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PMC11420315
core_pubmed_pmc
Population pharmacokinetics of TLD-1, a novel liposomal doxorubicin, in a phase I trial
Population pharmacokinetics of TLD-1, a novel liposomal doxorubicin, in a phase I trial Abstract Study objectives TLD-1 is a novel pegylated liposomal doxorubicin (PLD) formulation aiming to optimise the PLD efficacy-toxicity ratio. We aimed to characterise TLD-1’s population pharmacokinetics using non-compartmental an...
PMC11233223
core_pubmed_pmc
Cariprazine Orodispersible Tablet: A New Formulation for Cariprazine
Cariprazine Orodispersible Tablet: A New Formulation for Cariprazine Abstract Introduction Cariprazine is an atypical dopamine receptor partial agonist antipsychotic available in the form of capsules. Although capsules are one of the most desirable routes of administration, there are certain situations (e. g., in an ac...
PMC11750688
core_pubmed_pmc
stormTB: a web-based simulator of a murine minimal-PBPK model for anti-tuberculosis treatments
stormTB: a web-based simulator of a murine minimal-PBPK model for anti-tuberculosis treatments Abstract Abstract Introduction Tuberculosis (TB) poses a significant threat to global health, with millions of new infections and approximately one million deaths annually. Various modeling efforts have emerged, offering tail...
PMC7830259
core_pubmed_pmc
Colistimethate Acidic Hydrolysis Revisited: Arrhenius Equation Modeling Using UPLC-QToF MS
Colistimethate Acidic Hydrolysis Revisited: Arrhenius Equation Modeling Using UPLC-QToF MS Abstract Colistimethate (CMS), the prodrug of polymyxin E (colistin), is an antibiotic widely used as a last-line therapy against multidrug resistant Gram-negative bacteria, but little is known about its pharmacokinetics as its a...
PMC4878867
core_pubmed_pmc
The anti-tubercular drug delamanid as a potential oral treatment for visceral leishmaniasis
The anti-tubercular drug delamanid as a potential oral treatment for visceral leishmaniasis Abstract Abstract There is an urgent requirement for safe, oral and cost-effective drugs for the treatment of visceral leishmaniasis (VL). We report that delamanid (OPC-67683), an approved drug for multi-drug resistant tuberculo...
PMC5760825
core_pubmed_pmc
Precolumn derivatization LC–MS/MS method for the determination and pharmacokinetic study of glucosamine in human plasma and urine
Precolumn derivatization LC–MS/MS method for the determination and pharmacokinetic study of glucosamine in human plasma and urine Abstract Abstract A selective precolumn derivatization liquid chromatography–tandem mass spectrometric (LC–MS/MS) method for the determination of glucosamine in human plasma and urine has be...
PMC8290233
core_pubmed_pmc
Worse capecitabine treatment outcome in patients with a low skeletal muscle mass is not explained by altered pharmacokinetics
Worse capecitabine treatment outcome in patients with a low skeletal muscle mass is not explained by altered pharmacokinetics Abstract Abstract Background A low skeletal muscle mass (SMM) has been associated with increased toxicity and shorter survival in cancer patients treated with capecitabine, an oral prodrug of 5‐...
PMC4307648
core_pubmed_pmc
Effects of food and alcohol on the pharmacokinetics of an oral, extended-release formulation of hydrocodone in healthy volunteers
Effects of food and alcohol on the pharmacokinetics of an oral, extended-release formulation of hydrocodone in healthy volunteers Abstract Background The purpose of this study was to evaluate the pharmacokinetics, bioavailability, and safety of oral extended-release hydrocodone (HC-ER) when administered with food or al...
PMC12641134
core_pubmed_pmc
Results from the Survey of Antibiotic Resistance (SOAR) 2018–21 in India: data based on CLSI, EUCAST (dose-specific) and pharmacokinetic/pharmacodynamic (PK/PD) breakpoints
Results from the Survey of Antibiotic Resistance (SOAR) 2018–21 in India: data based on CLSI, EUCAST (dose-specific) and pharmacokinetic/pharmacodynamic (PK/PD) breakpoints Abstract Abstract Objectives Antibiotic susceptibility determination of community-acquired respiratory tract infection (CA-RTI) isolates of Strepto...
PMC8725905
core_pubmed_pmc
A novel irinotecan-lipiodol nanoemulsion for intravascular administration: pharmacokinetics and biodistribution in the normal and tumor bearing rat liver
A novel irinotecan-lipiodol nanoemulsion for intravascular administration: pharmacokinetics and biodistribution in the normal and tumor bearing rat liver Abstract Abstract Colorectal cancer is one of the most common cancers in the United States and treatment options are limited for patients who develop liver metastases...
PMC4544722
core_pubmed_pmc
Enhancement of absorption and bioavailability of echinacoside by verapamil or clove oil
Enhancement of absorption and bioavailability of echinacoside by verapamil or clove oil Abstract Purpose This present study investigated the absorption kinetics of echinacoside (ECH) in situ and in vitro and its oral bioavailability in rats. Additional aim was to find an agent(s) to promote ECH absorption and oral bioa...
PMC9399032
core_pubmed_pmc
Tigecycline Soft Tissue Penetration in Obese and Non-obese Surgical Patients Determined by Using In Vivo Microdialysis
Tigecycline Soft Tissue Penetration in Obese and Non-obese Surgical Patients Determined by Using In Vivo Microdialysis Abstract Background and Objective Tigecycline, a broad-spectrum glycylcycline antibiotic, is approved for use at a fixed dose irrespective of body weight. However, its pharmacokinetics may be altered i...
PMC11242948
core_pubmed_pmc
Selection and Mechanism Study of Q-Markers for Xanthocerais lignum Anti-Rheumatoid Arthritis Based on Serum Spectrum–Effect Correlation Analysis
Selection and Mechanism Study of Q-Markers for Xanthocerais lignum Anti-Rheumatoid Arthritis Based on Serum Spectrum–Effect Correlation Analysis Abstract Objective: To elucidate the chemical profile of Xanthocerais lignum’s extracts of different polarities and their impact on rheumatoid arthritis (RA), we identified an...
PMC11905262
core_pubmed_pmc
Data Mining of the FDA Adverse Event Reporting System and Animal Experiments for Assessment of Rhabdomyolysis Risk Associated with Lipid-lowering Drugs
Data Mining of the FDA Adverse Event Reporting System and Animal Experiments for Assessment of Rhabdomyolysis Risk Associated with Lipid-lowering Drugs Abstract Abstract Despite extensive research on pharmacokinetic interactions between hydroxymethylglutaryl-CoA reductase inhibitors (statins) and fibrates, the underlyi...
PMC8359322
core_pubmed_pmc
Safety, Tolerability, and Pharmacokinetics of Multiple Repeated Oral Doses of the α2/3/5‐Subtype Selective GABA A ‐Positive Allosteric Modulator PF‐06372865 in Healthy Volunteers
Safety, Tolerability, and Pharmacokinetics of Multiple Repeated Oral Doses of the α2/3/5‐Subtype Selective GABA A ‐Positive Allosteric Modulator PF‐06372865 in Healthy Volunteers Abstract Abstract Multiple‐dose pharmacokinetics (PK) and safety were investigated in this phase 1 study of PF‐06372865, a positive allosteri...
PMC9415024
core_pubmed_pmc
Population Pharmacodynamic Analyses of Human Anti-Rabies Virus Monoclonal Antibody (Ormutivimab) in Healthy Adult Subjects
Population Pharmacodynamic Analyses of Human Anti-Rabies Virus Monoclonal Antibody (Ormutivimab) in Healthy Adult Subjects Abstract Ormutivimab is the first recombinant human anti-rabies monoclonal antibody (rhRIG) approved for clinical application in China. In this study, a population pharmacodynamic (PPD) model was e...
PMC10999584
core_pubmed_pmc
Impact of bariatric surgery on cytochrome P 450 enzyme activity
Impact of bariatric surgery on cytochrome P 450 enzyme activity Abstract Abstract Bariatric surgeries are becoming more prevalent as obesity rates continue to rise. Being that it is an effective weight-loss procedure, it can induce significant anatomical, physiological, and metabolic alterations, which affect the pharm...
PMC12618306
core_pubmed_pmc
Therapeutic potential of purpurin, a natural anthraquinone dye, in neuroprotection and neurological disorders
Therapeutic potential of purpurin, a natural anthraquinone dye, in neuroprotection and neurological disorders Abstract Purpurin (1,2,4-trihydroxy-9,10-anthraquinone) is a naturally occurring anthraquinone pigment derived primarily from Rubia species. Beyond its traditional use as a natural dye, purpurin has recently ga...
PMC7485354
core_pubmed_pmc
Phase I Study of the Bifunctional Fusion Protein Bintrafusp Alfa in Asian Patients with Advanced Solid Tumors, Including a Hepatocellular Carcinoma Safety‐Assessment Cohort
Phase I Study of the Bifunctional Fusion Protein Bintrafusp Alfa in Asian Patients with Advanced Solid Tumors, Including a Hepatocellular Carcinoma Safety‐Assessment Cohort Abstract Abstract Lessons Learned Bintrafusp alfa had a manageable safety profile and demonstrated preliminary clinical activity in heavily pretrea...
PMC5107204
core_pubmed_pmc
Pharmacokinetics, Pharmacodynamics and Population Pharmacokinetic/Pharmacodynamic Modelling of Bilastine, a Second-Generation Antihistamine, in Healthy Japanese Subjects
Pharmacokinetics, Pharmacodynamics and Population Pharmacokinetic/Pharmacodynamic Modelling of Bilastine, a Second-Generation Antihistamine, in Healthy Japanese Subjects Abstract Abstract Background and objectives Bilastine is a novel second-generation antihistamine for the symptomatic treatment of allergic rhinitis an...
PMC3820704
core_pubmed_pmc
Pharmacokinetic comparison of the vasorelaxant compound ferulic acid following the administration of Guanxin II to healthy volunteers and patients with angina pectoris
Pharmacokinetic comparison of the vasorelaxant compound ferulic acid following the administration of Guanxin II to healthy volunteers and patients with angina pectoris Abstract Abstract Coronary heart disease (CHD) is the leading cause of mortality worldwide. The Chinese medicinal formula Guanxin II has been shown to h...
PMC3211509
core_pubmed_pmc
Investigation of utilization of nanosuspension formulation to enhance exposure of 1,3-dicyclohexylurea in rats: Preparation for PK/PD study via subcutaneous route of nanosuspension drug delivery
Investigation of utilization of nanosuspension formulation to enhance exposure of 1,3-dicyclohexylurea in rats: Preparation for PK/PD study via subcutaneous route of nanosuspension drug delivery Abstract 1,3-Dicyclohexylurea (DCU), a potent soluble epoxide hydrolase (sEH) inhibitor has been reported to lower systemic b...
PMC9144537
core_pubmed_pmc
Pharmacokinetics, Prostate Distribution and Metabolic Characteristics of Four Representative Flavones after Oral Administration of the Aerial Part of Glycyrrhiza uralensis in Rats
Pharmacokinetics, Prostate Distribution and Metabolic Characteristics of Four Representative Flavones after Oral Administration of the Aerial Part of Glycyrrhiza uralensis in Rats Abstract (1) Background: The aerial part of G. uralensis had pharmacological effects against chronic non-bacterial prostatitis (CNP), and fl...
PMC7817424
core_pubmed_pmc
Demographic representation in clinical trials for cell-based therapy
Demographic representation in clinical trials for cell-based therapy Abstract Inclusion of women and minorities in clinical research is critical to fully assess the safety and efficacy of innovative therapies. With inadequate representation of demography, generalizability is impaired since pharmacokinetics and pharmaco...
PMC7998425
core_pubmed_pmc
Pharmacokinetics of Meropenem in People with Cystic Fibrosis—A Proof of Concept Clinical Trial
Pharmacokinetics of Meropenem in People with Cystic Fibrosis—A Proof of Concept Clinical Trial Abstract Anti-infective treatment of pulmonary exacerbations is a major issue in people with cystic fibrosis (CF). Individualized dosing strategies and adaptation of infusion times are important concepts to optimize anti-infe...
PMC9765455
core_pubmed_pmc
S-217622, a SARS-CoV-2 main protease inhibitor, decreases viral load and ameliorates COVID-19 severity in hamsters
S-217622, a SARS-CoV-2 main protease inhibitor, decreases viral load and ameliorates COVID-19 severity in hamsters Abstract In parallel with vaccination, oral antiviral agents are highly anticipated to act as countermeasures for the treatment of the coronavirus disease 2019 (COVID-19) pandemic caused by severe acute re...
PMC9837366
core_pubmed_pmc
Effect of ANKK1 Polymorphisms on Serum Valproic Acid Concentration in Chinese Han Adult Patients in the Early Postoperative Period
Effect of ANKK1 Polymorphisms on Serum Valproic Acid Concentration in Chinese Han Adult Patients in the Early Postoperative Period Abstract Abstract Introduction This study aimed to investigate the relationship between gene polymorphisms and clinical factors with the concentrations of valproic acid (VPA) in adult patie...
PMC10508499
core_pubmed_pmc
Prediction of relative change in free nerve growth factor following subcutaneous administration of tanezumab, a novel monoclonal antibody to nerve growth factor
Prediction of relative change in free nerve growth factor following subcutaneous administration of tanezumab, a novel monoclonal antibody to nerve growth factor Abstract Abstract Tanezumab is a monoclonal antibody against nerve growth factor (NGF). We investigated tanezumab pharmacokinetic (PK)‐NGF relationships and pr...
PMC11022300
core_pubmed_pmc
Efficacy, safety, and pharmacokinetics of isoniazid affected by NAT2 polymorphisms in patients with tuberculosis: A systematic review
Efficacy, safety, and pharmacokinetics of isoniazid affected by NAT2 polymorphisms in patients with tuberculosis: A systematic review Abstract Abstract N‐acetyltransferase 2 ( NAT2 ) genetic polymorphisms might alter isoniazid metabolism leading to toxicity. We reviewed the impact of NAT2 genotype status on the pharmac...
PMC11258083
core_pubmed_pmc
Phase I pharmacokinetic, safety, and preliminary efficacy study of tiragolumab in combination with atezolizumab in Chinese patients with advanced solid tumors
Phase I pharmacokinetic, safety, and preliminary efficacy study of tiragolumab in combination with atezolizumab in Chinese patients with advanced solid tumors Abstract Abstract Purpose Tiragolumab is an immunoglobulin G1 monoclonal antibody targeting the immune checkpoint T cell immunoreceptor with immunoglobulin and i...
PMC4944667
core_pubmed_pmc
A Model for the Application of Target-Controlled Intravenous Infusion for a Prolonged Immersive DMT Psychedelic Experience
A Model for the Application of Target-Controlled Intravenous Infusion for a Prolonged Immersive DMT Psychedelic Experience Abstract Abstract The state of consciousness induced by N,N -dimethyltryptamine (DMT) is one of the most extraordinary of any naturally-occurring psychedelic substance. Users consistently report th...
PMC12949382
core_pubmed_pmc
Drug Polymer Nanoparticles: An Advancement in Biomedical Solutions and Targeted Drug Delivery
Drug Polymer Nanoparticles: An Advancement in Biomedical Solutions and Targeted Drug Delivery Abstract Abstract Polymer nanoparticles (PNPs) are compact particulate systems typically ranging from 10 to 1000 nm in size and have emerged as versatile platforms in modern biomedical research. Their growing importance stems ...
PMC8149334
core_pubmed_pmc
Niraparib with androgen receptor-axis-targeted therapy in patients with metastatic castration-resistant prostate cancer: safety and pharmacokinetic results from a phase 1b study (BEDIVERE)
Niraparib with androgen receptor-axis-targeted therapy in patients with metastatic castration-resistant prostate cancer: safety and pharmacokinetic results from a phase 1b study (BEDIVERE) Abstract Purpose To assess the safety and pharmacokinetics and determine the recommended phase 2 dose (RP2D) of niraparib with apal...
PMC3866786
core_pubmed_pmc
Exploratory Pharmacokinetics of Geniposide in Rat Model of Cerebral Ischemia Orally Administered with or without Baicalin and/or Berberine
Exploratory Pharmacokinetics of Geniposide in Rat Model of Cerebral Ischemia Orally Administered with or without Baicalin and/or Berberine Abstract Abstract Huang-Lian-Jie-Du-Tang (HLJDT), a classical Chinese prescription, has been clinically employed to treat cerebral ischemia for thousands of years. Geniposide is the...
PMC12783266
core_pubmed_pmc
A Population Pharmacokinetic and Exposure–Response Analysis for Baricitinib in Pediatric Patients with Atopic Dermatitis
A Population Pharmacokinetic and Exposure–Response Analysis for Baricitinib in Pediatric Patients with Atopic Dermatitis Abstract Background Baricitinib is approved for the treatment of adults with moderate-to-severe atopic dermatitis (AD) who are candidates for systemic therapy and has received regulatory authorizatio...
PMC10428525
core_pubmed_pmc
Effect of guselkumab on serum biomarkers in patients with active psoriatic arthritis and inadequate response to tumor necrosis factor inhibitors: results from the COSMOS phase 3b study
Effect of guselkumab on serum biomarkers in patients with active psoriatic arthritis and inadequate response to tumor necrosis factor inhibitors: results from the COSMOS phase 3b study Abstract Abstract Background Guselkumab is a selective interleukin (IL)-23 inhibitor targeting the IL-23p19 subunit. In the phase 3b CO...
PMC11830814
core_pubmed_pmc
Postpartum changes in maternal physiology and milk composition: a comprehensive database for developing lactation physiologically-based pharmacokinetic models
Postpartum changes in maternal physiology and milk composition: a comprehensive database for developing lactation physiologically-based pharmacokinetic models Abstract Abstract Introduction Pharmacotherapy during lactation often lacks reliable drug safety data, resulting in delayed treatment or early cessation of breas...
PMC11082534
core_pubmed_pmc
Half‐life extension of single‐domain antibody–drug conjugates by albumin binding moiety enhances antitumor efficacy
Half‐life extension of single‐domain antibody–drug conjugates by albumin binding moiety enhances antitumor efficacy Abstract Abstract Single‐domain antibody–drug conjugates (sdADCs) have been proven to have deeper solid tumor penetration and intratumor accumulation capabilities due to their smaller size compared with t...
PMC10544002
core_pubmed_pmc
First-in-human Study of AZD5153, A Small-molecule Inhibitor of Bromodomain Protein 4, in Patients with Relapsed/Refractory Malignant Solid Tumors and Lymphoma
First-in-human Study of AZD5153, A Small-molecule Inhibitor of Bromodomain Protein 4, in Patients with Relapsed/Refractory Malignant Solid Tumors and Lymphoma Abstract Abstract AZD5153, a reversible, bivalent inhibitor of the bromodomain and extraterminal family protein BRD4, has preclinical activity in multiple tumors...
PMC9495358
core_pubmed_pmc
The Current State of Knowledge in Biological Properties of Cirsimaritin
The Current State of Knowledge in Biological Properties of Cirsimaritin Abstract The search for natural plant-based products as new pharmacological alternatives to treat various human pathologies has taken on great importance for researchers and research laboratories. In this context, research has intensified to extrac...
PMC12583983
core_pubmed_pmc
Exposure–Response Analysis for Aripiprazole Once‐Monthly in Patients Diagnosed With Bipolar I Disorder
Exposure–Response Analysis for Aripiprazole Once‐Monthly in Patients Diagnosed With Bipolar I Disorder Abstract Abstract Aripiprazole once‐monthly (AOM) is approved for the maintenance monotherapy treatment of bipolar I disorder (BP‐I) in adults. A previously developed population pharmacokinetic model was validated by ...
PMC12823313
core_pubmed_pmc
Development of a Physiologically Based Model of Bilirubin Metabolism in Health and Disease and Its Comparison With Real‐World Data
Development of a Physiologically Based Model of Bilirubin Metabolism in Health and Disease and Its Comparison With Real‐World Data Abstract ABSTRACT Bilirubin is a breakdown product of erythrocytes and plays a crucial role in elimination of heme‐containing proteins. After its synthesis in the reticuloendothelial system...
PMC8615189
core_pubmed_pmc
Size Matters: The Influence of Patient Size on Antibiotics Exposure Profiles in Critically Ill Patients on Continuous Renal Replacement Therapy
Size Matters: The Influence of Patient Size on Antibiotics Exposure Profiles in Critically Ill Patients on Continuous Renal Replacement Therapy Abstract Abstract (1) Purpose of this study: To determine whether patient weight influences the probability of target attainment (PTA) over 72 h of initial therapy with beta-la...
PMC12313459
core_pubmed_pmc
Population pharmacokinetics of weight-based compared with fixed dosing of CAP256V2LS, a broadly neutralizing antibody for HIV prevention in women
Population pharmacokinetics of weight-based compared with fixed dosing of CAP256V2LS, a broadly neutralizing antibody for HIV prevention in women Abstract Abstract Introduction In the development of broadly neutralizing monoclonal antibodies (bNAb) for HIV prevention, there is a need for simpler dosing strategies. This...
PMC7775496
core_pubmed_pmc
Bictegravir Plus Tenofovir Alafenamide Nanoformulation as a Long-Acting Pre-Exposure Prophylaxis Regimen: Application of Modeling to Design Non-Human Primate Pharmacokinetic Experiments
Bictegravir Plus Tenofovir Alafenamide Nanoformulation as a Long-Acting Pre-Exposure Prophylaxis Regimen: Application of Modeling to Design Non-Human Primate Pharmacokinetic Experiments Abstract Abstract Bictegravir (BIC) and tenofovir alafenamide fumarate (TAF), two potent anti-HIV drugs, had been nanoformulated ( nBI...
PMC12512626
core_pubmed_pmc
Medical importance and pharmacokinetics of gold nanoparticles in the human body
Medical importance and pharmacokinetics of gold nanoparticles in the human body Abstract Abstract Gold nanoparticles (AuNPs) have emerged as versatile nanocarriers with promising potential in therapeutic applications due to their tunable physicochemical properties, ease of functionalization, and excellent biocompatibil...
PMC11098161
core_pubmed_pmc
Medication adherence framework: A population‐based pharmacokinetic approach and its application in antimalarial treatment assessments
Medication adherence framework: A population‐based pharmacokinetic approach and its application in antimalarial treatment assessments Abstract Abstract We reported here on the development of a pharmacometric framework to assess patient adherence, by using two population‐based approaches – the percentile and the Bayesia...
PMC9644403
core_pubmed_pmc
L-type Amino Acid Transporter 1 Utilizing Ferulic Acid Derivatives Show Increased Drug Delivery in the Mouse Pancreas Along with Decreased Lipid Peroxidation and Prostaglandin Production
L-type Amino Acid Transporter 1 Utilizing Ferulic Acid Derivatives Show Increased Drug Delivery in the Mouse Pancreas Along with Decreased Lipid Peroxidation and Prostaglandin Production Abstract Oxidative stress and pathological changes of Alzheimer’s disease (AD) overlap with metabolic diseases, such as diabetes mell...
PMC6152991
core_pubmed_pmc
Pharmacokinetics of intramuscular alfaxalone and its echocardiographic, cardiopulmonary and sedative effects in healthy dogs
Pharmacokinetics of intramuscular alfaxalone and its echocardiographic, cardiopulmonary and sedative effects in healthy dogs Abstract Abstract The pharmacokinetics and the effects of a single intramuscular (IM) dose of alfaxalone on sedation and cardiopulmonary and echocardiographic variables was studied in dogs. Twelv...
PMC10974275
core_pubmed_pmc
Pharmacokinetic Interaction of Kratom and Cannabidiol in Male Rats
Pharmacokinetic Interaction of Kratom and Cannabidiol in Male Rats Abstract Kratom and cannabidiol products are used to self-treat a variety of conditions, including anxiety and pain, and to elevate mood. Research into the individual pharmacokinetic properties of commercially available kratom and cannabidiol products h...
PMC11583597
core_pubmed_pmc
Brain uptake pharmacokinetics of albiglutide, dulaglutide, tirzepatide, and DA5-CH in the search for new treatments of Alzheimer’s and Parkinson’s diseases
Brain uptake pharmacokinetics of albiglutide, dulaglutide, tirzepatide, and DA5-CH in the search for new treatments of Alzheimer’s and Parkinson’s diseases Abstract ABSTRACT Background A number of peptide incretin receptor agonists (IRAs) show promise as therapeutics for Alzheimer’s disease (AD) and Parkinson’s disease...
PMC5947941
core_pubmed_pmc
Biological Cleavage of the C–P Bond in Perfluoroalkyl Phosphinic Acids in Male Sprague-Dawley Rats and the Formation of Persistent and Reactive Metabolites
Biological Cleavage of the C–P Bond in Perfluoroalkyl Phosphinic Acids in Male Sprague-Dawley Rats and the Formation of Persistent and Reactive Metabolites Abstract Abstract Background: Perfluoroalkyl phosphinic acids (PFPiAs) have been detected in humans, wildlife, and various environmental matrices. These compounds h...
PMC8067460
core_pubmed_pmc
Benzoquinoline Derivatives: A Straightforward and Efficient Route to Antibacterial and Antifungal Agents
Benzoquinoline Derivatives: A Straightforward and Efficient Route to Antibacterial and Antifungal Agents Abstract Abstract We report here the design, synthesis, experimental and in silico evaluation of the antibacterial and antifungal activity of some new benzo[f]quinoline derivatives. Two classes of benzo[f]quinoliniu...
PMC9097519
core_pubmed_pmc
A randomized, double-blind, three-arm, parallel group, single-dose phase I study to evaluate the pharmacokinetic similarity between SB12 (a proposed eculizumab biosimilar) and eculizumab (Soliris) in healthy subjects
A randomized, double-blind, three-arm, parallel group, single-dose phase I study to evaluate the pharmacokinetic similarity between SB12 (a proposed eculizumab biosimilar) and eculizumab (Soliris) in healthy subjects Abstract Abstract Objectives: To compare the pharmacokinetics (PK), pharmacodynamics (PD), safety, and ...
PMC11207296
core_pubmed_pmc
Development and Quality Control of a Population Pharmacokinetic Model Library for Caspofungin
Development and Quality Control of a Population Pharmacokinetic Model Library for Caspofungin Abstract Background: Caspofungin is an echinocandin antifungal agent commonly used as the first-line therapy for invasive candidiasis, salvage therapy for invasive aspergillosis, and empirical therapy for presumed fungal infec...
PMC10963087
core_pubmed_pmc
Comparative pharmacokinetics of tyrosine kinase inhibitor, lapatinib, in dogs and cats following single oral administration
Comparative pharmacokinetics of tyrosine kinase inhibitor, lapatinib, in dogs and cats following single oral administration Abstract Abstract Lapatinib is an orally administered tyrosine kinase inhibitor used to treat human epidermal growth factor receptor 2 (HER2) -overexpressing breast cancers in humans. Recently, th...
PMC8093413
core_pubmed_pmc
Antiseizure Medication use in Gastric Bypass Patients and Other Post-Surgical Malabsorptive States
Antiseizure Medication use in Gastric Bypass Patients and Other Post-Surgical Malabsorptive States Abstract Highlights • Patients with epilepsy undergoing bariatric surgery (or extensive intestinal resection for a different indication) should be followed by a multidisciplinary team including a pharmacist and a neurolog...
PMC10126081
core_pubmed_pmc
A Randomized, Open-Label, Multiple-Dose, Parallel-Arm, Pivotal Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of Aripiprazole 2-Month Long-Acting Injectable in Adults With Schizophrenia or Bipolar I Disorder
A Randomized, Open-Label, Multiple-Dose, Parallel-Arm, Pivotal Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of Aripiprazole 2-Month Long-Acting Injectable in Adults With Schizophrenia or Bipolar I Disorder Abstract Background Aripiprazole 2-month ready-to-use 960 mg (Ari 2MRTU 960) is a new long-act...
PMC10027504
core_pubmed_pmc
Safety and efficacy of classical complement pathway inhibition with sutimlimab in chronic immune thrombocytopenia
Safety and efficacy of classical complement pathway inhibition with sutimlimab in chronic immune thrombocytopenia Abstract Key Points • Classical complement pathway activation contributes to the pathophysiology and clinical heterogeneity of immune thrombocytopenia (ITP). • Sutimlimab rapidly and durably increased plate...
PMC12344431
core_pubmed_pmc
Factors associated with drug–drug interactions involving citalopram in the UK Biobank
Factors associated with drug–drug interactions involving citalopram in the UK Biobank Abstract Background Adults with mood and/or anxiety disorders have increased risks of comorbidities, chronic treatments and polypharmacy, increasing the risk of drug–drug interactions (DDIs) with antidepressants. Aims To use primary c...
PMC3256319
core_pubmed_pmc
Effect of ketoconazole on the pharmacokinetics of axitinib in healthy volunteers
Effect of ketoconazole on the pharmacokinetics of axitinib in healthy volunteers Abstract Summary Objective Axitinib (AG-013736), an oral, potent, and selective inhibitor of vascular endothelial growth factor receptors 1, 2, and 3, is metabolized primarily by cytochrome P450 (CYP) 3A with minor contributions from CYP1A...
PMC5774325
core_pubmed_pmc
Clinical relevancy and determinants of potential drug–drug interactions in chronic kidney disease patients: results from a retrospective analysis
Clinical relevancy and determinants of potential drug–drug interactions in chronic kidney disease patients: results from a retrospective analysis Abstract Background Chronic kidney disease (CKD) alters the pharmacokinetic and pharmacodynamic responses of various renally excreted drugs and increases the risk of drug-rel...
PMC8264055
core_pubmed_pmc
Pharmacokinetics of Colistin in the Gastrointestinal Tract of Poultry Following Dosing via Drinking Water and Its Bactericidal Impact on Enteric Escherichia coli
Pharmacokinetics of Colistin in the Gastrointestinal Tract of Poultry Following Dosing via Drinking Water and Its Bactericidal Impact on Enteric Escherichia coli Abstract Colistin, a last-line antibiotic of major importance in veterinary medicine and of critical importance in human medicine, is authorized to treat gast...
PMC12119952
core_pubmed_pmc
Drug repurposing targeting COVID-19 3CL protease using molecular docking and machine learning regression approaches
Drug repurposing targeting COVID-19 3CL protease using molecular docking and machine learning regression approaches Abstract Abstract The COVID-19 pandemic has initiated a global health emergency, with an exigent need for an effective cure. Progressively, drug repurposing is emerging as a promising solution for saving ...
PMC5982748
core_pubmed_pmc
Clinical implications of pharmacokinetics of sunitinib malate and N-desethyl-sunitinib plasma concentrations for treatment outcome in metastatic renal cell carcinoma patients
Clinical implications of pharmacokinetics of sunitinib malate and N-desethyl-sunitinib plasma concentrations for treatment outcome in metastatic renal cell carcinoma patients Abstract In this study, we examined the association between the pharmacokinetics (PK) level of sunitinib malate (SU) and its metabolite N-desethy...
PMC6585691
core_pubmed_pmc
Pharmacokinetics of Co‐Suspension Delivery Technology Budesonide/Glycopyrronium/Formoterol Fumarate Dihydrate (BGF MDI) and Budesonide/Formoterol Fumarate Dihydrate (BFF MDI) Fixed‐Dose Combinations Compared With an Active Control: A Phase 1, Randomized, Single‐Dose, Crossover Study in Healthy Adults
Pharmacokinetics of Co‐Suspension Delivery Technology Budesonide/Glycopyrronium/Formoterol Fumarate Dihydrate (BGF MDI) and Budesonide/Formoterol Fumarate Dihydrate (BFF MDI) Fixed‐Dose Combinations Compared With an Active Control: A Phase 1, Randomized, Single‐Dose, Crossover Study in Healthy Adults Abstract Abstract ...
PMC9516395
core_pubmed_pmc
Effect of X-ray radiation on the pharmacokinetics of apatinib in vivo in rats
Effect of X-ray radiation on the pharmacokinetics of apatinib in vivo in rats Abstract Abstract Purpose: The “radiotherapy-pharmacokinetic” (“RT-PK”) phenomenon refers to the fact that radiation can significantly alter the pharmacokinetic behavior of a drug. At present, it is not clear whether there is an “RT-PK” pheno...
PMC11685950
core_pubmed_pmc
Enhancement of in vitro transcellular absorption and in vivo oral bioavailability of apigenin by self-nanoemulsifying drug delivery systems
Enhancement of in vitro transcellular absorption and in vivo oral bioavailability of apigenin by self-nanoemulsifying drug delivery systems Abstract Abstract This study aims to develop a self-nanoemulsifying drug delivery system (SNEDDS) to solve the limited oral bioavailability problem of apigenin, a bioactive flavono...
PMC8915292
core_pubmed_pmc
Effect of CYP4F2 Polymorphisms on Ticagrelor Pharmacokinetics in Healthy Chinese Volunteers
Effect of CYP4F2 Polymorphisms on Ticagrelor Pharmacokinetics in Healthy Chinese Volunteers Abstract Background: Ticagrelor belongs to a new class of P2Y 12 receptor inhibitor that has been widely used for antiplatelet therapy. This study aimed to explore the effect of single nucleotide polymorphisms (SNPs) in metaboli...
PMC4702301
core_pubmed_pmc
Characterization of the infectious reservoir of malaria with an agent-based model calibrated to age-stratified parasite densities and infectiousness
Characterization of the infectious reservoir of malaria with an agent-based model calibrated to age-stratified parasite densities and infectiousness Abstract Background Elimination of malaria can only be achieved through removal of all vectors or complete depletion of the infectious reservoir in humans. Mechanistic mod...
PMC3827620
core_pubmed_pmc
A randomized, controlled cross-over trial of dermally-applied lavender ( Lavandula angustifolia ) oil as a treatment of agitated behaviour in dementia
A randomized, controlled cross-over trial of dermally-applied lavender ( Lavandula angustifolia ) oil as a treatment of agitated behaviour in dementia Abstract Background Lavender essential oil shows evidence of sedative properties in neurophysiological and animal studies but clinical trials of its effectiveness as a t...
PMC12069094
core_pubmed_pmc
Perfluorooctanoic acid serum concentrations and half-lives in a community exposed to contaminated drinking water in New York State
Perfluorooctanoic acid serum concentrations and half-lives in a community exposed to contaminated drinking water in New York State Abstract Background Investigations during 2014–2016 in two communities in New York State showed perfluorooctanoic acid (PFOA) in a public system serving 3800 residents (Hoosick Falls) avera...
PMC6272930
core_pubmed_pmc
Pharmacokinetic Evaluation of Clozapine in Concomitant Use of Radix Rehmanniae , Fructus Schisandrae , Radix Bupleuri , or Fructus Gardeniae in Rats
Pharmacokinetic Evaluation of Clozapine in Concomitant Use of Radix Rehmanniae , Fructus Schisandrae , Radix Bupleuri , or Fructus Gardeniae in Rats Abstract Radix Rehmanniae , Fructus Schisandrae , Radix Bupleuri , and Fructus Gardeniae are often used alongside with clozapine (CLZ) for schizophrenia patients in order ...
PMC12573091
core_pubmed_pmc
Comparative study of the pharmacokinetics, efficacy and safety of ET-26 in elderly and non-elderly subjects: the results of a phase I clinical trial
Comparative study of the pharmacokinetics, efficacy and safety of ET-26 in elderly and non-elderly subjects: the results of a phase I clinical trial Abstract Abstract Aim To evaluate the pharmacokinetics, pharmacodynamics, and safety of the novel systemic intravenous anesthetic ET-26—an etomidate derivative designed to...
PMC12055356
core_pubmed_pmc
Relaxin mimetic in pulmonary hypertension associated with left heart disease: Design and rationale of Re‐PHIRE
Relaxin mimetic in pulmonary hypertension associated with left heart disease: Design and rationale of Re‐PHIRE Abstract Abstract Aims Despite receiving guideline‐directed medical heart failure (HF) therapy, patients with pulmonary hypertension associated with left heart disease (PH‐LHD) experience higher mortality and ...
PMC9402319
core_pubmed_pmc
Effect of Chaihu Shugan Pills on the Pharmacokinetics of Duloxetine and its Metabolite 4-Hydroxyduloxetine in Beagle Dogs: A Herb-Drug Interaction Study
Effect of Chaihu Shugan Pills on the Pharmacokinetics of Duloxetine and its Metabolite 4-Hydroxyduloxetine in Beagle Dogs: A Herb-Drug Interaction Study Abstract The effect of Chaihu Shugan pills (CHSG) on the pharmacokinetics of duloxetine and its metabolite 4-hydroxyduloxetine in beagle dogs was investigated by estab...
PMC12044476
core_pubmed_pmc
A Dual Nanoapproach for the Treatment of Depression and Sleep Via a Novel Optimized Eugenol-Mucoadhesive Nanoemulsion
A Dual Nanoapproach for the Treatment of Depression and Sleep Via a Novel Optimized Eugenol-Mucoadhesive Nanoemulsion Abstract Abstract This study aimed to develop a chitosan (CHS)-coated eugenol (EUGE)-loaded nanoemulsion (CHS-EUGE-NE) to enhance brain bioavailability. A novel GC-MS/MS method was developed and validat...
PMC6001693
core_pubmed_pmc
Review article: nonclinical and clinical pharmacology, pharmacokinetics and pharmacodynamics of etrolizumab, an anti‐β7 integrin therapy for inflammatory bowel disease
Review article: nonclinical and clinical pharmacology, pharmacokinetics and pharmacodynamics of etrolizumab, an anti‐β7 integrin therapy for inflammatory bowel disease Abstract Summary Background Novel treatments with superior benefit‐risk profiles are needed to improve the long‐term prognosis of patients with inflamma...
PMC11157103
core_pubmed_pmc
Exploration of morpholine-thiophene hybrid thiosemicarbazones for the treatment of ureolytic bacterial infections via targeting urease enzyme: Synthesis, biochemical screening and computational analysis
Exploration of morpholine-thiophene hybrid thiosemicarbazones for the treatment of ureolytic bacterial infections via targeting urease enzyme: Synthesis, biochemical screening and computational analysis Abstract Abstract An important component of the pathogenicity of potentially pathogenic bacteria in humans is the ure...
PMC11245370
core_pubmed_pmc
3-Position Biaryl Endochin-like Quinolones with Enhanced Antimalarial Performance
3-Position Biaryl Endochin-like Quinolones with Enhanced Antimalarial Performance Abstract ELQ-300 is a potent antimalarial drug with activity against blood, liver, and vector stages of the disease. A prodrug, ELQ-331 , exhibits reduced crystallinity and improved in vivo efficacy in preclinical testing, and currently, ...
PMC12712010
core_pubmed_pmc
Tolvaptan pharmacokinetics and pharmacodynamics in adolescents with autosomal dominant polycystic kidney disease
Tolvaptan pharmacokinetics and pharmacodynamics in adolescents with autosomal dominant polycystic kidney disease Abstract Abstract Tolvaptan, an oral selective antagonist of the vasopressin V2 receptor, is the only medication for autosomal dominant polycystic kidney disease (ADPKD) with disease-modifying properties in ...
PMC11275093
core_pubmed_pmc
The Bright Side of Curcumin: A Narrative Review of Its Therapeutic Potential in Cancer Management
The Bright Side of Curcumin: A Narrative Review of Its Therapeutic Potential in Cancer Management Abstract Simple Summary This review comprehensively examines curcumin’s therapeutic potential in cancer treatment. It addresses the limitations of curcumin therapy due to its low bioavailability and potential side effects....
PMC7435008
core_pubmed_pmc
Analysis of Drug Metabolizing Gene Panel in Osteosarcoma Patients Identifies Association Between Variants in SULT1E1, CYP2B6 and CYP4F8 and Methotrexate Levels and Toxicities
Analysis of Drug Metabolizing Gene Panel in Osteosarcoma Patients Identifies Association Between Variants in SULT1E1, CYP2B6 and CYP4F8 and Methotrexate Levels and Toxicities Abstract High-dose methotrexate is a cornerstone agent in the chemotherapeutic treatment of patients with osteosarcoma. However, patients often d...
PMC6152432
core_pubmed_pmc
Development of a Target cell-Biologics-Effector cell (TBE) complex-based cell killing model to characterize target cell depletion by T cell redirecting bispecific agents
Development of a Target cell-Biologics-Effector cell (TBE) complex-based cell killing model to characterize target cell depletion by T cell redirecting bispecific agents Abstract ABSTRACT T-cell redirecting bispecific antibodies (bsAbs) or antibody-derived agents that combine tumor antigen recognition with CD3-mediated...
PMC11139978
core_pubmed_pmc
Identification of small molecular inhibitors of SIRT3 by computational and biochemical approaches a potential target of breast cancer
Identification of small molecular inhibitors of SIRT3 by computational and biochemical approaches a potential target of breast cancer Abstract Abstract Sirtuin 3 (SIRT3) belongs to the Sirtuin protein family, which consists of NAD + -dependent lysine deacylase, involved in the regulation of various cellular activities....
PMC4834548
core_pubmed_pmc
The selective sigma-1 receptor antagonist E-52862 attenuates neuropathic pain of different aetiology in rats
The selective sigma-1 receptor antagonist E-52862 attenuates neuropathic pain of different aetiology in rats Abstract E-52862 is a selective σ 1 R antagonist currently undergoing phase II clinical trials for neuropathic pain and represents a potential first-in-class analgesic. Here, we investigated the effect of single...
PMC11469322
core_pubmed_pmc
Anti‐HER2 Super Stealth Immunoliposomes for Targeted‐Chemotherapy
Anti‐HER2 Super Stealth Immunoliposomes for Targeted‐Chemotherapy Abstract Abstract Liposomes play an important role in the field of drug delivery by virtue of their biocompatibility and versatility as carriers. Stealth liposomes, obtained by surface decoration with hydrophilic polyethylene glycol (PEG) molecules, repr...
PMC7289225
core_pubmed_pmc
African potato ( Hypoxis hemerocallidea ): a systematic review of its chemistry, pharmacology and ethno medicinal properties
African potato ( Hypoxis hemerocallidea ): a systematic review of its chemistry, pharmacology and ethno medicinal properties Abstract Abstract Background African Potato ( hypoxis hemerocallidea), is used for enhancing immune system in Southern Africa. It is among the plants of intense commercial and scientific interest...
PMC7495146
core_pubmed_pmc
Prediction of potential inhibitors for RNA-dependent RNA polymerase of SARS-CoV-2 using comprehensive drug repurposing and molecular docking approach
Prediction of potential inhibitors for RNA-dependent RNA polymerase of SARS-CoV-2 using comprehensive drug repurposing and molecular docking approach Abstract The pandemic prevalence of COVID-19 has become a very serious global health issue. Scientists all over the world have been seriously attempting in the discovery ...
PMC12627865
core_pubmed_pmc
Add-on combination therapy with monoclonal antibodies: Implications for drug development
Add-on combination therapy with monoclonal antibodies: Implications for drug development Abstract Three anti-amyloid monoclonal antibodies (MABs) including aducanumab, lecanemab, and donanemab have been approved by the FDA and lecanemab and donanemab are available in the US market and a variety of other national market...
PMC6246626
core_pubmed_pmc
Polymorphisms in mTOR and Calcineurin Signaling Pathways Are Associated With Long-Term Clinical Outcomes in Kidney Transplant Recipients
Polymorphisms in mTOR and Calcineurin Signaling Pathways Are Associated With Long-Term Clinical Outcomes in Kidney Transplant Recipients Abstract Monitoring of immunosuppressive drugs, such as calcineurin and mTOR inhibitors, is essential to avoid undesirable kidney transplant outcomes. Polymorphisms in pharmacokinetic...
PMC7993266
core_pubmed_pmc
Clinical Pharmacokinetics and Pharmacodynamics of Cerliponase Alfa, Enzyme Replacement Therapy for CLN2 Disease by Intracerebroventricular Administration
Clinical Pharmacokinetics and Pharmacodynamics of Cerliponase Alfa, Enzyme Replacement Therapy for CLN2 Disease by Intracerebroventricular Administration Abstract Abstract Cerliponase alfa is recombinant human tripeptidyl peptidase 1 (TPP1) delivered by i.c.v. infusion for CLN2, a pediatric neurodegenerative disease ca...
PMC11097369
core_pubmed_pmc
Preclinical Evaluation of JAB-2485, a Potent AURKA Inhibitor with High Selectivity and Favorable Pharmacokinetic Properties
Preclinical Evaluation of JAB-2485, a Potent AURKA Inhibitor with High Selectivity and Favorable Pharmacokinetic Properties Abstract Abstract As a critical mitotic regulator, Aurora kinase A (AURKA) is aberrantly activated in a wide range of cancers. Therapeutic targeting of AUKRA is a promising strategy for the treatm...
PMC7984404
core_pubmed_pmc
Population Pharmacokinetics and Exposure‐Response Analyses to Guide Dosing of Icatibant in Pediatric Patients With Hereditary Angioedema
Population Pharmacokinetics and Exposure‐Response Analyses to Guide Dosing of Icatibant in Pediatric Patients With Hereditary Angioedema Abstract Abstract Elevated bradykinin levels are responsible for the development of clinical symptoms in patients with hereditary angioedema (HAE). Icatibant is a bradykinin type 2 re...
PMC4871170
core_pubmed_pmc
Management of Venous Thromboembolism
Management of Venous Thromboembolism Abstract Abstract Objective: To review clinical data on direct oral anticoagulants (DOACs) used in the acute treatment of venous thromboembolism (VTE) as well as practical considerations when using these products. Data Sources: Searches of PubMed and Google Scholar for VTE, deep vei...
PMC12856181
core_pubmed_pmc
Toxicokinetics and tissue-specific biotransformation of modified mycotoxin zearalenone-14-glucoside (ZEN-14-G) in broilers following oral administration
Toxicokinetics and tissue-specific biotransformation of modified mycotoxin zearalenone-14-glucoside (ZEN-14-G) in broilers following oral administration Abstract Zearalenone-14-glucoside (ZEN-14-G), a major modified mycotoxin, has attracted considerable attention due to its potential to convert back into free zearaleno...
PMC8708373
core_pubmed_pmc
In Vivo Efficacy of Voriconazole in a Galleria mellonella Model of Invasive Infection Due to Azole-Susceptible or Resistant Aspergillus fumigatus Isolates
In Vivo Efficacy of Voriconazole in a Galleria mellonella Model of Invasive Infection Due to Azole-Susceptible or Resistant Aspergillus fumigatus Isolates Abstract Aspergillus fumigatus is an environmental filamentous fungus responsible for life-threatening infections in humans and animals. Azoles are the first-line tr...
PMC7571451
core_pubmed_pmc
Pharmacodynamic Activity of the Novel Neurokinin-3 Receptor Antagonist SJX-653 in Healthy Men
Pharmacodynamic Activity of the Novel Neurokinin-3 Receptor Antagonist SJX-653 in Healthy Men Abstract Abstract Context SJX-653 is a novel neurokinin 3 receptor (NK3R) antagonist. The NK3 pathway is a central regulator of gonadotropin releasing hormone (GnRH) secretion and has also been implicated in the generation of ...
PMC8241405
core_pubmed_pmc
Effects of Recombinant Human Angiotensin-Converting Enzyme 2 on Response to Acute Hypoxia and Exercise: A Randomised, Placebo-Controlled Study
Effects of Recombinant Human Angiotensin-Converting Enzyme 2 on Response to Acute Hypoxia and Exercise: A Randomised, Placebo-Controlled Study Abstract Introduction Angiotensin-converting enzyme 2 (ACE2) is a key enzyme of the renin-angiotensin system (RAS) that has been implicated in the pathogenesis of acute respirat...
PMC12106892
core_pubmed_pmc
Preoperative activation of the renin–angiotensin system and myocardial injury in noncardiac surgery: exploratory mechanistic analysis of the SPACE randomised controlled trial
Preoperative activation of the renin–angiotensin system and myocardial injury in noncardiac surgery: exploratory mechanistic analysis of the SPACE randomised controlled trial Abstract Background Hypertension therapy in older adults is often suboptimal, in part because of inadequate suppression of the renin–angiotensin–...