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PMC5477375
core_pubmed_pmc
Cancer chemoprevention through dietary flavonoids: what’s limiting?
Cancer chemoprevention through dietary flavonoids: what’s limiting? Abstract Abstract Flavonoids are polyphenols that are found in numerous edible plant species. Data obtained from preclinical and clinical studies suggest that specific flavonoids are chemo-preventive and cytotoxic against various cancers via a multitud...
PMC12859431
core_pubmed_pmc
Mezigdomide combined with bortezomib disrupts the cell cycle and elicits superior antitumor effects in multiple myeloma
Mezigdomide combined with bortezomib disrupts the cell cycle and elicits superior antitumor effects in multiple myeloma Abstract Key Points • The combination of MEZI with BTZ increases cell death through disruption of the cell cycle. • The combination of MEZI/BTZ/DEX demonstrates superior efficacy compared with POM/BTZ...
PMC6263667
core_pubmed_pmc
PBPK Modeling of Coproporphyrin I as an Endogenous Biomarker for Drug Interactions Involving Inhibition of Hepatic OATP1B1 and OATP1B3
PBPK Modeling of Coproporphyrin I as an Endogenous Biomarker for Drug Interactions Involving Inhibition of Hepatic OATP1B1 and OATP1B3 Abstract Abstract The aim of the present study was to establish a physiologically based pharmacokinetic (PBPK) model for coproporphyrin I (CP‐I), a biomarker supporting the prediction o...
PMC7943388
core_pubmed_pmc
Environmental impact assessment of COVID-19 therapeutic solutions. A prospective analysis
Environmental impact assessment of COVID-19 therapeutic solutions. A prospective analysis Abstract Several medicinal products for human use are currently under consideration as potential treatment for COVID-19 pandemic. As proposals cover also prophylactic use, the treatment could be massive, resulting in unprecedent l...
PMC9293201
core_pubmed_pmc
Physiologically Based Pharmacokinetic Modeling to Assess the Impact of CYP2D6‐Mediated Drug‐Drug Interactions on Tramadol and O‐Desmethyltramadol Exposures via Allosteric and Competitive Inhibition
Physiologically Based Pharmacokinetic Modeling to Assess the Impact of CYP2D6‐Mediated Drug‐Drug Interactions on Tramadol and O‐Desmethyltramadol Exposures via Allosteric and Competitive Inhibition Abstract Abstract Tramadol is an opioid medication used to treat moderately severe pain. Cytochrome P450 (CYP) 2D6 inhibit...
PMC8675232
core_pubmed_pmc
Reduction in C-Peptide Levels and Influence on Pharmacokinetics and Pharmacodynamics of Insulin Preparations: How to Conduct a High-Quality Euglycemic Clamp Study
Reduction in C-Peptide Levels and Influence on Pharmacokinetics and Pharmacodynamics of Insulin Preparations: How to Conduct a High-Quality Euglycemic Clamp Study Abstract Abstract Objective: The aim of the study was to investigate the different extent of inhibition of endogenous insulin secretion by the reduction of C...
PMC10476617
core_pubmed_pmc
The Effect of Dihydromyricetin on the Pharmacokinetics of Fluconazole in Sprague-Dawley Rat Plasma, Based on High-Performance Liquid Chromatography–Tandem Mass Spectrometry
The Effect of Dihydromyricetin on the Pharmacokinetics of Fluconazole in Sprague-Dawley Rat Plasma, Based on High-Performance Liquid Chromatography–Tandem Mass Spectrometry Abstract Abstract Background The synergistic effect of dihydromyricetin (DHM) and fluconazole (FLC) can improve the killing effect of FLC-resistant...
PMC7392740
core_pubmed_pmc
Randomized, Parallel Group, Open-Label Bioequivalence Trial of Intramuscular Pegaspargase in Patients With Relapsed Acute Lymphoblastic Leukemia
Randomized, Parallel Group, Open-Label Bioequivalence Trial of Intramuscular Pegaspargase in Patients With Relapsed Acute Lymphoblastic Leukemia Abstract PURPOSE Pegylated asparaginase is comparatively safer than native asparaginase in the management of acute lymphoblastic leukemia (ALL). However, the high price and no...
PMC12239076
core_pubmed_pmc
Antitumor Efficacy, Pharmacokinetics, and Toxicity Studies of Novel Estrogen Receptors Targeted PEGylated Liposomes Encapsulating Paclitaxel and Cisplatin in SKOV‑3 Tumor-Bearing Nude Mice, ICR Mice, and SD Rats
Antitumor Efficacy, Pharmacokinetics, and Toxicity Studies of Novel Estrogen Receptors Targeted PEGylated Liposomes Encapsulating Paclitaxel and Cisplatin in SKOV‑3 Tumor-Bearing Nude Mice, ICR Mice, and SD Rats Abstract Ovarian malignancies overexpress estrogen receptors (ERs), offering a therapeutic avenue for target...
PMC6061395
core_pubmed_pmc
A Pharmacometric Approach to Substitute for a Conventional Dose-Finding Study in Rare Diseases: Example of Phase III Dose Selection for Emicizumab in Hemophilia A
A Pharmacometric Approach to Substitute for a Conventional Dose-Finding Study in Rare Diseases: Example of Phase III Dose Selection for Emicizumab in Hemophilia A Abstract Background Emicizumab (ACE910) is a bispecific antibody mimicking the cofactor function of activated coagulation factor VIII. In phase I–I/II studie...
PMC5394946
core_pubmed_pmc
Population pharmacokinetics of intravenous Erwinia asparaginase in pediatric acute lymphoblastic leukemia patients
Population pharmacokinetics of intravenous Erwinia asparaginase in pediatric acute lymphoblastic leukemia patients Abstract Abstract Erwinia asparaginase is an important component in the treatment of pediatric acute lymphoblastic leukemia. A large variability in serum concentrations has been observed after intravenous ...
PMC11196403
core_pubmed_pmc
Development and validation of UPLC-MS/MS method for icariin and its metabolites in mouse urine
Development and validation of UPLC-MS/MS method for icariin and its metabolites in mouse urine Abstract Abstract An ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) method was utilized to develop a technique for the simultaneous quantification of icariin and its primary metabolites in mouse...
PMC7136483
core_pubmed_pmc
Integrated Data Analysis of Six Clinical Studies Points Toward Model-Informed Precision Dosing of Tamoxifen
Integrated Data Analysis of Six Clinical Studies Points Toward Model-Informed Precision Dosing of Tamoxifen Abstract Abstract Introduction At tamoxifen standard dosing, ∼20% of breast cancer patients do not reach proposed target endoxifen concentrations >5.97 ng/mL. Thus, better understanding the large interindividual ...
PMC6160876
core_pubmed_pmc
Influence of sevoflurane anesthesia with mechanical ventilation and fluid-therapy on distribution of subcutaneously administered robenacoxib in dogs
Influence of sevoflurane anesthesia with mechanical ventilation and fluid-therapy on distribution of subcutaneously administered robenacoxib in dogs Abstract Abstract Robenacoxib is a novel nonsteroidal anti-inflammatory drug approved for dogs. The present study aimed to evaluate influences of sevoflurane anesthesia on...
PMC3898195
core_pubmed_pmc
Comparative Bioavailability and Tolerability of Single and Multiple Doses of 2 Diclofenac Sodium Sustained-Release Tablet Formulations in Fasting, Healthy Chinese Male Volunteers ☆
Comparative Bioavailability and Tolerability of Single and Multiple Doses of 2 Diclofenac Sodium Sustained-Release Tablet Formulations in Fasting, Healthy Chinese Male Volunteers ☆ Abstract Abstract Background Diclofenac is a nonsteroidal anti-inflammatory drug used for the treatment of patients with osteoarthritis. Ob...
PMC9255589
core_pubmed_pmc
Caplacizumab Model‐Based Dosing Recommendations in Pediatric Patients With Acquired Thrombotic Thrombocytopenic Purpura
Caplacizumab Model‐Based Dosing Recommendations in Pediatric Patients With Acquired Thrombotic Thrombocytopenic Purpura Abstract Abstract Acquired thrombotic thrombocytopenic purpura (aTTP) is a rare and life‐threatening autoimmune thrombotic microangiopathy. Caplacizumab, evaluated in phase II and III studies in adult...
PMC5344293
core_pubmed_pmc
A phase 1 dose-escalation and expansion study of binimetinib (MEK162), a potent and selective oral MEK1/2 inhibitor
A phase 1 dose-escalation and expansion study of binimetinib (MEK162), a potent and selective oral MEK1/2 inhibitor Abstract Background: Binimetinib (MEK162; ARRY-438162) is a potent and selective oral MEK 1/2 inhibitor. This phase 1 study determined the maximum tolerated dose (MTD), safety, pharmacokinetic and pharmac...
PMC5736852
core_pubmed_pmc
Global population pharmacokinetics of the investigational Aurora A kinase inhibitor alisertib in cancer patients: rationale for lower dosage in Asia
Global population pharmacokinetics of the investigational Aurora A kinase inhibitor alisertib in cancer patients: rationale for lower dosage in Asia Abstract Aims This population pharmacokinetic analysis was conducted to describe quantitatively the regional differences and sources of interpatient variability on the app...
PMC10684621
core_pubmed_pmc
Pharmacokinetics and Tolerability of Zibotentan in Patients with Concurrent Moderate Renal and Moderate Hepatic Impairment
Pharmacokinetics and Tolerability of Zibotentan in Patients with Concurrent Moderate Renal and Moderate Hepatic Impairment Abstract Abstract Background and Objective Zibotentan, a selective endothelin A receptor antagonist, is in development for chronic liver and kidney disease. The pharmacokinetics (PK) of zibotentan ...
PMC8909728
core_pubmed_pmc
Pharmacogenomics Testing in Phase I Oncology Clinical Trials: Constructive Criticism Is Warranted
Pharmacogenomics Testing in Phase I Oncology Clinical Trials: Constructive Criticism Is Warranted Abstract Simple Summary Phase I clinical trials are a cornerstone of pharmaceutical development in oncology. Many studies have now attempted to incorporate pharmacogenomics into phase I studies; however, many of these stud...
PMC11241437
core_pubmed_pmc
Structure-Based Analysis of Cefaclor Pharmacokinetic Diversity According to Human Peptide Transporter-1 Genetic Polymorphism
Structure-Based Analysis of Cefaclor Pharmacokinetic Diversity According to Human Peptide Transporter-1 Genetic Polymorphism Abstract Cefaclor is a substrate of human-peptide-transporter-1 (PEPT1), and the impact of inter-individual pharmacokinetic variation due to genetic polymorphisms of solute-carrier-family-15-memb...
PMC6305520
core_pubmed_pmc
Bioequivalence evaluation of two 5% ceftiofur hydrochloride sterile suspension in pigs
Bioequivalence evaluation of two 5% ceftiofur hydrochloride sterile suspension in pigs Abstract Abstract The purpose of this study was to evaluate the bioequivalence of 5% ceftiofur hydrochloride sterile suspension in two formulations, a test formulation (Saifukang 5% CEF, Hvsen) and a reference formulation (Excenel ® ...
PMC4873483
core_pubmed_pmc
Pharmacokinetics of 1-methyl-L-tryptophan after single and repeated subcutaneous application in a porcine model
Pharmacokinetics of 1-methyl-L-tryptophan after single and repeated subcutaneous application in a porcine model Abstract Increased activity of the tryptophan-metabolizing enzyme indoleamine 2,3-dioxygenase (IDO) is associated with immunological and neurological disorders, and inhibition of its enzyme activity could be ...
PMC8866625
core_pubmed_pmc
Assessment of mouse-specific pharmacokinetics in kidneys based on 131 I activity measurements using micro-SPECT
Assessment of mouse-specific pharmacokinetics in kidneys based on 131 I activity measurements using micro-SPECT Abstract Abstract Background In order to acquire accurate drug pharmacokinetic information, which is required for tissue dosimetry, micro-SPECT must be quantitative to allow for an accurate assessment of radi...
PMC11359485
core_pubmed_pmc
Innovative Approaches to Optimize Clinical Transporter Drug–Drug Interaction Studies
Innovative Approaches to Optimize Clinical Transporter Drug–Drug Interaction Studies Abstract Abstract Of the 450 cell membrane transporters responsible for shuttling substrates, nutrients, hormones, neurotransmitters, antioxidants, and signaling molecules, approximately nine are associated with clinically relevant dru...
PMC10577379
core_pubmed_pmc
Isolation of anticancer bioactive secondary metabolites from the sponge-derived endophytic fungi Penicillium sp . and in-silico computational docking approach
Isolation of anticancer bioactive secondary metabolites from the sponge-derived endophytic fungi Penicillium sp . and in-silico computational docking approach Abstract Introduction Fungus-derived secondary metabolites are fascinating with biomedical potential and chemical diversity. Mining endophytic fungi for drug can...
PMC12590001
core_pubmed_pmc
Development of the FGFR4-ADC bearing the ferroptosis inducer sulfasalazine for hepatocellular carcinoma
Development of the FGFR4-ADC bearing the ferroptosis inducer sulfasalazine for hepatocellular carcinoma Abstract Summary Hepatocellular carcinoma (HCC), the most prevalent liver cancer, accounts for ∼90% of all cases. Despite antibody-drug conjugates (ADCs) showing significant efficacy in treating various hematologic m...
PMC11823646
core_pubmed_pmc
Population pharmacokinetics of caspofungin in critically ill patients receiving extracorporeal membrane oxygenation—an ASAP ECMO study
Population pharmacokinetics of caspofungin in critically ill patients receiving extracorporeal membrane oxygenation—an ASAP ECMO study Abstract ABSTRACT This study aimed to describe the population pharmacokinetics of caspofungin in critically ill patients receiving extracorporeal membrane oxygenation (ECMO) and to iden...
PMC10146820
core_pubmed_pmc
ADME, Pharmacokinetic Scaling, Pharmacodynamic and Prediction of Human Dose and Regimen of Novel Antiviral Drugs
ADME, Pharmacokinetic Scaling, Pharmacodynamic and Prediction of Human Dose and Regimen of Novel Antiviral Drugs Abstract The search for new drugs is an extremely time-consuming and expensive endeavour. Much of that time and money go into generating predictive human pharmacokinetic profiles from preclinical efficacy an...
PMC3082690
core_pubmed_pmc
The role of population PK–PD modelling in paediatric clinical research
The role of population PK–PD modelling in paediatric clinical research Abstract Abstract Children differ from adults in their response to drugs. While this may be the result of changes in dose exposure (pharmacokinetics [PK]) and/or exposure response (pharmacodynamics [PD]) relationships, the magnitude of these changes...
PMC7066095
core_pubmed_pmc
Dotinurad: a clinical pharmacokinetic study of a novel, selective urate reabsorption inhibitor in subjects with hepatic impairment
Dotinurad: a clinical pharmacokinetic study of a novel, selective urate reabsorption inhibitor in subjects with hepatic impairment Abstract Abstract Background Dotinurad is a novel, selective urate reabsorption inhibitor, which reduces serum uric acid levels by inhibiting the urate transporter 1 (URAT1). We compared th...
PMC12374872
core_pubmed_pmc
A comparison between venous blood sampling and capillary volumetric absorptive microsampling for antibiotics levels monitoring in individuals with and without periodontal disease
A comparison between venous blood sampling and capillary volumetric absorptive microsampling for antibiotics levels monitoring in individuals with and without periodontal disease Abstract Abstract Objectives We aimed to compare the antibiotic concentrations obtained using the volumetric absorptive microsampling (VAMS) ...
PMC9314272
core_pubmed_pmc
Dose Finding in Oncology: What is Impeding Coming of Age?
Dose Finding in Oncology: What is Impeding Coming of Age? Abstract Abstract After a drug molecule enters clinical trials, there are primarily three levers to enhance probability of success: patient selection, dose selection and choice of combination agents. Of these, dose selection remains an under-appreciated aspect i...
PMC9577085
core_pubmed_pmc
Design and evaluation of rufinamide nanocrystals loaded thermoresponsive nasal in situ gelling system for improved drug distribution to brain
Design and evaluation of rufinamide nanocrystals loaded thermoresponsive nasal in situ gelling system for improved drug distribution to brain Abstract Abstract Rufinamide (Rufi) is an antiepileptic drug used to manage Lennox-Gastaut Syndrome and partial seizures. The oral bioavailability of Rufi is less due to its poor...
PMC3830644
core_pubmed_pmc
Pharmacodynamic study of Disulfiram in Men with Non-metastatic Recurrent Prostate Cancer
Pharmacodynamic study of Disulfiram in Men with Non-metastatic Recurrent Prostate Cancer Abstract Background Preclinical drug screens identified disulfiram as a potent in vitro inhibitor of prostate cancer cell growth. Although many mechanisms for its anticancer activity have been proposed, tumor suppressor gene re-exp...
PMC10143751
core_pubmed_pmc
In Silico Analyses of a Promising Drug Candidate for the Treatment of Amyotrophic Lateral Sclerosis Targeting Superoxide Dismutase I Protein
In Silico Analyses of a Promising Drug Candidate for the Treatment of Amyotrophic Lateral Sclerosis Targeting Superoxide Dismutase I Protein Abstract Amyotrophic lateral sclerosis (ALS) is the most prevalent motor neuron disorder in adults, which is associated with a highly disabling condition. To date, ALS remains inc...
PMC11410373
core_pubmed_pmc
The Dosage of Muscle Relaxants in Morbidly Obese Patients in Daily Practice – A Narrative Review
The Dosage of Muscle Relaxants in Morbidly Obese Patients in Daily Practice – A Narrative Review Abstract Abstract The prevalence of morbid obesity in today’s population around the world is alarming. Morbid obesity involves substantial changes in body composition and function, which can affect the pharmacodynamics and ...
PMC10269160
core_pubmed_pmc
Phase I Single Ascending Dose and Food Effect Study in Healthy Adults and Phase I/IIa Multiple Ascending Dose Study in Patients with Pulmonary Tuberculosis to Assess Pharmacokinetics, Bactericidal Activity, Tolerability, and Safety of OPC-167832
Phase I Single Ascending Dose and Food Effect Study in Healthy Adults and Phase I/IIa Multiple Ascending Dose Study in Patients with Pulmonary Tuberculosis to Assess Pharmacokinetics, Bactericidal Activity, Tolerability, and Safety of OPC-167832 Abstract ABSTRACT OPC-167832, an inhibitor of decaprenylphosphoryl-β- d -r...
PMC7982063
core_pubmed_pmc
Pharmacogenomics biomarkers for personalized methadone maintenance treatment: The mechanism and its potential use
Pharmacogenomics biomarkers for personalized methadone maintenance treatment: The mechanism and its potential use Abstract Methadone has a wide pharmacokinetic interindividual variability, resulting in unpredicted treatment response. Pharmacogenomic biomarkers seem promising for personalized methadone maintenance treat...
PMC11206329
core_pubmed_pmc
Fluconazole Analogs and Derivatives: An Overview of Synthesis, Chemical Transformations, and Biological Activity
Fluconazole Analogs and Derivatives: An Overview of Synthesis, Chemical Transformations, and Biological Activity Abstract Abstract Fluconazole (2-(2,4-difluorophenyl)-1,3-bis(1 H -1,2,4-triazol-1-yl)propan-2-ol), which was patented in 1981 and introduced for commercial use in 1988, is a widely utilized antifungal drug ...
PMC11825798
core_pubmed_pmc
Metformin dosage and galectin-3 levels: insights from PCOS patients preparing for IVF
Metformin dosage and galectin-3 levels: insights from PCOS patients preparing for IVF Abstract Abstract This study explores the impact of metformin dosage and hyperprolactinemia on galectin-3 levels in women with Polycystic Ovary Syndrome (PCOS), providing novel insights into their roles in the metabolic and hormonal m...
PMC9411638
core_pubmed_pmc
Pharmacokinetics of Dantrolene in the Plasma Exchange Treatment of Malignant Hyperthermia in a 14-Year-Old Chinese Boy: A Case Report and Literature Review
Pharmacokinetics of Dantrolene in the Plasma Exchange Treatment of Malignant Hyperthermia in a 14-Year-Old Chinese Boy: A Case Report and Literature Review Abstract Abstract Malignant hyperthermia (MH) is a rare life-threatening response that is triggered by exposure to specific anesthetics commonly used during surgica...
PMC12473915
core_pubmed_pmc
Smoking Topography, Nicotine Kinetics, and Subjective Smoking Experience of Mentholated and Non-Mentholated Heated Tobacco Products in Occasional Smokers
Smoking Topography, Nicotine Kinetics, and Subjective Smoking Experience of Mentholated and Non-Mentholated Heated Tobacco Products in Occasional Smokers Abstract Background: Heated tobacco products (HTPs) are marketed as reduced-harm alternatives to conventional cigarettes (CCs) and are increasingly used by young adul...
PMC9540525
core_pubmed_pmc
Clinical activity of CC‐90011, an oral, potent, and reversible LSD1 inhibitor, in advanced malignancies
Clinical activity of CC‐90011, an oral, potent, and reversible LSD1 inhibitor, in advanced malignancies Abstract Abstract Background CC‐90011 is an oral, potent, selective, reversible inhibitor of lysine‐specific demethylase 1 (LSD1) that was well tolerated, with encouraging activity in patients who had advanced solid ...
PMC11388068
core_pubmed_pmc
Amide naphthotube as a novel supramolecular sequestration agent for tetracaine and decamethonium
Amide naphthotube as a novel supramolecular sequestration agent for tetracaine and decamethonium Abstract Abstract Rationale: Anesthetics are widely used for optimizing surgical conditions, postoperative pain management, and treating various chronic pain conditions. Tetracaine and decamethonium are representative drugs...
PMC11540874
core_pubmed_pmc
Pharmacokinetics and brain uptake of sodium selenate and selenium in naïve rats and a lateral fluid percussion injury rat model
Pharmacokinetics and brain uptake of sodium selenate and selenium in naïve rats and a lateral fluid percussion injury rat model Abstract Abstract Post‐traumatic epilepsy (PTE) is a life‐long complication of traumatic brain injury (TBI). The development of PTE is associated with neurological morbidity and increases the ...
PMC12671102
core_pubmed_pmc
Safety, Tolerability, Pharmacokinetics, Pharmacodynamics, and Food Effects of Single and Multiple Oral Doses of ABP-671 in Healthy and Hyperuricemic Subjects
Safety, Tolerability, Pharmacokinetics, Pharmacodynamics, and Food Effects of Single and Multiple Oral Doses of ABP-671 in Healthy and Hyperuricemic Subjects Abstract Abstract Purpose To evaluate the safety, tolerability, pharmacokinetics (PK), pharmacodynamics (PD), and food effects of single and multiple oral doses o...
PMC10029972
core_pubmed_pmc
A Novel Strategy for Liposomal Drug Separation in Plasma by TiO 2 Microspheres and Application in Pharmacokinetics
A Novel Strategy for Liposomal Drug Separation in Plasma by TiO 2 Microspheres and Application in Pharmacokinetics Abstract Abstract Purpose Liposomes are nano-scale materials with a biofilm-like structure. They have excellent biocompatibility and are increasingly useful in drug delivery systems. However, the in vivo f...
PMC7165800
core_pubmed_pmc
Phase 1 Study of Molibresib (GSK525762), a Bromodomain and Extra-Terminal Domain Protein Inhibitor, in NUT Carcinoma and Other Solid Tumors
Phase 1 Study of Molibresib (GSK525762), a Bromodomain and Extra-Terminal Domain Protein Inhibitor, in NUT Carcinoma and Other Solid Tumors Abstract Abstract Background Bromodomain and extra-terminal domain proteins are promising epigenetic anticancer drug targets. This first-in-human study evaluated the safety, recomm...
PMC9314939
core_pubmed_pmc
Dose banding – Weighing up benefits, risks and therapeutic failure
Dose banding – Weighing up benefits, risks and therapeutic failure Abstract Aims Dose banding is a method of dose individualisation in which all patients with similar characteristics are allocated to the same dose. Dose banding results in some patients receiving less intensive treatment which risks a reduction in thera...
PMC9784526
core_pubmed_pmc
Total and Unbound Pharmacokinetics of Cefiderocol in Critically Ill Patients
Total and Unbound Pharmacokinetics of Cefiderocol in Critically Ill Patients Abstract Abstract Background: Cefiderocol is a siderophore cephalosporin antibiotic active against Gram-negative bacteria, including extended-spectrum beta-lactamase and carbapenemase-producing strains. The pharmacokinetics of cefiderocol has ...
PMC9222498
core_pubmed_pmc
Macrophage membrane-biomimetic adhesive polycaprolactone nanocamptothecin for improving cancer-targeting efficiency and impairing metastasis
Macrophage membrane-biomimetic adhesive polycaprolactone nanocamptothecin for improving cancer-targeting efficiency and impairing metastasis Abstract Abstract The recent remarkable success and safety of mRNA lipid nanoparticle technology for producing severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) vaccine...
PMC9549831
core_pubmed_pmc
Evaluation of drug interactions of saxagliptin with sildenafil in healthy volunteers
Evaluation of drug interactions of saxagliptin with sildenafil in healthy volunteers Abstract Purpose The purpose of this study is to investigate the effect of sildenafil a CYP3A4 substrate and inhibitor on the pharmacokinetics and safety of saxagliptin. Methods Eighteen healthy volunteers were recruited in sequential;...
PMC12330068
core_pubmed_pmc
First-in-human study of neuron regenerative therapy NNI-362 to evaluate the safety, pharmacokinetics, and pharmacodynamics in healthy aged population
First-in-human study of neuron regenerative therapy NNI-362 to evaluate the safety, pharmacokinetics, and pharmacodynamics in healthy aged population Abstract Abstract Background A placebo-controlled, double-blind Phase 1a trial examined the safety, tolerability, and pharmacokinetics of NNI-362 as well as the pharmacod...
PMC12193158
core_pubmed_pmc
Anticoagulation in Patients with End-Stage Renal Disease: A Critical Review
Anticoagulation in Patients with End-Stage Renal Disease: A Critical Review Abstract Background: Chronic kidney disease (CKD) and its advanced stage, end-stage renal disease (ESRD), affect millions worldwide and are associated with a paradoxical hemostatic imbalance—marked by both increased thrombotic and bleeding risk...
PMC7038258
core_pubmed_pmc
Pharmacokinetics and Tolerability of Intravenous Sulbactam-Durlobactam with Imipenem-Cilastatin in Hospitalized Adults with Complicated Urinary Tract Infections, Including Acute Pyelonephritis
Pharmacokinetics and Tolerability of Intravenous Sulbactam-Durlobactam with Imipenem-Cilastatin in Hospitalized Adults with Complicated Urinary Tract Infections, Including Acute Pyelonephritis Abstract Durlobactam (DUR; ETX2514) is a novel β-lactamase inhibitor with broad-spectrum activity against Ambler class A, C, an...
PMC12115119
core_pubmed_pmc
Coumarins in Anticancer Therapy: Mechanisms of Action, Potential Applications and Research Perspectives
Coumarins in Anticancer Therapy: Mechanisms of Action, Potential Applications and Research Perspectives Abstract Abstract Coumarins are natural organic compounds widely found in plants that show promising anticancer properties. This article reviews the current research on the mechanisms of action of coumarins in cancer...
PMC6647993
core_pubmed_pmc
Poly(ethylene glycol)-Based Peptidomimetic “PEGtide” of Oligo-Arginine Allows for Efficient siRNA Transfection and Gene Inhibition
Poly(ethylene glycol)-Based Peptidomimetic “PEGtide” of Oligo-Arginine Allows for Efficient siRNA Transfection and Gene Inhibition Abstract Abstract While a wide range of experimental and commercial transfection reagents are currently available, persistent problems remain regarding their suitability for continued devel...
PMC9108585
core_pubmed_pmc
Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of the Positive Modulator of HGF/MET, Fosgonimeton, in Healthy Volunteers and Subjects with Alzheimer’s Disease: Randomized, Placebo-Controlled, Double-Blind, Phase I Clinical Trial
Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of the Positive Modulator of HGF/MET, Fosgonimeton, in Healthy Volunteers and Subjects with Alzheimer’s Disease: Randomized, Placebo-Controlled, Double-Blind, Phase I Clinical Trial Abstract Abstract Background: Fosgonimeton (ATH-1017) is being developed as a...
PMC9732544
core_pubmed_pmc
Fibroblast growth factor 2 is a druggable target against glioblastoma: A computational investigation
Fibroblast growth factor 2 is a druggable target against glioblastoma: A computational investigation Abstract Fibroblast growth factor 2 (FGF2) is a key player in cancer and tissue homeostasis and regulates renewal of several stem cell types. The FGF2 role in malignant glioma is proven and tagged FGF2, a novel druggabl...
PMC12104660
core_pubmed_pmc
Global research on the utilization of population pharmacokinetic model: a bibliometric analysis from 2000 to 2024
Global research on the utilization of population pharmacokinetic model: a bibliometric analysis from 2000 to 2024 Abstract Abstract Objective Population pharmacokinetic (PPK) model is capable of identifying the factors that influence the variability of pharmacokinetic (PK) profiles and the degree of their influence, ef...
PMC6787861
core_pubmed_pmc
A nonlinear mixed‐effects modeling approach for ecological data: Using temporal dynamics of vegetation moisture as an example
A nonlinear mixed‐effects modeling approach for ecological data: Using temporal dynamics of vegetation moisture as an example Abstract Abstract Increasingly, often ecologist collects data with nonlinear trends, heterogeneous variances, temporal correlation, and hierarchical structure. Nonlinear mixed‐effects models off...
PMC9306507
core_pubmed_pmc
Acute response to cholinergic challenge predicts long‐term response to galantamine treatment in patients with Alzheimer's disease
Acute response to cholinergic challenge predicts long‐term response to galantamine treatment in patients with Alzheimer's disease Abstract Aims Cholinesterase inhibitors (CEIs) have been shown to improve cognitive functioning in Alzheimer's disease (AD) patients, but are associated with multiple side effects and only 2...
PMC11354571
core_pubmed_pmc
Advancements in Telomerase-Targeted Therapies for Glioblastoma: A Systematic Review
Advancements in Telomerase-Targeted Therapies for Glioblastoma: A Systematic Review Abstract Glioblastoma (GBM) is a primary CNS tumor that is highly lethal in adults and has limited treatment options. Despite advancements in understanding the GBM biology, the standard treatment for GBM has remained unchanged for more ...
PMC12415664
core_pubmed_pmc
Nanobubble-Enhanced Oral Delivery of Bortezomib: Optimizing Preparation and Characterization through Design of Experiment (DOE)
Nanobubble-Enhanced Oral Delivery of Bortezomib: Optimizing Preparation and Characterization through Design of Experiment (DOE) Abstract Objectives Bortezomib (BTZ) functions as an androgen receptor signalling inhibitor, is used for the treatment of prostate cancer, and has been sanctioned by the United States Food and...
PMC3322959
core_pubmed_pmc
A phase I, dose-escalation study of TB-403, a monoclonal antibody directed against PlGF, in patients with advanced solid tumours
A phase I, dose-escalation study of TB-403, a monoclonal antibody directed against PlGF, in patients with advanced solid tumours Abstract Background: TB-403 (RO 5323441), a humanised monoclonal antibody, is a novel antiangiogenesis agent directed against placental growth factor. The safety, pharmacokinetics (PK), and a...
PMC9305487
core_pubmed_pmc
Pharmacokinetic Differences of Wuji Pill Components in Normal and Chronic Visceral Hypersensitivity Irritable Bowel Syndrome Rats Attributable to Changes in Tight Junction and Transporters
Pharmacokinetic Differences of Wuji Pill Components in Normal and Chronic Visceral Hypersensitivity Irritable Bowel Syndrome Rats Attributable to Changes in Tight Junction and Transporters Abstract Abstract The Wuji pill, also called Wuji Wan (WJW), is an effective traditional medicine for the clinical treatment of irr...
PMC9889864
core_pubmed_pmc
Exploration of sodium homeostasis and pharmacokinetics in bile duct-ligated rats treated by anti-cirrhosis herbal formula plus spironolactone
Exploration of sodium homeostasis and pharmacokinetics in bile duct-ligated rats treated by anti-cirrhosis herbal formula plus spironolactone Abstract Abstract Renal sodium retention is an essential indicator that is used for the prognosis of cirrhosis with ascites that requires diuretic treatment to restore sodium hom...
PMC10217343
core_pubmed_pmc
Numerical Optimization of Prednisolone–Tacrolimus Loaded Ultraflexible Transethosomes for Transdermal Delivery Enhancement; Box–Behnken Design, Evaluation, Optimization, and Pharmacokinetic Study
Numerical Optimization of Prednisolone–Tacrolimus Loaded Ultraflexible Transethosomes for Transdermal Delivery Enhancement; Box–Behnken Design, Evaluation, Optimization, and Pharmacokinetic Study Abstract Abstract The aim of the present study is to formulate highly permeable carriers (i.e., transethosomes) for enhancin...
PMC7180005
core_pubmed_pmc
Efficient Pharmacokinetic Modeling Workflow With the MonolixSuite: A Case Study of Remifentanil
Efficient Pharmacokinetic Modeling Workflow With the MonolixSuite: A Case Study of Remifentanil Abstract Abstract MonolixSuite is a software widely used for model‐based drug development. It contains interconnected applications for data visualization, noncompartmental analysis, nonlinear mixed effect modeling, and clini...
PMC7712135
core_pubmed_pmc
Cancer Immunotherapy Dosing: A Pharmacokinetic/Pharmacodynamic Perspective
Cancer Immunotherapy Dosing: A Pharmacokinetic/Pharmacodynamic Perspective Abstract Immune check-point inhibitors are drugs that are markedly different from other anticancer drugs because of their indirect mechanisms of antitumoral action and their apparently random effect in terms of efficacy and toxicity. This marked...
PMC7745548
core_pubmed_pmc
In Silico ADME, Metabolism Prediction and Hydrolysis Study of Melatonin Derivatives
In Silico ADME, Metabolism Prediction and Hydrolysis Study of Melatonin Derivatives Abstract Abstract Melatonin (MLT) is a well-known pineal hormone possessed with remarkable biological activities. However, its low oral bioavailability and high first-pass metabolism rate are important pharmacokinetics problems. Therefo...
PMC9693387
core_pubmed_pmc
Dose Optimization of Meropenem in Patients on Veno-Arterial Extracorporeal Membrane Oxygenation in Critically Ill Cardiac Patients: Pharmacokinetic/Pharmacodynamic Modeling
Dose Optimization of Meropenem in Patients on Veno-Arterial Extracorporeal Membrane Oxygenation in Critically Ill Cardiac Patients: Pharmacokinetic/Pharmacodynamic Modeling Abstract Abstract Background: Our objective was to determine an optimal dosage regimen of meropenem in patients receiving veno-arterial extracorpor...
PMC7993323
core_pubmed_pmc
Estimation of Body Fat Percentage for Clinical Pharmacokinetic Studies in Children
Estimation of Body Fat Percentage for Clinical Pharmacokinetic Studies in Children Abstract Obesity is a prevalent childhood condition and the degree of adiposity appears likely to be an important covariate in the pharmacokinetics (PKs) of many drugs. We undertook these studies to facilitate the evaluation and, where a...
PMC10984296
core_pubmed_pmc
Pharmacokinetics and safety of brivaracetam in neonates with repeated electroencephalographic seizures: A multicenter, open‐label, single‐arm study
Pharmacokinetics and safety of brivaracetam in neonates with repeated electroencephalographic seizures: A multicenter, open‐label, single‐arm study Abstract Abstract Objective To evaluate the pharmacokinetics (PK), safety, and tolerability of brivaracetam (BRV) in neonates with repeated electroencephalographic seizures...
PMC5427156
core_pubmed_pmc
Influence of CYP2C19*2/*17 genotype on adverse drug reactions of voriconazole in patients after allo-HSCT: a four-case report
Influence of CYP2C19*2/*17 genotype on adverse drug reactions of voriconazole in patients after allo-HSCT: a four-case report Abstract Abstract Purpose Voriconazole (VCZ) is a new-generation triazol antifungal agent. CYP2C19 mutations have been reported to cause variability in VCZ pharmacokinetics, and thus lead to und...
PMC11315838
core_pubmed_pmc
Pharmacokinetic Bioequivalence and Safety Assessment of Two Venlafaxine Hydrochloride Extended-Release Capsules in Healthy Chinese Subjects Under Fed Conditions: A Randomized, Open-Label, Single-Dose, Crossover Study
Pharmacokinetic Bioequivalence and Safety Assessment of Two Venlafaxine Hydrochloride Extended-Release Capsules in Healthy Chinese Subjects Under Fed Conditions: A Randomized, Open-Label, Single-Dose, Crossover Study Abstract Background and Objective Venlafaxine hydrochloride extended-release (ER) capsules are commonly...
PMC11972338
core_pubmed_pmc
Traditional Chinese medicine-based therapeutics for Pediatric pneumonia-related acute lung injury and acute respiratory distress syndrome
Traditional Chinese medicine-based therapeutics for Pediatric pneumonia-related acute lung injury and acute respiratory distress syndrome Abstract Pediatric pneumonia remains a leading cause of morbidity and mortality among children worldwide, necessitating the exploration of novel therapeutic interventions. Traditiona...
PMC12659968
core_pubmed_pmc
Effect of Bariatric Surgery on the Pharmacokinetics of Codeine, Oxycodone and Tramadol—A Case Series
Effect of Bariatric Surgery on the Pharmacokinetics of Codeine, Oxycodone and Tramadol—A Case Series Abstract ABSTRACT Background The impact of bariatric surgery on the pharmacokinetics of codeine, oxycodone or tramadol is largely unknown. Methods In patients treated with these opioids before and after bariatric surger...
PMC4504918
core_pubmed_pmc
Bioequivalence of Generic and Brand Name Clozapine in Korean Schizophrenic Patients: A Randomized, Two-Period, Crossover Study
Bioequivalence of Generic and Brand Name Clozapine in Korean Schizophrenic Patients: A Randomized, Two-Period, Crossover Study Abstract Abstract Objective Clozapine is the treatment of choice for refractory schizophrenia. The aim of this study was to compare the pharmacokinetics of the brand name (Clozaril) formulation...
PMC10663244
core_pubmed_pmc
Pharmacokinetics, pharmacodynamics and efficacy of pemigatinib (a selective inhibitor of fibroblast growth factor receptor 1–3) monotherapy in Chinese patients with advanced solid tumors: a phase i clinical trial
Pharmacokinetics, pharmacodynamics and efficacy of pemigatinib (a selective inhibitor of fibroblast growth factor receptor 1–3) monotherapy in Chinese patients with advanced solid tumors: a phase i clinical trial Abstract Abstract Pemigatinib is a selective fibroblast growth factor receptor (FGFR)1–3 inhibitor and has ...
PMC3835942
core_pubmed_pmc
Pharmacokinetics of Drugs in Cachectic Patients: A Systematic Review
Pharmacokinetics of Drugs in Cachectic Patients: A Systematic Review Abstract Cachexia is a weight-loss process caused by an underlying chronic disease such as cancer, chronic heart failure, chronic obstructive pulmonary disease, or rheumatoid arthritis. It leads to changes in body structure and function that may influ...
PMC7781809
core_pubmed_pmc
Predicting human pharmacokinetics from preclinical data: volume of distribution
Predicting human pharmacokinetics from preclinical data: volume of distribution Abstract Abstract This tutorial introduces background and methods to predict the human volume of distribution (V d ) of drugs using in vitro and animal pharmacokinetic (PK) parameters. The physiologically based PK (PBPK) method is based on ...
PMC6533444
core_pubmed_pmc
Pharmacokinetics and pharmacodynamics of voxelotor (GBT440) in healthy adults and patients with sickle cell disease
Pharmacokinetics and pharmacodynamics of voxelotor (GBT440) in healthy adults and patients with sickle cell disease Abstract Aims Voxelotor (previously GBT440) is a haemoglobin (Hb) modulator that increases Hb‐oxygen affinity, thereby reducing Hb polymerization and sickling of red blood cells (RBCs), being developed as...
PMC3991570
core_pubmed_pmc
A Novel Highly Potent Autotaxin/ENPP2 Inhibitor Produces Prolonged Decreases in Plasma Lysophosphatidic Acid Formation In Vivo and Regulates Urethral Tension
A Novel Highly Potent Autotaxin/ENPP2 Inhibitor Produces Prolonged Decreases in Plasma Lysophosphatidic Acid Formation In Vivo and Regulates Urethral Tension Abstract Autotaxin, also known as ectonucleotide pyrophosphatase/phosphodiesterase 2 (ENPP2), is a secreted enzyme that has lysophospholipase D activity, which co...
PMC8241194
core_pubmed_pmc
Critical physicochemical and biological attributes of nanoemulsions for pulmonary delivery of rifampicin by nebulization technique in tuberculosis treatment
Critical physicochemical and biological attributes of nanoemulsions for pulmonary delivery of rifampicin by nebulization technique in tuberculosis treatment Abstract Abstract The study investigated aerosolization, pulmonary inhalation, intracellular trafficking potential in macrophages and pharmacokinetics profiles of ...
PMC11076959
core_pubmed_pmc
A first-in-human phase I study of the PD-1 inhibitor, retifanlimab (INCMGA00012), in patients with advanced solid tumors (POD1UM-101)
A first-in-human phase I study of the PD-1 inhibitor, retifanlimab (INCMGA00012), in patients with advanced solid tumors (POD1UM-101) Abstract Background Retifanlimab is a humanized, hinge-stabilized immunoglobulin G4κ monoclonal antibody against human programmed cell death protein 1 (PD-1). This first-in-human, phase ...
PMC3908364
core_pubmed_pmc
Mechanism-based approach using a biomarker response to evaluate tocilizumab subcutaneous injection in patients with rheumatoid arthritis with an inadequate response to synthetic DMARDs (MATSURI study)
Mechanism-based approach using a biomarker response to evaluate tocilizumab subcutaneous injection in patients with rheumatoid arthritis with an inadequate response to synthetic DMARDs (MATSURI study) Abstract Abstract A multicenter, open-label, dose-escalation phase 1/2 study was undertaken to evaluate the optimal sub...
PMC12356828
core_pubmed_pmc
Integrative snRNA‐seq, molecular docking and dynamics simulations identifies Lasmiditan as drug candidate for Alzheimer's disease
Integrative snRNA‐seq, molecular docking and dynamics simulations identifies Lasmiditan as drug candidate for Alzheimer's disease Abstract Abstract Background Alzheimer's disease (AD) is a growing healthcare crisis with limited effective therapies. This study aims to identify new candidate drugs that can be repurposed ...
PMC5297680
core_pubmed_pmc
Simultaneous Determination and Pharmacokinetic Study of Six Components in Rat Plasma by HPLC-MS/MS after Oral Administration of Acanthopanax sessiliflorus Fruit Extract
Simultaneous Determination and Pharmacokinetic Study of Six Components in Rat Plasma by HPLC-MS/MS after Oral Administration of Acanthopanax sessiliflorus Fruit Extract Abstract Abstract A specific and reliable HPLC-MS/MS method was developed and validated for the simultaneous determination of protocatechuic acid (PCA)...
PMC5256963
core_pubmed_pmc
Polymicrobial Ventilator-Associated Pneumonia: Fighting In Vitro Candida albicans-Pseudomonas aeruginosa Biofilms with Antifungal-Antibacterial Combination Therapy
Polymicrobial Ventilator-Associated Pneumonia: Fighting In Vitro Candida albicans-Pseudomonas aeruginosa Biofilms with Antifungal-Antibacterial Combination Therapy Abstract Abstract The polymicrobial nature of ventilator-associated pneumonia (VAP) is now evident, with mixed bacterial-fungal biofilms colonizing the VAP ...
PMC12198689
core_pubmed_pmc
Effects of Antiepileptic Drugs, Carbamazepine and Phenytoin, on Plasma Concentrations of Clozapine and Its N ‐Desmethyl and N ‐Oxide Metabolites in Japanese Patients With Schizophrenia
Effects of Antiepileptic Drugs, Carbamazepine and Phenytoin, on Plasma Concentrations of Clozapine and Its N ‐Desmethyl and N ‐Oxide Metabolites in Japanese Patients With Schizophrenia Abstract ABSTRACT Clozapine (CLZ) is used for treatment‐resistant schizophrenia. However, in Japanese patients, its pharmacokinetics ar...
PMC4046969
core_pubmed_pmc
Pharmacokinetics of Naja sumatrana (Equatorial Spitting Cobra) Venom and Its Major Toxins in Experimentally Envenomed Rabbits
Pharmacokinetics of Naja sumatrana (Equatorial Spitting Cobra) Venom and Its Major Toxins in Experimentally Envenomed Rabbits Abstract Abstract Background The optimization of snakebite management and the use of antivenom depend greatly on the knowledge of the venom's composition as well as its pharmacokinetics. To date...
PMC8295162
core_pubmed_pmc
Factors Influencing Infusion-Related Reactions Following Dosing of Reference Rituximab and PF-05280586, a Rituximab Biosimilar
Factors Influencing Infusion-Related Reactions Following Dosing of Reference Rituximab and PF-05280586, a Rituximab Biosimilar Abstract Background Infusion-related reactions (IRRs) are the most common adverse event (AE) associated with infusion of rituximab, an anti-CD20 monoclonal antibody. Objective Our objective was...
PMC10344758
core_pubmed_pmc
Effects of food on pharmacokinetics and safety of metformin hydrochloride tablets: A meta-analysis of pharmacokinetic, bioavailability, or bioequivalence studies
Effects of food on pharmacokinetics and safety of metformin hydrochloride tablets: A meta-analysis of pharmacokinetic, bioavailability, or bioequivalence studies Abstract Abstract Background The effects of food on the pharmacokinetics and safety of metformin hydrochloride (MH) are unclear. Objective To discover the eff...
PMC12691685
core_pubmed_pmc
Pharmacokinetic/pharmacodynamic optimization of temocillin treatment against CTX-M-15-producing Klebsiella pneumoniae isolates in a hollow-fiber infection model
Pharmacokinetic/pharmacodynamic optimization of temocillin treatment against CTX-M-15-producing Klebsiella pneumoniae isolates in a hollow-fiber infection model Abstract ABSTRACT Temocillin, a β-lactam antibiotic, has been proposed as an alternative to carbapenems for the treatment of ESBL-producing Enterobacteriaceae....
PMC4674817
core_pubmed_pmc
Multiscale Framework for Imaging Radiolabeled Therapeutics
Multiscale Framework for Imaging Radiolabeled Therapeutics Abstract Abstract The resistance of a tumor to a drug is the result of bulk properties of the tumor tissue as well as phenotypic variations displayed by single cells. Here, we show that radioisotopic detection methods, commonly used for tracking the tissue dist...
PMC7401509
core_pubmed_pmc
Levelling the Translational Gap for Animal to Human Efficacy Data
Levelling the Translational Gap for Animal to Human Efficacy Data Abstract Simple Summary The value of animal research has been increasingly debated, owing to high failure rates in drug development. A potential contributor to this situation is the lack of predictivity of animal models of disease. Until recently, most i...
PMC5884041
core_pubmed_pmc
A nutraceutical combination of Cinnamomum cassia & Nigella sativa for Type 1 diabetes mellitus
A nutraceutical combination of Cinnamomum cassia & Nigella sativa for Type 1 diabetes mellitus Abstract Background Nigella sativa (black cumin) and Cinnamomum cassia (Cinnamon) are an integral part of the Indian diet, and have also been sourced in the ayurveda, the traditional Indian system of medicine, for their medic...
PMC11070952
core_pubmed_pmc
Fabrication of nanocrystal forms of ᴅ-cycloserine and their application for transdermal and enteric drug delivery systems
Fabrication of nanocrystal forms of ᴅ-cycloserine and their application for transdermal and enteric drug delivery systems Abstract ᴅ-cycloserine (DCS), an FDA-approved medicine for the treatment of tuberculosis, is also a partial agonist at the glycine recognition site of N -methyl-ᴅ-aspartate (NMDA) receptor and has s...