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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 | core_pubmed_pmc | 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 | core_pubmed_pmc | 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 | core_pubmed_pmc | 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 | core_pubmed_pmc | 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... |
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