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PMC10989571 | core_pubmed_pmc | Interactions of linagliptin, rabeprazole sodium, and their formed complex with bovine serum albumin: Computational docking and fluorescence spectroscopic methods | Interactions of linagliptin, rabeprazole sodium, and their formed complex with bovine serum albumin: Computational docking and fluorescence spectroscopic methods Abstract Abstract The foremost aim of this thermodynamic study was to evaluate the pharmacokinetics (PK) and pharmacodynamics (PD) profiles of linagliptin (LG... |
PMC7576618 | core_pubmed_pmc | Safety and pharmacokinetic profiles of MGS0274 besylate (TS‐134), a novel metabotropic glutamate 2/3 receptor agonist prodrug, in healthy subjects | Safety and pharmacokinetic profiles of MGS0274 besylate (TS‐134), a novel metabotropic glutamate 2/3 receptor agonist prodrug, in healthy subjects Abstract Aims The safety and pharmacokinetics of single and multiple doses of a novel mGlu 2/3 receptor agonist prodrug, MGS0274 besylate (TS‐134), were investigated in heal... |
PMC3229842 | core_pubmed_pmc | Optimisation of the Anti- Trypanosoma brucei Activity of the Opioid Agonist U50488 | Optimisation of the Anti- Trypanosoma brucei Activity of the Opioid Agonist U50488 Abstract Screening of the Sigma–Aldrich Library of Pharmacologically Active Compounds (LOPAC) against cultured Trypanosoma brucei , the causative agent of African sleeping sickness, resulted in the identification of a number of compounds... |
PMC12066371 | core_pubmed_pmc | Pharmacokinetic profile of novel reduced-dose Danziten ™ (nilotinib tablets) versus Tasigna ® (nilotinib capsules): in vivo bioequivalence and population pharmacokinetic analysis | Pharmacokinetic profile of novel reduced-dose Danziten ™ (nilotinib tablets) versus Tasigna ® (nilotinib capsules): in vivo bioequivalence and population pharmacokinetic analysis Abstract Abstract Purpose To evaluate single dose pharmacokinetics (PK) of novel reduced-dose film coated Danziten ™ (nilotinib tablets) usin... |
PMC9274295 | core_pubmed_pmc | Estrone-Conjugated PEGylated Liposome Co-Loaded Paclitaxel and Carboplatin Improve Anti-Tumor Efficacy in Ovarian Cancer and Reduce Acute Toxicity of Chemo-Drugs | Estrone-Conjugated PEGylated Liposome Co-Loaded Paclitaxel and Carboplatin Improve Anti-Tumor Efficacy in Ovarian Cancer and Reduce Acute Toxicity of Chemo-Drugs Abstract Abstract Purpose Ovarian cancer is the most lethal gynecologic malignancy. The combination of paclitaxel (PTX) and carboplatin (CBP) is the first-lin... |
PMC4937655 | core_pubmed_pmc | Effect of the CYP3A inhibitors, diltiazem and ketoconazole, on ticagrelor pharmacokinetics in healthy volunteers | Effect of the CYP3A inhibitors, diltiazem and ketoconazole, on ticagrelor pharmacokinetics in healthy volunteers Abstract Abstract Objectives Two open-label, two-period, crossover studies in healthy volunteers were designed to determine the pharmacokinetic interactions between ticagrelor, a P2Y 12 receptor antagonist, ... |
PMC5945515 | core_pubmed_pmc | Measuring glucocorticoid receptor expression in vivo with PET | Measuring glucocorticoid receptor expression in vivo with PET Abstract The glucocorticoid receptor (GR) is an emerging drug target for several common and deadly solid tumors like breast and prostate cancer, and clinical trials studying the antitumor effects of GR antagonists are beginning. Since GR expression can be va... |
PMC8876931 | core_pubmed_pmc | Pharmacokinetic, Metabolomic, and Stability Assessment of Ganoderic Acid H Based Triterpenoid Enriched Fraction of Ganoderma lucidum P. Karst | Pharmacokinetic, Metabolomic, and Stability Assessment of Ganoderic Acid H Based Triterpenoid Enriched Fraction of Ganoderma lucidum P. Karst Abstract Abstract Ganoderma lucidum P. karst is an edible fungus that is used in traditional medicine and contains triterpenoids as the major phytoconstituents. Ganoderic acids a... |
PMC9298293 | core_pubmed_pmc | Chemotherapy, targeted therapy and immunotherapy: Which drugs can be safely used in the solid organ transplant recipients? | Chemotherapy, targeted therapy and immunotherapy: Which drugs can be safely used in the solid organ transplant recipients? Abstract Summary In solid organ transplant recipients, cancer is associated with worse prognosis than in the general population. Among the causes of increased cancer‐associated mortality, are the l... |
PMC10059925 | core_pubmed_pmc | Recovery from Exercise in Persons with Myalgic Encephalomyelitis/Chronic Fatigue Syndrome (ME/CFS) | Recovery from Exercise in Persons with Myalgic Encephalomyelitis/Chronic Fatigue Syndrome (ME/CFS) Abstract Background and Objectives : Post-exertional malaise (PEM) is the hallmark of myalgic encephalomyelitis/chronic fatigue syndrome (ME/CFS), but there has been little effort to quantitate the duration of PEM symptom... |
PMC4992249 | core_pubmed_pmc | In vivo biodistribution and physiologically based pharmacokinetic modeling of inhaled fresh and aged cerium oxide nanoparticles in rats | In vivo biodistribution and physiologically based pharmacokinetic modeling of inhaled fresh and aged cerium oxide nanoparticles in rats Abstract Background Cerium oxide (CeO 2 ) nanoparticles used as a diesel fuel additive can be emitted into the ambient air leading to human inhalation. Although biological studies have... |
PMC4348051 | core_pubmed_pmc | Pharmacokinetic-pharmacodynamic analysis to evaluate the effect of moxifloxacin on QT interval prolongation in healthy Korean male subjects | Pharmacokinetic-pharmacodynamic analysis to evaluate the effect of moxifloxacin on QT interval prolongation in healthy Korean male subjects Abstract Abstract A single 400 mg dose of moxifloxacin has been the standard positive control for thorough QT (TQT) studies. However, it is not clearly known whether a 400 mg dose ... |
PMC11736998 | core_pubmed_pmc | Pharmacokinetics and Alterations in Glucose and Insulin Levels After a Single Dose of Canagliflozin in Healthy Icelandic Horses | Pharmacokinetics and Alterations in Glucose and Insulin Levels After a Single Dose of Canagliflozin in Healthy Icelandic Horses Abstract ABSTRACT Canagliflozin (CFZ) is a sodium‐glucose cotransporter‐2 inhibitor that has shown promising results as a drug for the treatment of insulin dysregulation in horses. Even though... |
PMC8401959 | core_pubmed_pmc | Development, Characterization and In Vivo Pharmacokinetic Assessment of Rectal Suppositories Containing Combination Antiretroviral Drugs for HIV Prevention | Development, Characterization and In Vivo Pharmacokinetic Assessment of Rectal Suppositories Containing Combination Antiretroviral Drugs for HIV Prevention Abstract Abstract Receptive anal intercourse (RAI) contributes significantly to HIV acquisition underscoring the need to develop HIV prevention options for populati... |
PMC10135341 | core_pubmed_pmc | Linezolid Pharmacokinetics and Its Association with Adverse Drug Reactions in Patients with Drug-Resistant Pulmonary Tuberculosis | Linezolid Pharmacokinetics and Its Association with Adverse Drug Reactions in Patients with Drug-Resistant Pulmonary Tuberculosis Abstract Abstract We evaluated the relationship between the pharmacokinetic parameters of linezolid (LZD) and development of adverse drug reactions (ADRs) in patients with pulmonary drug-res... |
PMC9915979 | core_pubmed_pmc | Health Risk Assessment in Children Occupationally and Para-Occupationally Exposed to Benzene Using a Reverse-Translation PBPK Model | Health Risk Assessment in Children Occupationally and Para-Occupationally Exposed to Benzene Using a Reverse-Translation PBPK Model Abstract Abstract Benzene is a known human carcinogen and one of the ten chemicals of major public health concern identified by the World Health Organization. Our objective was to evaluate... |
PMC9807554 | core_pubmed_pmc | Effects of Aficamten on cardiac contractility in a feline translational model of hypertrophic cardiomyopathy | Effects of Aficamten on cardiac contractility in a feline translational model of hypertrophic cardiomyopathy Abstract Abstract Hypertrophic cardiomyopathy (HCM) is the most prevalent inherited cardiac disease in humans and cats and lacks efficacious pharmacologic interventions in the preclinical phase of disease. LV ou... |
PMC10272808 | core_pubmed_pmc | Neuroprotection after cardiac arrest with 2-iminobiotin: a single center phase IIa study on safety, tolerability, and pharmacokinetics | Neuroprotection after cardiac arrest with 2-iminobiotin: a single center phase IIa study on safety, tolerability, and pharmacokinetics Abstract Background Brain injury is a serious problem in patients who survive out-of-hospital cardiac arrest (OHCA). Neuroprotective drugs could reduce hypoxic–ischemic reperfusion inju... |
PMC12962402 | core_pubmed_pmc | Integrating B Cell Differentiation Model With Real‐World Data Informs Determinants for Antibody‐Secreting Cell Depletions in Systemic Sclerosis | Integrating B Cell Differentiation Model With Real‐World Data Informs Determinants for Antibody‐Secreting Cell Depletions in Systemic Sclerosis Abstract ABSTRACT Systemic sclerosis (SSc) is a complex autoimmune disorder characterized by extensive fibrosis, vascular abnormalities, and immune dysregulation, affecting cli... |
PMC6319427 | core_pubmed_pmc | Bioequivalence of two quetiapine extended release tablets in Chinese healthy volunteers under fasting and fed conditions and effects of food on pharmacokinetic profiles | Bioequivalence of two quetiapine extended release tablets in Chinese healthy volunteers under fasting and fed conditions and effects of food on pharmacokinetic profiles Abstract Abstract Objective The objectives of this study were to evaluate the bioequivalence of Quesero extended release (Quesero XR) tablets and Seroq... |
PMC6567139 | core_pubmed_pmc | Development of an intravaginal ring delivering simultaneously anastrozole and levonorgestrel: a pharmacokinetic perspective | Development of an intravaginal ring delivering simultaneously anastrozole and levonorgestrel: a pharmacokinetic perspective Abstract Abstract Intravaginal rings (IVRs) are an option for continuous administration of drugs in women. As an attractive approach for the treatment of endometriosis-associated pelvic pain, IVRs... |
PMC7887337 | core_pubmed_pmc | Ultra-Performance Liquid Chromatography-Tandem Mass Spectrometry for Simultaneous Determination of Antipsychotic Drugs in Human Plasma and Its Application in Therapeutic Drug Monitoring | Ultra-Performance Liquid Chromatography-Tandem Mass Spectrometry for Simultaneous Determination of Antipsychotic Drugs in Human Plasma and Its Application in Therapeutic Drug Monitoring Abstract Purpose We developed and validated an ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) method fo... |
PMC7109168 | core_pubmed_pmc | Clinical Pharmacokinetics and Impact of Hematocrit on Monitoring and Dosing of Tacrolimus Early After Heart and Lung Transplantation | Clinical Pharmacokinetics and Impact of Hematocrit on Monitoring and Dosing of Tacrolimus Early After Heart and Lung Transplantation Abstract The calcineurin inhibitor tacrolimus is an effective immunosuppressant and is extensively used in solid organ transplantation. In the first week after heart and lung transplantat... |
PMC7359855 | core_pubmed_pmc | Novel pH-Sensitive Urushiol-Loaded Polymeric Micelles for Enhanced Anticancer Activity | Novel pH-Sensitive Urushiol-Loaded Polymeric Micelles for Enhanced Anticancer Activity Abstract Abstract Purpose The aim of this study was to develop a means of improving the bioavailability and anticancer activity of urushiol by developing an urushiol-loaded novel tumor-targeted micelle delivery system based on amphip... |
PMC12656303 | core_pubmed_pmc | Lymph-Targeted Delivery of CUR-NLCs Enhances Oral Bioavailability: Evidence from a Double-Catheterized Rat Model | Lymph-Targeted Delivery of CUR-NLCs Enhances Oral Bioavailability: Evidence from a Double-Catheterized Rat Model Abstract Abstract Background/Objectives: Curcumin (CUR), a natural polyphenol with poor solubility and significant first-pass metabolism, shows extremely low oral bioavailability. Although CUR-loaded nanostr... |
PMC8004917 | core_pubmed_pmc | Hair Growth Promoting Activity of Cedrol Nanoemulsion in C57BL/6 Mice and Its Bioavailability | Hair Growth Promoting Activity of Cedrol Nanoemulsion in C57BL/6 Mice and Its Bioavailability Abstract As the main component of Platycladus orientalis , cedrol has known germinal activity. A range of cedrol formulations have been developed to prevent hair-loss, but compliance remains key issues. In this study, we prepa... |
PMC12056373 | core_pubmed_pmc | Pharmacokinetics and bioequivalence assessment of two prucalopride formulations in healthy Chinese women: a randomized, open-label, two-period, two-sequence, self-crossover study | Pharmacokinetics and bioequivalence assessment of two prucalopride formulations in healthy Chinese women: a randomized, open-label, two-period, two-sequence, self-crossover study Abstract Objective This study aimed to evaluate the pharmacokinetic (PK) bioequivalence of generic and branded prucalopride formulations. Met... |
PMC11866436 | core_pubmed_pmc | Phase 1/2 trial of brogidirsen: Dual-targeting antisense oligonucleotides for exon 44 skipping in Duchenne muscular dystrophy | Phase 1/2 trial of brogidirsen: Dual-targeting antisense oligonucleotides for exon 44 skipping in Duchenne muscular dystrophy Abstract Summary Duchenne muscular dystrophy (DMD) is a severe muscle disorder caused by mutations in the DMD gene, leading to dystrophin deficiency. Antisense oligonucleotide (ASO)-mediated exo... |
PMC12314523 | core_pubmed_pmc | IGM-7354, an Immunocytokine with IL15 Fused to an Anti–PD-L1 IgM, Induces NK and CD8 + T cell–Mediated Cytotoxicity of PD-L1–Positive Tumor Cells | IGM-7354, an Immunocytokine with IL15 Fused to an Anti–PD-L1 IgM, Induces NK and CD8 + T cell–Mediated Cytotoxicity of PD-L1–Positive Tumor Cells Abstract Abstract IgM antibodies are preformed pentameric or hexameric molecules that can be engineered to generate high-affinity and high-avidity fully human antibody therap... |
PMC11953061 | core_pubmed_pmc | Carotenoids Modulate FoxO‐Induced Cell Cycle Arrest in Human Cancer Cell Lines: A Scoping Review | Carotenoids Modulate FoxO‐Induced Cell Cycle Arrest in Human Cancer Cell Lines: A Scoping Review Abstract ABSTRACT Carotenoids, a class of antioxidants, have shown great potential for cancer management. This scoping review aimed to elucidate the anticancer mechanisms of carotenoids by using a protein interactions and p... |
PMC7689742 | core_pubmed_pmc | Understanding the Effect of Hydroxypropyl‐β‐Cyclodextrin on Fenebrutinib Absorption in an Itraconazole–Fenebrutinib Drug–Drug Interaction Study | Understanding the Effect of Hydroxypropyl‐β‐Cyclodextrin on Fenebrutinib Absorption in an Itraconazole–Fenebrutinib Drug–Drug Interaction Study Abstract Cyclodextrins are widely used pharmaceutical excipients, particularly for insoluble compounds dosed orally, such as the oral solution of itraconazole, which is frequen... |
PMC8949268 | core_pubmed_pmc | Continuous Versus Intermittent Linezolid Infusion for Critically Ill Patients with Hospital-Acquired and Ventilator-Associated Pneumonia: Efficacy and Safety Challenges | Continuous Versus Intermittent Linezolid Infusion for Critically Ill Patients with Hospital-Acquired and Ventilator-Associated Pneumonia: Efficacy and Safety Challenges Abstract High variability of linezolid blood concentrations with partial subtherapeutic levels was observed in critically ill patients who received a s... |
PMC9782218 | core_pubmed_pmc | Optimized Therapeutic 177 Lu-Labeled PSMA-Targeted Ligands with Improved Pharmacokinetic Characteristics for Prostate Cancer | Optimized Therapeutic 177 Lu-Labeled PSMA-Targeted Ligands with Improved Pharmacokinetic Characteristics for Prostate Cancer Abstract Clinical trials have shown the significant efficacy of [ 177 Lu]Lu-PSMA-617 for treating prostate cancer. However, the pharmacokinetic characteristics and therapeutic performance of [ 17... |
PMC5765671 | core_pubmed_pmc | Dynamic changes in 18 F-borono-L-phenylalanine uptake in unresectable, advanced, or recurrent squamous cell carcinoma of the head and neck and malignant melanoma during boron neutron capture therapy patient selection | Dynamic changes in 18 F-borono-L-phenylalanine uptake in unresectable, advanced, or recurrent squamous cell carcinoma of the head and neck and malignant melanoma during boron neutron capture therapy patient selection Abstract Abstract Background We evaluated dynamic changes in 18 F–borono-L-phenylalanine ( 18 F–BPA) up... |
PMC12584229 | core_pubmed_pmc | Interaction between rasagiline and Pueraria radix in in vitro models of parkinson’s disease | Interaction between rasagiline and Pueraria radix in in vitro models of parkinson’s disease Abstract Background The management of Parkinson’s disease (PD) remains challenging owing to the limitations of current therapies. Although rasagiline (RASA), a monoamine oxidase-B (MAO-B) inhibitor, offers advantages over levodo... |
PMC10300166 | core_pubmed_pmc | Pharmacotherapies in Older Adults with COPD: Challenges and Opportunities | Pharmacotherapies in Older Adults with COPD: Challenges and Opportunities Abstract Abstract Older adults have a higher prevalence of chronic obstructive pulmonary disease (COPD), which will likely increase substantially in the coming decades owing to aging populations and increased long-term exposure to risk factors fo... |
PMC9810492 | core_pubmed_pmc | Predicting the systemic exposure and lung concentration of nafamostat using physiologically-based pharmacokinetic modeling | Predicting the systemic exposure and lung concentration of nafamostat using physiologically-based pharmacokinetic modeling Abstract Abstract Nafamostat has been actively studied for its neuroprotective activity and effect on various indications, such as coronavirus disease 2019 (COVID-19). Nafamostat has low water solu... |
PMC12439009 | core_pubmed_pmc | Tocilizumab Dosing for Management of T Cell‐Engaging Bispecific Antibody‐Related CRS in Patients With R/R B‐Cell NHL | Tocilizumab Dosing for Management of T Cell‐Engaging Bispecific Antibody‐Related CRS in Patients With R/R B‐Cell NHL Abstract Abstract The recent surge in T‐cell‐engaging and chimeric antigen receptor (CAR) T‐cell therapies is changing the landscape of cancer therapy. Cytokine release syndrome (CRS) is a systemic infla... |
PMC10781817 | core_pubmed_pmc | Development, Physicochemical Characteristics and Pharmacokinetics of a New Sustained-Release Bilayer Tablet Formulation of Tramadol with an Immediate-Release Component for Twice-Daily Administration | Development, Physicochemical Characteristics and Pharmacokinetics of a New Sustained-Release Bilayer Tablet Formulation of Tramadol with an Immediate-Release Component for Twice-Daily Administration Abstract Background and Objective There are some potential concerns about the currently marketed solid oral dosage forms ... |
PMC11579541 | core_pubmed_pmc | In vitro , in vivo , and in silico approaches for evaluating the preclinical DMPK profiles of ammoxetine, a novel chiral serotonin and norepinephrine reuptake inhibitor | In vitro , in vivo , and in silico approaches for evaluating the preclinical DMPK profiles of ammoxetine, a novel chiral serotonin and norepinephrine reuptake inhibitor Abstract Background and Aim Ammoxetine, a novel chiral serotonin and norepinephrine reuptake inhibitor, holds promise for major depressive disorder tre... |
PMC6976993 | core_pubmed_pmc | Long-noncoding RNAs (lncRNAs) in drug metabolism and disposition, implications in cancer chemo-resistance | Long-noncoding RNAs (lncRNAs) in drug metabolism and disposition, implications in cancer chemo-resistance Abstract Abstract Drug metabolism is an orchestrated process in which drugs are metabolized and disposed through a series of specialized enzymes and transporters. Alterations in the expression and/or activity of th... |
PMC6089104 | core_pubmed_pmc | No pharmacokinetic interactions between candesartan and amlodipine following multiple oral administrations in healthy subjects | No pharmacokinetic interactions between candesartan and amlodipine following multiple oral administrations in healthy subjects Abstract Purpose To evaluate the pharmacokinetics and pharmacodynamics of candesartan and amlodipine in the absence and presence of each other in healthy subjects. Methods This study consisted ... |
PMC11375898 | core_pubmed_pmc | Pharmacokinetics and safety profiles of beinaglutide injection, a recombinant human GLP-1, in adults with overweight/obesity: results from a phase I clinical trial | Pharmacokinetics and safety profiles of beinaglutide injection, a recombinant human GLP-1, in adults with overweight/obesity: results from a phase I clinical trial Abstract Abstract Background Beinaglutide, whose active ingredient is rhGLP-1, has been widely used as a pharmacological therapy for T2DM. We explored the s... |
PMC5049930 | core_pubmed_pmc | The Non-Linear Child: Ontogeny, Isoniazid Concentration, and NAT2 Genotype Modulate Enzyme Reaction Kinetics and Metabolism | The Non-Linear Child: Ontogeny, Isoniazid Concentration, and NAT2 Genotype Modulate Enzyme Reaction Kinetics and Metabolism Abstract Abstract N-acetyltransferase 2 (NAT2) catalyzes the acetylation of isoniazid to N-acetylisoniazid. NAT2 polymorphism explains 88% of isoniazid clearance variability in adults. We examined... |
PMC6249674 | core_pubmed_pmc | The Nonclinical Safety Profile of GalNAc-conjugated RNAi Therapeutics in Subacute Studies | The Nonclinical Safety Profile of GalNAc-conjugated RNAi Therapeutics in Subacute Studies Abstract Short interfering RNAs (siRNAs) and antisense oligonucleotides (ASOs) are the most clinically advanced oligonucleotide-based platforms. A number of N -acetylgalactosamine (GalNAc)-conjugated siRNAs (GalNAc-siRNAs), also r... |
PMC9107587 | core_pubmed_pmc | Translation of liver stage activity of M5717, a Plasmodium elongation factor 2 inhibitor: from bench to bedside | Translation of liver stage activity of M5717, a Plasmodium elongation factor 2 inhibitor: from bench to bedside Abstract Abstract Background Targeting the asymptomatic liver stage of Plasmodium infection through chemoprevention could become a key intervention to reduce malaria-associated incidence and mortality. Method... |
PMC9767744 | core_pubmed_pmc | Discrepancies Between Bayesian Vancomycin Models Can Affect Clinical Decisions in the Critically Ill | Discrepancies Between Bayesian Vancomycin Models Can Affect Clinical Decisions in the Critically Ill Abstract Abstract Purpose To assess the agreement in 24-hour area under the curve (AUC 24 ) value estimates between commonly used vancomycin population pharmacokinetic models in the critically ill. Materials and Methods... |
PMC9658400 | core_pubmed_pmc | Duplication, Loss, and Evolutionary Features of Specific UDP-Glucuronosyltransferase Genes in Carnivora (Mammalia, Laurasiatheria) | Duplication, Loss, and Evolutionary Features of Specific UDP-Glucuronosyltransferase Genes in Carnivora (Mammalia, Laurasiatheria) Abstract Abstract Simple Summary In this study, we clarified the evolutional features of the UGT gene family in Carnivora. We firstly analyzed the gene synteny of UGT1As, 2Bs, ana 2Es and f... |
PMC10640543 | core_pubmed_pmc | Oral ketamine may offer a solution to the ketamine conundrum | Oral ketamine may offer a solution to the ketamine conundrum Abstract Abstract Ketamine has received considerable attention for its rapid and robust antidepressant response over the past decade. Current evidence, in clinical populations, predominantly relates to parenterally administered ketamine, which is reported to ... |
PMC9091372 | core_pubmed_pmc | Effect of Baicalein on the Pharmacokinetics of Cilostazol and Its Two Metabolites in Rat Plasma Using UPLC-MS/MS Method | Effect of Baicalein on the Pharmacokinetics of Cilostazol and Its Two Metabolites in Rat Plasma Using UPLC-MS/MS Method Abstract This study aimed to explore the effect of baicalein on the pharmacokinetics of cilostazol (CLZ) and its two metabolites 3,4-dehydro cilostazol (3,4-CLZ) and 4′-trans-hydroxy cilostazol (4′-CL... |
PMC9133488 | core_pubmed_pmc | Application of Physiologically Based Pharmacokinetic Modeling in Preclinical Studies: A Feasible Strategy to Practice the Principles of 3Rs | Application of Physiologically Based Pharmacokinetic Modeling in Preclinical Studies: A Feasible Strategy to Practice the Principles of 3Rs Abstract Abstract Pharmacokinetic characterization plays a vital role in drug discovery and development. Although involving numerous laboratory animals with error-prone, labor-inte... |
PMC3839800 | core_pubmed_pmc | Development of PLGA-based itraconazole injectable nanospheres for sustained release | Development of PLGA-based itraconazole injectable nanospheres for sustained release Abstract Purpose Itraconazole (ITZ) is a synthetic triazole antifungal agent, which is widely used for treatment and prevention of fungal infections. The purpose of this study is to develop ITZ-loaded poly(lactic-co-glycolic acid) (PLGA... |
PMC8301559 | core_pubmed_pmc | Safety, tolerability, pharmacokinetics, and pharmacodynamics of a TLR7 agonist prodrug RO6870868 in healthy volunteers | Safety, tolerability, pharmacokinetics, and pharmacodynamics of a TLR7 agonist prodrug RO6870868 in healthy volunteers Abstract Abstract RO6870868 is an oral prodrug of the toll‐like receptor 7 (TLR7) specific agonist, RO6871765. TLR7 agonists augment host immune activity and are in development to treat hepatitis B inf... |
PMC12651208 | core_pubmed_pmc | Lights and Shadows of Essential Oil-Derived Compounds: Antimicrobial and Anti-Inflammatory Properties of Eugenol, Thymol, Cinnamaldehyde, and Carvacrol | Lights and Shadows of Essential Oil-Derived Compounds: Antimicrobial and Anti-Inflammatory Properties of Eugenol, Thymol, Cinnamaldehyde, and Carvacrol Abstract Essential oil-derived compounds such as eugenol, thymol, cinnamaldehyde, and carvacrol exhibit potent antimicrobial and anti-inflammatory properties, making th... |
PMC9790982 | core_pubmed_pmc | Establishment of a novel method to assess MEK1/2 inhibition in PBMCs for clinical drug development | Establishment of a novel method to assess MEK1/2 inhibition in PBMCs for clinical drug development Abstract The Raf/MEK/ERK signaling pathway plays a key role in regulating cellular proliferation, differentiation, apoptosis, cytokine production, and immune responses. However, it is also involved in diseases such as can... |
PMC6413069 | core_pubmed_pmc | Development and Validation of an Ultra-Performance Liquid Chromatography Method for the Determination of Wedelolactone in Rat Plasma and its Application in a Pharmacokinetic Study | Development and Validation of an Ultra-Performance Liquid Chromatography Method for the Determination of Wedelolactone in Rat Plasma and its Application in a Pharmacokinetic Study Abstract Abstract Wedelolactone is a coumarin ether with significant hepatoprotective effects. However, there are few pharmacokinetic studie... |
PMC5562267 | core_pubmed_pmc | Bradycardia and Hypothermia Complicating Azithromycin Treatment | Bradycardia and Hypothermia Complicating Azithromycin Treatment Abstract Patient: Male, 4 Final Diagnosis: Febrile neutropenia Symptoms: Fever Medication: Azithromycin Clinical Procedure: — Specialty: Infectious Diseases Objective: Unusual or unexpected effect of treatment Background: Azithromycin is a macrolide antibi... |
PMC6321473 | core_pubmed_pmc | Enhanced Bioavailability of Tadalafil after Intranasal Administration in Beagle Dogs | Enhanced Bioavailability of Tadalafil after Intranasal Administration in Beagle Dogs Abstract Tadalafil is an oral selective phosphodiesterase type-5 inhibitor with demonstrated efficacy and safety that is used to treat erectile dysfunction. The purpose of this study is to compare the pharmacokinetic properties of tada... |
PMC10390488 | core_pubmed_pmc | Knowledge-based mechanistic modeling accurately predicts disease progression with gefitinib in EGFR -mutant lung adenocarcinoma | Knowledge-based mechanistic modeling accurately predicts disease progression with gefitinib in EGFR -mutant lung adenocarcinoma Abstract Abstract Lung adenocarcinoma (LUAD) is associated with a low survival rate at advanced stages. Although the development of targeted therapies has improved outcomes in LUAD patients wi... |
PMC10253893 | core_pubmed_pmc | Comparison of Estetrol Exposure between Women and Mice to Model Preclinical Experiments and Anticipate Human Treatment | Comparison of Estetrol Exposure between Women and Mice to Model Preclinical Experiments and Anticipate Human Treatment Abstract Abstract Estetrol (E4) is a natural estrogen with promising therapeutic applications in humans. The European Medicines Agency and the Food and Drug Administration have approved the use of 15 m... |
PMC6658777 | core_pubmed_pmc | Randomized, Double-Blind, Placebo-Controlled, Single-Ascending-Dose Study of the Penetration of a Monoclonal Antibody Combination (ASN100) Targeting Staphylococcus aureus Cytotoxins in the Lung Epithelial Lining Fluid of Healthy Volunteers | Randomized, Double-Blind, Placebo-Controlled, Single-Ascending-Dose Study of the Penetration of a Monoclonal Antibody Combination (ASN100) Targeting Staphylococcus aureus Cytotoxins in the Lung Epithelial Lining Fluid of Healthy Volunteers Abstract ASN100 is a novel antibody combination of two fully human IgG1(κ) monoc... |
PMC9784730 | core_pubmed_pmc | Exploring the Antimicrobial and Pharmacological Potential of NF22 as a Potent Inhibitor of E. coli DNA Gyrase: An In Vitro and In Silico Study | Exploring the Antimicrobial and Pharmacological Potential of NF22 as a Potent Inhibitor of E. coli DNA Gyrase: An In Vitro and In Silico Study Abstract Abstract Toward the search for novel antimicrobial agents to control pathogenic E. coli -associated infections, a series of novel norfloxacin derivatives were screened ... |
PMC3852505 | core_pubmed_pmc | Pharmacokinetic study and evaluation of the safety of taurolidine for dogs with osteosarcoma | Pharmacokinetic study and evaluation of the safety of taurolidine for dogs with osteosarcoma Abstract Abstract Background Osteosarcoma in dogs and humans share many similarities and the dog has been described as an excellent model to study this disease. The median survival in dogs has not improved in the last 25 years.... |
PMC12107830 | core_pubmed_pmc | Drug-drug interaction of paroxetine on olanzapine and initial dosage optimization in patients with major depressive disorder based on population pharmacokinetics | Drug-drug interaction of paroxetine on olanzapine and initial dosage optimization in patients with major depressive disorder based on population pharmacokinetics Abstract Abstract Objective Olanzapine is already used to treat patients with major depressive disorder; however, whether complex drug–drug interaction (DDI) ... |
PMC12655704 | core_pubmed_pmc | In Vitro and in Vivo Efficacy of Different Ointment Formulations Containing Centaurium erythraea Rafn. Aerial Extract | In Vitro and in Vivo Efficacy of Different Ointment Formulations Containing Centaurium erythraea Rafn. Aerial Extract Abstract Background: Centaurium erythraea Rafn . ( C. erythraea ) is a medicinal plant traditionally used in European folk medicine for the treatment of wounds, skin inflammations, and other dermatologi... |
PMC12128664 | core_pubmed_pmc | Does one model fit all mAbs? An evaluation of population pharmacokinetic models | Does one model fit all mAbs? An evaluation of population pharmacokinetic models Abstract ABSTRACT Antibodies are extensively used in treating various diseases, with over 100 canonical monoclonal antibodies (mAbs) approved. Population pharmacokinetic (PK) models are typically developed for each individual mAb, despite t... |
PMC9181587 | core_pubmed_pmc | Pharmacokinetic Pharmacodynamic Modelling Contributions to Improve Paediatric Anaesthesia Practice | Pharmacokinetic Pharmacodynamic Modelling Contributions to Improve Paediatric Anaesthesia Practice Abstract Abstract The use of pharmacokinetic-pharmacodynamic models has improved anaesthesia practice in children through a better understanding of dose-concentration-response relationships, developmental pharmacokinetic ... |
PMC9292185 | core_pubmed_pmc | Population pharmacokinetics of roxadustat in Japanese dialysis‐dependent chronic kidney disease patients with anaemia | Population pharmacokinetics of roxadustat in Japanese dialysis‐dependent chronic kidney disease patients with anaemia Abstract Abstract Aims Our objective was to develop a population pharmacokinetic (PK) model to describe roxadustat plasma concentrations in Japanese dialysis‐dependent chronic kidney disease (DD‐CKD) pa... |
PMC12457114 | core_pubmed_pmc | Comparison of the pharmacokinetic profiles of three triterpenoids after oral administration of a cucurbitacin tablet and nanosuspension by UHPLC-MS/MS | Comparison of the pharmacokinetic profiles of three triterpenoids after oral administration of a cucurbitacin tablet and nanosuspension by UHPLC-MS/MS Abstract Abstract Introduction Cucurbitacin, a class of triterpenoid compounds isolated from Pedicellus Melo , possesses various biological activities and is the primary... |
PMC4862513 | core_pubmed_pmc | Population Pharmacokinetics of Isavuconazole in Subjects with Mild or Moderate Hepatic Impairment | Population Pharmacokinetics of Isavuconazole in Subjects with Mild or Moderate Hepatic Impairment Abstract Isavuconazole, administered as the prodrug isavuconazonium sulfate, was recently approved by the U.S. Food and Drug Administration and the European Medicines Agency for the treatment of adults with invasive asperg... |
PMC9468561 | core_pubmed_pmc | Recent advances and clinical pharmacology aspects of Chimeric Antigen Receptor (CAR) T‐cellular therapy development | Recent advances and clinical pharmacology aspects of Chimeric Antigen Receptor (CAR) T‐cellular therapy development Abstract Abstract Advances in immuno‐oncology have provided a variety of novel therapeutics that harness the innate immune system to identify and destroy neoplastic cells. It is noteworthy that acceptable... |
PMC7184219 | core_pubmed_pmc | The acute effect of metabolic cofactor supplementation: a potential therapeutic strategy against non‐alcoholic fatty liver disease | The acute effect of metabolic cofactor supplementation: a potential therapeutic strategy against non‐alcoholic fatty liver disease Abstract Abstract The prevalence of non‐alcoholic fatty liver disease (NAFLD) continues to increase dramatically, and there is no approved medication for its treatment. Recently, we predict... |
PMC8179755 | core_pubmed_pmc | Pharmacokinetics, Tolerability and Pharmacogenetics of DA-8031 After Multiple Ascending Doses in Healthy Male Subjects | Pharmacokinetics, Tolerability and Pharmacogenetics of DA-8031 After Multiple Ascending Doses in Healthy Male Subjects Abstract Abstract Purpose DA-8031 is a novel selective serotonin reuptake inhibitor for the treatment of premature ejaculation. This study investigated the pharmacokinetics, safety and tolerability of ... |
PMC7083806 | core_pubmed_pmc | Pharmacokinetics and Clinical Pharmacology of Monoclonal Antibodies in Pediatric Patients | Pharmacokinetics and Clinical Pharmacology of Monoclonal Antibodies in Pediatric Patients Abstract Monoclonal antibodies (mAbs) and their derivatives are increasingly used in pediatric pharmacotherapy, and the number of antibody-based drug products with approved pediatric indications is continuously growing. In most in... |
PMC12845255 | core_pubmed_pmc | Bovine Mastitis Therapy at a Crossroads: Pharmacokinetic Barriers, Biofilms, Antimicrobial Resistance, and Emerging Solutions | Bovine Mastitis Therapy at a Crossroads: Pharmacokinetic Barriers, Biofilms, Antimicrobial Resistance, and Emerging Solutions Abstract Abstract Bovine mastitis remains a major challenge in dairy production despite extensive antimicrobial use, with therapeutic failure increasingly attributed to factors beyond classical ... |
PMC6346694 | core_pubmed_pmc | A Novel Ingestion Strategy for Sodium Bicarbonate Supplementation in a Delayed-Release Form: a Randomised Crossover Study in Trained Males | A Novel Ingestion Strategy for Sodium Bicarbonate Supplementation in a Delayed-Release Form: a Randomised Crossover Study in Trained Males Abstract Abstract Background Sodium bicarbonate (NaHCO 3 ) is a well-established nutritional ergogenic aid, though gastrointestinal (GI) distress is a common side-effect. Delayed-re... |
PMC4025172 | core_pubmed_pmc | Ultra-low-dose estriol and Lactobacillus acidophilus vaginal tablets (Gynoflor ® ) for vaginal atrophy in postmenopausal breast cancer patients on aromatase inhibitors: pharmacokinetic, safety, and efficacy phase I clinical study | Ultra-low-dose estriol and Lactobacillus acidophilus vaginal tablets (Gynoflor ® ) for vaginal atrophy in postmenopausal breast cancer patients on aromatase inhibitors: pharmacokinetic, safety, and efficacy phase I clinical study Abstract Phase I pharmacokinetic (PK) study assessed circulating estrogens in breast cance... |
PMC9704437 | core_pubmed_pmc | Assessment of flomoxef combined with amikacin in a hollow-fibre infection model for the treatment of neonatal sepsis in low- and middle-income healthcare settings | Assessment of flomoxef combined with amikacin in a hollow-fibre infection model for the treatment of neonatal sepsis in low- and middle-income healthcare settings Abstract Abstract Background Annual mortality from neonatal sepsis is an estimated 430 000–680 000 infants globally, most of which occur in low- and middle-i... |
PMC12690059 | core_pubmed_pmc | Dose-Dependent Cardioprotection of Pterocarpus indicus Extract in Rats With Myocardial Ischemia: Targeting Oxidative Stress, Inflammation, and Apoptosis | Dose-Dependent Cardioprotection of Pterocarpus indicus Extract in Rats With Myocardial Ischemia: Targeting Oxidative Stress, Inflammation, and Apoptosis Abstract Abstract Background and Aim This study investigated the dose-dependent cardioprotective effects of Pterocarpus indicus extract (P.indicus; LD: 27, MD: 54, HD:... |
PMC11602934 | core_pubmed_pmc | Model‐based comparisons of post‐treatment free IgE and FEV1 between omalizumab asthma dosing tables in the United States and European Union | Model‐based comparisons of post‐treatment free IgE and FEV1 between omalizumab asthma dosing tables in the United States and European Union Abstract Abstract Aims Omalizumab is an anti‐immunoglobulin E (IgE) monoclonal antibody that was first approved by the United States (US) Food and Drug Administration (FDA) for the... |
PMC6610527 | core_pubmed_pmc | Preparation and in vitro and in vivo evaluations of 10-hydroxycamptothecin liposomes modified with stearyl glycyrrhetinate | Preparation and in vitro and in vivo evaluations of 10-hydroxycamptothecin liposomes modified with stearyl glycyrrhetinate Abstract Abstract 10-Hydroxycamptothecin (HCPT) liposomes surface modified with stearyl glycyrrhetinate (SG) were prepared by the film dispersion method. Characterization of the liposomes, includin... |
PMC11336359 | core_pubmed_pmc | Assessment of metabolic interaction between curcumin and tramadol using the isolated perfused rat liver | Assessment of metabolic interaction between curcumin and tramadol using the isolated perfused rat liver Abstract Abstract Introduction The presence of phytochemicals in herbal medicines can lead to herb-drug interactions, altering the levels of these compounds and conventional drugs in the bloodstream by influencing CY... |
PMC11588801 | core_pubmed_pmc | Fludrocortisone dose–response relationship in septic shock: a randomised phase II trial | Fludrocortisone dose–response relationship in septic shock: a randomised phase II trial Abstract Abstract Background The combination of intravenous hydrocortisone and enteral fludrocortisone may reduce mortality in patients with septic shock. The optimal dose and reliability of absorption of fludrocortisone in critical... |
PMC7179175 | core_pubmed_pmc | Preparation of Nanocrystals for Insoluble Drugs by Top-Down Nanotechnology with Improved Solubility and Bioavailability | Preparation of Nanocrystals for Insoluble Drugs by Top-Down Nanotechnology with Improved Solubility and Bioavailability Abstract Abstract Midazolam is a rapidly effective benzodiazepine drug that is widely used as a sedative worldwide. Due to its poor solubility in a neutral aqueous solution, the clinical use of midazo... |
PMC3132447 | core_pubmed_pmc | Comparative pharmacodynamic and pharmacokinetic characteristics of subcutaneous insulin glulisine and insulin aspart prior to a standard meal in obese subjects with type 2 diabetes | Comparative pharmacodynamic and pharmacokinetic characteristics of subcutaneous insulin glulisine and insulin aspart prior to a standard meal in obese subjects with type 2 diabetes Abstract Abstract Aims: A multinational, randomized, double-blind, two-way crossover trial to compare the pharmacokinetic and pharmacodynam... |
PMC6215751 | core_pubmed_pmc | The novel ghrelin receptor inverse agonist PF-5190457 administered with alcohol: preclinical safety experiments and a phase 1b human laboratory study | The novel ghrelin receptor inverse agonist PF-5190457 administered with alcohol: preclinical safety experiments and a phase 1b human laboratory study Abstract Rodent studies indicate that ghrelin receptor blockade reduces alcohol consumption. However, no ghrelin receptor blockers have been administered to heavy drinkin... |
PMC10088087 | core_pubmed_pmc | A combined physiologically‐based pharmacokinetic and quantitative systems pharmacology model for modeling amyloid aggregation in Alzheimer's disease | A combined physiologically‐based pharmacokinetic and quantitative systems pharmacology model for modeling amyloid aggregation in Alzheimer's disease Abstract Abstract Antibody‐mediated removal of aggregated β‐amyloid (Aβ) is the current, most clinically advanced potential disease‐modifying treatment approach for Alzhei... |
PMC12905782 | core_pubmed_pmc | Red blood cell-conjugated biomimetic nanomedicine for enhanced therapy of non-small cell lung cancer | Red blood cell-conjugated biomimetic nanomedicine for enhanced therapy of non-small cell lung cancer Abstract Abstract Rationale: Epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKIs) are a standard therapy for non-small cell lung cancer (NSCLC). Despite their clinical efficacy, dose-limiting systemic... |
PMC11610134 | core_pubmed_pmc | Deciphering the effects of radiopharmaceutical therapy in the tumor microenvironment of prostate cancer: an in-silico exploration with spatial transcriptomics | Deciphering the effects of radiopharmaceutical therapy in the tumor microenvironment of prostate cancer: an in-silico exploration with spatial transcriptomics Abstract Radiopharmaceutical therapy (RPT) is an emerging prostate cancer treatment that delivers radiation to specific molecules within the tumor microenvironme... |
PMC9416565 | core_pubmed_pmc | Improvements to Hybridization-Ligation ELISA Methods to Overcome Bioanalytical Challenges Posed by Novel Oligonucleotide Therapeutics | Improvements to Hybridization-Ligation ELISA Methods to Overcome Bioanalytical Challenges Posed by Novel Oligonucleotide Therapeutics Abstract As oligonucleotides (ONs) and similar nucleic acid therapeutic modalities enter development pipelines, there is continual need to develop bioanalytical methodologies addressing ... |
PMC10687849 | core_pubmed_pmc | Extensive preclinical evaluation of combined mangiferin and glycyrrhizic acid for restricting synovial neovascularization in rheumatoid arthritis | Extensive preclinical evaluation of combined mangiferin and glycyrrhizic acid for restricting synovial neovascularization in rheumatoid arthritis Abstract Background Synovial neovascularization promotes rheumatoid arthritis (RA) progression. Baihu guizhi decoction (BHGZD) has a potential in restricting this pathologica... |
PMC8643217 | core_pubmed_pmc | Critical Appraisal of Cenobamate as Adjunctive Treatment of Focal Seizures in Adults | Critical Appraisal of Cenobamate as Adjunctive Treatment of Focal Seizures in Adults Abstract Abstract Cenobamate (CNB) is the latest antiseizure medication (ASM) authorized for the treatment of focal-onset seizures in adults. Although the precise mechanism of action of CNB is not yet fully understood, this drug inhibi... |
PMC12404254 | core_pubmed_pmc | Determination of 5-Fluorouracil in Dried Blood Spots for Therapeutic Drug Monitoring and Adverse Event Assessment in Breast Cancer Patients | Determination of 5-Fluorouracil in Dried Blood Spots for Therapeutic Drug Monitoring and Adverse Event Assessment in Breast Cancer Patients Abstract Background 5-Fluorouracil (5-FU) is a chemotherapy drug used to treat breast cancer. Monitoring 5-FU levels in blood is essential due to its narrow therapeutic range, high... |
PMC8113176 | core_pubmed_pmc | Limited Systemic Exposure with Topical Glycopyrronium Tosylate in Primary Axillary Hyperhidrosis | Limited Systemic Exposure with Topical Glycopyrronium Tosylate in Primary Axillary Hyperhidrosis Abstract Abstract Background Glycopyrronium tosylate (GT; Qbrexza ® [glycopyrronium] cloth, 2.4%) is a topical anticholinergic approved (USA) for primary axillary hyperhidrosis in patients aged ≥ 9 years. Objective The obje... |
PMC3880476 | core_pubmed_pmc | Ultra-Long Pharmacokinetic Properties of Insulin Degludec are Comparable in Elderly Subjects and Younger Adults with Type 1 Diabetes Mellitus | Ultra-Long Pharmacokinetic Properties of Insulin Degludec are Comparable in Elderly Subjects and Younger Adults with Type 1 Diabetes Mellitus Abstract Abstract Background Management of diabetes in elderly subjects is complex and careful management of glucose levels is of particular importance in this population because... |
PMC9598816 | core_pubmed_pmc | Off-Label Use of Dalbavancin for Sequential Treatment of Spondylodiscitis by Methicillin-Resistant Staphylococcus aureus : A Retrospective Single-Centre Experience | Off-Label Use of Dalbavancin for Sequential Treatment of Spondylodiscitis by Methicillin-Resistant Staphylococcus aureus : A Retrospective Single-Centre Experience Abstract Abstract Background: Our aim was to describe the clinical outcome and safety of the sequential treatment with off-label dalbavancin in patients wit... |
PMC3831261 | core_pubmed_pmc | Assessing radiotracer kinetics in the Langendorff perfused heart | Assessing radiotracer kinetics in the Langendorff perfused heart Abstract Abstract Background The Langendorff perfused heart is a physiologically relevant and controllable model with potential for assessing the pharmacokinetics of new radiotracers under a range of pathophysiological conditions.. We assess the feasibili... |
PMC9112969 | core_pubmed_pmc | Delamanid Added to an Optimized Background Regimen in Children with Multidrug-Resistant Tuberculosis: Results of a Phase I/II Clinical Trial | Delamanid Added to an Optimized Background Regimen in Children with Multidrug-Resistant Tuberculosis: Results of a Phase I/II Clinical Trial Abstract ABSTRACT Delamanid has been demonstrated to be safe and effective for treatment of adult multidrug-resistant tuberculosis (MDR-TB) and has been approved by the European C... |
PMC10008261 | core_pubmed_pmc | Piperacillin/Tazobactam in critically ill morbidly obese patients: A case series: The first One‐Centre experience with TDM | Piperacillin/Tazobactam in critically ill morbidly obese patients: A case series: The first One‐Centre experience with TDM Abstract Abstract The aim of this article is to demonstrate extreme interindividual variability of piperacilin/tazobactam (PIP/TAZO) pharmacokinetics in critically ill morbidly obese patients and t... |
PMC4303919 | core_pubmed_pmc | Joint Feedback Analysis Modeling of Nonesterified Fatty Acids in Obese Zucker Rats and Normal Sprague–Dawley Rats after Different Routes of Administration of Nicotinic Acid | Joint Feedback Analysis Modeling of Nonesterified Fatty Acids in Obese Zucker Rats and Normal Sprague–Dawley Rats after Different Routes of Administration of Nicotinic Acid Abstract Data were pooled from several studies on nicotinic acid (NiAc) intervention of fatty acid turnover in normal Sprague–Dawley and obese Zuck... |
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