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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–... |
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