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PMC7938184
core_pubmed_pmc
NaPi-IIb Inhibition for Hyperphosphatemia in CKD Hemodialysis Patients
NaPi-IIb Inhibition for Hyperphosphatemia in CKD Hemodialysis Patients Abstract Abstract Introduction Chronic kidney disease (CKD) has a prevalence of 9.1% globally, and frequently results in elevated serum phosphate, increasing cardiovascular morbidity and mortality risk in hemodialysis (HD) patients. DS-2330b, an ora...
PMC7570683
core_pubmed_pmc
Conceptual DFT-Based Computational Peptidology of Marine Natural Compounds: Discodermins A–H
Conceptual DFT-Based Computational Peptidology of Marine Natural Compounds: Discodermins A–H Abstract Abstract A methodology based on the concepts that arise from Density Functional Theory named Conceptual Density Functional Theory (CDFT) was chosen for the calculation of some global and local reactivity descriptors of...
PMC7497698
core_pubmed_pmc
Phase I dose-escalation study of the safety, tolerability, and pharmacokinetics of aflibercept in combination with S-1 in Japanese patients with advanced solid malignancies
Phase I dose-escalation study of the safety, tolerability, and pharmacokinetics of aflibercept in combination with S-1 in Japanese patients with advanced solid malignancies Abstract Summary Background Aflibercept, a recombinant fusion protein binding VEGF-A, VEGF-B and placental growth factor, inhibits tumor growth by ...
PMC11661981
core_pubmed_pmc
Navigating Treatment-Resistant Major Depressive Disorder With Suicidal Ideation: Exploring the Efficacy of Spravato (Esketamine) in an 86-Year-Old Male
Navigating Treatment-Resistant Major Depressive Disorder With Suicidal Ideation: Exploring the Efficacy of Spravato (Esketamine) in an 86-Year-Old Male Abstract This case study examines the novel application of Spravato (intranasal esketamine) to address treatment-resistant Major Depressive Disorder (MDD) in an 86-year...
PMC8542123
core_pubmed_pmc
Phase 1b dose-escalation, safety, and pharmacokinetic study of IC14, a monoclonal antibody against CD14, for the treatment of amyotrophic lateral sclerosis
Phase 1b dose-escalation, safety, and pharmacokinetic study of IC14, a monoclonal antibody against CD14, for the treatment of amyotrophic lateral sclerosis Abstract Abstract Background: The primary objective was to demonstrate the safety and tolerability of monoclonal antibody against CD14 (IC14) (atibuclimab) in amyot...
PMC12195781
core_pubmed_pmc
Triple Non-Statin Therapy with Ezetimibe, Inclisiran, and Bempedoic Acid in Patients with Genetically Confirmed Statin-Induced Rhabdomyolysis: A Dual Case Report
Triple Non-Statin Therapy with Ezetimibe, Inclisiran, and Bempedoic Acid in Patients with Genetically Confirmed Statin-Induced Rhabdomyolysis: A Dual Case Report Abstract Background: Statin intolerance is a serious therapeutic dilemma in secondary cardiovascular prevention (e.g., ESC/EAS Guidelines 2023). This is espec...
PMC9964825
core_pubmed_pmc
A Scoping Assessment of Implemented Toxicokinetic Models of Per- and Polyfluoro-Alkyl Substances, with a Focus on One-Compartment Models
A Scoping Assessment of Implemented Toxicokinetic Models of Per- and Polyfluoro-Alkyl Substances, with a Focus on One-Compartment Models Abstract Toxicokinetic (TK) models have been used for decades to estimate concentrations of per-and polyfluoroalkyl substances (PFAS) in serum. However, model complexity has varied ac...
PMC12737079
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Fritillaria pallidiflora Schrenk ex Fisch. & C.A.Mey. (Yi Beimu): Ethnopharmacology, Phytochemistry, Pharmacological Insights, and Future Prospects
Fritillaria pallidiflora Schrenk ex Fisch. & C.A.Mey. (Yi Beimu): Ethnopharmacology, Phytochemistry, Pharmacological Insights, and Future Prospects Abstract Abstract Fritillaria pallidiflora Schrenk ex Fisch. & C.A.Mey. (Yi Beimu) is a culturally significant Beimu drug in Northwest China, officially listed in the Chine...
PMC5446369
core_pubmed_pmc
Real-World Experience with Oritavancin Therapy in Invasive Gram-Positive Infections
Real-World Experience with Oritavancin Therapy in Invasive Gram-Positive Infections Abstract Introduction Oritavancin is a novel lipoglycopeptide approved for acute bacterial skin and skin structure infections. The pharmacokinetic profile and convenient one-time dosing make oritavancin an enticing option for other seri...
PMC8445563
core_pubmed_pmc
Safety, Efficacy, and Pharmacodynamics of Tremelimumab Plus Durvalumab for Patients With Unresectable Hepatocellular Carcinoma: Randomized Expansion of a Phase I/II Study
Safety, Efficacy, and Pharmacodynamics of Tremelimumab Plus Durvalumab for Patients With Unresectable Hepatocellular Carcinoma: Randomized Expansion of a Phase I/II Study Abstract PURPOSE This phase I/II study evaluated tremelimumab (anticytotoxic T-lymphocyte–associated antigen-4 monoclonal antibody) and durvalumab (a...
PMC9363158
core_pubmed_pmc
In vitro assessment of the potential for dolutegravir to affect hepatic clearance of levonorgestrel
In vitro assessment of the potential for dolutegravir to affect hepatic clearance of levonorgestrel Abstract Abstract Objectives: The World Health Organization recommends that all countries adopt dolutegravir-based antiretroviral therapy as the preferred regimen for all individuals living with HIV. Levonorgestrel is a ...
PMC12617643
core_pubmed_pmc
Pharmacokinetics and metabolic effects of ketone monoester supplementation: The first simultaneous CKM and CGM study under normal diet and activities
Pharmacokinetics and metabolic effects of ketone monoester supplementation: The first simultaneous CKM and CGM study under normal diet and activities Abstract Abstract Exogenous ketone supplementation has gained attention for its potential health and performance benefits, yet its real-world pharmacokinetics and metabol...
PMC10635330
core_pubmed_pmc
Pharmacokinetics of Temozolomide in a Patient With Glioblastoma Undergoing Hemodialysis: A Short Communication
Pharmacokinetics of Temozolomide in a Patient With Glioblastoma Undergoing Hemodialysis: A Short Communication Abstract Supplemental Digital Content is Available in the Text. Key Words: temozolomide, pharmacokinetics, hemodialysis, glioblastoma, malignant glioma Abstract Background: Temozolomide (TMZ) is an alkylating ...
PMC11705451
core_pubmed_pmc
Unique pharmacological properties of etrasimod among S1P receptor modulators
Unique pharmacological properties of etrasimod among S1P receptor modulators Abstract Abstract Etrasimod (ADP334) is an oral, once‐daily, selective sphingosine 1‐phosphate (S1P) 1,4,5 receptor modulator for the treatment of moderately to severely active ulcerative colitis and in development for the treatment of immune‐...
PMC10232755
core_pubmed_pmc
Evaluation of the potential herb-drug interaction between Bojungikki-tang and PD-L1 immunotherapy in a syngeneic mouse model
Evaluation of the potential herb-drug interaction between Bojungikki-tang and PD-L1 immunotherapy in a syngeneic mouse model Abstract Abstract Atezolizumab (a PD-L1 inhibitor) has shown remarkable efficacy and tolerability in various cancer types. Despite its efficacy and safety, atezolizumab monotherapy has limitation...
PMC11359404
core_pubmed_pmc
Genetic Variation in CYP2D6 , UGT1A4 , SLC6A2 and SLCO1B1 Alters the Pharmacokinetics and Safety of Mirabegron
Genetic Variation in CYP2D6 , UGT1A4 , SLC6A2 and SLCO1B1 Alters the Pharmacokinetics and Safety of Mirabegron Abstract Abstract Mirabegron is a drug used in overactive bladder (OAB) treatment. Genetic variation in pharmacogenes might alter its pharmacokinetics, affecting its efficacy and safety. This research aimed to...
PMC5681454
core_pubmed_pmc
Piperacillin–tazobactam as alternative to carbapenems for ICU patients
Piperacillin–tazobactam as alternative to carbapenems for ICU patients Abstract Several studies suggest that alternatives to carbapenems, and particulary beta-lactam/beta-lactamase inhibitor combinations, can be used for therapy of extended-spectrum beta-lactamase-producing Enterobacteriaceae (ESBL-PE)-related infectio...
PMC11783731
core_pubmed_pmc
Increasing brain half-life of antibodies by additional binding to myelin oligodendrocyte glycoprotein, a CNS specific protein
Increasing brain half-life of antibodies by additional binding to myelin oligodendrocyte glycoprotein, a CNS specific protein Abstract Background Therapeutic antibodies for the treatment of neurological disease show great potential, but their applications are rather limited due to limited brain exposure. The most well-...
PMC10980772
core_pubmed_pmc
Quantifying in vitro B. anthracis growth and PA production and decay: a mathematical modelling approach
Quantifying in vitro B. anthracis growth and PA production and decay: a mathematical modelling approach Abstract Protective antigen (PA) is a protein produced by Bacillus anthracis . It forms part of the anthrax toxin and is a key immunogen in US and UK anthrax vaccines. In this study, we have conducted experiments to ...
PMC11754405
core_pubmed_pmc
Computer-assisted discovery of natural inhibitors for platelet-derived growth factor alpha as novel therapeutics for thyroid cancer
Computer-assisted discovery of natural inhibitors for platelet-derived growth factor alpha as novel therapeutics for thyroid cancer Abstract Abstract Platelet-derived growth factor alpha (PDGFRA) plays a significant role in various malignant tumors. PDGFRA expression boosts thyroid cancer cell proliferation and metasta...
PMC7587234
core_pubmed_pmc
Pharmacokinetics of novel Fc-engineered monoclonal and multispecific antibodies in cynomolgus monkeys and humanized FcRn transgenic mouse models
Pharmacokinetics of novel Fc-engineered monoclonal and multispecific antibodies in cynomolgus monkeys and humanized FcRn transgenic mouse models Abstract ABSTRACT Monoclonal antibodies (mAbs) are among the fastest growing and most effective therapies for myriad diseases. Multispecific antibodies are an emerging class o...
PMC5042751
core_pubmed_pmc
Impact of quercetin-induced changes in drug-metabolizing enzyme and transporter expression on the pharmacokinetics of cyclosporine in rats
Impact of quercetin-induced changes in drug-metabolizing enzyme and transporter expression on the pharmacokinetics of cyclosporine in rats Abstract Abstract The aim of the present study was to evaluate whether quercetin (Que) modulates the mRNA and protein expression levels of drug-metabolizing enzymes (DMEs) and drug ...
PMC8665708
core_pubmed_pmc
Pharmacokinetic/Pharmacodynamic Considerations of Alternate Dosing Strategies of Tocilizumab in COVID-19
Pharmacokinetic/Pharmacodynamic Considerations of Alternate Dosing Strategies of Tocilizumab in COVID-19 Abstract Abstract Tocilizumab is one of few treatments that have been shown to improve mortality in patients with coronavirus disease 2019 (COVID-19), but increased demand has led to relative global shortages. Recen...
PMC9298631
core_pubmed_pmc
A rapid LC-MS/MS method for simultaneous determination of quetiapine and duloxetine in rat plasma and its application to pharmacokinetic interaction study
A rapid LC-MS/MS method for simultaneous determination of quetiapine and duloxetine in rat plasma and its application to pharmacokinetic interaction study Abstract Abstract Combinations of new antidepressants like duloxetine and second-generation antipsychotics like quetiapine are used in clinical treatment of major de...
PMC4215334
core_pubmed_pmc
Mathematical Modeling of HIV Dynamics After Antiretroviral Therapy Initiation: A Review
Mathematical Modeling of HIV Dynamics After Antiretroviral Therapy Initiation: A Review Abstract Abstract This review shows the potential ground-breaking impact that mathematical tools may have in the analysis and the understanding of the HIV dynamics. In the first part, early diagnosis of immunological failure is infe...
PMC9599051
core_pubmed_pmc
New Betulin Derivatives with Nitrogen Heterocyclic Moiety—Synthesis and Anticancer Activity In Vitro
New Betulin Derivatives with Nitrogen Heterocyclic Moiety—Synthesis and Anticancer Activity In Vitro Abstract As part of the search for new medicinal substances with potential application in oncology, the synthesis of new compounds combining the betulin molecule and the indole system was carried out. The structure of t...
PMC6250104
core_pubmed_pmc
Efficacy of isothiocyanate-based compounds on different forms of persistent pain
Efficacy of isothiocyanate-based compounds on different forms of persistent pain Abstract Abstract Purpose Current pharmacotherapy for persistent pain related to neuropathy or articular diseases is unsatisfactory, due to the large number of unresponsive patients and side effects. Isothiocyanates (ITCs) are a class of n...
PMC10883330
core_pubmed_pmc
Herb-drug interactions of silybinin and cilofexor in beagle dogs based on pharmacokinetics by UPLC-MS/MS
Herb-drug interactions of silybinin and cilofexor in beagle dogs based on pharmacokinetics by UPLC-MS/MS Abstract Objective: A remarkably sensitive, accurate, and efficient ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) approach was developed as a facile and expeditious method for measuri...
PMC6890782
core_pubmed_pmc
Population pharmacokinetics of afatinib and exposure-safety relationships in Japanese patients with EGFR mutation-positive non-small cell lung cancer
Population pharmacokinetics of afatinib and exposure-safety relationships in Japanese patients with EGFR mutation-positive non-small cell lung cancer Abstract Abstract To investigate the exposure–safety relationships of afatinib in Japanese population, we performed population pharmacokinetics (PK) analysis of afatinib ...
PMC12371689
core_pubmed_pmc
Engineering Fusion Proteins for Nanomedicine-Based Cytokine Therapy
Engineering Fusion Proteins for Nanomedicine-Based Cytokine Therapy Abstract Cytokines play a crucial role in cell communication and immunity, making them interesting potential therapeutics for immune-mediated conditions. However, cytokine therapeutics’ clinical translation is hampered by their short blood half-lives a...
PMC11571218
core_pubmed_pmc
68 Ga-Labeled TRAP-Based Glycoside Trimers for Imaging of the Functional Liver Reserve
68 Ga-Labeled TRAP-Based Glycoside Trimers for Imaging of the Functional Liver Reserve Abstract The exclusive asialoglycoprotein receptor (ASGR) expression on hepatocytes makes it an attractive target for imaging of the functional liver reserve. Here, we present a set of TRAP-based glycoside trimers and evaluate their ...
PMC6784111
core_pubmed_pmc
Optimization of an Antibody Light Chain Framework Enhances Expression, Biophysical Properties and Pharmacokinetics
Optimization of an Antibody Light Chain Framework Enhances Expression, Biophysical Properties and Pharmacokinetics Abstract Efficacy, safety, and manufacturability of therapeutic antibodies are influenced by their biopharmaceutical and biophysical properties. These properties can be optimized by library approaches or r...
PMC6927760
core_pubmed_pmc
Heparin chromatography as an in vitro predictor for antibody clearance rate through pinocytosis
Heparin chromatography as an in vitro predictor for antibody clearance rate through pinocytosis Abstract ABSTRACT The pharmacokinetic (PK) properties of therapeutic antibodies directly affect efficacy, dose and dose intervals, application route and tissue penetration. In indications where health-care providers and pati...
PMC8069034
core_pubmed_pmc
Pharmacokinetic-Pharmacodynamic Modelling of Systemic IL13 Blockade by Monoclonal Antibody Therapy: A Free Assay Disguised as Total
Pharmacokinetic-Pharmacodynamic Modelling of Systemic IL13 Blockade by Monoclonal Antibody Therapy: A Free Assay Disguised as Total Abstract A sequential pharmacokinetic (PK) and pharmacodynamic (PD) model was built with Nonlinear Mixed Effects Modelling based on data from a first-in-human trial of a novel biologic, ME...
PMC8601347
core_pubmed_pmc
Efficacy and Safety of Vilobelimab (IFX-1), a Novel Monoclonal Anti-C5a Antibody, in Patients With Early Severe Sepsis or Septic Shock—A Randomized, Placebo-Controlled, Double-Blind, Multicenter, Phase IIa Trial (SCIENS Study)
Efficacy and Safety of Vilobelimab (IFX-1), a Novel Monoclonal Anti-C5a Antibody, in Patients With Early Severe Sepsis or Septic Shock—A Randomized, Placebo-Controlled, Double-Blind, Multicenter, Phase IIa Trial (SCIENS Study) Abstract Supplemental Digital Content is available in the text. Keywords: adult, antibodies, ...
PMC6154303
core_pubmed_pmc
ABC Transport Proteins in Cardiovascular Disease—A Brief Summary
ABC Transport Proteins in Cardiovascular Disease—A Brief Summary Abstract Abstract Adenosine triphosphate (ATP)-binding cassette (ABC) transporters may play an important role in the pathogenesis of atherosclerotic vascular diseases due to their involvement in cholesterol homeostasis, blood pressure regulation, endothel...
PMC6994432
core_pubmed_pmc
High Variability of Whole-Blood Tacrolimus Pharmacokinetics Early After Thoracic Organ Transplantation
High Variability of Whole-Blood Tacrolimus Pharmacokinetics Early After Thoracic Organ Transplantation Abstract Background and Objective Oral tacrolimus is initiated perioperatively in heart and lung transplantation patients. There have been few studies on oral tacrolimus pharmacokinetics early post-transplantation, ev...
PMC7761579
core_pubmed_pmc
Clinically Relevant Interactions between Atypical Antipsychotics and Anti-Infective Agents
Clinically Relevant Interactions between Atypical Antipsychotics and Anti-Infective Agents Abstract This is a comprehensive review of the literature on drug interactions (DIs) between atypical antipsychotics and anti-infective agents that focuses on those DIs with the potential to be clinically relevant and classifies ...
PMC11271341
core_pubmed_pmc
The OCT2/MATE1 Interaction Between Trifluridine, Metformin and Cimetidine: A Crossover Pharmacokinetic Study
The OCT2/MATE1 Interaction Between Trifluridine, Metformin and Cimetidine: A Crossover Pharmacokinetic Study Abstract Background and Objectives Trifluridine/tipiracil, registered for the treatment of patients with metastatic gastric and colorectal cancer, is a substrate and inhibitor for the organic cation transporter ...
PMC5321809
core_pubmed_pmc
p16 INK4a , a Senescence Marker, Influences Tenofovir/Emtricitabine Metabolite Disposition in HIV‐Infected Subjects
p16 INK4a , a Senescence Marker, Influences Tenofovir/Emtricitabine Metabolite Disposition in HIV‐Infected Subjects Abstract Abstract The goal of this study was to explore the relationships between tenofovir (TFV) and emtricitabine (FTC) disposition and markers of biologic aging, such as the frailty phenotype and p16 I...
PMC4306193
core_pubmed_pmc
A Prospective Population Pharmacokinetic Analysis of Sapropterin Dihydrochloride in Infants and Young Children with Phenylketonuria
A Prospective Population Pharmacokinetic Analysis of Sapropterin Dihydrochloride in Infants and Young Children with Phenylketonuria Abstract Abstract Background and Objectives Untreated phenylketonuria (PKU), a hereditary metabolic disorder caused by a genetic mutation in phenylalanine hydroxylase (PAH), is characteriz...
PMC9359604
core_pubmed_pmc
The importance of pharmacokinetics and pharmacodynamics in antimicrobial drug development and their influence on the success of agents developed to combat resistant gram negative pathogens: A review
The importance of pharmacokinetics and pharmacodynamics in antimicrobial drug development and their influence on the success of agents developed to combat resistant gram negative pathogens: A review Abstract Abstract A deep understanding of an antimicrobial’s critical pharmacokinetic and pharmacodynamic properties is c...
PMC11028011
core_pubmed_pmc
Reducing neonatal Fc receptor binding enhances clearance and brain-to-blood ratio of TfR-delivered bispecific amyloid-β antibody
Reducing neonatal Fc receptor binding enhances clearance and brain-to-blood ratio of TfR-delivered bispecific amyloid-β antibody Abstract ABSTRACT Recent development of amyloid-β (Aβ)-targeted immunotherapies for Alzheimer’s disease (AD) have highlighted the need for accurate diagnostic methods. Antibody-based positron...
PMC6921013
core_pubmed_pmc
Preparation, Characterization, and In Vivo Pharmacokinetic Study of the Supercritical Fluid-Processed Liposomal Amphotericin B
Preparation, Characterization, and In Vivo Pharmacokinetic Study of the Supercritical Fluid-Processed Liposomal Amphotericin B Abstract Here, we aimed to prepare and optimize liposomal amphotericin B (AmB) while using the supercritical fluid of carbon dioxide (SCF-CO 2 ) method and investigate the characteristics and p...
PMC4599605
core_pubmed_pmc
Preparation and characterization of cefditoren pivoxil-loaded liposomes for controlled in vitro and in vivo drug release
Preparation and characterization of cefditoren pivoxil-loaded liposomes for controlled in vitro and in vivo drug release Abstract Background The application of antibiotics has been limited due to weak biodistribution and pharmacokinetics. Encapsulation of these drugs in lipid vesicles might be a good solution for obtai...
PMC12111380
core_pubmed_pmc
Bibliometric Analysis of Research Trends and Global Collaborations in Anesthesia on Neuromuscular Blockers and Antagonists (2000–2024)
Bibliometric Analysis of Research Trends and Global Collaborations in Anesthesia on Neuromuscular Blockers and Antagonists (2000–2024) Abstract Abstract (1) Background: The aim of this bibliometric study is to analyze global research trends, citation impact, and scientific collaborations in the field of neuromuscular b...
PMC9373814
core_pubmed_pmc
3p-C-NETA: A versatile and effective chelator for development of Al 18 F-labeled and therapeutic radiopharmaceuticals
3p-C-NETA: A versatile and effective chelator for development of Al 18 F-labeled and therapeutic radiopharmaceuticals Abstract Abstract Background : Radiolabeled somatostatin analogues ( e.g. [ 68 Ga]Ga-DOTATATE and [ 177 Lu]Lu-DOTATATE) have been used to diagnose, monitor, and treat neuroendocrine tumour (NET) patient...
PMC3214562
core_pubmed_pmc
Therapeutic drug monitoring of vancomycin in an obese patient with renal insufficiency
Therapeutic drug monitoring of vancomycin in an obese patient with renal insufficiency Abstract We report the pharmacokinetics of vancomycin in an obese patient with renal insufficiency using pharmacokinetic equations, and comparing them with actual levels. A 47-year-old man with morbid obesity had a complicated hospit...
PMC9502382
core_pubmed_pmc
Promising Nanocarriers to Enhance Solubility and Bioavailability of Cannabidiol for a Plethora of Therapeutic Opportunities
Promising Nanocarriers to Enhance Solubility and Bioavailability of Cannabidiol for a Plethora of Therapeutic Opportunities Abstract Abstract In recent years, the interest in cannabidiol (CBD) has increased because of the lack of psychoactive properties. However, CBD has low solubility and bioavailability, variable pha...
PMC9896117
core_pubmed_pmc
De Novo Seizures, Obsessive Compulsive Symptoms and Neutropenias in Patients on Clozapine: A Retrospective Cohort Study
De Novo Seizures, Obsessive Compulsive Symptoms and Neutropenias in Patients on Clozapine: A Retrospective Cohort Study Abstract Background: Clozapine has well-documented inter-ethnic variations in pharmacokinetics. There is a paucity of data about clozapine use and associated adverse events such as seizures, obsessive...
PMC11530583
core_pubmed_pmc
Molecular mechanisms of sulforaphane in Alzheimer’s disease: insights from an in-silico study
Molecular mechanisms of sulforaphane in Alzheimer’s disease: insights from an in-silico study Abstract This study was to identify the molecular pathways that may explain sulforaphane’s Alzheimer’s disease (AD) benefits using multiple advanced in silico approaches. We found that sulforaphane regulates 45 targets, includ...
PMC6309049
core_pubmed_pmc
Pre-Existing Liver Disease and Toxicity of Antifungals
Pre-Existing Liver Disease and Toxicity of Antifungals Abstract Abstract Pre-existing liver disease in patients with invasive fungal infections further complicates their management. Altered pharmacokinetics and tolerance issues of antifungal drugs are important concerns. Adjustment of the dosage of antifungal agents in...
PMC6896251
core_pubmed_pmc
Exposure–Response Analyses of Upadacitinib Efficacy in Phase II Trials in Rheumatoid Arthritis and Basis for Phase III Dose Selection
Exposure–Response Analyses of Upadacitinib Efficacy in Phase II Trials in Rheumatoid Arthritis and Basis for Phase III Dose Selection Abstract Abstract The relationships between upadacitinib, an oral selective Janus kinase 1 inhibitor, plasma exposures, and its efficacy (assessed by the American College of Rheumatology...
PMC11419873
core_pubmed_pmc
Spectroscopic, anti-cancer, anti-bacterial and theoretical studies of new bivalent Schiff base complexes derived from 4-bromo-2,6-dichloroaniline
Spectroscopic, anti-cancer, anti-bacterial and theoretical studies of new bivalent Schiff base complexes derived from 4-bromo-2,6-dichloroaniline Abstract Abstract In this paper, four new mono-nuclear Ni(II), Pd(II), Pt(II) and Zn(II) complexes were prepared by using a bi-dentate Schiff base ligand, ( E )-2-(((4-bromo-...
PMC12298532
core_pubmed_pmc
Exploring the Phytochemical Profile and Therapeutic Potential of Saudi Native Santolina chamaecyparissus L. Essential Oil
Exploring the Phytochemical Profile and Therapeutic Potential of Saudi Native Santolina chamaecyparissus L. Essential Oil Abstract Abstract Background/Objectives: Medicinal plants such as Santolina chamaecyparissus L., an evergreen shrub from the Asteraceae family, have long been valued for their bioactive compounds an...
PMC4289315
core_pubmed_pmc
Treatment of bloodstream infections in ICUs
Treatment of bloodstream infections in ICUs Abstract Abstract Bloodstream infections (BSIs) are frequent in ICU and is a prognostic factor of severe sepsis. Community acquired BSIs usually due to susceptible bacteria should be clearly differentiated from healthcare associated BSIs frequently due to resistant hospital s...
PMC4407781
core_pubmed_pmc
High variability in the dosing of commonly used antibiotics revealed by a Europe-wide point prevalence study: implications for research and dissemination
High variability in the dosing of commonly used antibiotics revealed by a Europe-wide point prevalence study: implications for research and dissemination Abstract Abstract Background Antibiotic dosing in neonates varies between countries and centres, suggesting suboptimal exposures for some neonates. We aimed to descri...
PMC9007598
core_pubmed_pmc
Efficient simulation of clinical target response surfaces
Efficient simulation of clinical target response surfaces Abstract Abstract Simulation of combination therapies is challenging due to computational complexity. Either a simple model is used to simulate the response for many combinations of concentration to generate a response surface but parameter variability and uncer...
PMC3582054
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Bioequivalence Study of Pantoprazole Sodium-HPBCD and Conventional Pantoprazole Sodium Enteric-Coated Tablet Formulations
Bioequivalence Study of Pantoprazole Sodium-HPBCD and Conventional Pantoprazole Sodium Enteric-Coated Tablet Formulations Abstract Abstract The objective of this study was to investigate the bioequivalence of two formulations of 40 mg pantoprazole sodium enteric-coated tablets: Tripepsa as the test and Pantocid as the ...
PMC9217999
core_pubmed_pmc
Cobimetinib in Pediatric and Young Adult Patients with Relapsed or Refractory Solid Tumors (iMATRIX-cobi): A Multicenter, Phase I/II Study
Cobimetinib in Pediatric and Young Adult Patients with Relapsed or Refractory Solid Tumors (iMATRIX-cobi): A Multicenter, Phase I/II Study Abstract Background The MAPK pathway is an emerging target across a number of adult and pediatric tumors. Targeting the downstream effector of MAPK, MEK1, is a proposed strategy to ...
PMC4834099
core_pubmed_pmc
Effect of hepatic or renal impairment on the pharmacokinetics of evacetrapib
Effect of hepatic or renal impairment on the pharmacokinetics of evacetrapib Abstract Purpose The aim of this study is to investigate the effect of hepatic or renal impairment on the pharmacokinetics of a single 130-mg evacetrapib dose. Methods Two open-label, parallel-design studies in males and females with normal he...
PMC12265985
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Clinical Pharmacology and Medication Safety: A Remote Learning Elective Designed for Senior Medical Students
Clinical Pharmacology and Medication Safety: A Remote Learning Elective Designed for Senior Medical Students Abstract ABSTRACT In the United States, medical educators have expressed concern that an integrated and condensed pre‐clerkship curriculum risks leaving gaps in student pharmacology knowledge. This study evaluat...
PMC3974692
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Fc-fusion technology and recombinant FVIII and FIX in the management of the hemophilias
Fc-fusion technology and recombinant FVIII and FIX in the management of the hemophilias Abstract Abstract Prophylaxis with regular infusions of factor VIII (FVIII)- or factor IX (FIX)- containing products is the mainstay of modern hemophilia care. However, this therapeutic regimen is inconvenient, requiring repeated in...
PMC6540481
core_pubmed_pmc
Therapeutic levetiracetam monitoring during pregnancy: “mind the gap”
Therapeutic levetiracetam monitoring during pregnancy: “mind the gap” Abstract Background: Epilepsy is one of the most common chronic neurological conditions and its treatment during pregnancy is challenging. Levetiracetam (LEV) is an antiepileptic medication frequently used during pregnancy. Only a few small studies h...
PMC9653995
core_pubmed_pmc
New Positive TRPC6 Modulator Penetrates Blood–Brain Barrier, Eliminates Synaptic Deficiency and Restores Memory Deficit in 5xFAD Mice
New Positive TRPC6 Modulator Penetrates Blood–Brain Barrier, Eliminates Synaptic Deficiency and Restores Memory Deficit in 5xFAD Mice Abstract Abstract Synapse loss in the brain of Alzheimer’s disease patients correlates with cognitive dysfunctions. Drugs that limit synaptic loss are promising pharmacological agents. T...
PMC5573752
core_pubmed_pmc
Exposure–response relationship of ramucirumab in patients with advanced second-line colorectal cancer: exploratory analysis of the RAISE trial
Exposure–response relationship of ramucirumab in patients with advanced second-line colorectal cancer: exploratory analysis of the RAISE trial Abstract Purpose To characterize ramucirumab exposure–response relationships for efficacy and safety in patients with metastatic colorectal cancer (mCRC) using data from the RAI...
PMC9349145
core_pubmed_pmc
Safety, Pharmacodynamics, and Pharmacokinetics of P2X3 Receptor Antagonist Eliapixant (BAY 1817080) in Healthy Subjects: Double-Blind Randomized Study
Safety, Pharmacodynamics, and Pharmacokinetics of P2X3 Receptor Antagonist Eliapixant (BAY 1817080) in Healthy Subjects: Double-Blind Randomized Study Abstract Background and Objective There is no licensed treatment for refractory chronic cough; off-label therapies have limited efficacy and can produce adverse effects....
PMC11701948
core_pubmed_pmc
Pharmacokinetics and Bioequivalence of a Generic Ticagrelor 90‐mg Formulation Versus the Innovator Product in Healthy White Subjects Under Fasting Conditions
Pharmacokinetics and Bioequivalence of a Generic Ticagrelor 90‐mg Formulation Versus the Innovator Product in Healthy White Subjects Under Fasting Conditions Abstract Abstract Ticagrelor is a key antiplatelet agent used to prevent thrombotic events in patients with acute coronary syndrome. This open‐label, 2‐period, cr...
PMC8464313
core_pubmed_pmc
Stability of Amoxicillin and Clavulanic Acid in Separate Containers for Administration via a Y-Site
Stability of Amoxicillin and Clavulanic Acid in Separate Containers for Administration via a Y-Site Abstract Abstract Rationale With the discovery of new antibiotics diminishing, optimising the administration of existing antibiotics such as amoxicillin-clavulanic acid has become a necessity. At present, the optimal app...
PMC8486002
core_pubmed_pmc
Quantification of CYP3A and Drug Transporters Activity in Healthy Young, Healthy Elderly and Chronic Kidney Disease Elderly Patients by a Microdose Cocktail Approach
Quantification of CYP3A and Drug Transporters Activity in Healthy Young, Healthy Elderly and Chronic Kidney Disease Elderly Patients by a Microdose Cocktail Approach Abstract Abstract Background: Ageing and chronic kidney disease (CKD) affect pharmacokinetic (PK) parameters. Since mechanisms are related and remain uncl...
PMC11287820
core_pubmed_pmc
Drug–drug interactions between pemafibrate and statins on pharmacokinetics in healthy male volunteers: Open‐label, randomized, 6‐sequence, 3‐period crossover studies
Drug–drug interactions between pemafibrate and statins on pharmacokinetics in healthy male volunteers: Open‐label, randomized, 6‐sequence, 3‐period crossover studies Abstract Abstract Elevated triglyceride levels are associated with an increased risk of cardiovascular events despite guideline‐based statin treatment of ...
PMC8522722
core_pubmed_pmc
Safety and Pharmacokinetics in Human Volunteers of Taniborbactam (VNRX-5133), a Novel Intravenous β-Lactamase Inhibitor
Safety and Pharmacokinetics in Human Volunteers of Taniborbactam (VNRX-5133), a Novel Intravenous β-Lactamase Inhibitor Abstract ABSTRACT Taniborbactam (formerly VNRX-5133), an investigational β-lactamase inhibitor active against both serine- and metallo-β-lactamases, is being developed in combination with cefepime to ...
PMC8117418
core_pubmed_pmc
Applications of Virtual Screening in Bioprospecting: Facts, Shifts, and Perspectives to Explore the Chemo-Structural Diversity of Natural Products
Applications of Virtual Screening in Bioprospecting: Facts, Shifts, and Perspectives to Explore the Chemo-Structural Diversity of Natural Products Abstract Natural products are continually explored in the development of new bioactive compounds with industrial applications, attracting the attention of scientific researc...
PMC4134498
core_pubmed_pmc
Phase I study of olaparib in combination with liposomal doxorubicin in patients with advanced solid tumours
Phase I study of olaparib in combination with liposomal doxorubicin in patients with advanced solid tumours Abstract Abstract Background: Olaparib, an oral PARP inhibitor, has shown antitumour activity as monotherapy in patients with germline BRCA1/2 (gBRCA)-mutated breast and ovarian cancer. This study evaluated olapa...
PMC6133083
core_pubmed_pmc
Pharmacokinetics of the P-gp Inhibitor Tariquidar in Rats After Intravenous, Oral, and Intraperitoneal Administration
Pharmacokinetics of the P-gp Inhibitor Tariquidar in Rats After Intravenous, Oral, and Intraperitoneal Administration Abstract Abstract Background and objective P-glycoprotein (P-gp), a transmembrane transporter expressed at the blood–brain barrier, restricts the distribution of diverse central nervous system-targeted ...
PMC11104392
core_pubmed_pmc
Key Transdermal Patch Using Cannabidiol-Loaded Nanocarriers with Better Pharmacokinetics in vivo
Key Transdermal Patch Using Cannabidiol-Loaded Nanocarriers with Better Pharmacokinetics in vivo Abstract Abstract Purpose Cannabidiol (CBD) is a promising therapeutic drug with low addictive potential and a favorable safety profile. However, CBD did face certain challenges, including poor solubility in water and low o...
PMC4791488
core_pubmed_pmc
Accelerating Monte Carlo power studies through parametric power estimation
Accelerating Monte Carlo power studies through parametric power estimation Abstract Estimating the power for a non-linear mixed-effects model-based analysis is challenging due to the lack of a closed form analytic expression. Often, computationally intensive Monte Carlo studies need to be employed to evaluate the power...
PMC9990447
core_pubmed_pmc
The Use of Muscle Relaxants in Pregnancy and Puerperium Period
The Use of Muscle Relaxants in Pregnancy and Puerperium Period Abstract Abstract Introduction Anaesthetising a pregnant woman and during the postpartum period is challenging for most anaesthetists. There are many factors involved, including all the physiological changes that occur in the body of such a woman. Particula...
PMC8921106
core_pubmed_pmc
Chlordecone: development of a physiologically based pharmacokinetic tool to support human health risks assessments
Chlordecone: development of a physiologically based pharmacokinetic tool to support human health risks assessments Abstract Chlordecone (CD; Kepone™) is a carcinogenic organochlorine insecticide with neurological, reproductive, and developmental toxicity that was widely used in the French West Indies (FWI) from 1973 to...
PMC12856013
core_pubmed_pmc
An integrative computational approach for identification of NLRP3 inhibitors through machine learning, docking, dynamics and DFT analysis
An integrative computational approach for identification of NLRP3 inhibitors through machine learning, docking, dynamics and DFT analysis Abstract Abstract Neuroinflammation, mediated by NLR family pyrin domain containing 3 (NLRP3) inflammasome, plays a crucial role in the development of many central nervous system (CN...
PMC10244018
core_pubmed_pmc
Population Pharmacokinetic−Pharmacodynamic Modeling of Carvedilol to Evaluate the Effect of Cytochrome P450 2D6 Genotype on the Heart Rate Reduction
Population Pharmacokinetic−Pharmacodynamic Modeling of Carvedilol to Evaluate the Effect of Cytochrome P450 2D6 Genotype on the Heart Rate Reduction Abstract Background Carvedilol is a beta-adrenergic receptor antagonist primarily metabolized by cytochromes P450 (CYP) 2D6. This study established a carvedilol population...
PMC11655901
core_pubmed_pmc
Mass balance, metabolic disposition, and pharmacokinetics of a single IV dose of [14C]CA102N in HT-29 xenograft athymic nude mice
Mass balance, metabolic disposition, and pharmacokinetics of a single IV dose of [14C]CA102N in HT-29 xenograft athymic nude mice Abstract Abstract Introduction CA102N is a novel anticancer drug developed by covalently linking H-Nim (N-(4-Amino-2-phenoxyphenyl methanesulfonamide) to Hyaluronic Acid to target CD44 recep...
PMC10140125
core_pubmed_pmc
A phase I dose-escalation study of SYHA1813, a VEGFR and CSF1R inhibitor, in patients with recurrent High-Grade Gliomas or Advanced Solid Tumors
A phase I dose-escalation study of SYHA1813, a VEGFR and CSF1R inhibitor, in patients with recurrent High-Grade Gliomas or Advanced Solid Tumors Abstract SYHA1813 is a potent multikinase inhibitor that targets vascular endothelial growth factor receptors (VEGFRs)/colony-stimulating factor 1 receptor (CSF1R). This study...
PMC5786764
core_pubmed_pmc
Extreme Drug Tolerance of Mycobacterium tuberculosis in Caseum
Extreme Drug Tolerance of Mycobacterium tuberculosis in Caseum Abstract ABSTRACT Tuberculosis (TB) recently became the leading infectious cause of death in adults, while attempts to shorten therapy have largely failed. Dormancy, persistence, and drug tolerance are among the factors driving the long therapy duration. As...
PMC12676261
core_pubmed_pmc
Managing Delayed or Missed Doses of Prolonged‐Release Tacrolimus in Transplant Recipients: Implications for Drug Exposure and Recovery Strategies
Managing Delayed or Missed Doses of Prolonged‐Release Tacrolimus in Transplant Recipients: Implications for Drug Exposure and Recovery Strategies Abstract ABSTRACT In lifelong immunosuppressive therapy, missed doses of prolonged‐release tacrolimus are almost inevitable and may reduce drug exposure, compromising transpl...
PMC9786613
core_pubmed_pmc
Clinical Pharmacology Perspectives for Adoptive Cell Therapies in Oncology
Clinical Pharmacology Perspectives for Adoptive Cell Therapies in Oncology Abstract Abstract Adoptive cell therapies (ACTs) have shown transformative efficacy in oncology with five US Food and Drug Administration (FDA) approvals for chimeric antigen receptor (CAR) T‐cell therapies in hematological malignancies, and pro...
PMC3218805
core_pubmed_pmc
Accelerating drug discovery for Alzheimer's disease: best practices for preclinical animal studies
Accelerating drug discovery for Alzheimer's disease: best practices for preclinical animal studies Abstract Animal models have contributed significantly to our understanding of the underlying biological mechanisms of Alzheimer's disease (AD). As a result, over 300 interventions have been investigated and reported to mi...
PMC12907775
core_pubmed_pmc
Development of Pediatric Dosing for Mepolizumab in Severe Asthma Based on Extrapolation of Data From Adult Patients and a Phase II Open‐Label Pediatric Trial
Development of Pediatric Dosing for Mepolizumab in Severe Asthma Based on Extrapolation of Data From Adult Patients and a Phase II Open‐Label Pediatric Trial Abstract Abstract The benefit–risk profile of mepolizumab in severe asthma was established through clinical trials in adults, leading to EU and US approvals in 20...
PMC12423445
core_pubmed_pmc
Pharmacokinetic and Pharmacodynamic Interaction of Metformin and Ojeok-san in Healthy Volunteers
Pharmacokinetic and Pharmacodynamic Interaction of Metformin and Ojeok-san in Healthy Volunteers Abstract Abstract Purpose This study aimed to evaluate the pharmacokinetics and pharmacodynamics of metformin and Ojeok-san (OJS) co-administration to healthy volunteers compared to those with metformin alone. Methods This ...
PMC6277320
core_pubmed_pmc
Isavuconazole Kinetic Exploration for Clinical Practice
Isavuconazole Kinetic Exploration for Clinical Practice Abstract Abstract Background Isavuconazole is a new antifungal prodrug for the treatment of invasive aspergillosis and mucormycosis. As no clear pharmacokinetic-pharmacodynamic relationship has been established for patients, therapeutic drug monitoring is not curr...
PMC7051925
core_pubmed_pmc
Clinical Pharmacokinetics and Pharmacodynamics of Risankizumab in Psoriasis Patients
Clinical Pharmacokinetics and Pharmacodynamics of Risankizumab in Psoriasis Patients Abstract Abstract Risankizumab is a humanized immunoglobulin (Ig) G1 monoclonal antibody developed and approved for the treatment of moderate-to-severe plaque psoriasis at a dose of 150 mg administered subcutaneously at weeks 0 and 4, ...
PMC11312735
core_pubmed_pmc
Advances in Psychotropic Treatment for Pregnant Women: Efficacy, Adverse Outcomes, and Therapeutic Monitoring
Advances in Psychotropic Treatment for Pregnant Women: Efficacy, Adverse Outcomes, and Therapeutic Monitoring Abstract Advancements in psychotropic therapy for pregnant women are pivotal for addressing maternal mental health during the perinatal period. Screening for mood and anxiety symptoms during pregnancy is recomm...
PMC8752533
core_pubmed_pmc
Effects of Cytochrome P450 3A4 Induction and Inhibition on the Pharmacokinetics of BI 425809, a Novel Glycine Transporter 1 Inhibitor
Effects of Cytochrome P450 3A4 Induction and Inhibition on the Pharmacokinetics of BI 425809, a Novel Glycine Transporter 1 Inhibitor Abstract Background and Objective Increased glycine availability at the synaptic cleft may enhance N -methyl-D-aspartate receptor signalling and provide a promising therapeutic strategy ...
PMC7682229
core_pubmed_pmc
Pharmacokinetics and tolerability of LIQ861, a novel dry-powder formulation of treprostinil
Pharmacokinetics and tolerability of LIQ861, a novel dry-powder formulation of treprostinil Abstract A dry-powder inhaled formulation of treprostinil (LIQ861) produced using PRINT® technology offers a substantial advantage over current nebulized therapy. Treprostinil is a synthetic prostacyclin analogue that is current...
PMC11213902
core_pubmed_pmc
Enhancing hepatoprotective action: oxyberberine amorphous solid dispersion system targeting TLR4
Enhancing hepatoprotective action: oxyberberine amorphous solid dispersion system targeting TLR4 Abstract Abstract Oxyberberine (OBB) is a significant natural compound, with excellent hepatoprotective properties. However, the poor water solubility of OBB hinders its release and absorption thus resulting in low bioavail...
PMC6202466
core_pubmed_pmc
Physiologically Based Pharmacokinetic Approach to Determine Dosing on Extracorporeal Life Support: Fluconazole in Children on ECMO
Physiologically Based Pharmacokinetic Approach to Determine Dosing on Extracorporeal Life Support: Fluconazole in Children on ECMO Abstract Extracorporeal life support (e.g., dialysis, extracorporeal membrane oxygenation ( ECMO )) can affect drug disposition, placing patients at risk for therapeutic failure. In this po...
PMC5789074
core_pubmed_pmc
Pharmacokinetics and in vitro/in vivo antitumor efficacy of aptamer-targeted Ecoflex ® nanoparticles for docetaxel delivery in ovarian cancer
Pharmacokinetics and in vitro/in vivo antitumor efficacy of aptamer-targeted Ecoflex ® nanoparticles for docetaxel delivery in ovarian cancer Abstract Abstract Purpose Epithelixal ovarian cancer is the fourth cause of cancer death in developed countries with 77% of ovarian cancer cases diagnosed with regional or distan...
PMC9188616
core_pubmed_pmc
A Phase 1, Open-Label Study to Evaluate the Effects of Food and Evening Dosing on the Pharmacokinetics of Oral Trofinetide in Healthy Adult Subjects
A Phase 1, Open-Label Study to Evaluate the Effects of Food and Evening Dosing on the Pharmacokinetics of Oral Trofinetide in Healthy Adult Subjects Abstract Abstract Background and Objective Trofinetide, a synthetic analog of tripeptide glycine-proline-glutamate, is an investigational agent for the treatment of Rett s...
PMC4249437
core_pubmed_pmc
A First-in-Human Randomized, Double-Blind, Placebo-Controlled, Single- and Multiple-Ascending Oral Dose Study of Novel Imidazolopiperazine KAF156 To Assess Its Safety, Tolerability, and Pharmacokinetics in Healthy Adult Volunteers
A First-in-Human Randomized, Double-Blind, Placebo-Controlled, Single- and Multiple-Ascending Oral Dose Study of Novel Imidazolopiperazine KAF156 To Assess Its Safety, Tolerability, and Pharmacokinetics in Healthy Adult Volunteers Abstract KAF156 belongs to a new class of antimalarial, the imidazolopiperazines, and is ...
PMC5542428
core_pubmed_pmc
Exploring public genomics data for population pharmacogenomics
Exploring public genomics data for population pharmacogenomics Abstract Racial and ethnic differences in drug responses are now well studied and documented. Pharmacogenomics research seeks to unravel the genetic underpinnings of inter-individual variability with the aim of tailored-made theranostics and therapeutics. T...