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PMC6327336
core_pubmed_pmc
Potential Anti-Cancer Flavonoids Isolated From Caesalpinia bonduc Young Twigs and Leaves: Molecular Docking and In Silico Studies
Potential Anti-Cancer Flavonoids Isolated From Caesalpinia bonduc Young Twigs and Leaves: Molecular Docking and In Silico Studies Abstract Abstract Tyrosine kinase (TK), vascular endothelial growth factor (VEGF), and matrix metalloproteinases (MMP) are important cancer therapeutic target proteins. Based on reported ant...
PMC3794864
core_pubmed_pmc
Steady-state bioavailability of prescription omega-3 on a low-fat diet is significantly improved with a free fatty acid formulation compared with an ethyl ester formulation: the ECLIPSE II study
Steady-state bioavailability of prescription omega-3 on a low-fat diet is significantly improved with a free fatty acid formulation compared with an ethyl ester formulation: the ECLIPSE II study Abstract The systemic bioavailability of free fatty acid (FFA) forms of eicosapentaenoic acid (EPA) and docosahexaenoic acid ...
PMC8590161
core_pubmed_pmc
Intravitreal HDAC Inhibitor Belinostat Effectively Eradicates Vitreous Seeds Without Retinal Toxicity In Vivo in a Rabbit Retinoblastoma Model
Intravitreal HDAC Inhibitor Belinostat Effectively Eradicates Vitreous Seeds Without Retinal Toxicity In Vivo in a Rabbit Retinoblastoma Model Abstract Purpose Current melphalan-based regimens for intravitreal chemotherapy for retinoblastoma vitreous seeds are effective but toxic to the retina. Thus, alternative agents...
PMC12177941
core_pubmed_pmc
Rational Design of Safer Inorganic Nanoparticles via Mechanistic Modeling-Informed Machine Learning
Rational Design of Safer Inorganic Nanoparticles via Mechanistic Modeling-Informed Machine Learning Abstract The safety of inorganic nanoparticles (NPs) remains a critical challenge for their clinical translation. To address this, we developed a machine learning (ML) framework that predicts NP toxicity both in vitro an...
PMC6189874
core_pubmed_pmc
Pharmacokinetics of β-Lactam Antibiotics: Clues from the Past To Help Discover Long-Acting Oral Drugs in the Future
Pharmacokinetics of β-Lactam Antibiotics: Clues from the Past To Help Discover Long-Acting Oral Drugs in the Future Abstract Abstract β-Lactams represent perhaps the most important class of antibiotics yet discovered. However, despite many years of active research, none of the currently approved drugs in this class com...
PMC9604962
core_pubmed_pmc
Insights into CD24 and Exosome Physiology and Potential Role in View of Recent Advances in COVID-19 Therapeutics: A Narrative Review
Insights into CD24 and Exosome Physiology and Potential Role in View of Recent Advances in COVID-19 Therapeutics: A Narrative Review Abstract Abstract Cluster of differentiation (CD) 24, a long-known protein with multifaceted functions, has gained attention as a possible treatment for Coronavirus Disease 19 (COVID-19) ...
PMC2958653
core_pubmed_pmc
Developmental Pharmacogenetics in Pediatric Rheumatology: Utilizing a New Paradigm to Effectively Treat Patients with Juvenile Idiopathic Arthritis with Methotrexate
Developmental Pharmacogenetics in Pediatric Rheumatology: Utilizing a New Paradigm to Effectively Treat Patients with Juvenile Idiopathic Arthritis with Methotrexate Abstract Abstract Although methotrexate is widely used in clinical practice there remains significant lack of understanding of its mechanisms of action an...
PMC12395082
core_pubmed_pmc
Computational modeling of drug-eluting balloons in peripheral artery disease: Mechanisms, optimization, and translational insights
Computational modeling of drug-eluting balloons in peripheral artery disease: Mechanisms, optimization, and translational insights Abstract Abstract Drug-eluting balloons (DEBs) represent a promising alternative to stent-based interventions for peripheral artery disease (PAD), and their therapeutic efficacy is dependen...
PMC12491691
core_pubmed_pmc
Metallic nanomedicine in cancer immunotherapy
Metallic nanomedicine in cancer immunotherapy Abstract Immunotherapy has become a pivotal modality in clinical cancer treatment. However, its effectiveness is limited to a small subset of patients due to the low antigenicity, impaired innate response, and various adaptive immune resistance mechanisms of the tumor micro...
PMC8253325
core_pubmed_pmc
Evaluation of pharmacokinetics of single-dose primaquine in undernourished versus normally nourished children diagnosed with Plasmodium vivax malaria in Mumbai
Evaluation of pharmacokinetics of single-dose primaquine in undernourished versus normally nourished children diagnosed with Plasmodium vivax malaria in Mumbai Abstract Abstract Background: The pharmacokinetics of primaquine [PQ] have been the subject of studies in both adults and healthy participants. However, there i...
PMC12840083
core_pubmed_pmc
Targeting CRHR1 Signaling in Experimental Infantile Epileptic Spasms Syndrome: Evidence for Route-Dependent Efficacy
Targeting CRHR1 Signaling in Experimental Infantile Epileptic Spasms Syndrome: Evidence for Route-Dependent Efficacy Abstract Abstract Highlights What are the main findings? CRHR1 antagonists suppress experimental infantile spasms in a route-, drug-, and brain-site-specific manner. Systemic SN003 reduces spasms, wherea...
PMC4702464
core_pubmed_pmc
Intranasal Human Growth Hormone (hGH) Induces IGF-1 Levels Comparable With Subcutaneous Injection With Lower Systemic Exposure to hGH in Healthy Volunteers
Intranasal Human Growth Hormone (hGH) Induces IGF-1 Levels Comparable With Subcutaneous Injection With Lower Systemic Exposure to hGH in Healthy Volunteers Abstract Context: The development of an improved, efficacious human GH (hGH) product administered by a noninjectable route of delivery such as the nasal route is hi...
PMC11445346
core_pubmed_pmc
Preparation and characterization of Sorafenib nano-emulsion: impact on pharmacokinetics and toxicity; an in vitro and in vivo study
Preparation and characterization of Sorafenib nano-emulsion: impact on pharmacokinetics and toxicity; an in vitro and in vivo study Abstract Hepatocellular carcinoma (HCC) ranks as the third leading cause of cancer-related deaths worldwide. Current treatment strategies include surgical resection, liver transplantation,...
PMC12525650
core_pubmed_pmc
Pharmacokinetic Profile of Extracts from the Chayote ( Sechium edule ) H387 07 Hybrid and Phytochemical Characterization of Its Segregant H387 M16 for Potential Therapeutic Applications
Pharmacokinetic Profile of Extracts from the Chayote ( Sechium edule ) H387 07 Hybrid and Phytochemical Characterization of Its Segregant H387 M16 for Potential Therapeutic Applications Abstract Abstract The hybrid Sechium edule H387 07, commonly known as chayote, has shown potential as an antiproliferative, cytotoxic,...
PMC8309110
core_pubmed_pmc
Quantification of Ceftaroline in Human Plasma Using High-Performance Liquid Chromatography with Ultraviolet Detection: Application to Pharmacokinetic Studies
Quantification of Ceftaroline in Human Plasma Using High-Performance Liquid Chromatography with Ultraviolet Detection: Application to Pharmacokinetic Studies Abstract This study was conducted to develop a rapid, simple and reproducible method for the quantification of ceftaroline in plasma samples by high-performance l...
PMC12521055
core_pubmed_pmc
Machine Learning‐Based Model Selection and Averaging Outperform Single‐Model Approaches for a Priori Vancomycin Precision Dosing
Machine Learning‐Based Model Selection and Averaging Outperform Single‐Model Approaches for a Priori Vancomycin Precision Dosing Abstract ABSTRACT Selecting an appropriate population pharmacokinetic (PK) model for individual patients in model‐informed precision dosing (MIPD) can be challenging, particularly in the abse...
PMC9144954
core_pubmed_pmc
Epidural Oxycodone for Acute Pain
Epidural Oxycodone for Acute Pain Abstract Epidural analgesia is commonly used in labour analgesia and in postoperative pain after major surgery. It is highly effective in severe acute pain, has minimal effects on foetus and newborn, may reduce postoperative complications, and enhance patient satisfaction. In epidural ...
PMC11732092
core_pubmed_pmc
Pharmacokinetic/pharmacodynamic issues for optimizing treatment with beta-lactams of Gram-negative infections in critically ill orthotopic liver transplant recipients: a comprehensive review
Pharmacokinetic/pharmacodynamic issues for optimizing treatment with beta-lactams of Gram-negative infections in critically ill orthotopic liver transplant recipients: a comprehensive review Abstract Orthotopic liver transplant (OLT) represents the standard of care for managing patients affected by end-stage and life-t...
PMC2829539
core_pubmed_pmc
Unchanged triclabendazole kinetics after co-administration with ivermectin and methimazole: failure of its therapeutic activity against triclabendazole-resistant liver flukes
Unchanged triclabendazole kinetics after co-administration with ivermectin and methimazole: failure of its therapeutic activity against triclabendazole-resistant liver flukes Abstract Background The reduced drug accumulation based on enhanced drug efflux and metabolic capacity, identified in triclabendazole (TCBZ)-resi...
PMC12845070
core_pubmed_pmc
Development and Application of an LC-MS/MS Method for Simultaneous Quantification of Azathioprine and Its Metabolites: Pharmacokinetic and Microbial Metabolism Study of a Colon-Targeted Nanoparticle
Development and Application of an LC-MS/MS Method for Simultaneous Quantification of Azathioprine and Its Metabolites: Pharmacokinetic and Microbial Metabolism Study of a Colon-Targeted Nanoparticle Abstract Background/Objectives : Given the clinical limitations of azathioprine (AZA) in treating inflammatory bowel dise...
PMC6205597
core_pubmed_pmc
Faster emergence behavior from ketamine/xylazine anesthesia with atipamezole versus yohimbine
Faster emergence behavior from ketamine/xylazine anesthesia with atipamezole versus yohimbine Abstract Recent interest in reversal of the hypnotic effects of anesthesia has mainly focused on overcoming a surge in GABA-mediated inhibitory signaling through activation of subcortical arousal circuits or antagonizing GABA ...
PMC12364634
core_pubmed_pmc
Trial in progress: phase I study of non-viral gene-modified CAR-T cell therapy for malignant solid tumors expressing EPHB4 receptor (CARTiEr)
Trial in progress: phase I study of non-viral gene-modified CAR-T cell therapy for malignant solid tumors expressing EPHB4 receptor (CARTiEr) Abstract Abstract Background Ephrin type-B receptor 4 (EPHB4) is overexpressed on the surface of various tumor cells, including cells from malignant bone and soft-tissue tumors. ...
PMC11766596
core_pubmed_pmc
Efficacy and Safety Assessment of Antifungal Prophylaxis with Posaconazole Using Therapeutic Drug Monitoring in Pediatric Patients with Oncohematological Disorders—A Single-Centre Study
Efficacy and Safety Assessment of Antifungal Prophylaxis with Posaconazole Using Therapeutic Drug Monitoring in Pediatric Patients with Oncohematological Disorders—A Single-Centre Study Abstract Introduction: Posaconazole is recommended for prophylaxis in pediatric immunocompromised patients. Due to its variability in ...
PMC8130657
core_pubmed_pmc
The role of sex, age and genetic polymorphisms of CYP enzymes on the pharmacokinetics of anticholinergic drugs
The role of sex, age and genetic polymorphisms of CYP enzymes on the pharmacokinetics of anticholinergic drugs Abstract Abstract There is evidence that use of drugs with anticholinergic properties increases the risk of cognitive impairment, and increased exposure to these drugs potentiates this risk. Anticholinergic dr...
PMC3589633
core_pubmed_pmc
A Phase I, open-label, dose-escalation study of continuous once-daily oral treatment with afatinib in patients with advanced solid tumors
A Phase I, open-label, dose-escalation study of continuous once-daily oral treatment with afatinib in patients with advanced solid tumors Abstract Summary Background This trial evaluated the safety, tolerability and maximum tolerated dose (MTD) of afatinib, a novel ErbB Family Blocker. Methods In this open-label, dose-...
PMC5836974
core_pubmed_pmc
Pharmacokinetics of concentrated naloxone nasal spray for opioid overdose reversal: Phase I healthy volunteer study *
Pharmacokinetics of concentrated naloxone nasal spray for opioid overdose reversal: Phase I healthy volunteer study * Abstract Abstract Background and Aims Take‐home naloxone can prevent death from heroin/opioid overdose, but pre‐provision is difficult because naloxone is usually given by injection. Non‐injectable alte...
PMC4964204
core_pubmed_pmc
Invasiveness of pharmacokinetic studies in children: a systematic review
Invasiveness of pharmacokinetic studies in children: a systematic review Abstract Abstract Objectives To explore whether pharmacokinetic (PK) studies in paediatric patients are becoming less invasive. This will be evaluated by analysing the number of samples and volume of blood collected for each study within four diff...
PMC6678684
core_pubmed_pmc
Potential Adverse Drug Events and Drug–Drug Interactions with Medical and Consumer Cannabidiol (CBD) Use
Potential Adverse Drug Events and Drug–Drug Interactions with Medical and Consumer Cannabidiol (CBD) Use Abstract Abstract Cannabidiol (CBD) is ubiquitous in state-based medical cannabis programs and consumer products for complementary health or recreational use. CBD has intrinsic pharmacologic effects and associated a...
PMC10465962
core_pubmed_pmc
Metabolomics in drug research and development: The recent advances in technologies and applications
Metabolomics in drug research and development: The recent advances in technologies and applications Abstract Abstract Emerging evidence has demonstrated the vital role of metabolism in various diseases or disorders. Metabolomics provides a comprehensive understanding of metabolism in biological systems. With advanced a...
PMC11730072
core_pubmed_pmc
Risk Factors and Patterns of Drug‐Drug Interactions in Two Categories of Level‐3 Hospitals in Dhaka: A Cross‐Sectional Study
Risk Factors and Patterns of Drug‐Drug Interactions in Two Categories of Level‐3 Hospitals in Dhaka: A Cross‐Sectional Study Abstract ABSTRACT Background and Aims Drug‐drug interactions (DDIs) are a significant health issue that may adversely affect the health and well‐being of patients. This study assesses and compare...
PMC5599956
core_pubmed_pmc
Effect of Food Intake on the Pharmacodynamics of Tenapanor: A Phase 1 Study
Effect of Food Intake on the Pharmacodynamics of Tenapanor: A Phase 1 Study Abstract Abstract Tenapanor (RDX5791/AZD1722) is a minimally systemic small‐molecule inhibitor of the sodium/hydrogen exchanger NHE3. Tenapanor acts in the gut to reduce absorption of sodium and phosphate. This phase 1 open‐label, 3‐way crossov...
PMC6267664
core_pubmed_pmc
Phase I trial of afatinib and 3-weekly trastuzumab with optimal anti-diarrheal management in patients with HER2-positive metastatic cancer
Phase I trial of afatinib and 3-weekly trastuzumab with optimal anti-diarrheal management in patients with HER2-positive metastatic cancer Abstract Background Trastuzumab is the mainstay of therapy for patients with HER2-positive breast and gastric cancer but resistance frequently occurs. Afatinib, an irreversible oral...
PMC6895912
core_pubmed_pmc
Galeterone and The Next Generation Galeterone Analogs, VNPP414 and VNPP433-3β Exert Potent Therapeutic Effects in Castration-/Drug-Resistant Prostate Cancer Preclinical Models In Vitro and In Vivo
Galeterone and The Next Generation Galeterone Analogs, VNPP414 and VNPP433-3β Exert Potent Therapeutic Effects in Castration-/Drug-Resistant Prostate Cancer Preclinical Models In Vitro and In Vivo Abstract Abstract These studies compared the efficacies of our clinical agent galeterone (Gal) and the FDA-approved prostat...
PMC6030777
core_pubmed_pmc
Characterization of differential patient profiles and therapeutic responses of pharmacy customers for four ambroxol formulations
Characterization of differential patient profiles and therapeutic responses of pharmacy customers for four ambroxol formulations Abstract Background Ambroxol relieves cough symptoms based on its secretagogue, anti-inflammatory, anti-oxidant, anti-bacterial, anti-viral, immunomodulatory and local anesthetic effects. The...
PMC9930700
core_pubmed_pmc
Results From a Randomized, Open-Label, Crossover Study Evaluating the Effect of the Aldosterone Synthase Inhibitor Baxdrostat on the Pharmacokinetics of Metformin in Healthy Human Subjects
Results From a Randomized, Open-Label, Crossover Study Evaluating the Effect of the Aldosterone Synthase Inhibitor Baxdrostat on the Pharmacokinetics of Metformin in Healthy Human Subjects Abstract Background Due to the high comorbidity of diabetes and hypertension, co-administration of metformin with anti-hypertensive...
PMC11988034
core_pubmed_pmc
Exposure–Response Relationships for Toceranib in Dogs with Solid Tumors: A Pilot Study
Exposure–Response Relationships for Toceranib in Dogs with Solid Tumors: A Pilot Study Abstract Simple Summary Toceranib phosphate, the most commonly used tyrosine kinase inhibitor in veterinary oncology, meets most of the criteria for therapeutic drug monitoring (TDM); however, its exposure–response relationships have...
PMC4320559
core_pubmed_pmc
Efficacy of intranasal administration of artesunate in experimental cerebral malaria
Efficacy of intranasal administration of artesunate in experimental cerebral malaria Abstract Abstract Background Improving management of patients suffering from cerebral malaria is needed to reduce the devastating mortality and morbidity of the disease in endemic areas. Intravenous artesunate is currently the first-li...
PMC10042133
core_pubmed_pmc
The use of nanoparticles for targeted drug delivery in non-small cell lung cancer
The use of nanoparticles for targeted drug delivery in non-small cell lung cancer Abstract Lung cancer is a global health problem affecting millions of people each year. Non-small cell lung cancer (NSCLC) is the most common form of lung cancer with various conventional treatment available in the clinic. Application of ...
PMC3797760
core_pubmed_pmc
Influence of Obstructive Jaundice on Pharmacodynamics of Rocuronium
Influence of Obstructive Jaundice on Pharmacodynamics of Rocuronium Abstract Background Anesthetics are variable in patients with obstructive jaundice. The minimum alveolar concentration awake of desflurane is reduced in patients with obstructive jaundice, while it has no effect on pharmacodynamics and pharmacokinetics...
PMC10386724
core_pubmed_pmc
Establishment and Evaluation of a Parametric Population Pharmacokinetic Model Repository for Ganciclovir and Valganciclovir
Establishment and Evaluation of a Parametric Population Pharmacokinetic Model Repository for Ganciclovir and Valganciclovir Abstract Background: Ganciclovir and valganciclovir are used for prophylaxis and treatment of cytomegalovirus infection. However, there is great interindividual variability in ganciclovir’s pharma...
PMC7823237
core_pubmed_pmc
Optimal Monitoring of Weekly IGF-I Levels During Growth Hormone Therapy With Once-Weekly Somapacitan
Optimal Monitoring of Weekly IGF-I Levels During Growth Hormone Therapy With Once-Weekly Somapacitan Abstract Abstract Context Somapacitan is a long-acting growth hormone (GH) in development for once-weekly treatment of GH deficiency (GHD). Optimal monitoring of insulin-like growth factor-I (IGF-I) levels must account ...
PMC8024110
core_pubmed_pmc
Rational design of flavonoid based potential inhibitors targeting SARS-CoV 3CL protease for the treatment of COVID-19
Rational design of flavonoid based potential inhibitors targeting SARS-CoV 3CL protease for the treatment of COVID-19 Abstract Abstract The current outbreak of Coronavirus Disease 2019 (COVID-19) pandemic has reported thousands of deaths worldwide due to the rapid transmission rate and the lack of antiviral drugs and v...
PMC11384081
core_pubmed_pmc
Population-based model selection for an accurate estimation of time-integrated activity using non-linear mixed-effects modelling
Population-based model selection for an accurate estimation of time-integrated activity using non-linear mixed-effects modelling Abstract Purpose Personalized treatment planning in Molecular Radiotherapy (MRT) with accurately determining the absorbed dose is highly desirable. The absorbed dose is calculated based on th...
PMC8047826
core_pubmed_pmc
Alfuzosin for the medical treatment of benign prostatic hyperplasia and lower urinary tract symptoms: a systematic review of the literature and narrative synthesis
Alfuzosin for the medical treatment of benign prostatic hyperplasia and lower urinary tract symptoms: a systematic review of the literature and narrative synthesis Abstract Abstract Background: Lower urinary tract symptoms (LUTS) secondary to benign prostatic hyperplasia (BPH) are a bothersome frequent symptom in adult...
PMC5340007
core_pubmed_pmc
A phase I dose-escalation study of selumetinib in combination with docetaxel or dacarbazine in patients with advanced solid tumors
A phase I dose-escalation study of selumetinib in combination with docetaxel or dacarbazine in patients with advanced solid tumors Abstract Abstract Background The RAS/RAF/MEK/ERK pathway is constitutively activated in many cancers. Selumetinib (AZD6244, ARRY-142886) is an oral, potent and highly selective, allosteric ...
PMC11335869
core_pubmed_pmc
Physiologically-based pharmacokinetic/pharmacodynamic modeling of meropenem in critically ill patients
Physiologically-based pharmacokinetic/pharmacodynamic modeling of meropenem in critically ill patients Abstract This study aimed to develop a physiologically based pharmacokinetic/pharmacodynamic model (PBPK/PD) of meropenem for critically ill patients. A PBPK model of meropenem in healthy adults was established using ...
PMC11094190
core_pubmed_pmc
A simple and highly sensitive LC–MS workflow for characterization and quantification of ADC cleavable payloads
A simple and highly sensitive LC–MS workflow for characterization and quantification of ADC cleavable payloads Abstract Abstract Antibody–drug conjugates (ADC) payloads are cleavable drugs that act as the warhead to exert an ADC’s cytotoxic effects on cancer cells intracellularly. A simple and highly sensitive workflow...
PMC10145339
core_pubmed_pmc
Influence of Intramuscular Injection Sites on Pharmacokinetics of Amoxicillin in Olive Flounder ( Paralichthys olivaceus ) and Its Implication for Antibacterial Efficacy
Influence of Intramuscular Injection Sites on Pharmacokinetics of Amoxicillin in Olive Flounder ( Paralichthys olivaceus ) and Its Implication for Antibacterial Efficacy Abstract Abstract This study aimed to investigate the effects of different injection sites, including dorsal, cheek, and pectoral fin muscles, on the ...
PMC8000608
core_pubmed_pmc
Receptor-Based Pharmacophore Modeling in the Search for Natural Products for COVID-19 M pro
Receptor-Based Pharmacophore Modeling in the Search for Natural Products for COVID-19 M pro Abstract Abstract Considering the urgency of the COVID-19 pandemic, we developed a receptor-based pharmacophore model for identifying FDA-approved drugs and hits from natural products. The COVID-19 main protease (M pro ) was sel...
PMC7081932
core_pubmed_pmc
Preparation, characterization, and in vitro/vivo evaluation of polymer-assisting formulation of atorvastatin calcium based on solid dispersion technique
Preparation, characterization, and in vitro/vivo evaluation of polymer-assisting formulation of atorvastatin calcium based on solid dispersion technique Abstract Due to low solubility and bioavailability, atorvastatin calcium is confronted with challenge in conceiving appropriate formulation. Solid dispersion of atorva...
PMC12524202
core_pubmed_pmc
Liver-Specific Nanoparticle-Mediated Delivery and MMP-Triggered Release of Veratridine to Effectively Target Metastatic Colorectal Cancer
Liver-Specific Nanoparticle-Mediated Delivery and MMP-Triggered Release of Veratridine to Effectively Target Metastatic Colorectal Cancer Abstract Abstract Simple Summary Encapsulating an anti-metastatic molecule, veratridine (VTD), by mesoporous silica nanoparticles (MSNs) and calcium carbonate submicroparticles (CCSM...
PMC10309101
core_pubmed_pmc
Characterization of Extended-Release Lorazepam
Characterization of Extended-Release Lorazepam Abstract Purpose/Background Once-daily extended-release (ER) lorazepam was developed to reduce fluctuations in plasma levels compared with lorazepam immediate-release (IR) for short-term anxiety relief. Here we report a series of phase 1 randomized, open-label, multiperiod...
PMC11775251
core_pubmed_pmc
Evaluation of ampicillin plus ceftobiprole combination therapy in treating Enterococcus faecalis infective endocarditis and bloodstream infection
Evaluation of ampicillin plus ceftobiprole combination therapy in treating Enterococcus faecalis infective endocarditis and bloodstream infection Abstract Abstract Enterococcus faecalis is responsible for numerous serious infections, and treatment options often include ampicillin combined with an aminoglycoside or dual...
PMC11094416
core_pubmed_pmc
Lipid-Encapsulated mRNAs Encoding Complex Fusion Proteins Potentiate Antitumor Immune Responses
Lipid-Encapsulated mRNAs Encoding Complex Fusion Proteins Potentiate Antitumor Immune Responses Abstract Abstract Lipid nanoparticle (LNP)–encapsulated mRNA has been used for in vivo production of several secreted protein classes, such as IgG, and has enabled the development of personalized vaccines in oncology. Establ...
PMC12254004
core_pubmed_pmc
Exosomal delivery of IL-10: Biodistribution, pharmacokinetics, and preterm birth prevention strategies
Exosomal delivery of IL-10: Biodistribution, pharmacokinetics, and preterm birth prevention strategies Abstract Abstract This study investigates the potential of extracellular vesicles (EVs) loaded with interleukin-10 (IL-10) to reduce infection-induced preterm birth (PTB). IL-10 has shown promise in reducing PTB by da...
PMC12354565
core_pubmed_pmc
Influence of Pharmacokinetic-Pharmacodynamic Failure Mechanisms on Outcomes in Biologic Therapy Sequencing in Inflammatory Bowel Disease: A Retrospective Cohort Study
Influence of Pharmacokinetic-Pharmacodynamic Failure Mechanisms on Outcomes in Biologic Therapy Sequencing in Inflammatory Bowel Disease: A Retrospective Cohort Study Abstract Background Increasing therapeutic options for inflammatory bowel disease calls for tools to aid choice of sequencing. We investigated if pharmac...
PMC12409547
core_pubmed_pmc
Biological Evaluation of Cleavable Linkers in Exatecan-Based Antibody–Drug Conjugates: A Comparative Study of DXd and Exo-Linker Platforms
Biological Evaluation of Cleavable Linkers in Exatecan-Based Antibody–Drug Conjugates: A Comparative Study of DXd and Exo-Linker Platforms Abstract Antibody–drug conjugates (ADCs) represent a transformative class of cancer therapies that combine the specificity of monoclonal antibodies with the cytotoxicity of potent d...
PMC8374649
core_pubmed_pmc
IBI362 (LY3305677), a weekly-dose GLP-1 and glucagon receptor dual agonist, in Chinese adults with overweight or obesity: A randomised, placebo-controlled, multiple ascending dose phase 1b study
IBI362 (LY3305677), a weekly-dose GLP-1 and glucagon receptor dual agonist, in Chinese adults with overweight or obesity: A randomised, placebo-controlled, multiple ascending dose phase 1b study Abstract Background IBI362 (LY3305677) is a novel weekly-dose glucagon-like peptide-1 and glucagon receptor dual agonist bein...
PMC11570808
core_pubmed_pmc
JAK inhibitors: an evidence-based choice of the most appropriate molecule
JAK inhibitors: an evidence-based choice of the most appropriate molecule Abstract Janus kinase inhibitors (JAKis) represent a fundamental therapeutic tool for the treatment of patients with immune-mediated inflammatory diseases. Although JAKis are often considered a homogeneous class of drugs whose members are thought...
PMC12784194
core_pubmed_pmc
Comprehensive pharmacokinetic/pharmacodynamic analysis of commercially available premixed daptomycin preparations against Staphylococcus aureus and Enterococcus spp. bloodstream infections using Monte Carlo simulation in adult patients
Comprehensive pharmacokinetic/pharmacodynamic analysis of commercially available premixed daptomycin preparations against Staphylococcus aureus and Enterococcus spp. bloodstream infections using Monte Carlo simulation in adult patients Abstract Abstract Objectives The current approach to dosing daptomycin is primarily ...
PMC12781667
core_pubmed_pmc
Management of anticoagulation in patients with atrial fibrillation and renal dysfunction: A systematic review
Management of anticoagulation in patients with atrial fibrillation and renal dysfunction: A systematic review Abstract BACKGROUND Atrial fibrillation (AF) is a prevalent cardiac arrhythmia associated with significant morbidity and mortality, particularly in patients with concomitant renal dysfunction. Anticoagulation t...
PMC9416163
core_pubmed_pmc
Antiproliferative Copper(II) Complexes Bearing Mixed Chelating Ligands: Structural Characterization, ROS Scavenging, In Silico Studies, and Anti-Melanoma Activity
Antiproliferative Copper(II) Complexes Bearing Mixed Chelating Ligands: Structural Characterization, ROS Scavenging, In Silico Studies, and Anti-Melanoma Activity Abstract Melanoma is a skin cancer characterized by rapid growth and spread for which current therapies produce both resistance and increased risk of infecti...
PMC10053447
core_pubmed_pmc
Oral Administration as a Potential Alternative for the Delivery of Small Extracellular Vesicles
Oral Administration as a Potential Alternative for the Delivery of Small Extracellular Vesicles Abstract Abstract Small extracellular vesicles (sEVs) have burst into biomedicine as a natural therapeutic alternative for different diseases. Considered nanocarriers of biological origin, various studies have demonstrated t...
PMC11923969
core_pubmed_pmc
Supramolecular Modulation of Tumor Microenvironment Through Host−Guest Recognition and Metal Coordination to Potentiate Cancer Chemoimmunotherapy
Supramolecular Modulation of Tumor Microenvironment Through Host−Guest Recognition and Metal Coordination to Potentiate Cancer Chemoimmunotherapy Abstract Abstract The massive amount of indoleamine 2,3‐dioxygenase 1 (IDO‐1) in tumor cells and tumor‐associated immune cells forms a feedback loop that maintains immunosupp...
PMC7935699
core_pubmed_pmc
Population Pharmacokinetics and Bayesian Dose Adjustment to Advance TDM of Anti-TB Drugs
Population Pharmacokinetics and Bayesian Dose Adjustment to Advance TDM of Anti-TB Drugs Abstract Abstract Tuberculosis (TB) is still the number one cause of death due to an infectious disease. Pharmacokinetics and pharmacodynamics of anti-TB drugs are key in the optimization of TB treatment and help to prevent slow re...
PMC9795234
core_pubmed_pmc
Mathematical modeling of antihypertensive therapy
Mathematical modeling of antihypertensive therapy Abstract Hypertension is a multifactorial disease arising from complex pathophysiological pathways. Individual characteristics of patients result in different responses to various classes of antihypertensive medications. Therefore, evaluating the efficacy of therapy bas...
PMC9541865
core_pubmed_pmc
Clinical Pharmacology of Insulin Aspart Biosimilar GP40071: Pharmacokinetic/Pharmacodynamic Comparability in Hyperinsulinemic Euglycemic Clamp Procedure
Clinical Pharmacology of Insulin Aspart Biosimilar GP40071: Pharmacokinetic/Pharmacodynamic Comparability in Hyperinsulinemic Euglycemic Clamp Procedure Abstract Abstract Insulin aspart is a short‐acting insulin analogue that is used to control postprandial glycemia levels in diabetic patients. The aim of this clinical...
PMC9056957
core_pubmed_pmc
Improving the solubility and bioavailability of anti-hepatitis B drug PEC via PEC–fumaric acid cocrystal †
Improving the solubility and bioavailability of anti-hepatitis B drug PEC via PEC–fumaric acid cocrystal † Abstract PEC is a new generation of phosphamide ester anti-hepatitis B virus drug. It is a prodrug of tenofovir and can be rapidly metabolized to tenofovir. However, its poor solubility in water (0.219 mg mL −1 at...
PMC4346004
core_pubmed_pmc
New insights into the use of currently available non-steroidal anti-inflammatory drugs
New insights into the use of currently available non-steroidal anti-inflammatory drugs Abstract Non-steroidal anti-inflammatory drugs (NSAIDs), which act via inhibition of the cyclooxygenase (COX) isozymes, were discovered more than 100 years ago. They remain a key component of the pharmacological management of acute a...
PMC8683663
core_pubmed_pmc
Oral etoposide and zosuquidar bioavailability in rats: Effect of co-administration and in vitro - in vivo correlation of P-glycoprotein inhibition
Oral etoposide and zosuquidar bioavailability in rats: Effect of co-administration and in vitro - in vivo correlation of P-glycoprotein inhibition Abstract P-glycoprotein inhibitors, like zosuquidar, have widely been used to study the role of P-glycoprotein in oral absorption. Still, systematic studies on the inhibitor...
PMC11106146
core_pubmed_pmc
Personalized Antifungal Therapy Through Model-Informed Precision Dosing of Posaconazole
Personalized Antifungal Therapy Through Model-Informed Precision Dosing of Posaconazole Abstract Background and Objective Posaconazole is a pharmacotherapeutic pillar for prophylaxis and treatment of invasive fungal diseases. Dose individualization is of utmost importance as achieving adequate antifungal exposure is as...
PMC12596047
core_pubmed_pmc
Antagonistic interaction between posaconazole and olorofim in a murine model of invasive pulmonary aspergillosis
Antagonistic interaction between posaconazole and olorofim in a murine model of invasive pulmonary aspergillosis Abstract Abstract Background Olorofim is a new antifungal agent with a novel mechanism of action with in vitro activity against Aspergillus fumigatus and other clinically important moulds. As antifungal comb...
PMC11781947
core_pubmed_pmc
Transfer of the Oral Gonadotropin‐Releasing Hormone Receptor Antagonist Relugolix Into Breast Milk of Healthy Lactating Women
Transfer of the Oral Gonadotropin‐Releasing Hormone Receptor Antagonist Relugolix Into Breast Milk of Healthy Lactating Women Abstract ABSTRACT Relugolix is an oral gonadotropin‐releasing hormone receptor antagonist that suppresses sex steroid hormones and is approved as monotherapy for prostate cancer and as a fixed‐d...
PMC9674622
core_pubmed_pmc
Anticalcification effects of DS-1211 in pseudoxanthoma elasticum mouse models and the role of tissue-nonspecific alkaline phosphatase in ABCC6-deficient ectopic calcification
Anticalcification effects of DS-1211 in pseudoxanthoma elasticum mouse models and the role of tissue-nonspecific alkaline phosphatase in ABCC6-deficient ectopic calcification Abstract Pseudoxanthoma elasticum (PXE) is a multisystem, genetic, ectopic mineralization disorder with no effective treatment. Inhibition of tis...
PMC7398395
core_pubmed_pmc
A population pharmacokinetic model is beneficial in quantifying hair concentrations of ritonavir-boosted atazanavir: a study of HIV-infected Zimbabwean adolescents
A population pharmacokinetic model is beneficial in quantifying hair concentrations of ritonavir-boosted atazanavir: a study of HIV-infected Zimbabwean adolescents Abstract Background Adolescents experience higher levels of non-adherence to HIV treatment. Drug concentration in hair promises to be reliable for assessing...
PMC7195552
core_pubmed_pmc
Efficacy and Safety of High Vs Standard Daptomycin Doses Examined in Chinese Patients With Severe Burn Injuries by Pharmacokinetic Evaluation
Efficacy and Safety of High Vs Standard Daptomycin Doses Examined in Chinese Patients With Severe Burn Injuries by Pharmacokinetic Evaluation Abstract Abstract Previous studies and the concentration-dependent antibacterial actions of daptomycin suggested that a high dose would be needed for difficult-to-treat infection...
PMC10301358
core_pubmed_pmc
Prediction of CYP-Mediated Drug Interaction Using Physiologically Based Pharmacokinetic Modeling: A Case Study of Salbutamol and Fluvoxamine
Prediction of CYP-Mediated Drug Interaction Using Physiologically Based Pharmacokinetic Modeling: A Case Study of Salbutamol and Fluvoxamine Abstract Abstract Drug–drug interactions (DDIs) represent a significant concern in healthcare, particularly for patients undergoing polytherapy. DDIs can lead to a range of outcom...
PMC9301199
core_pubmed_pmc
Semi-PBPK Modeling and Simulation to Evaluate the Local and Systemic Pharmacokinetics of OC-01(Varenicline) Nasal Spray
Semi-PBPK Modeling and Simulation to Evaluate the Local and Systemic Pharmacokinetics of OC-01(Varenicline) Nasal Spray Abstract This study aimed to build a nasal semi-physiologically based pharmacokinetic (PBPK) model to predict the intranasal pharmacokinetic (PK) of the OC-01(varenicline) nasal spray and accelerate t...
PMC9290993
core_pubmed_pmc
Safety, tolerability, and pharmacokinetics of casimersen in patients with Duchenne muscular dystrophy amenable to exon 45 skipping: A randomized, double‐blind, placebo‐controlled, dose‐titration trial
Safety, tolerability, and pharmacokinetics of casimersen in patients with Duchenne muscular dystrophy amenable to exon 45 skipping: A randomized, double‐blind, placebo‐controlled, dose‐titration trial Abstract Abstract Introduction/Aims Duchenne muscular dystrophy (DMD) is caused by mutations in the DMD gene resulting ...
PMC7617756
core_pubmed_pmc
Temporal changes in SARS-CoV-2 clearance kinetics and the optimal design of antiviral pharmacodynamic studies: an individual patient data meta-analysis of a randomised, controlled, adaptive platform study (PLATCOV)
Temporal changes in SARS-CoV-2 clearance kinetics and the optimal design of antiviral pharmacodynamic studies: an individual patient data meta-analysis of a randomised, controlled, adaptive platform study (PLATCOV) Abstract Summary Background Effective antiviral drugs prevent hospitalisation and death from COVID-19. An...
PMC7775628
core_pubmed_pmc
Potential natural inhibitors of xanthine oxidase and HMG-CoA reductase in cholesterol regulation: in silico analysis
Potential natural inhibitors of xanthine oxidase and HMG-CoA reductase in cholesterol regulation: in silico analysis Abstract Abstract Background Hypercholesterolemia has posed a serious threat of heart diseases and stroke worldwide. Xanthine oxidase (XO), the rate-limiting enzyme in uric acid biosynthesis, is regarded...
PMC7318171
core_pubmed_pmc
Predicting Clinical Effects of CYP3A4 Modulators on Abemaciclib and Active Metabolites Exposure Using Physiologically Based Pharmacokinetic Modeling
Predicting Clinical Effects of CYP3A4 Modulators on Abemaciclib and Active Metabolites Exposure Using Physiologically Based Pharmacokinetic Modeling Abstract Abstract Abemaciclib, a selective inhibitor of cyclin‐dependent kinases 4 and 6, is metabolized mainly by cytochrome P450 (CYP)3A4. Clinical studies were performe...
PMC7982486
core_pubmed_pmc
Simplified Dosing Regimens for Gentamicin in Neonatal Sepsis
Simplified Dosing Regimens for Gentamicin in Neonatal Sepsis Abstract Abstract Background: The effectiveness of antibiotics for the treatment of severe bacterial infections in newborns in resource-limited settings has been determined by empirical evidence. However, such an approach does not warrant optimal exposure to ...
PMC12608915
core_pubmed_pmc
Unlocking Mangiferin: A Therapeutic Candidate Revolutionizing Liver Disease Therapy
Unlocking Mangiferin: A Therapeutic Candidate Revolutionizing Liver Disease Therapy Abstract Abstract Mangiferin (MF), a natural component widely found in fruits, vegetables, and herbs, has garnered increasing attention for its potent antioxidative properties and therapeutic potential. This bioactive xanthone compound ...
PMC12816422
core_pubmed_pmc
Model‐Informed Drug Development for Daprodustat Supports the Design of Individualized Dosing Regimens in Chronic Kidney Disease Patients With Anemia
Model‐Informed Drug Development for Daprodustat Supports the Design of Individualized Dosing Regimens in Chronic Kidney Disease Patients With Anemia Abstract Model‐informed drug development (MIDD) played a crucial role in the successful development and regulatory approval of daprodustat, a novel oral hypoxia‐inducible ...
PMC12523803
core_pubmed_pmc
Glycoengineering of plant-produced Pembrolizumab enhances FcRn binding and extends serum half-life in mice
Glycoengineering of plant-produced Pembrolizumab enhances FcRn binding and extends serum half-life in mice Abstract Abstract Plant systems offer scalable and cost-effective platforms for antibody production, but plant-specific glycans may affect pharmacokinetics and immunogenicity. To evaluate the impact of Fc glycosyl...
PMC11904623
core_pubmed_pmc
Challenges and opportunities in uncertainty quantification for healthcare and biological systems
Challenges and opportunities in uncertainty quantification for healthcare and biological systems Abstract Abstract Uncertainty quantification (UQ) is an essential aspect of computational modelling and statistical prediction. Multiple applications, including geophysics, climate science and aerospace engineering, incorpo...
PMC4020257
core_pubmed_pmc
Pharmacokinetics, pharmacodynamics, safety and tolerability of 4 weeks' treatment with empagliflozin in Japanese patients with type 2 diabetes mellitus
Pharmacokinetics, pharmacodynamics, safety and tolerability of 4 weeks' treatment with empagliflozin in Japanese patients with type 2 diabetes mellitus Abstract Abstract Introduction To evaluate the pharmacodynamics, pharmacokinetics, safety and tolerability of empagliflozin in Japanese patients with type 2 diabetes me...
PMC4426534
core_pubmed_pmc
Estimation of creatinine clearance using plasma creatinine or cystatin C: a secondary analysis of two pharmacokinetic studies in surgical ICU patients
Estimation of creatinine clearance using plasma creatinine or cystatin C: a secondary analysis of two pharmacokinetic studies in surgical ICU patients Abstract Abstract Background In ICU patients, glomerular filtration is often impaired, but also supraphysiological values are observed (“augmented renal clearance”, >130...
PMC4767861
core_pubmed_pmc
A survey of new oncology drug approvals in the USA from 2010 to 2015: a focus on optimal dose and related postmarketing activities
A survey of new oncology drug approvals in the USA from 2010 to 2015: a focus on optimal dose and related postmarketing activities Abstract The maximally tolerated dose (MTD) of cytotoxic agents has historical precedence in treating cancer, as it was believed that dose and therapeutic effect are intrinsically linked an...
PMC10916623
core_pubmed_pmc
Tissue distribution and pharmacokinetics of isoxanthohumol from hops in rodents
Tissue distribution and pharmacokinetics of isoxanthohumol from hops in rodents Abstract Abstract Vegetables and fruits contain prenylflavonoids with biological functions that might improve human health. The prenylflavonoid isoxanthohumol (IXA) and its derivative, 8‐prenylnaringenin (8‐PN), have beneficial activities, ...
PMC6201592
core_pubmed_pmc
Pharmacokinetics and tissue distribution of monotropein and deacetyl asperulosidic acid after oral administration of extracts from Morinda officinalis root in rats
Pharmacokinetics and tissue distribution of monotropein and deacetyl asperulosidic acid after oral administration of extracts from Morinda officinalis root in rats Abstract Abstract Background Iridoid glycosides (IGs), including monotropein (MON) and deacetyl asperulosidic acid (DA) as the main ingredients, are the maj...
PMC4426839
core_pubmed_pmc
ADME SARfari: comparative genomics of drug metabolizing systems
ADME SARfari: comparative genomics of drug metabolizing systems Abstract Abstract Motivation: ADME SARfari is a freely available web resource that enables comparative analyses of drug-disposition genes. It does so by integrating a number of publicly available data sources, which have subsequently been used to build dat...
PMC10467640
core_pubmed_pmc
Current Status of Endothelin Receptor Antagonists in Pulmonary Arterial Hypertension: A Combined Study Results and Pharmacology-Based Review
Current Status of Endothelin Receptor Antagonists in Pulmonary Arterial Hypertension: A Combined Study Results and Pharmacology-Based Review Abstract Pulmonary arterial hypertension (PAH) affects a wide range of people globally and has a poor prognosis despite many advancements in available treatment options. Among the...
PMC11141576
core_pubmed_pmc
Population Pharmacokinetic Models of Venetoclax in Hematologic Malignancies: A Systematic Review
Population Pharmacokinetic Models of Venetoclax in Hematologic Malignancies: A Systematic Review Abstract Abstract Several population pharmacokinetic (PPK) models of B cell lymphoma-2 (BCL-2) venetoclax (VEN) have been developed and published to characterize the influencing factors of pharmacokinetics in hematologic ma...
PMC11387684
core_pubmed_pmc
Pharmacokinetics and pharmacodynamics of low doses of recombinant tissue plasminogen activator to establish a model for biosimilarity comparisons
Pharmacokinetics and pharmacodynamics of low doses of recombinant tissue plasminogen activator to establish a model for biosimilarity comparisons Abstract Background Recombinant tissue plasminogen activator (rt-PA) is a thrombolytic agent and essential in emergency medical care. Given recent supply shortages, the avail...
PMC5613178
core_pubmed_pmc
Determination of Plasma Concentration Reference Ranges for Risperidone and Paliperidone
Determination of Plasma Concentration Reference Ranges for Risperidone and Paliperidone Abstract Schizophrenia is a common disease managed by a range of interventions, with the primary treatment being antipsychotic medications (APS). Inadequate response, lack of adherence, and/or adverse events often prevent optimal th...
PMC12472293
core_pubmed_pmc
Characterizing Population Pharmacokinetics of Vatiquinone in Healthy Volunteers and Patients with Friedreich’s Ataxia
Characterizing Population Pharmacokinetics of Vatiquinone in Healthy Volunteers and Patients with Friedreich’s Ataxia Abstract Introduction: Vatiquinone is a first-in-class, small molecule designed to maintain mitochondrial function in the disorders like Friedreich’s ataxia (FA). Vatiquinone inhibits 15-lipoxygenase, c...
PMC12852546
core_pubmed_pmc
Evaluation of INR101, a PSMA-Targeted 18 F PET Tracer, for suspected prostate cancer: A multicenter phase I/IIa trial with histopathologic confirmation
Evaluation of INR101, a PSMA-Targeted 18 F PET Tracer, for suspected prostate cancer: A multicenter phase I/IIa trial with histopathologic confirmation Abstract Background Prostate cancer (PCa) is one of the most common malignancies among men worldwide. Early detection relies heavily on imaging accuracy, yet convention...
PMC12554956
core_pubmed_pmc
Structure-based screening and molecular dynamics of phytophytochemicals against pseudomonas aeruginosa quorum sensing systems
Structure-based screening and molecular dynamics of phytophytochemicals against pseudomonas aeruginosa quorum sensing systems Abstract Abstract Pseudomonas aeruginosa employs quorum sensing (QS) to regulate virulence and antibiotic resistance, making QS inhibition a promising anti-infective strategy. Here, we computati...