Dipeptidyl peptidase-4 inhibition to prevent progression of calcific aortic stenosis
Dipeptidyl peptidase-4 inhibition to prevent progression of calcific aortic stenosis Abstract Abstract Objective To evaluate whether the use of dipeptidyl peptidase-4 (DPP-4) inhibitors and their cardiac tissue distribution profile and anticalcification abilities are associated with risk of aortic stenosis (AS) progres...
PMC4251377
core_pubmed_pmc
Cases of Adverse Reaction to Psychotropic Drugs and Possible Association with Pharmacogenetics
Cases of Adverse Reaction to Psychotropic Drugs and Possible Association with Pharmacogenetics Abstract Thousands of samples for pharmacogenetic tests have been analysed in our laboratory since its establishment. In this article we describe some of the most interesting cases of CYP poor metabolisers associated with adv...
PMC8241087
core_pubmed_pmc
Comparison of pharmacokinetics and drug release in tissues after transarterial chemoembolization with doxorubicin using diverse lipiodol emulsions and CalliSpheres Beads in rabbit livers
Comparison of pharmacokinetics and drug release in tissues after transarterial chemoembolization with doxorubicin using diverse lipiodol emulsions and CalliSpheres Beads in rabbit livers Abstract Abstract CalliSpheres ® Beads (CB) is the first drug-eluting bead (DEB) product in China. Our aim was to compare the effect ...
PMC11749330
core_pubmed_pmc
Nivolumab plasma concentration and clearance associated with overall survival in patients with renal cell carcinoma
Nivolumab plasma concentration and clearance associated with overall survival in patients with renal cell carcinoma Abstract Abstract Background Nivolumab is an immune checkpoint inhibitor (ICI) that selectively inhibits programmed cell death protein 1 activation, restoring antitumor immunity. ICIs are indicated for va...
PMC12486408
core_pubmed_pmc
Impact of liposomal delivery on coenzyme Q10 absorption: a double-blind, placebo-controlled, randomized trial
Impact of liposomal delivery on coenzyme Q10 absorption: a double-blind, placebo-controlled, randomized trial Abstract Abstract Background Coenzyme Q10 (CoQ-10) plays a vital role in cellular energy production and protection against oxidative stress. However, its absorption from orally administered forms is limited due...
PMC10891214
core_pubmed_pmc
Effects of food and ethnicity on the pharmacokinetics of venadaparib, a next-generation PARP inhibitor, in healthy Korean, Caucasian, and Chinese male subjects
Effects of food and ethnicity on the pharmacokinetics of venadaparib, a next-generation PARP inhibitor, in healthy Korean, Caucasian, and Chinese male subjects Abstract Aim Venadaparib is a next-generation poly(ADP-ribose) polymerase inhibitor under development for treating gastric cancer. This study aimed to evaluate ...
PMC6785705
core_pubmed_pmc
Oral Fluoroquinolone or Trimethoprim-Sulfamethoxazole vs ß-Lactams as Step-Down Therapy for Enterobacteriaceae Bacteremia: Systematic Review and Meta-analysis
Oral Fluoroquinolone or Trimethoprim-Sulfamethoxazole vs ß-Lactams as Step-Down Therapy for Enterobacteriaceae Bacteremia: Systematic Review and Meta-analysis Abstract Abstract Background Using published data, we sought to compare outcomes in patients transitioned to either oral fluoroquinolones (FQs) or trimethoprim-s...
PMC10442107
core_pubmed_pmc
A3907, a systemic ASBT inhibitor, improves cholestasis in mice by multiorgan activity and shows translational relevance to humans
A3907, a systemic ASBT inhibitor, improves cholestasis in mice by multiorgan activity and shows translational relevance to humans Abstract Abstract Background and Aims: Cholestasis is characterized by intrahepatic accumulation of bile constituents, including bile acids (BAs), which promote liver damage. The apical sodi...
PMC10175790
core_pubmed_pmc
Pharmacokinetics and bioequivalence study of esomeprazole magnesium enteric-coated tablets 20 mg in healthy Chinese subjects under fasting and fed conditions
Pharmacokinetics and bioequivalence study of esomeprazole magnesium enteric-coated tablets 20 mg in healthy Chinese subjects under fasting and fed conditions Abstract Objective: The main purpose of this study was to evaluate the pharmacokinetics, bioequivalence, and safety properties between a new generic and a brand r...
PMC11206555
core_pubmed_pmc
Impact of Body Mass Index in the Cardioverter Efficacy of Amiodarone in Persistent Atrial Fibrillation
Impact of Body Mass Index in the Cardioverter Efficacy of Amiodarone in Persistent Atrial Fibrillation Abstract Background: Amiodarone is an anti-arrhythmic drug that has extensive tissue distribution and substantial storage in the fat tissue. Different studies have described some implications of body fat composition i...
PMC5798537
core_pubmed_pmc
Advances in the treatment of soft tissue sarcoma: focus on eribulin
Advances in the treatment of soft tissue sarcoma: focus on eribulin Abstract Abstract Eribulin mesylate is a synthetic derivative of halichondrin B isolated from a marine sponge. Its mechanism of action is through microtubule inhibition, which is different from that of taxanes. Eribulin has been approved for the treatm...
PMC12617623
core_pubmed_pmc
FRONTIER1 multiple ascending dose extension: a safety, tolerability, pharmacokinetics, and pharmacodynamics study of Mim8 in people with hemophilia A
FRONTIER1 multiple ascending dose extension: a safety, tolerability, pharmacokinetics, and pharmacodynamics study of Mim8 in people with hemophilia A Abstract Background Mim8 (denecimig) is a next-generation, factor VIIIa mimetic, human bispecific antibody for hemophilia A. Mim8 was well tolerated in the phase 1/2 FRON...
PMC10514181
core_pubmed_pmc
Pharmacokinetic and Exposure Response Analysis of the Double-Blind Randomized Study of Posaconazole and Voriconazole for Treatment of Invasive Aspergillosis
Pharmacokinetic and Exposure Response Analysis of the Double-Blind Randomized Study of Posaconazole and Voriconazole for Treatment of Invasive Aspergillosis Abstract Abstract Background and Objective A double-blind phase 3 study was conducted to compare posaconazole 300 mg intravenously (IV)/300 mg orally once daily (t...
PMC7904827
core_pubmed_pmc
Development of water-soluble prodrugs of the bisdioxopiperazine topoisomerase IIβ inhibitor ICRF-193 as potential cardioprotective agents against anthracycline cardiotoxicity
Development of water-soluble prodrugs of the bisdioxopiperazine topoisomerase IIβ inhibitor ICRF-193 as potential cardioprotective agents against anthracycline cardiotoxicity Abstract Abstract The bisdioxopiperazine topoisomerase IIβ inhibitor ICRF-193 has been previously identified as a more potent analog of dexrazoxa...
PMC7444137
core_pubmed_pmc
Initial dose recommendation for sirolimus in paediatric kaposiform haemangioendothelioma patients based on population pharmacokinetics and pharmacogenomics
Initial dose recommendation for sirolimus in paediatric kaposiform haemangioendothelioma patients based on population pharmacokinetics and pharmacogenomics Abstract Objective Sirolimus has been used to treat paediatric kaposiform haemangioendothelioma patients. However, there is considerable pharmacokinetic variability...
PMC8646822
core_pubmed_pmc
Understanding the clinical utility of favipiravir (T-705) in coronavirus disease of 2019: a review
Understanding the clinical utility of favipiravir (T-705) in coronavirus disease of 2019: a review Abstract The coronavirus disease of 2019 (COVID-19) has caused significant morbidity and mortality among infected individuals across the world. High transmissibility rate of the causative virus – Severe Acute Respiratory ...
PMC11597846
core_pubmed_pmc
Zingiber officinale Uncovered: Integrating Experimental and Computational Approaches to Antibacterial and Phytochemical Profiling
Zingiber officinale Uncovered: Integrating Experimental and Computational Approaches to Antibacterial and Phytochemical Profiling Abstract Abstract Background: Zingiber officinale rhizome is widely cultivated in the central region of Sudan (Gezira) and data on the biological properties of this variety grown in Sudan’s ...
PMC12743173
core_pubmed_pmc
Population Pharmacokinetic and Pharmacodynamic Prediction for Tebipenem Pivoxil Treatment of Pediatric Shigellosis
Population Pharmacokinetic and Pharmacodynamic Prediction for Tebipenem Pivoxil Treatment of Pediatric Shigellosis Abstract ABSTRACT Increasing antimicrobial resistance poses a serious challenge for the treatment of Shigella infections, and there is an urgent need for alternative antibacterial treatments. We conducted ...
PMC4811503
core_pubmed_pmc
A method for quantification of exportin-1 (XPO1) occupancy by Selective Inhibitor of Nuclear Export (SINE) compounds
A method for quantification of exportin-1 (XPO1) occupancy by Selective Inhibitor of Nuclear Export (SINE) compounds Abstract Selective Inhibitor of Nuclear Export (SINE) compounds are a family of small-molecules that inhibit nuclear export through covalent binding to cysteine 528 (Cys528) in the cargo-binding pocket o...
PMC7717049
core_pubmed_pmc
Population Pharmacokinetic Analysis and Exploratory Exposure–Bleeding Rate Relationship of Emicizumab in Adult and Pediatric Persons with Hemophilia A
Population Pharmacokinetic Analysis and Exploratory Exposure–Bleeding Rate Relationship of Emicizumab in Adult and Pediatric Persons with Hemophilia A Abstract Abstract Background Emicizumab is a bispecific monoclonal antibody developed for routine prophylaxis of bleeding in people with hemophilia A (PwHA). This work c...
PMC3608154
core_pubmed_pmc
Pharmacokinetics of a peroral single dose of two long-acting formulations and an aqueous formulation of doxycycline hyclate in horses
Pharmacokinetics of a peroral single dose of two long-acting formulations and an aqueous formulation of doxycycline hyclate in horses Abstract Abstract Background Doxycyline (Dox) is a semisynthetic antibacterial drug with pharmacological advantages over its parent drug (tetracycline) in the treatment of various bacter...
PMC7329762
core_pubmed_pmc
Oral Yohimbine as a New Probe Drug to Predict CYP2D6 Activity: Results of a Fixed-Sequence Phase I Trial
Oral Yohimbine as a New Probe Drug to Predict CYP2D6 Activity: Results of a Fixed-Sequence Phase I Trial Abstract Objective Yohimbine pharmacokinetics were determined after oral administration of a single oral dose of yohimbine 5 mg and a microdose of yohimbine 50 µg in relation to different cytochrome P450 ( CYP ) 2D6...
PMC9763385
core_pubmed_pmc
Low attainment to PK/PD-targets for β-lactams in a multi-center study on the first 72 h of treatment in ICU patients
Low attainment to PK/PD-targets for β-lactams in a multi-center study on the first 72 h of treatment in ICU patients Abstract Abstract Severe infections are life-threatening conditions commonly seen in the intensive care units (ICUs). Antibiotic treatment with adequate concentrations is of great importance during the f...
PMC3132875
core_pubmed_pmc
Effect of Administration of Moxifloxacin plus Rifampin against Mycobacterium tuberculosis for 7 of 7 Days versus 5 of 7 Days in an In Vitro Pharmacodynamic System
Effect of Administration of Moxifloxacin plus Rifampin against Mycobacterium tuberculosis for 7 of 7 Days versus 5 of 7 Days in an In Vitro Pharmacodynamic System Abstract ABSTRACT Some trials administered antituberculosis agents for 5 of 7 days (5/7-day regimen) to optimize adherence. Since moxifloxacin has a longer h...
PMC9345052
core_pubmed_pmc
Prophylactic surgery plus hyperthermic intraperitoneal chemotherapy (HIPEC CO2) versus standard surgery in colorectal carcinoma at high risk of peritoneal carcinomatosis: short-term and long-term outcomes from the CHECK study – protocol for a randomised, multicentre, phase 3 trial
Prophylactic surgery plus hyperthermic intraperitoneal chemotherapy (HIPEC CO2) versus standard surgery in colorectal carcinoma at high risk of peritoneal carcinomatosis: short-term and long-term outcomes from the CHECK study – protocol for a randomised, multicentre, phase 3 trial Abstract Abstract Introduction Up to o...
PMC10684480
core_pubmed_pmc
Natural compound targeting BDNF V66M variant: insights from in silico docking and molecular analysis
Natural compound targeting BDNF V66M variant: insights from in silico docking and molecular analysis Abstract Abstract Brain-Derived Neurotrophic Factor ( BDNF ) is a neurotrophin gene family gene that encodes proteins vital for the growth, maintenance, and survival of neurons in the nervous system. The study aimed to ...
PMC4621699
core_pubmed_pmc
Budesonide Foam Has a Favorable Safety Profile for Inducing Remission in Mild-to-Moderate Ulcerative Proctitis or Proctosigmoiditis
Budesonide Foam Has a Favorable Safety Profile for Inducing Remission in Mild-to-Moderate Ulcerative Proctitis or Proctosigmoiditis Abstract Abstract Background Budesonide foam, a rectally administered, second-generation corticosteroid with extensive hepatic first-pass metabolism, is efficacious for the treatment of mi...
PMC10892459
core_pubmed_pmc
The Status Quo of Pharmacogenomics of Tyrosine Kinase Inhibitors in Precision Oncology: A Bibliometric Analysis of the Literature
The Status Quo of Pharmacogenomics of Tyrosine Kinase Inhibitors in Precision Oncology: A Bibliometric Analysis of the Literature Abstract Abstract Precision oncology and pharmacogenomics (PGx) intersect in their overarching goal to institute the right treatment for the right patient. However, the translation of these ...
PMC11528546
core_pubmed_pmc
Do dietary interventions exert clinically important effects on the bioavailability of β-lactam antibiotics? A systematic review with meta-analyses
Do dietary interventions exert clinically important effects on the bioavailability of β-lactam antibiotics? A systematic review with meta-analyses Abstract Abstract Background Managing drug–food interactions may help to achieve the optimal action and safety profile of β-lactam antibiotics. Methods We conducted a system...
PMC7032962
core_pubmed_pmc
Performance of a mixture model by the degree of a missing categorical covariate when estimating clearance in NONMEM
Performance of a mixture model by the degree of a missing categorical covariate when estimating clearance in NONMEM Abstract Abstract The accuracy and predictability of mixture models in NONMEM® may change depending on the relative size of inter-individual differences and the size of the differences in the parameters b...
PMC10674160
core_pubmed_pmc
Synthesis and Preclinical Evaluation of Radiolabeled [ 103 Ru]BOLD-100
Synthesis and Preclinical Evaluation of Radiolabeled [ 103 Ru]BOLD-100 Abstract The first-in-class ruthenium-based chemotherapeutic agent BOLD-100 (formerly IT-139, NKP-1339, KP1339) is currently the subject of clinical evaluation for the treatment of gastric, pancreatic, colorectal and bile duct cancer. A radiolabeled...
PMC12367910
core_pubmed_pmc
High-resolution quantitative mapping of extracellular pH by ratiometric MRI with iron chelates in a tumor mouse model
High-resolution quantitative mapping of extracellular pH by ratiometric MRI with iron chelates in a tumor mouse model Abstract Abstract Purpose The aim of this study was to generate quantitative extracellular pH maps of tumors using a combination of a pH-sensitive iron chelate-based contrast agent (IBCA) and a pH-insen...
PMC3219006
core_pubmed_pmc
Recommended β-lactam regimens are inadequate in septic patients treated with continuous renal replacement therapy
Recommended β-lactam regimens are inadequate in septic patients treated with continuous renal replacement therapy Abstract Abstract Introduction Sepsis is responsible for important alterations in the pharmacokinetics of antibiotics. Continuous renal replacement therapy (CRRT), which is commonly used in septic patients,...
PMC10440458
core_pubmed_pmc
Oral treatment with the all- d -peptide RD2 enhances cognition in aged beagle dogs – A model of sporadic Alzheimer’s disease
Oral treatment with the all- d -peptide RD2 enhances cognition in aged beagle dogs – A model of sporadic Alzheimer’s disease Abstract Abstract Disease-modifying therapies to treat Alzheimer's disease (AD) are of fundamental interest for aging humans, societies, and health care systems. Predictable disease progression i...
PMC3792006
core_pubmed_pmc
Self-aggregated nanoparticles based on amphiphilic poly(lactic acid)-grafted-chitosan copolymer for ocular delivery of amphotericin B
Self-aggregated nanoparticles based on amphiphilic poly(lactic acid)-grafted-chitosan copolymer for ocular delivery of amphotericin B Abstract Abstract Background The purpose of this study was to develop a self-aggregated nanoparticulate vehicle using an amphiphilic poly(lactic acid)-grafted-chitosan (PLA-g-CS) copolym...
PMC7841297
core_pubmed_pmc
Time-Dependent Distribution of Hydroxychloroquine in Cynomolgus Macaques Using Population Pharmacokinetic Modeling Method
Time-Dependent Distribution of Hydroxychloroquine in Cynomolgus Macaques Using Population Pharmacokinetic Modeling Method Abstract To evaluate the biodistribution of hydroxychloroquine (HCQ) in cynomolgus macaques and receive dynamic quantitative relationship between plasma, blood, and lung tissue concentration using t...
PMC11919266
core_pubmed_pmc
A Multiple‐Model‐Informed Drug‐Development Approach for Optimal Regimen Selection of an Oncolytic Virus in Combination With Pembrolizumab
A Multiple‐Model‐Informed Drug‐Development Approach for Optimal Regimen Selection of an Oncolytic Virus in Combination With Pembrolizumab Abstract ABSTRACT The antitumor efficacy of an intratumoral injection of a genetically engineered oncolytic vaccinia virus carrying human IL‐7 and murine IL‐12 genes (hIL‐7/mIL‐12‐VV...
PMC12868246
core_pubmed_pmc
The microevolutionary trajectory of endemic multidrug-resistant tuberculosis strains in Portugal toward increased drug resistance levels and its clinical significance
The microevolutionary trajectory of endemic multidrug-resistant tuberculosis strains in Portugal toward increased drug resistance levels and its clinical significance Abstract Portugal has one of the highest incidence rates of tuberculosis (TB) in Western Europe and, historically, multidrug-resistant (MDR) cases have b...
PMC11695277
core_pubmed_pmc
Combining solubilization and controlled release strategies to prepare pH-sensitive solid dispersion loaded with albendazole: in vitro and in vivo studies
Combining solubilization and controlled release strategies to prepare pH-sensitive solid dispersion loaded with albendazole: in vitro and in vivo studies Abstract Albendazole (ABZ), classified as a class II basic drug under the Biopharmaceutics Classification System (BCS), is widely recognized for its therapeutic effic...
PMC9002453
core_pubmed_pmc
Rasagiline Pharmacokinetics in CYP1A2 Variant Healthy Smokers & Non-smokers in Different Doses
Rasagiline Pharmacokinetics in CYP1A2 Variant Healthy Smokers & Non-smokers in Different Doses Abstract Objectives: Rasagiline, a drug for Parkinson’s disease is metabolized by CYP1A2 enzyme. The objective of the study was to investigate the influence of cytochrome P450 1A2 variants and smoking status of healthy indivi...
PMC6956809
core_pubmed_pmc
Improving nanotherapy delivery and action through image-guided systems pharmacology
Improving nanotherapy delivery and action through image-guided systems pharmacology Abstract Abstract Despite recent advances in the translation of therapeutic nanoparticles (TNPs) into the clinic, the field continues to face challenges in predictably and selectively delivering nanomaterials for the treatment of solid ...
PMC9287616
core_pubmed_pmc
Dynamics of tumor-associated macrophages in a quantitative systems pharmacology model of immunotherapy in triple-negative breast cancer
Dynamics of tumor-associated macrophages in a quantitative systems pharmacology model of immunotherapy in triple-negative breast cancer Abstract Summary Quantitative systems pharmacology (QSP) modeling is an emerging mechanistic computational approach that couples drug pharmacokinetics/pharmacodynamics and the course o...
PMC11134224
core_pubmed_pmc
The estimation and translation uncertainties in applying NOAEL to clinical dose escalation
The estimation and translation uncertainties in applying NOAEL to clinical dose escalation Abstract Abstract The systemic exposure at the no‐observed‐adverse‐effect‐level (NOAEL) estimated from animals is an important criterion commonly applied to guard the safety of participants in clinical trials of investigational d...
PMC10720538
core_pubmed_pmc
Population pharmacokinetic modeling and target attainment analyses of rezafungin for the treatment of candidemia and invasive candidiasis
Population pharmacokinetic modeling and target attainment analyses of rezafungin for the treatment of candidemia and invasive candidiasis Abstract ABSTRACT Rezafungin is a chemically and metabolically stable echinocandin with a longer half-life than other echinocandins, allowing for a once-weekly intravenous infusion v...
PMC12598906
core_pubmed_pmc
Effect of Gender on the Pharmacokinetics of Meloxicam in Sheep
Effect of Gender on the Pharmacokinetics of Meloxicam in Sheep Abstract ABSTRACT The objective of this investigation was to ascertain the impact of gender on the pharmacokinetics of meloxicam in sheep. The research was carried out on six female and six male Romanov sheep. Meloxicam was administered intravenously to she...
PMC4908408
core_pubmed_pmc
Human Food Safety Implications of Variation in Food Animal Drug Metabolism
Human Food Safety Implications of Variation in Food Animal Drug Metabolism Abstract Abstract Violative drug residues in animal-derived foods are a global food safety concern. The use of a fixed main metabolite to parent drug (M/D) ratio determined in healthy animals to establish drug tolerances and withdrawal times in ...
PMC8228246
core_pubmed_pmc
Highly Potent GalNAc-Conjugated Tiny LNA Anti-miRNA-122 Antisense Oligonucleotides
Highly Potent GalNAc-Conjugated Tiny LNA Anti-miRNA-122 Antisense Oligonucleotides Abstract The development of clinically relevant anti-microRNA antisense oligonucleotides (anti-miRNA ASOs) remains a major challenge. One promising configuration of anti-miRNA ASOs called “tiny LNA (tiny Locked Nucleic Acid)” is an unusu...
PMC5997317
core_pubmed_pmc
Artemether-lumefantrine dosing for malaria treatment in young children and pregnant women: A pharmacokinetic-pharmacodynamic meta-analysis
Artemether-lumefantrine dosing for malaria treatment in young children and pregnant women: A pharmacokinetic-pharmacodynamic meta-analysis Abstract Background The fixed dose combination of artemether-lumefantrine (AL) is the most widely used treatment for uncomplicated Plasmodium falciparum malaria. Relatively lower cu...
PMC11449231
core_pubmed_pmc
Slow clearance of histidine-rich protein-2 in Gabonese with uncomplicated malaria
Slow clearance of histidine-rich protein-2 in Gabonese with uncomplicated malaria Abstract ABSTRACT Malaria rapid diagnostic tests (RDTs), which detect Plasmodium falciparum (Pf)-specific histidine-rich protein-2 (HRP2), have increasing importance for the diagnosis and control of malaria, especially also in regions whe...